- COMPOUNDS AND THEIR USES AS SPLEEN TYROSINE KINASE INHIBITORS
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Provided are compounds of Formula (I) which can be used as Syk inhibitors and potently as therapeutic agents against diseases mediated by Syk.
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Paragraph 0085
(2021/12/28)
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- A class of FLT3 kinase inhibitors, preparation and application thereof
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The invention relates to a class of FLT3 kinase inhibitors, preparation and application thereof, wherein specifically the compound has a structure represented by a formula (I), and all groups and substituents are defined in the specification. The invention also discloses a preparation method of the compound, and application of the compound in inhibition of FLT3.
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- QUINOLINE AND QUINAZOLINE COMPOUNDS AND METHODS OF USE THEREOF
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Compounds and methods for their preparation and use as therapeutic or prophylactic agents, fo example for treatment of cancer, bacterial or viral diseases by targeting Ectonucleotide Pyrophosphatase/Phosphodiesterase- 1 (ENPP1).
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- PYRROLONE OR PYRROLIDINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
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The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are melanin concentrating hormone receptor-1 (MCHR1) antagonists which may be used as medicaments.
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- VEGFR TYROSINE KINASE INHIBITORS
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Novel compounds, their prodrugs, and the pharmaceutically acceptable salts as pharmaceutical compositions containing such compounds useful in treating certain diseases modulated by the inhibition of vascular endothelial growth factors (VEGFs) receptor tyrosine kinases are provided. In particular, compounds and compositions and the methods for the prophylaxis, management and treatment of cancers through the inhibition of VEGF receptor tyrosine kinases are provided.
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Page/Page column 32
(2014/12/12)
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- IMIDAZOPYRAZINE SYK INHIBITORS
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Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suf-fering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or dis-order are provided.
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- Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors
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The insulin-like growth factor-1 receptor (IGF-1R) plays an important role in the regulation of cell growth and differentiation, and in protection from apoptosis. IGF-1R has been shown to be an appealing target for the treatment of human cancer. Herein, w
- Buchanan, John L.,Newcomb, John R.,Carney, David P.,Chaffee, Stuart C.,Chai, Lilly,Cupples, Rod,Epstein, Linda F.,Gallant, Paul,Gu, Yan,Harmange, Jean-Christophe,Hodge, Kathy,Houk, Brett E.,Huang, Xin,Jona, Janan,Joseph, Smriti,Jun, H. Toni,Kumar, Rakesh,Li, Chun,Lu, John,Menges, Tom,Morrison, Michael J.,Novak, Perry M.,Van Der Plas, Simon,Radinsky, Robert,Rose, Paul E.,Sawant, Satin,Sun, Ji-Rong,Surapaneni, Sekhar,Turci, Susan M.,Xu, Keyang,Yanez, Evelyn,Zhao, Huilin,Zhu, Xiaotian
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p. 2394 - 2399
(2011/05/15)
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- COMBINATION THERAPY OF SUBSTITUTED OXAZOLIDINONES
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The present invention relates to combinations of A) oxazolidinones of the formula (I) with B) acetylsalicylic acid (aspirin) and C) an ADP receptor antagonist, in particular P2Y12 purinoreceptor blocker, to a process for producing these combinations and to the use thereof as medicaments, in particular for the prophylaxis and/or treatment of thromboembolic disorders.
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- MICROANGIOPATHY TREATMENT AND PREVENTION
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The present invention relates to the use of selective factor Xa inhibitors, in particular of oxazolidinones of the formula (I) for the treatment and/or prophylaxis of microangiopathies and also their use for the production of medicaments for the treatment and/or prophylaxis of microangiopathies.
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- Combination Therapy Comprising Substituted Oxazolidinones for the Prevention and Treatment of Cerebral Circulatory Disorders
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The present invention relates to combinations of A) oxazolidinones of the formula (I), with B) antiarrhythmics, processes for the production of these combinations, their use for the prophylaxis and/or treatment of diseases, and their use for the manufacture of medicaments for the prophylaxis and/or treatment of diseases, especially of thromboembolic disorders and/or complications.
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- 4-ARYL-2-AMINO-PYRIMIDINES OR 4-ARYL-2-AMINOALKYL-PYRIMIDINES AS JAK-2 MODULATORS AND METHODS OF USE
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This invention relates to certain pyrimidine derivative inhibitors of JAK-2, having Formula (I): wherein D, E, L, Z, R1, R2, R25, and n1 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 236
(2008/06/13)
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- THIAZOLOPYRIDINONE DERIVATES AS MCH RECEPTOR ANTAGONISTS
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The present invention relates to a melanin concentrating hormone antagonist compound of formula (I); wherein w, R1, q, p, R2, t, Ar1, L1, R3 and R4 are as defined, or a pharmaceutically acceptable salt, solvate, or enantiomer thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.
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Page/Page column 61
(2008/06/13)
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- MORPHOLINYLANILINOQUINAZO- LINE DERIVATIVES FOR USE AS ANTIVIRAL AGENTS
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Compounds of formula (Ia) are found to be active in inhibiting replication of flaviviridae viruses, wherein R1, R2, R3 and R4 are as defined in the claims.
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- Substituted oxazolidinones and their in the field of blood coagulation
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The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
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- Amino-substituted pyrimidinyl derivatives and methods of use
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The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer.
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