- Pyrrolopyrazole derivatives and preparation method thereof, and application of pyrrolopyrazole derivatives in medicines
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The invention relates to pyrrolopyrazole derivatives and a preparation method thereof, and application of the pyrrolopyrazole derivatives in medicines. Specifically, the invention relates to novel pyrrolopyrazole derivatives as shown in a general formula (I) in the specification, the preparation method of the pyrrolopyrazole derivatives and application of the pyrrolopyrazole derivatives or pharmaceutical compositions containing the pyrrolopyrazole derivatives as therapeutic agents, particularly as gastric acid secretion inhibitors and potassium ion competitive acid blockers P-CABs) in biological medicines. All the substituents (R1, R2, R3 and R4) and groups (X and Y) in the general formula (I) are as defined in the specification.
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- Pyrrolopyrazole derivative and preparation method and medical application thereof
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The invention relates to a pyrrolopyrazole derivative and a preparation method and a medical application thereof. Specifically, the invention relates to a new pyrrolopyrazole derivative as shown in ageneral formula (I), a preparation method of the pyrrolopyrazole derivative and application of the pyrrolopyrazole derivative or a pharmaceutical composition containing the pyrrolopyrazole derivativeas a therapeutic agent, particularly as a gastric acid secretion inhibitor and potassium ion competitive acid blockers (P-CABs) in biological medicines, wherein substituents (R1, R2, R3 and R4) and groups (X) in the general formula (I) are the same as defined in the specification.
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- Pyrrolopyrazole derivatives and preparation method thereof, and application of pyrrolopyrazole derivatives in medicines
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The invention relates to pyrrolopyrazole derivatives and a preparation method thereof, and application of the pyrrolopyrazole derivatives in medicines. Specifically, the invention relates to novel pyrrolopyrazole derivatives as shown in a general formula (I) in the specification, the preparation method of the pyrrolopyrazole derivatives and application of the pyrrolopyrazole derivatives or pharmaceutical compositions containing the pyrrolopyrazole derivatives as therapeutic agents, particularly as gastric acid secretion inhibitors and potassium ion competitive acid blockers P-CABs) in biological medicines. All the substituents (R1, R2, R3, R4 and R5) and a group (X) in the general formula (I) are as defined in the specification.
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- Pyrrolopyrazole derivatives and preparation method thereof, and application of pyrrolopyrazole derivatives in medicines
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The invention relates to pyrrolopyrazole derivatives and a preparation method thereof, and application of the pyrrolopyrazole derivatives in medicines. Specifically, the invention relates to novel pyrrolopyrazole derivatives as shown in a general formula (I) in the specification, the preparation method of the pyrrolopyrazole derivatives and application of the pyrrolopyrazole derivatives or pharmaceutical compositions containing the pyrrolopyrazole derivatives as therapeutic agents, particularly as gastric acid secretion inhibitors and potassium ion competitive acid blockers (P-CABs) in biological medicines. All the substituents (R1, R2, R3 and R4) in the general formula (I) are as defined in the specification.
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- Preparation method for omarigliptin midbody
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The invention provides an efficient and simple preparation method for omarigliptin midbody pyrrole and [3,4-c] pyrazol-5(2H,4H,6H)-carboxylic acid tert-butyl ester, wherein the total recovery ratio is close to 50%. The preparation method is easy to operate, the recovery ratio is higher, three produced wastes are less, and the method is suitable for industrialized production.
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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 23
(2017/06/23)
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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 39; 40; 41
(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; 43
(2017/09/20)
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- AMINOTETRAHYDROPYRAN DERIVATIVE USED AS DIPEPTIDYL PEPTIDASE-IV INHIBITOR
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Provided is an Aminotetrahydropyran derivative represented by general formula (I), a preparation method for the derivative, a pharmaceutical composition containing the derivative, and the use of the derivative to prepare a therapeutic agent, especially a dipeptidyl peptidase-IV inhibitor.
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- Amino 6-membered ring derivative and pharmaceutical applications thereof including the use for manufacturing dipeptidyl peptidase-4(IDPP-IV) inhibitor
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The present invention relates to an amino 6-membered ring derivative and pharmaceutical applications thereof, which specifically relates to the amino 6-membered ring derivative represented by the general formula (I) or stereoisomers thereof, pharmaceutically acceptable salts thereof, a prodrug, a pharmaceutical composition comprising the derivative, and the pharmaceutical use for manufacturing dipeptidyl peptidase-4(IDPP-IV) inhibitor, wherein the definition of each substituent in the general formula (I) is the same as described in the specification.
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Page/Page column 53; 54
(2017/07/31)
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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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- PROCESS FOR PREPARING CHIRAL DIPEPTIDYL PEPTIDASE-IV INHIBITORS
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A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of, reductive amination of:.
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Page/Page column 20; 21
(2016/02/12)
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- TREATING DIABETES WITH DIPEPTIDYL PEPTIDASE-IV INHIBITORS
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The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-N 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 30
(2014/02/16)
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- PYRIDINYL AND PYRIMIDINYL SULFOXIDE AND SULFONE DERIVATIVES
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Disclosed are certain pyridinyl and pyrimidinyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds and methods of treatment using such compounds.
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Page/Page column 97; 98
(2013/09/12)
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- Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: Profile of clinical candidate (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 (23)
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A series of novel tri-2,3,5-substituted tetrahydropyran analogs were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type 2 diabetes. Optimization of the series provided inhibitors with good DPP-4 potency and selectivity over other peptidases (QPP, DPP8, and FAP). Compound 23, which is very potent, selective, efficacious in the diabetes PD model, and has an excellent pharmacokinetic profile, is selected as a clinical candidate.
- Biftu, Tesfaye,Qian, Xiaoxia,Chen, Ping,Feng, Dennis,Scapin, Giovanna,Gao, Ying-Duo,Cox, Jason,Sinha Roy, Ranabir,Eiermann, George,He, Huabing,Lyons, Kathy,Salituro, Gino,Patel, Sangita,Petrov, Alexander,Xu, Feng,Xu, Shiyao Sherrie,Zhang, Bei,Caldwell, Charles,Wu, Joseph K.,Weber, Ann E.
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p. 5361 - 5366
(2013/09/23)
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- From partial to full agonism: Identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor
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A novel GPR119 agonist based on the 2,4,5,6-tetrahydropyrrolo[3,4-c] pyrazole scaffold was designed through lead optimization starting from pyrazole-based GPR119 agonist 1. The design is centered on the conformational restriction of the core scaffold, while minimizing the change in spatial relationships of two key pharmacophoric elements (piperidine-carbamate and aryl sulfone).
- Futatsugi, Kentaro,Mascitti, Vincent,Guimar?es, Cristiano R.W.,Morishita, Nao,Cai, Cuiman,Deninno, Michael P.,Gao, Hua,Hamilton, Michael D.,Hank, Richard,Harris, Anthony R.,Kung, Daniel W.,Lavergne, Sophie Y.,Lefker, Bruce A.,Lopaze, Michael G.,McClure, Kim F.,Munchhof, Michael J.,Preville, Cathy,Robinson, Ralph P.,Wright, Stephen W.,Bonin, Paul D.,Cornelius, Peter,Chen, Yue,Kalgutkar, Amit S.
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p. 194 - 197
(2013/02/25)
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- SUBSTITUTED AMINOPIPERIDINES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES
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The present invention is directed to novel substituted aminopiperidines 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-?V 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 44
(2011/04/24)
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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 55
(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 61
(2011/12/04)
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