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IRM LLC

IRM LLC Patent applications
Patent application numberTitlePublished
20120129766METHODS OF TREATING FGF21-ASSOCIATED DISORDERS - The invention relates to the identification of new polypeptide and protein variants of fibroblast growth factor 21 (FGF21) that have improved pharmaceutical properties. Also disclosed are methods for treating FGF21-associated disorders, including metabolic conditions.05-24-2012
20120065184COMPOUNDS AND COMPOSITIONS AS TRK INHIBITORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity.03-15-2012
20120027756METHODS AND COMPOSITIONS FOR TREATING ALLERGIC DISEASES - Disclosed in the present invention are antibodies that specifically recognize and antagonize human TSLP receptor, and methods of employing these antibodies to treat or ameliorate diseases or disorder mediated by TSLP signaling.02-02-2012
20110312510High-Throughput Complement-Mediated Antibody-Dependent and Opsonic Bactericidal Assays - The disclosure provides methods and kits for performing automated high-throughput assays to measure bactericidal activity in samples, such as plasma or sera from vaccinated subjects to evaluate the efficacy of vaccines against bacterial pathogens. The method combines obligatory linear-range data analysis, plate sealing and liquid volume handling for all assay steps to provide an automated, high-throughput measurement of bactericidal activity with favorable inter-assay and inter-operator variability.12-22-2011
20110306625COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.12-15-2011
20110263610COMPOUNDS AND COMPOSITIONS AS ITPKB INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).10-27-2011
20110263557COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119; such as, but not limited to, diabetes, obesity and associated metabolic disorders. Formula (I) is a compound, in which A can have up to 2 ring —CH2- group substituted with —C(O)— and can be partially unsaturated with up to 2 double bonds; Wi and W2 are independently selected from CR10 and N; wherein R10 is selected from hydrogen and C1_6alkyl; Yi is selected from NRn, O and S; wherein Rn is selected from hydrogen and C1_6alkyl; Y2 and Y3 are independently selected from CH and N; Y4 is selected from CH2, OCH2 and NR15; wherein R15 is selected from hydrogen and C1_6alkyl; or the pharmaceutically acceptable salts thereof.10-27-2011
20110257155COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.10-20-2011
20110257154COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.10-20-2011
20110257077COMPOUNDS AND COMPOSITIONS AS CHANNEL ACTIVATING PROTEASE INHIBITORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.10-20-2011
20110245220COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.10-06-2011
20110237573N- (HETERO)ARYL, 2- (HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS - The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A09-29-2011
201101902984-PHENOXYMETHYLPIPERIDINES AS MODULATORS OF GPR119 ACTIVITY - The present invention provides compounds of Formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent; diseases or disorders associated with the activity of GPR119.08-04-2011
20110190264COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS - The invention relates to triazine and pyrimidine derivatives having Formula (1) or (2), and methods for using such compounds. For example, the compounds of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-IR), and/or insulin receptor (InsR) or a combination thereof.08-04-2011
20110190263COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds of Formula (I): pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.08-04-2011
20110190259COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.08-04-2011
20110183997HETEROCYCLIC COMPOUNDS AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS - The invention provides a novel class of compounds of Formula I: (I) pharmaceutical compositions comprising such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases.07-28-2011
20110177055COMPOUNDS AND COMPOSITIONS AS CHANNEL ACTIVATING PROTEASE INHIBITORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase,07-21-2011
20110172278COMPOUNDS AND METHODS FOR MODULATING G PROTEIN-COUPLED RECEPTORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by G protein-coupled receptors, in particular G protein-coupled receptor 120.07-14-2011
20110172244COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, of Formula I: pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.07-14-2011
20110166176COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.07-07-2011
20110166133FUSED NITROGEN CONTAINING HETEROCYCLES AND COMPOSITIONS THEREOF AS KINASE INHIBITORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Ros, KDR, FMS, C-FMS, FLT3, c-Kit, JAK2, JAK3, Aurora, PDGFR, Lck, TrkA, TrkB, TrkC, IGF-IR, ALK4, ALK5 and ALK or combinations thereof.07-07-2011
