- FUSED PYRIMIDINE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF FIBROTIC DISEASES
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The present invention discloses compounds according to Formula I: Wherein A, B, R1, R2, and Cy are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, pain, and/or abnormal angiogenesis associated diseases by administering the compounds of the invention.
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Paragraph 0282-0283
(2021/02/25)
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- MODULATORS OF AMPA RECEPTOR SIGNALING
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The present disclosure relates to compounds of the Formula (I) which have shown utility in modulating AMPA receptor signaling and thus preventing AMPA receptor-mediated toxicity, which may find use in the treatment of diseases in which AMPA receptor activ
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Paragraph 0169
(2020/09/19)
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- 2,4-Diamino-8-quinazoline carboxamides as novel, potent inhibitors of the NAD hydrolyzing enzyme CD38: Exploration of the 2-position structure-activity relationships
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Starting from 4-amino-8-quinoline carboxamide lead 1a and scaffold hopping to the chemically more tractable quinazoline, a systematic exploration of the 2-substituents of the quinazoline ring, utilizing structure activity relationships and conformational constraint, resulted in the identification of 39 novel CD38 inhibitors. Eight of these analogs were 10–100-fold more potent human CD38 inhibitors, including the single digit nanomolar inhibitor 1am. Several of these molecules also exhibited improved therapeutic indices relative to hERG activity. A representative analog 1r exhibited suitable pharmacokinetic parameters for in vivo animal studies, including moderate clearance and good oral bioavailability. These inhibitor compounds will aid in the exploration of the enzymatic functions of CD38, as well as furthering the study of the therapeutic implications of NAD enhancement in metabolic disease models.
- Deaton, David N.,Haffner, Curt D.,Henke, Brad R.,Jeune, Michael R.,Shearer, Barry G.,Stewart, Eugene L.,Stuart, J. Darren,Ulrich, John C.
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p. 2107 - 2150
(2018/03/28)
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- AMINO PYRANOID RING DERIVATIVE AND COMPOSITION AND USE THEREOF
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The present invention relates to an amino pyran ring derivative and a composition and use thereof, and in particular, to an amino pyran ring derivative represented by general formula (I) or a stereoisomer, a pharmaceutically acceptable salt or a prodrug thereof, a pharmaceutical composition comprising the derivative, and their medical use in the manufacture of a di-peptidyl peptidase IV (DPP-IV) inhibitor, in formula (I) the substituents are defined the same as those in the specification.
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Paragraph 0108; 0109
(2017/05/02)
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- Aminopyran ring derivative and its composition and application wherein the dipeptidyl peptidase IV (DPP-IV) inhibitor is used for preparing the drugs for treating metabolic diseases
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The present invention relates to an aminopyran ring derivative and its composition and application, specifically speaking, relating to the aminopyran ring derivative represented by the general formula (I) or its stereoisomer, pharmaceutically acceptable salt, prodrug, pharmaceutical composition containing the derivative and the preparation of dipeptidyl peptidase IV (DPP-IV) inhibitor for medical use, wherein the definitions of the substituents in the general formula (I) are the same as those defined in the patent specification.
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Page/Page column 40
(2017/08/22)
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- Amino six member ring derivatives and their use in medicine (by machine translation)
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The invention relates to a six-member ring amino derivatives and its application in medicine, specifically relates to the general formula (I) as shown by the six-member ring of the amino derivative or its stereoisomer, pharmaceutically acceptable salt, prodrug, pharmaceutical composition containing the derivative of the dipeptidyl peptidase IV and the preparation (dPP CGI-iV) inhibitors of their medical use, wherein the general formula (I) definition of each substituent in the definition of the description of the same. (by machine translation)
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Page/Page column 42
(2017/09/20)
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- PROCESS FOR THE PREPARATION OF OMARIGLIPTIN
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The present invention provides a process for preparing omarigliptin.
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Page/Page column 22; 23
(2017/06/23)
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- 4,6 DIHYDROPYRROLO [3,4-C] PYRAZOLE-5 (1H)-CARBONITRILE DERIVATES FOR TRATING CANCER
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The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs) and/ or desumoylating enzymes. In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 7 or
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Page/Page column 42
(2017/10/13)
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- Crystalline forms of a dipeptidyl peptidase-IV inhibitors
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Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
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Page/Page column 11
(2015/11/30)
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- Omarigliptin (MK-3102): A novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes
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In our effort to discover DPP-4 inhibitors with added benefits over currently commercially available DPP-4 inhibitors, MK-3102 (omarigliptin), was identified as a potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor with an excellent pharmacokinetic profile amenable for once-weekly human dosing and selected as a clinical development candidate. This manuscript summarizes the mechanism of action, scientific rationale, medicinal chemistry, pharmacokinetic properties, and human efficacy data for omarigliptin, which is currently in phase 3 clinical development.
- Biftu, Tesfaye,Sinha-Roy, Ranabir,Chen, Ping,Qian, Xiaoxia,Feng, Dennis,Kuethe, Jeffrey T.,Scapin, Giovanna,Gao, Ying Duo,Yan, Youwei,Krueger, Davida,Bak, Annette,Eiermann, George,He, Jiafang,Cox, Jason,Hicks, Jacqueline,Lyons, Kathy,He, Huaibing,Salituro, Gino,Tong, Sharon,Patel, Sangita,Doss, George,Petrov, Aleksandr,Wu, Joseph,Xu, Shiyao Sherrie,Sewall, Charles,Zhang, Xiaoping,Zhang, Bei,Thornberry, Nancy A.,Weber, Ann E.
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p. 3205 - 3212
(2014/05/20)
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- NOVEL CRYSTALLINE FORMS OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR
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Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
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Page/Page column 13
(2013/03/26)
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- AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
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The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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Page/Page column 58-59
(2011/04/14)
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- SUBSTITUTED AMINOTETRAHYDROTHIOPYRANS AND DERIVATIVES THEREOF AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES
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The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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Page/Page column 54-55; 56-57
(2011/09/19)
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- SUBSTITUTED SEVEN-MEMBERED HETEROCYCLIC COMPOUNDS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES
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The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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Page/Page column 52
(2011/12/04)
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- AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
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The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved
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Page/Page column 22
(2010/06/11)
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- NOVEL CRYSTALLINE FORM OF A DIHYDROCHLORIDE SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR
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The present invention relates to a novel crystalline form of the dihydrochloride salt of (2R,3S,5S)-2-(2,5-difluorophenyl)-5-(4,6-dihydropyrrolo[3,4-c]pyrazol-5(1H)-yl)tetrahydro-2H-pyran-3-amine as well as a process for its preparation, pharmaceutical compositions containing this novel form, and methods of use of the novel form and pharmaceutical compositions for the treatment of Type 2 diabetes, hyperglycemia, insulin resistance, obesity, and high blood pressure.
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Page/Page column 9
(2009/03/07)
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- Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
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The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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Page/Page column 17
(2008/06/13)
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- AMINOCYCLOHEXANES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
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The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (""DPP-IV inhibitors"") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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Page/Page column 38-39; 41
(2008/06/13)
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