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NERVIANO MEDICAL SCIENCES S.R.L.

NERVIANO MEDICAL SCIENCES S.R.L. Patent applications
Patent application numberTitlePublished
20120122882Substituted Pyrrolo-Pyrimidine Derivatives, Process for Their Preparation and Their Use as Kinase Inhibitors - Substituted pyrrolo-pyrimidine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer.05-17-2012
20120121716PHARMACEUTICAL COMPOSITION OF AN ANTHRACYCLINE - The present invention relates to pharmaceutical composition containing nemorubicin hydrochloride incorporated in microspheres. The compositions are useful for chemoembolisation, particularly for loco regional treatment of tumors.05-17-2012
20120114641THERAPEUTIC COMBINATION COMPRISING A PLK1 INHIBITOR AND AN ANTINEOPLASTIC AGENT - The present invention provides a combination comprising (a) a compound of formula (I) and (b) one or more antineoplastic agents selected from the group consisting of an antimetabolite agent, analkylating or alkylating-like agent, an intercalating agent, a topoisomerase I or II inhibitor, an antimitotic agent, a kinase inhibitor, a proteasome inhibitor and an antibody inhibiting a growth factor or its receptor, wherein active ingredients of the combination are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate or solvate thereof, useful in the treatment of tumors.05-10-2012
20120077819USE OF KINASE INHIBITOR FOR THE TREATMENT OF THYMOMA - The invention provides a low molecular weight ATP-competitive CDK inhibitor and TRKA inhibitor of formula (I) for use in the treatment of thymoma and thymic carcinoma. The compound can be administered together with one or more cytotoxic or cytostatic agents.03-29-2012
20120065192N-ARYL-2-(2-ARYLAMINOPYRIMIDIN-4-YL)PYRROL-4-CARBOXAMIDE DERIVATIVES AS MPS1 KINASE INHIBITORS - The present invention relates to substituted pyrrolyl-pyrimidines which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular MPS1. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.03-15-2012
20120046266RESORCINOL DERIVATIVES AS HSP90 INHIBITORS - The present invention relates to substituted resorcinol derivatives which inhibit the activity of Heat Shock Protein HSP90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, pharmaceutical compositions comprising them, methods of treating diseases and the pharmaceutical compositions comprising these compounds.02-23-2012
20120041007CDK INHIBITOR SALTS - The present invention relates to novel crystalline form(s) of water-soluble salts and of free base of a cdk inhibitor. Such crystal salts are for example fumarate, L-malate, maleate, succinate, adipate, malonate, glycolate, phosphate, mesylate, L-lactate, hydrochloride, di-hydrochloride, tri-hydrochloride. Hydrates and polymorphs of such new salt forms, a process for their preparation, their utility in therapy and to the pharmaceutical compositions containing them are also claimed and described in the present application.02-16-2012
20110312909THERAPEUTIC COMBINATION COMPRISING A CDKS INHIBITOR AND AN ANTINEOPLASTIC AGENT - The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of alkylating or alkylating-like agents, antimetabolite agents and topoisomerase I inhibitors, wherein the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.12-22-2011
20110294790BICYCLIC PYRAZOLE AND ISOXAZOLE DERIVATIVES AS ANTITUMOR AND ANTINEURODEGENERATIVE AGENTS - Bicyclic pyrazole and isoxazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases mediated by HSP90 protein, like cancer and neurodegenerative disorders.12-01-2011
20110281843SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.11-17-2011
20110257165BICYCLIC PYRAZOLES AS PROTEIN KINASE INHIBITORS - 3,4-diaryl-bicyclicpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.10-20-2011
201102511793,4-DIHYDRO-2H-PYRROLO[1,2-a]PYRAZIN-1-ONE DERIVATIVES - Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.10-13-2011
20110230470SUBSTITUTED PYRAZOLO[4,3-C]PYRIDINE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted pyrazolo[4,3-c]pyridine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer.09-22-2011
20110224222CDK INHIBITOR FOR THE TREATMENT OF MESOTHELIOMA - The invention provides a low molecular weight ATP-competitive CDK inhibitor for use in the treatment of mesothelioma. The compound can be administered together with one or more cytotoxic or cytostatic agents.09-15-2011