20110158999ANTAGONISTS OF PROTEASE ACTIVATED RECEPTOR-1 (PAR1) - The present invention provides antibodies or antigen-binding molecules that specifically recognize and antagonize human PAR1 receptor. Also provided in the invention are polynucleotides and vectors that encode such molecules and host cells that harbor the polynucleotides or vectors.06-30-2011
20110152282HEDGEHOG PATHWAY MODULATORS - The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).06-23-2011
20110144107COMPOUNDS AND COMPOSITIONS USEFUL FOR THE TREATMENT OF MALARIA - The invention provides a class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.06-16-2011
20110142849PCSK9 ANTAGONISTS - The present invention provides antibody antagonists against proprotein convertase subtilisin/kexin type 9a (“PCSK9”) and methods of using such antibodies.06-16-2011
201100982802,4-PYRIMIDINEDIAMINES USEFUL IN THE TREATMENT OF NEOPLASTIC DISEASES, INFLAMMATORY AND IMMUNE SYSTEM DISORDERS - Novel pyrimidine derivatives of formula I04-28-2011
20110097326ANTI-TRKB ANTIBODIES - The present invention provides improved antibodies or antigen-binding molecules that specifically recognize and agonize the tyrosine receptor kinase B (TrkB) receptor, and methods of their use. Also provided in the invention are polynucleotides and vectors that encode such molecules and host cells that harbor the polynucleotides or vectors.04-28-2011
20110081365COMPOUNDS AND COMPOSITIONS AS TLR ACTIVITY MODULATORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors, including TLR7 and TLR8. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine (formula I) wherein: X04-07-2011
20110059934COMPOUNDS AND COMPOSITIONS USEFUL FOR THE TREATMENT OF PARASITIC DISEASES - The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.03-10-2011
201100539522-HETEROARYLAMINO-PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS - The invention provides compounds of Formula (I) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFRα, PDGFRβ, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGFβ, SRC, EGFR, trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2β, BRK, Fms, KDR, c-raf or b-raf kinases.03-03-2011
20110053897COMPOUNDS AND COMPOSITIONS AS SYK KINASE INHIBITORS - Provided herein area novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated Syk kinase activity.03-03-2011
20110053893COMPOUNDS AND COMPOSITIONS AS TLR ACTIVITY MODULATORS - The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 7. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.03-03-2011
20110044991METHODS AND COMPOSITIONS FOR TREATING LYMPHOMA AND MYELOMA - This invention relates to the use of antagonists of the hedgehog signaling pathway to induce apoptosis of lymphoma and myeloma cells and to treat subjects suffering from various forms of lymphoma or myeloma.02-24-2011
20110021524COMPOSITIONS AND METHODS FOR TREATING CANCERS - This invention provides a combination of ATP-competitive BCR-ABL inhibitor and a non-ATP competitive BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with BCR-ABL.01-27-2011
20110003798COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS - The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat o prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT*, c-Kit, RET, TrkA, TrkB, TrkC-GR-1R, Alk, c-FMS or combinations thereof.01-06-2011
20110003790PYRIDO [4, 3-D] PYRIMIDINONE DERIVATIVES AS KINASE INHIBITORS - The invention provides a class of compounds of Formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT3, c-Kit, RET, TrkA, TrkB, TrkC, IGR-IR, AIk, c-FMS, or combinations thereof.01-06-2011
20100330090ANTAGONIST ANTIBODIES OF PROTEASE ACTIVATED RECEPTOR-1 (PAR1) - The present invention provide antibodies or antigen-binding molecules that specifically recognize and antagonize the PAR1 receptor. Also provided in the invention are polynucleotides and vectors that encode such molecules and host cells that harbor the polynucleotides or vectors.12-30-2010
20100324062COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, Aurora-A, Axl, BMX, CHK2, c-RAF, cSRC, Fes, FGFR3, Flt3, IKKα, IR, JNK2α2, Lck, Met, MKK6, MST2, p70S6K, PDGFRα, PKA, PKD2, ROCK-II, Ros, Rsk1, SAPK2α, SAPK2β, SAPK3, SAPK4, Syk, Tie2 and TrkB kinases.12-23-2010
201002982952-BIPHENYLAMINO-4-AMINOPYRIMIDINE DERIVATIVES AS KINASE INHIBITORS - The invention provides novel pyrimidine derivatives of formula (1) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-1R) or anaplastic lymphoma kinase (ALK).11-25-2010
20100239551COMPOUNDS AND COMPOSITIONS AS CHANNEL ACTIVATING PROTEASE INHIBITORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating chan-nel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSSI1E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.09-23-2010
