Sugen Incorporated

Xcovery Holding Company LLC

The Scripps Research Institute

Pharmacia & Upjohn Company

Tyrogenex, Inc.

Other

Agouron Pharmaceuticals, Inc.

Equinox Sciences, LLC

Hangzhou Highlightll Pharmaceutical Co., Ltd.

Xcovery Holdings Company, LLC

Tll Pharmaceutical, LLC

Lysoway Therapeutics, Inc.

Xcovery Holding, LLC

Xcovery Holdings, Inc.

Betta Pharmaceuticals Co., Ltd.

Congxin Liang

Peng Cho Tang

Li Hsiang Sun

Chung Chen Wei

Tomas Vojkovsky

Huiping Guan

Zhigang Li

Todd Anthony Miller

Asaad S Nematalla

Jingrong Jean Cui

Xiaoyuan Li

Connie Li Sun

Paul M Herrinton

Michael A Mauragis

Shahrzad Shirazian

Gerald McMahon

Ping Huang

Marcel Koenig

Michael John Hawley

Ming Qi

Shu Gao

Klaus Peter Hirth

Yuanjun He

G Davis Harris, Jr

Ngoc My Tran

Anh Thi Nguyen

Qingwu Jin

Qingwu (Alan) Jin

Pen Cho Tang

Lihua Xie

Par Holmberg

Wei He

Steven Huy Do

John Yudhistir Ramphal

Matthew N Mattson

G Davis Harris

Fang-Jie Zhang

Yangbo Feng

Robert A Blake

Pär Holmberg

Laibao Wang

Haihui Liu

Kenneth E Lipson

Yongbin Ma

The invention discloses polymorphic forms of a compound of formula I, pharmaceutical compositions containing same, preparation method therefor and use thereof. The compound of formula I of the present invention is as shown in formula I, of which the crystalline form can be crystalline form 1, crystalline form 2, crystalline form 3, crystalline form 5, crystalline form 6 or crystalline form 7. All the crystalline forms of the compound of formula I in the present invention have good crystalline stability and chemical stability and a decrease in purity of their main ingredient less than 2%. The preparation method of the present invention may be used to produce the various crystalline forms of the compound of formula I with high purity, and suitable for large scale production.

Polymorphic forms of kinase inhibitor compound, pharmaceutical composition containing same, preparation method therefor and use thereof

Provided is a method for synthesizing a compound 2-[(2R,5S)-5-[2-[(R)-1-hydroxyethyl]furo[3,2-b]imidazo[4,5-d]pyridin-1-yl]tetrahydropyran-2-yl]acetonitrile as a selective JAK1/TYK2 kinase inhibitor. The compound is prepared by nucleophilic substitution, palladium on carbon reduction, and cyclization reaction using 7-chloro-6-nitrofuro[3,2-b]pyridine as a starting material. The synthesis method has mild reaction conditions, high product yield, and high purity, and is suitable for industrial production. Further provided are a crystal form of the compound, crystal forma of its salts, and their preparation methods. The crystal form of the compound and the crystal forms of its salts have good physical and chemical properties and are suitable for drug development.

Synthesis method of furoimidazopyridine compound, crystal form of furoimidazopyridine compound, and crystal form of salt thereof

The new 1H-furo[3,2-b]imidazo[4,5-d]pyridine derivatives are selective Jak1 kinase inhibitors useful in treating disorders related to Jak1 activities such as autoimmune diseases or disorders, inflammatory diseases or disorders, and cancer or neoplastic diseases or disorders.

Jak1 selective inhibitors and uses thereof

The invention discloses polymorphic forms of a compound of formula I, pharmaceutical compositions containing same, preparation method therefor and use thereof. The compound of formula I of the present invention is as shown in formula I, of which the crystalline form can be crystalline form 1, crystalline form 2, crystalline form 3, crystalline form 5, crystalline form 6 or crystalline form 7. All the crystalline forms of the compound of formula I in the present invention have good crystalline stability and chemical stability and a decrease in purity of their main ingredient less than 2%. The preparation method of the present invention may be used to produce the various crystalline forms of the compound of formula I with high purity, and suitable for large scale production. 

Provided are a compound as represented by structural formula (I) ({5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-6-aminopyridazin-3-yl}-N-{4-[((3S,5R)-3,5-di methylpiperazinyl)carbonyl]phenyl}carboxamide hydrochloride) and a novel crystalline form of a hydrate or solvate of the compound. Further provided are a manufacturing method of the compound and crystalline form, a related intermediate, a pharmaceutical composition comprising the compound, an application using the compound or the crystalline form for preparing a pharmaceutical product for treating a disease, symptom, or disorder, and a therapeutic method for treating a disease, symptom, or disorder. 

Crystalline form of compound suppressing protein kinase activity, and application thereof

The new piperazine derivatives are modulators of TRPML and are useful in treating disorders related to TRPML activities such as lysosome storage diseases, muscular dystrophy, age-related common neurodegenerative diseases, oxidative stress or reactive oxygen species (ROS) related diseases, and ageing.

Piperazine derivatives as TRPML modulators

JAK1 selective inhibitors and uses thereof

The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.

Inhibitors of focal adhesion kinase

Pyridazine derivatives (e.g., Formula I) have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer. 

Substituted pyridazinecarboxamides as kinase inhibitors

The new pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases especially against c-Met and are useful in treating disorders related to abnormal protein kinase activities such as cancer.

Substituted pyridazine carboxamide compounds as kinase inhibitor compounds

The new pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases especially against ALK and are useful in treating disorders related to abnormal protein kinase activities such as cancer, neurological and psychiatric diseases.

Substituted pyridazine carboxamide compounds

The 4-urea-phenyl substituted 6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidine derivatives are potent and selective inhibitors of mTOR kinase and are useful in treating disorders related to abnormal mTOR activities such as cancer, immune disorders, cardiovascular disease, ocular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.

mTOR selective kinase inhibitors

Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.

6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidine and 2-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidine derivatives have unexpected drug properties as inhibitors of PI3 and/or mTOR kinases and are useful in treating disorders related to abnormal PI3K/mT0R activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.

PI3K/mTOR kinase inhibitors

Novel PI3K, especially PI3K delta isoform, selective inhibitors are disclosed. The compounds are useful in treating disorders related to abnormal PI3K or PI3K&#x3b4; activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.

PI3K (delta) selective inhibitors

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Congxin Liang