- Amino tetrahydropyrane derivatives
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The invention provides amino tetrahydropyrane derivatives, pharmaceutically-acceptable salts, hydrates, solvates, stereoisomers and prodrugs of the amino tetrahydropyrane derivatives, a preparation method of the amino tetrahydropyrane derivatives and a pharmaceutical composition containing the compounds. A formula (I) of the amino tetrahydropyrane derivatives is as shown in the specification. The compounds are capable of inhibiting activity of DPP-IV (dipeptidyl peptidase IV) and can be used for treating dipeptidyl peptidase IV associated diseases such as diabetes, obesity and other metabolic diseases.
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Paragraph 0173-0175
(2017/08/28)
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- Inhibitor for dipeptidyl peptidase-IV
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The invention provides an aminotetrahydropyran derivative with a general formula (I) as described in the specification, pharmaceutically acceptable salts, hydrates, solvates and stereoisomers thereof, a preparation method for the aminotetrahydropyran derivative, and a pharmaceutical composition containing the aminotetrahydropyran derivative. The aminotetrahydropyran derivative provided by the invention can inhibit the activity of dipeptidyl peptidase-IV(DPP-IV), and can be used for treatment of diseases related to dipeptidyl peptidase-IV, especially for treatment of diabetes.
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Paragraph 0111; 0112
(2017/08/28)
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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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- 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 59
(2011/04/14)
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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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- 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 57
(2011/09/19)
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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 10
(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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