20100234406COMPOUNDS AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFR and PDGFR kinases.09-16-2010
20100234400COMPOUNDS THAT MAINTAIN PLURIPOTENCY OF EMBRYONIC STEM CELLS - The present invention relates to methods and compositions for culturing embryonic stem (ES) cells. The methods relate to growing the ES cells in the presence of small molecules of formula (I) that maintain the pluripotency/self-renewal of the cells without feeder cells and LIF in serum-free conditions. These methods in part facilitate much more consistency in embryonic stem cell production, providing, for example, new avenues in the practical applications of embryonic stem cells in regenerative medicine.09-16-2010
20100234365COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF CANNABINOID RECEPTOR 1 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).09-16-2010
20100204200INHIBITORS OF CATHEPSIN S - The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula 1:08-12-2010
20100197659BIPHENYLCARBOXAMIDE DERIVATIVES AS HEDGEHOD PATHWAY MODULATORS - The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.08-05-2010
20100190811PYRIMIDINE DERIVATIVES AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS - The invention provides a novel class of pyrimidine derivatives, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases.07-29-2010
20100184791COMPOUNDS AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases.07-22-2010
20100184748COMPOUNDS AND COMPOSITIONS AS ITPKB INHIBITORS - The invention provides a novel class of compounds of formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or dysregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).07-22-2010
20100183564COMPOUNDS THAT EXPAND HEMATOPOIETIC STEM CELLS - The present invention relates to compounds and compositions for expanding the number of CD34+ cells for transplantation. The invention further relates to a cell population comprising expanded hematopoietic stem cells (HSCs) and its use in autologous or allogeneic transplantation for the treatment of patients with inherited immunodeficient and autoimmune diseases and diverse hematopoietic disorders to reconstitute the hematopoietic cell lineages and immune system defense.07-22-2010
20100168182COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly TrkA, TrkB, TrkC, PDGFR and c-kit.07-01-2010
20100150914AGONIST TRKB ANTIBODIES AND USES THEREOF - TrkB agonist antibodies and methods of their use are provided.06-17-2010
20100120807COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.05-13-2010
20100087464PROTEIN KINASE INHIBITORS AND METHODS FOR USING THEREOF - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of TrkA, TrkB, TrkC, Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKCα, Raf, ROCK-II, Rsk1, and SGK kinases, or a combination thereof.04-08-2010
20100081656COMPOSITIONS AND METHODS FOR MODULATING C-KIT AND PDGFR RECEPTORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFRα, PDGFRβ, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGFβ, SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2β, BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.04-01-2010
20100056756COMPOUNDS AND COMPOSITIONS AS CHANNEL ACTIVATING PROTEASE INHIBITORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.03-04-2010
20100056494PURINE COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS FOR THE TREATMENT OF PLASMODIUM RELATED DISEASES - The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with kinase activity, particularly malaria.03-04-2010
20100048552COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, Bcr-Abl(T315I), ALK, BLK, BMX, BRK, C-kit, c-RAF, CSK, c-SRC, EGFR, Fes, FGFR3, Flt3, Fms, Fyn, IGF-1R, IR, JAK(2), JAK(3), KDR, Lck, NLK, p70S6K, PDGFRα, Ros, SAPK2α, SGK, SIK, Syk, Tie2 and TrkB kinases.02-25-2010
20100048539COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to beat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases. Formula (I).02-25-2010
20100048453OXAZOLE AND THIAZOLE PPAR MODULATOR - The invention provides compounds (I) pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPARδ.02-25-2010
20100041732METHODS FOR IDENTIFYING COMPOUNDS THAT INHIBIT HIV INFECTION - This invention provides novel methods for identifying agents that inhibit HIV infection. The anti-HIV agents are identified by screening test compounds for ability to down-regulate the kinase activity or the expression of a PAK3 molecule. Such PAK3 modulators can be further examined for their activity in inhibiting HIV infection. These novel anti-HIV agents are useful in the prevention or treatment of HIV infection and conditions associated with HIV infection.02-18-2010
20100035944COMPOUNDS AND METHODS FOR MODULATING G PROTEIN-COUPLED RECEPTORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating G protein-coupled receptor 20 (GPR20), and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated GPR20.02-11-2010
