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1. 发明申请

WO2018129274A1 OXADIAZOLE INHIBITORS OF HIPK2 FOR TREATING KIDNEY FIBROSIS 审中-公开
公开(公告)号：WO2018129274A1
公开(公告)日：2018-07-12
申请号：PCT/US2018/012512
申请日：2018-01-05
申请人： ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI , UNIVERSITY OF KANSAS
发明人： HE, John Cijiang , LIU, Ruijie , DAS, Bhaskar , XIAO, Wenzhen , LI, Zhengzhe , LEE, Kyung
IPC分类号： C07D271/04 , C07D271/06 , C07D271/07 , C07D271/08 , C07D271/10 , C07D271/107
摘要： Compounds that are selective inhibitors of Smad3 activation are disclosed. The compounds have the structure (I) in which Z is an oxadiazole. The compounds disclosed are useful in treatment of fibrotic disease, particularly renal fibrosis, and similar diseases associated with the dysregulation of the HIPK2/Smad3 signaling pathway.

2. 发明申请

WO2009117421A3 HETEROCYCLIC MODULATORS OF GPR119 FOR TREATMENT OF DISEASE 审中-公开
标题翻译： GPR119用于治疗疾病的杂环调节剂
公开(公告)号：WO2009117421A3
公开(公告)日：2010-01-07
申请号：PCT/US2009037408
申请日：2009-03-17
申请人： KALYPSYS INC , SMITH NICHOLAS , BONNEFOUS CELINE , GOVEK STEVEN P , WU DONGPEI , PINKERTON ANTHONY B , KAHRAMAN MEHMET , COOK TRAVIS , NOBLE STEWART A , BORCHARDT ALLEN J , PRINS THOMAS
发明人： SMITH NICHOLAS , BONNEFOUS CELINE , GOVEK STEVEN P , WU DONGPEI , PINKERTON ANTHONY B , KAHRAMAN MEHMET , COOK TRAVIS , NOBLE STEWART A , BORCHARDT ALLEN J , PRINS THOMAS
IPC分类号： C07D271/04 , A61P9/00 , C07D257/04 , C07D285/04 , C07D403/14
CPC分类号： C07D401/14 , C07D207/34 , C07D277/56 , C07D401/04 , C07D401/12 , C07D403/10 , C07D405/14 , C07D413/12 , C07D413/14
摘要： The present invention relates to compounds and methods which may be useful as inhibitors of GPR119 for the treatment or prevention of metabolic, cardiovascular, and metabolic diseases.
摘要翻译：本发明涉及可用作GPR119抑制剂用于治疗或预防代谢，心血管和代谢疾病的化合物和方法。

3. 发明申请

WO00012084A1 GEOMETRICALLY RESTRICTED 2-INDOLINONE DERIVATIVES AS MODULATORS OF PROTEIN KINASE ACTIVITY 审中-公开
标题翻译：作为蛋白激酶活性调节剂的几何限制性2-吲哚啉酮衍生物
公开(公告)号：WO00012084A1
公开(公告)日：2000-03-09
申请号：PCT/US1999/019948
申请日：1999-08-30
IPC分类号： A61K31/404 , A61K31/34 , A61K31/35 , A61K31/36 , A61K31/38 , A61K31/385 , A61K31/39 , A61K31/40 , A61K31/403 , A61K31/405 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/535 , A61K31/54 , A61P3/10 , A61P7/00 , A61P9/08 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/02 , A61P43/00 , C07D209/12 , C07D209/34 , C07D231/54 , C07D235/02 , C07D237/26 , C07D239/70 , C07D241/36 , C07D249/16 , C07D251/16 , C07D251/72 , C07D253/065 , C07D253/08 , C07D257/04 , C07D257/08 , C07D257/10 , C07D261/08 , C07D261/20 , C07D263/32 , C07D263/52 , C07D265/12 , C07D265/16 , C07D265/34 , C07D265/36 , C07D271/04 , C07D271/06 , C07D271/08 , C07D271/10 , C07D271/12 , C07D273/04 , C07D275/02 , C07D275/04 , C07D279/06 , C07D279/08 , C07D279/12 , C07D279/14 , C07D279/16 , C07D285/06 , C07D285/08 , C07D285/10 , C07D285/12 , C07D285/14 , C07D285/18 , C07D285/20 , C07D285/22 , C07D285/34 , C07D291/02 , C07D291/08 , C07D307/36 , C07D307/38 , C07D307/40 , C07D307/52 , C07D307/77 , C07D311/02 , C07D311/94 , C07D317/04 , C07D317/06 , C07D317/14 , C07D317/44 , C07D317/46 , C07D319/06 , C07D319/08 , C07D319/12 , C07D319/14 , C07D319/16 , C07D323/02 , C07D323/04 , C07D327/04 , C07D327/06 , C07D327/10 , C07D333/06 , C07D333/50 , C07D401/02 , C07D401/10 , C07D403/04 , C07D471/02 , C07D487/02
CPC分类号： C07D209/34
摘要： The present invention relates to novel geometrically restricted 2-indolinones and physiologically acceptable salts thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
摘要翻译：本发明涉及调节蛋白激酶活性的新颖的几何限制性2-二氢吲哚酮及其生理上可接受的盐，因此预期可用于预防和治疗与蛋白激酶相关的细胞病症例如癌症。