20110190311USE OF CDK INHIBITOR FOR THE TREATMENT OF GLIOMA - The invention provides a low molecular weight ATP-competitive CDK inhibitor able to cross the blood brain barrier for use in the treatment of malignant glioma and, in particular, of glioblastoma. The compound can be administered together with one or more agents selected from the group consisting of cytotoxic or cytostatic agents and ionizing radiation.08-04-2011
201101839713,4-DIHYDRO-2H-PYRAZINO[1,2-A]INDOL-1-ONE DERIVATIVES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM - Compounds which are 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.07-28-2011
201101440683,4-DIARYLPYRAZOLES AS PROTEIN KINASE INHIBITORS - 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.06-16-2011
20110129467THERAPEUTIC COMBINATION COMPRISING AN AURORA KINASE INHIBITOR AND ANTIPROLIFERATIVE AGENTS - The present invention provides a combination comprising a compound 1 of formula (A) and one or more antineo-plastic agents selected from the group consisting of an antibody inhibiting a growth factor or a receptor of the growth factor, a proteasome inhibitor or a derivative or prodrug thereof, and a kinase inhibitor or a derivative or prodrug thereof useful in the treatment of tumors.06-02-2011
20110118278CARBAMOYL DERIVATIVES OF BICYCLIC CARBONYLAMINO-PYRAZOLES AS PRODRUGS - There are provided bicyclic carbonylamino-pyrazoles of formula (I), wherein the variables are as specified in the claims, for use as medicament, in particular for the treatment of diseases due to the malfunctioning of protein kinases (PKs), such as cancer, pharmaceutical compositions comprising such carbamoyl derivatives, and their use as prodrugs of therapeutically active agents. Method of treatment and some new bicyclic carbonylamino-pyrazoles are also object of the present invention.05-19-2011
20110117212THERAPEUTIC COMBINATION COMPRISING AN AURORA KINASE INHIBITOR AND AN ANTINEOPLASTIC AGENT - The present invention provides a therapeutic combination comprising (a) compound 1 of formula (A) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of platinum derivatives, antimetabolite agents, topoisomerase I inhibitors and antimicrotubule agents, wherein the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.05-19-2011
20110105542PYRAZOLO--QUINAZOLINES - The present invention relates to pyrazolo-quinazolines, characterized by an ortho-substituted-arylamino, heterocyclylamino- or C05-05-2011
20110053944SUBSTITUTED DIHYDROPTERIDIN-6-ONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS - Dihydropteridin-6-one derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.03-03-2011
20110040090PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES - The present invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. 5-(2-Amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides are described and claimed in W02007110344, which also discloses processes for their preparation. These compounds can be advantageously prepared through a process which allows to obtain the desired products in high yields and purity and with a limited number of steps. The synthesis is starting from a cyano pyrrole derivative, and is characterized from the final hydrolysis of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carbonitrile. The compounds prepared according to the process of the present invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are therefore useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.02-17-2011
20110021517ANTITUMOR COMBINATION COMPRISING A MORPHOLINYL ANTHRACYCLINE DERIVATIVE AND DEMETHYLATING AGENTS - The present invention provides a combination of a morpholinyl anthracycline derivative, in particular a methoxy morpholino doxorubicin derivative, or a pharmaceutically acceptable salt thereof, and a demethylating agent, having an antineo-plastic effect. Also provided is the use of the said combinations in the treatment or prevention of metastasis, in the treatment of tumors, as well for reversing the resistance in cells resistant to such a methoxy morpholino doxorubicin derivative.01-27-2011
20100292207SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.11-18-2010
20100216808SUBSTITUTED PYRAZOLO-QUINAZOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS - Pyrazolo-quinazoline derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.08-26-2010
20100197665INDAZOLE DERIVATIVES AS KINASE INHIBITORS FOR THE TREATMENT OF CANCER - Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer formula (I).08-05-2010