20100022592THIAZOLE DERIVATIVES AS MODULATORS OF G PROTEIN-COUPLED RECEPTORS - The invention provides compounds of formula (IA) or (IB) and pharmaceutical compositions thereof, which are useful for modulating G protein-coupled receptor 120 (GPR120), and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated GPR120.01-28-2010
20100022515COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising compound of following formula (I), and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119 (G protein-coupled receptor 119) such as obesity, diabetes and hyperlipidemia.01-28-2010
20100016379Terephthalamate Compounds and Compositions, and Their Use as HIV Integrase Inhibitors - Described herein are compounds having a terephthalamate structural feature. Also described herein, are methods of making such compounds, methods of using such compounds to modulate the activity of HIV integase, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology of AIDS or infection with HIV.01-21-2010
20090325981Compounds and compositions as lxr modulators - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).12-31-2009
20090312321COMPOSITIONS AND METHODS FOR FGF RECEPTOR KINASES INHIBITORS - Described are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent disease or disordered associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activity of kinases such as Abl, ALK, AMPK, Aurora, Axl, Bcr-Abl, BIK, Bmx, BRK, BTK, c-Kit, CSK, cSrc, CDK1, CHK2, CK1, CK2, CaMKII, CaMKIV, DYRK2, EGFR, EphB1, FES, FGFR1, FGFR2, FGFR3, Flt1, Flt3, FMS, Fyn, GSK3β, IGF-1R, IKKα, IKKβ, IR, IRAK4, ITK, JAK2, JAK3, JNK1α1, JNK2α, KDR, Lck, LYN, MAPK1, MAPKAP-K2, MEK1, MET, MKK4, MKK6, MST2, NEK2, NLK, p70S6K, PAK2, PDGFR, PDGFRα, PDK1, Pim-2, Plk3, PKA, PKBα, PKCα, PKCtheta, PKD2, c-Raf, RET, ROCK-I, ROCK-II, Ron, Ros, Rsk1, SAPK2a, SAPK2b, SAPK3, SAPK4, SGK, SIK, Syk, Tie2, TrkB, WNK3, and ZAP-70.12-17-2009
20090312308COMPOUNDS AND COMPOSITIONS AS HEDGEHOG SIGNALING PATHWAY MODULATORS - The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.12-17-2009
20090298872COMPOUNDS AND COMPOSITIONS AS MODULATORS OF STEROIDAL RECEPTORS AND CALCIUM CHANNEL ACTIVITIES - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorder associated with the activation of steroid hormone nuclear receptors.12-03-2009
20090270409COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.10-29-2009
20090264649DIARYLAMINE-CONTAINING COMPOUNDS AND COMPOSITIONS, AND THEIR USE AS MODULATORS OF C-KIT RECEPTORS - Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.10-22-2009
20090258910COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, PDGF-R, lck, SAPK2α, p38, TGFβ, KDR, c-Kit, b-RAF, c-RAF, FLT1 and FLT4 kinases.10-15-2009
20090252757METHODS AND COMPOSITIONS FOR INHIBITING HIV INFECTION - This invention provides novel HIV-interacting host factors. The invention also provides methods of using the HIV-interacting host factors to screen for compounds that inhibit HIV infection. The methods comprise first screening test compounds for modulators of an HIV interacting host factor disclosed herein, and then further screening the identified modulating compounds for ability to inhibit HIV infection. The invention further provides methods and pharmaceutical compositions for treating diseases and conditions associated with HIV infection.10-08-2009
20090247556Azolopyrimidines as Inhibitors of Cannabinoid 1 Activity - The invention provides compounds of formula (Ia), (Ic), (Ig) and (Ik), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).10-01-2009
20090221547Immunosuppressant Compounds and Compositions - The present invention relates to immunosuppressants, processes for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction. This application relates to compounds selected from Formula (Ia), (Ib), (Ic) and (Id).09-03-2009
20090209573COMPOUNDS AND COMPOSITIONS AS HEDGEHOG PATHWAY MODULATORS - The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.08-20-2009
20090203666COMPOUNDS AND COMPOSITIONS AS HEDGEHOG PATHWAY MODULATORS - The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.08-13-2009
20090192203COMPOUNDS AND COMPOSITIONS AS PPAR MODULATORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families.07-30-2009
20090175882METHODS AND COMPOSITIONS FOR TREATING HYPERALGESIA - This invention provides compounds which specifically inhibit TRPA1 but not other members of the thermoTRP ion channel family. Also provided in the invention are methods of using TRPA1-specific inhibitors to treat or alleviate pains mediated by noxious mechanosensation.07-09-2009
20090156523METHODS AND COMPOSITIONS FOR MODULATING FOXO1 ACTIVITY AND INSULIN SIGNALING - The invention provides methods for modulating insulin signaling pathway and methods for treating insulin resistance. The methods employ agents which modulate FOXO1 subcellular localization. The invention also provides methods of screening for compounds that modulate insulin signaling related activities such as gluconeogenesis and cell proliferation.06-18-2009
