114 results about "Syk" patented technology

The present invention provides a compound of formula I: or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3, Aurora2, and Syk mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.

The present invention relates to novel compounds of formula (I)that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and / or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

The present invention provides methods and compositions for attenuating expression of Spleen Tyrosine Kinase, Syk. In general, the described methodology involves the use of RNAi constructs that are targeted to a Syk mRNA sequence.

The present invention provides compounds of formula I:These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK2, SRC, SYK, and Aurora-2. Accordingly, compounds and compositions of the invention are useful for treating or lessening the severity of a variety of disorders, including, but not limited to, heart disease, diabetes, Alzheimer's disease, immunodeficiency disorders, inflammatory diseases, allergic diseases, autoimmune diseases, destructive bone disorders such as osteoporosis, proliferative disorders, infectious diseases and viral diseases.

The present invention is directed to compounds of formula (I)-(II) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and / or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and / or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and / or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

Disclosed is an aminopyridine compound represented by the formula (I) below or a salt thereof. Also disclosed is an Syk inhibitor containing such a compound or salt as an active constituent. In the formula (I) below, X<1>, X<2>, X<3>, Z, Y<1> and Y<2> respectively represent a carbon atom or a nitrogen atom; R, R<1>, R<5> and R<6> respectively represent a hydrogen atom, an alkyl group or the like; and R<7> represents a hydrogen atom, a halogen atom, a nitro group, a cyano group, -CpH2(p1)(R)(R)-O-R, -C(=O)-R, a five-membered or six-membered saturated heterocyclic group, an aromatic heterocyclic group, -N(R )(R ) or the like. The aminopyridine compound has not only high Syk inhibitory activity but also characteristics of selectively inhibiting Syk. C07D 409 / 14 A61K 31 / 4436 A61K 31 / 4439 A61K 31 / 444 A61K 31 / 4545 A61K 31 / 496 A61K 31 / 506 A61K 31 / 5377 A61K 31 / 541 A61P 11 / 06 A61P 17 / 00 A61P 19 / 02 A61P 25 / 00 A61P 27 / 02 A61P 27 / 16 A61P 29 / 00 A61P 35 / 00 A61P 35 / 02 A61P 37 / 02 A61P 37 / 08 A61P 43 / 00 C07D 417 / 14 C07D 413 / 14 0 343 63 2006 / 2 / 24 101166734 2008 / 4 / 23 000000000 Japan Tobacco Inc. Japan Kodama Yoshitoshi Noji Satoru Imamura Katsuaki Mizojiri Ryo Aoki Kenta Takagi Hideo Naka Yuichi Ito Goro Shinoda Kiyotaka Fujiwara Akihito Kurihara Kazunori Tanaka Masaru ligui liang 11021 The Patent Agency of the Chinese Academy of Sciences Inside the Chinese Academy of Sciences, No.52 Sanlihe Road, Fuwai, Beijing 100864 Japan 2005 / 2 / 28 052469 / 2005 United 2005 / 3 / 4 60 / 658,885 Japan 2006 / 1 / 19 011751 / 2006 United 2006 / 1 / 27 60 / 763,045 2007 / 10 / 17 PCT / JP2006 / 304034 2006 / 2 / 24 WO2006 / 093247 2006 / 9 / 8 Japanese

Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and / or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and / or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and / or JAK kinase activity, such as cardiovascular disease, inflammatory disease, autoimmune disease and cell proliferative disorder, thrombosis, allergy, asthma, rheumatoid arthritis, leukemia, or non-Hodgkin's lymphoma. The formula I-II is shown in the description.

Compounds, particularly compounds having spleen tyrosine kinase (Syk) inhibition activity, having the following structure:or a pharmaceutically acceptable salt thereof,wherein R1 is structure (a), (b), (c) or (d):and Ra, Rb, Rc, R2, R3, R4, R5, R6 and R7 are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed, as well as uses of the same to treat a condition or disorder mediated by a Syk and / or JAK kinase.

The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFRβ, PDGFRα or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.

The invention comprises for methods of identifying pharmacophores based on the spleen tyrosine kinase (SYK) protein or fragment thereof. The invention further provides methods of identifying SYK inhibitors using pharmacophores that are identified from co-crystals of SYK and its ligands. Further, the invention comprises methods of inhibiting SYK comprising contacting the residues lining the binding site with an inhibitor compound identified from pharmacophores.

The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods ofinhibilion the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as cardiovascular disease, inflammatory disease and autoimmune disease and cell proliferative disorder. Formula (I) Y1 is selected from the group consisting of: (a) and (b); Z is O or S; D1 is selected from the group consisting of: (a) phenyl substituted with a group, R5 (b) naphthyl (c) C3-8cycloalkyl (d) heteroaryl (e) heterocyclyl.

The invention relates to pharmaceutical formulations containing combinations of ciclesonide and a syk inhibitor and the use of such pharmaceutical compositions in medicine, in particular in the prophylaxis and treatment of respiratory disease.

The invention provides certain 3-pyridyl carboxamide-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.

The invention provides certain amino-pyridine-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R3, R4, R5, R6, and the subscript n are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.

The invention provides certain substituted diazine and triazine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.

The present invention provides crystalline molecules and molecular complexes that comprise binding pockets of Sykcat and its homologues. The invention also provides crystals comprising the catalytic domain of Syk protein. The invention further provides a computer comprising a data storage medium encoded with the structure coordinates of Sykcat binding pockets and methods for using a computer to evaluate the ability of a chemical entity or compounds to bind to a crystalline molecule or molecular complex of the invention. This invention also provides methods of using the structure coordinates to solve the structure homologous proteins or protein complexes. The invention further provides methods of using the structure coordinates to screen for, design and optimize chemical entities or compounds, including inhibitory compounds, that bind to the catalytic domain of Syk or homologues thereof.

The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.

The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.

The present invention provides novel imidazole analogs of Formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

The present invention is concerned with substituted azole derivatives that selectively modulate, regulate, and / or inhibit signal transduction mediated by certain native and / or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. In particular, several of these compounds are potent and selective Flt-3 inhibitors or / and syk inhibitors.

The present invention relates to ophthalmic compositions comprising inhibitors of spleen tyrosine kinase (syk). The compositions are particularly well suited for the treatment of ophthalmic infection such as fungal keratitis. The compositions optionally comprise an antiinfective compound such as an antibacterial or antifungal compound. The present invention also relates to methods for treating fungal keratitis using compositions comprising syk inhibitors.