20100190736MORPHOLINYL ANTHRACYCLINE DERIVATIVE COMBINED WITH PROTEIN KINASE INHIBITORS - The present invention provides the combined use of a morpholinyl anthracycline derivative of formula (I) as defined in the specification or a pharmaceutically acceptable salt thereof, such as nemorubicin hydrochloride, and a protein kinase (PK) inhibitor, in the treatment of tumors. Also provided is the use of the said combinations in the treatment or prevention of metastasis or in the treatment of tumors by inhibition of angiogenesis.07-29-2010
20100104566ANTITUMOR COMBINATION COMPRISING A MORPHOLINYL ANTHRACYCLINE AND AN ANTIBODY - The present invention provides the combined use of a morpholinyl anthracycline derivative of formula (I) or a pharmaceutically acceptable salt thereof, such as nemorubicin hydrochloride, and an antibody inhibiting a growth factor or its receptor, in the treatment of tumors. Also provided is the use of the said combinations in the treatment or prevention of metastasis or in the treatment of tumors by inhibition of angiogenesis.04-29-2010
20100075998TRICYCLIC INDOLES AND (4,5-DIHYDRO) INDOLES - The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, 03-25-2010
20100069317CRYSTALLINE NEMORUBICIN HYDROCHLORIDE - This invention relates to a novel crystalline polymorphic form of nemorubicin hydrochloride dihydrate, useful for the preparation of pharmaceutical composition for the treatment of tumors. A process for preparing this novel polymorphic form, named form A, is within the scope of the present invention.03-18-2010
20100056556ISOQUINOLINOPYRROLOPYRIDINONES ACTIVE AS KINASE INHIBITORS - Heteroarylpyridinone derivatives represented by formula (I) wherein R03-04-2010
20100035876Use of a Kinase Inhibitor for the Treatment of Particular Resistant Tumors - The invention provides low molecular weight compounds, namely tetrahydropyrrolo[3,4-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.02-11-2010
20100022553Therapeutic Combination Comprising an Aurora Kinase Inhibitor and Imatinib - The present invention provides a therapeutic combination comprising (a) a compound 1 of formula (A) as set forth in the specification and (b) a BCR-ABL kinase inhibitor selected from the group consisting of Imatinib, Dasatinib, Nilotinib, Bosutinib and Inno-406, wherein the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.01-28-2010
20100022532USE OF A KINASE INHIBITOR FOR THE TREATMENT OF PARTICULAR RESISTANT TUMORS - The invention provides low molecular weight compounds, namely 1H-thieno[2,3-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.01-28-2010
20100010008SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES AS KINASE INHIBITORS - Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.01-14-2010
200902399241H-FURO[3,2-C]PYRAZOLE COMPOUNDS USEFUL AS KINASE INHIBITORS - Furo[3,2-c]pyrazole derivatives of formula (I) as defined in the description, and pharmaceutically acceptable salts thereof, wherein A is an aryl or heteroaryl ring, —NHZR09-24-2009
20090163503SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.06-25-2009
200901494571H-Thieno[2,3-c]Pyrazole Compounds Useful as Kinase Inhibitors - There are provided thieno[2,3-c]pyrazole derivatives of formula (I), wherein A is an aryl or heteroaryl ring, on which the substituent-NHZR06-11-2009
20090136513BICYCLO-PYRAZOLES ACTIVE AS KINASE INHIBITORS - A compound having formula (I): wherein: R, A, R05-28-2009
20090124605Pyrazolo-Quinazoline Derivatives, Process for Their Preparation and Their Use as Kinase Inhibitors - Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.05-14-2009
20090099221PYRIDYL-AND PYRIMIDINYL-SUBSTITUTED PYRROLE-, THIOPHENE-AND FURANE-DERIVATIVES AS KINASE INHIBITORS - The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R04-16-2009
20090023745Substituted Pyrazolo[4,3-c]Pyridine Derivatives Active as Kinase Inhibitors - Substituted pyrazolo[4,3-c]pyridine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer.01-22-2009
20090017025Combinations Comprising a CDK Inhibitor and a Growth Factor Antibody or Anti-Mitotic - The present invention provides a combination comprising a compound A of formula (I) as set forth in the specification or a pharmaceutically acceptable salt thereof, and an antibody inhibiting a growth factor or its receptor and/or an antimitotic agent or a derivative or prodrug thereof, useful in the treatment of tumors. The chemical name of compound A is 8-[4-(4-methyl-piper-azin-1-yl)-phenylamino]-1,4,4-trimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid methylamide.01-15-2009

Patent applications by NERVIANO MEDICAL SCIENCES S.R.L.