20090142793SCREENING ASSAY TO IDENTIFY MODULATORS OF THE SLEEP/WAKE CYCLE - Screening assays for identifying agents that modulate BK channel activity and further modulate the sleep/wake cycle in a subject, circadian regulated locomotor activity in a subject, or both are provided, as are agents identified using such screening assays. Also provided are methods of modulating the sleep/wake cycle in a subject and methods of modulating circadian regulated locomotor activity in a subject by administering an agent that modulates BK channel activity to the subject, for example, an agent identified by a screening assay as disclosed.06-04-2009
20090137610SPIRO IMIDOZOLE DERIVATIVES AS PPAR MODULATORS - The invention provides compounds (Ia), (Ib) and (Ic), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families.05-28-2009
20090137591COMPOUNDS AND COMPOSITIONS AS PPAR MODULATORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPARδ.05-28-2009
20090137570INHIBITORS OF CATHEPSIN S - The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.05-28-2009
20090137555Compounds and Compositions as Protein Kinase Inhibitors - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases and disorders associated with kinase activity, particularly diseases associated with the activity of CDK1, CDK2, CDK4, CDK5, GSK3β, Bcr-abl, Flt-3, c-Kit, PDGFRβ, Src, Mek1 and CK1.05-28-2009
20090131400IMMUNOSUPPRESSANT COMPOUNDS AND COMPOSITIONS - The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.05-21-2009
20090105250COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, FGFR3, PDGFRβ and b-Raf kinases.04-23-2009
20090088368COMPOSITIONS COMPRISING THEM AS PPAR MODULATORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families.04-02-2009
20090075996HETEROTETRACYCLIC COMPOUNDS AS TPO MIMETICS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.03-19-2009
20090075927SWEET TASTE RECEPTORS - This invention provides novel genes and polypeptides of the sweet receptor family, methods for production of the polypeptides, methods for screening compounds that specifically bind to and/or modulate the activity of these polypeptides; and antibodies specific for the polypeptides.03-19-2009
20090069327COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, Bmx, b-RAF, c-RAF, c-SRC, KDR, CSK, FGFR3, JAK2, Lck, Met, PKCα, SAPK2α, Tie2, TrkB and P70S6K kinases.03-12-2009
20090062260COMPOUNDS AND COMPOSITIONS AS LXR MODULATORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).03-05-2009
20090054417COMPOUNDS AND COMPOSITIONS AS MODULATORS OF STEROID HORMONE NUCLEAR RECEPTORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activation of steroid hormone nuclear receptors.02-26-2009
20090042281COMPOUND PROFILING DEVICES, SYSTEMS, AND RELATED METHODS - High throughput compound profiling systems, and related devices and sub-systems that can be used to perform various compound profiling processes are provided. These systems typically include work perimeters that are organized for optimum efficiency and processing accuracy. Further, these systems are readily adaptable for performing a wide array of assays, as many different system components are easily incorporated or interchangeable in a particular system. System components that are provided by the invention include cell culture dissociators, which can be used, e.g., to effect cell wetting, dissociation, and/or agitation applications. In some embodiments, these cell culture dissociators are included as components of automated cell culture passaging stations. Dispensing devices that permit on-the-fly fluid temperature regulation are also provided. In addition, various compound profiling methods, cell dissociation methods, uniform cell concentration dispensing methods, among other processes, are also provided.02-12-2009
20090023572CAPACITY ALTERING DEVICE, HOLDER, AND METHODS OF SAMPLE PROCESSING - This invention provides capacity altering devices that facilitate the processing of samples whose volume exceeds the capacity of external sample processing regions (e.g., sample tubes or wells). The invention also provides holders that can be used with such devices, e.g., to allow centrifugation of the devices and/or to minimize handling of the external processing regions. Methods of processing samples, particularly samples whose volume exceeds the capacity of the external processing regions, and methods of collecting compounds in external processing regions are another feature of the invention.01-22-2009
20090012097Polycyclic 1,2,3,4-Tetrahydro-Isoquinoline Derivatives and Compositions Comprising Them As Ppar Modulators - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families.01-08-2009
