- COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS
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The invention relates to a compound of Formula I, pharmaceutical compositions comprising a compound of Formula I, and pharmaceutically acceptable slats thereof, pharmaceutical compositions comprising such compounds and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I to a subject in need thereof.
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Page/Page column 159
(2020/08/22)
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- Preparation and application of novel 4,6-disubstituted aminopyrimidine JAK (janus kinase) inhibitor
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The invention discloses preparation and application of novel 4,6-disubstituted aminopyrimidine JAK (janus kinase) inhibitors, and provide drugs which can be used for preventing, treating and/or improving autoimmune diseases (for example, psoriasis, rheumatoid arthritis, inflammatory enteritis diseases, Jagren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus, etc.), and have excellent JAK inhibitory activity. The invention also provides pharmaceutically acceptable composition containing the compounds and methods for preparing the compounds.
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Paragraph 0202-0207
(2019/05/08)
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- SULPHONYL UREA DERIVATIVES AS NLRP3 INFLAMMASOME MODULATORS
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The present disclosure relates to compounds of Formula (I): (I) and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
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Paragraph 0857
(2019/07/13)
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- Substitutive phenyl pyrimidine derivative as JAK kinase inhibitor or medicinal salt, preparation method and application thereof
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The invention discloses a substitutive phenyl pyrimidine derivative as shown in a formula (I) as a JAK kinase inhibitor or medicinal salt, a preparation method and application thereof. The compound has excellent JAK inhibiting action and is used for preparing a drug for preventing, treating or improving autoimmune disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus and the like. The high activity JAK-3 inhibiting action IC50 shown by the compound can reach 1.7 n. The substitutive phenyl pyrimidine derivative is simple in synthetic route and high in implementation.
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Paragraph 0076; 0086; 0087; 0089; 0090
(2019/10/23)
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- HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY
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Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X, X, and Xare N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I foranddiagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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Paragraph 1084; 1086
(2015/11/16)
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- BIARYL COMPOUNDS USEFUL FOR THE TREATMENT OF HUMAN DISEASES IN ONCOLOGY, NEUROLOGY AND IMMUNOLOGY
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The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
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Paragraph 0280
(2015/06/25)
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- Five-And-Six-Membered Heterocyclic Compound, And Preparation Method, Pharmaceutical Composition And Use Thereof
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A five-and-six-membered heterocyclic compound as represented by general formula I, pharmaceutically acceptable salt, metabolite, metabolic precursors or drug precursors thereof, preparation method, pharmaceutical composition, and use thereof; the five-and-six-membered heterocyclic compound has activity as a Janus kinase (JAK) inhibitor, and can be used to prepare drugs for treating diseases caused by the abnormal activity of kinase, such as cell proliferation diseases like cancer.
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Paragraph 0329; 0330
(2015/12/07)
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- COMPOUNDS USEFUL AS CCR9 MODULATORS
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The present invention relates to compounds useful as CCR9 modulators, to compositions containing them, to methods of making them, and to methods of using them. In particular, the present invention relates to compounds capable of modulating the function of the CCR9 receptor by acting as partial agonists, antagonists or inverse agonists. Such compounds may be useful to treat, prevent or ameliorate a disease or condition associated with CCR9 activation, including inflammatory and immune disorder diseases or conditions such as inflammatory bowel diseases (IBD).
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Page/Page column 136; 137
(2015/07/15)
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- QUINOLINE AND ISOQUINOLINE COMPOUNDS AND METHODS OF USE THEREOF
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Provided herein are compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds a
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Page/Page column 103
(2012/03/26)
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- QUINAZOLINE COMPOUNDS AND METHODS OF USE THEREOF
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Provided herein are quinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
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Page/Page column 57
(2012/03/12)
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- CYSTEINE PROTEASE INHIBITORS
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Compounds of the formula (I) wherein One of A1 and A2 is N-CH3 and the other is CH; R1 is C1-C6alkyl, C1-C6haloalkyl, C3-C6cycloalkyl or oxetan-3-yl, wherein C3-C6cycloalkyl is optionally substituted with one, two or three fluoro or with CF3; R2a and R2b are independently selected from H, halo, C1-C4alkyl, C1-C4haloalkyl and C1- C4alkoxy; R3 is CH3 or F; n is 1, 2, 3 or 4; or a pharmaceutically acceptable salt, hydrate or N-oxide thereof for the use in the prophylaxis and/or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
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Page/Page column 28
(2013/02/28)
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- HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS JAK INHIBITORS
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The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
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Page/Page column 201
(2011/05/06)
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- HETEROCYCLIC JAK KINASE INHIBITORS
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The present invention relates to compounds of Formula (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer
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Page/Page column 69
(2010/04/27)
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- Potent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer's disease
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Utilizing structure-based drug design, a 4-aminoimidazole heterocyclic core was synthesized as a replacement for a 2-aminothiazole due to potential metabolically mediated toxicity. The synthetic route utilized allowed for ready synthesis of 1-substituted-4-aminoimidazoles. SAR exploration resulted in the identification of a novel cis-substituted cyclobutyl group that gave improved enzyme and cellular potency against cdk5/p25 with up to 30-fold selectivity over cdk2/cyclin E.
- Helal, Christopher J.,Kang, Zhijun,Lucas, John C.,Gant, Thomas,Ahlijanian, Michael K.,Schachter, Joel B.,Richter, Karl E.G.,Cook, James M.,Menniti, Frank S.,Kelly, Kristin,Mente, Scot,Pandit, Jay,Hosea, Natalie
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scheme or table
p. 5703 - 5707
(2010/04/30)
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- TRICYCLIC 2,4-DIAMIN0-L,3,5-TRIAZINE DERIVATIVES USEFUL FOR THE TREATMENT OF CANCER AND MYELOPROLIFERATIVE DISORDERS
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The present invention relates to compounds of Formula (I): (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer.
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Page/Page column 68
(2010/01/07)
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- A convenient route to the imidazo[4,5-b]pyridines
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The reaction of the acroleins possessing a leaving group, derived from alkenyl sulfides by Vilsmeier reaction, with 4-amino-1-methylimidazole provided a new and convenient route to the imidazo[4,5-b]pyridines, the reaction mechanisms of which were examined by a deuterium labelled experiment.
- Harada, Kenichi,Choshi, Tominari,Sugino, Eiichi,Sato, Koichi,Hibino, Satoshi
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p. 213 - 218
(2007/10/02)
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- The Preparation and Properties of Partially Protected 4-Amino-1-methylimidazole-2-carboxylic Acids to be Used as Intermediates in the Synthesis of Analogues of Distamycin A
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Partially protected 4-amino-1-methylimidazole-2-carboxylic acid derivatives have been prepared by a convenient route from the corresponding nitro analogue.Such derivatives, blocked on the amino function with tert-butyloxycarbonyl (4) or formyl groups (8)
- Grehn, Leif,Ding, Lu,Ragnarsson, Ulf
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