20080300246Compounds and Compositions as Protein Kinase Inhibitors - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, BMX, BTK, CHK2, b-RAF, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKKα, IKKβ, JNK2α 2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFRβ, PKA, PKBα, PKD2, Rsk1, SAPK2α, SAPK2β, SAPK3, SGK, Tie2 and TrkB kinases.12-04-2008
20080292608Compounds and Compositions as Ppar Modulators - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families.11-27-2008
20080287516Phenyl-Substituted Pyrrolidones - The present invention relates to phenyl-substituted pyrrolidones and compounds related to phenyl-substituted pyrrolidones. One use of these compounds is for the inhibition of viruses, e.g., HIV. The invention further relates to methods of malting these compounds, methods of identifying the efficacy of these compounds, and methods of using these compounds to inhibit or prevent HIV infection and related disease states such as AIDS.11-20-2008
20080287432Compounds and Compositions as Protein Kinase Inhibitors - The invention provides a novel class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the AbI, Bcr-AbI, Aurora-A, SGK, Tie-2, Trk-B, FGFR3, c-kit, b-RAF, c-RAF, DYRK2, Fms, Fyn and PDGFRalpha and PDGFR&bgr; kinases.11-20-2008
20080255136PYRROLIDONES WITH ANTI-HIV ACTIVITY - The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.10-16-2008
20080253927HIGH THROUGHPUT PROCESSING SYSTEM AND METHOD OF USING - The present invention provides a system and method for high throughput processing using sample holders. The system has a plurality of work perimeters, with a rotational robot preferably associated with each work perimeter. At least one transfer station area is provided between adjacent work perimeters to facilitate robotic transfer of sample holders from one work perimeter to another area. Each work perimeter typically includes a plurality of defined station locations, with each station location positioned to be accessible by the robot associated with that area. In addition, each station location is typically configured to receive a device, such as an automated instrument or a holding nest. Device components are arranged at selected station locations according to specific application requirements to provide a flexible, robust, reliable, and accurate high throughput processing system.10-16-2008
20080250516Prohormone Convertase 1 Mutation Associated with Obesity - The invention provides novel prohormone convertase 1 mutants that have at least partially defective enzymatic activities. These mutant PC1 enzymes are defective in their autocatalytic activities, but appear to have normal ability in processing proGHRH to its mature form. Also provided in the invention are non-human animals that harbor such a mutant PC1 gene. These non-human animals are obese due to the mutant PC1 gene.10-09-2008
20080242838LABELING REAGENT AND METHODS OF USE - The present invention provides compounds which are useful as multifunctional labels in proteomics studies. The labels of the present invention are both lysine specific and increase the overall sequence coverage obtained in polypeptide mapping experiments, by for example, increasing the ionization efficiencies of lysine-terminated tryptic fragments. In certain aspects, the labels of the present invention can be used to measure differential quantitation, as for example, deuterium(s) can easily be introduced during their synthesis. In one aspect, a C-terminal derivatized lysine biases the fragment ion intensities strongly toward C-terminal fragment ions, resulting in a highly simplified tandem mass spectrum. In further aspects, the number of lysine residues can be determined in a polypeptide.10-02-2008
20080242671INHIBITORS OF CATHEPSIN S - The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.10-02-2008
200802277835-Substituted Thiazol-2-Yl Amino Compounds and Compositions as Protein Kinase Inhibitors - The invention provides 5-substituted thiazol-2-yl amino compounds of Formula (I): pharmaceutical compositions comprising such compounds and the use of such compounds for the treatment or prevention of diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of Ab 1, Aurora-A, Ber-Ab1, Bmx, CDKI/cyclinB, CHK2, Fes, FGFR3, Flt3, GSK3β, JNK1α1, Lck, MKK4 and TrkB kinases.09-18-2008
20080221192Compounds and Compositions as Protein Kinase Inhibitors - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC kinases.09-11-2008
20080221098COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, Bmx, c-Raf, Csk, Fes, FGFR, Flt3, Ikk, IR, JNK, Lck, Mkk, PKC, PKD, Rsk, SAPK, Syk, Trk, BTK, Src, EGFR, IGF, Mek, Ros and Tie2 kinases.09-11-2008
20080214541COMPOSITIONS AND METHODS FOR INDUCING OSTEOGENESIS - The present invention provides compositions and methods for differentiating and transdifferentiating mammalian cells into cells of an osteoblast lineage.09-04-2008

Patent applications by IRM LLC