4. 发明申请

WO99037608A1 NOVEL NAPHTHYL SUBSTITUTED AND HETEROCYCLIC SUBSTITUTED SULFONAMIDES 审中-公开
标题翻译： NEW萘基和杂环取代的磺酰胺
公开(公告)号：WO99037608A1
公开(公告)日：1999-07-29
申请号：PCT/EP1999/000134
申请日：1999-01-12
IPC分类号： A61K31/167 , A61K31/18 , A61K31/215 , A61K31/277 , A61K31/337 , A61K31/357 , A61K31/39 , A61K31/4245 , A61K31/433 , A61P31/12 , C07C311/21 , C07C311/29 , C07C311/37 , C07C311/44 , C07C311/46 , C07D271/04 , C07D271/12 , C07D285/14 , C07D305/08 , C07D319/06 , C07D327/04 , C07D233/26
CPC分类号： C07C311/21 , C07C311/29 , C07C311/37 , C07C2601/02 , C07C2601/14 , C07C2603/74 , C07D271/12 , C07D305/08 , C07D319/06
摘要： The invention relates to novel naphthyl substituted and heterocyclic substituted sulfonamides of general formula (I) in which A, D, E, R and R have the meanings given in the description. The invention also relates to a method for the production thereof and to the utilization thereof as antiviral agents, especially against cytomegaloviruses.
摘要翻译：本发明涉及新的萘基和通式（I）的杂环基取代的磺酰胺，其中A，D，E，R <1>和R <2>的含义给出，其制备方法和它们的用途以及方法抗病毒药物，特别是对巨细胞病毒。

5. 发明申请

WO1991014681A1 INCLUSION COMPLEXES OF 3-MORPHOLINO-SYDNONIMINE OR ITS SALTS OR ITS TAUTOMER ISOMER, PROCESS FOR THE PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 审中-公开
标题翻译：包括3-吗啉代 - 邻氨基苯胺或其盐或其衍生物异构体的复合物，其制备方法和含有它们的药物组合物
公开(公告)号：WO1991014681A1
公开(公告)日：1991-10-03
申请号：PCT/HU1991000013
申请日：1991-03-28
申请人： CHINOIN GYOGYSZER- ÉS VEGYÉSZETI TERMÉKEK GYARA ... , VIKMON, Mária , SZEJTLI, József , SZENTE, Lajos , GAAL, József , HERMECZ, István , HORVATH, Agnes , MARMAROSI, Katalin , HORVATH, Gábor , MUNKACSI, Irén
发明人： CHINOIN GYOGYSZER- ÉS VEGYÉSZETI TERMÉKEK GYARA ...
IPC分类号： C07D271/04
CPC分类号： C08B37/0015 , C07D271/04 , Y10S514/821 , Y10S514/969
摘要： The invention relates to inclusion complexes of 3-morpholino-sydnonimine or its salts or its tautomer isomer, process for the preparation thereof and pharmaceutical compositions containing the same. The inclusion complex of 3-morpholino-sydnonimine or its salt formed with cyclodextrin derivative is prepared by (a) reacting the 3-morpholino-sydnonimine or its salt in an aqueous medium with a cyclodextrin derivative and the complex is isolated from the solution by dehydratation, or (b) high energy milling of 3-morpholino-sydnonimine or its salt and a cyclodextrin derivative.
摘要翻译：本发明涉及3-吗啉代 - 脱水亚胺或其盐或其互变异构体的包合物，其制备方法和含有它们的药物组合物。通过（a）使3-吗啉代 - 脱水亚胺或其盐在水性介质中与环糊精衍生物反应制备3-吗啉代 - 二氢化茚或其与环糊精衍生物形成的盐的络合物，并通过脱水从溶液中分离复合物，或（b）3-吗啉代 - 二氢亚胺或其盐和环糊精衍生物的高能研磨。

6. 发明申请

WO2021094505A8 HERBICIDAL COMPOUNDS 审中-公开
公开(公告)号：WO2021094505A8
公开(公告)日：2021-05-20
申请号：PCT/EP2020/081995
申请日：2020-11-13
申请人： SYNGENTA CROP PROTECTION AG
发明人： BURTON, Paul, Matthew , RAJAN, Ramya , EMERY, Katie , MITCHELL, Glynn , BURNS, David , MCGRANAGHAN, Andrea
IPC分类号： C07D257/04 , C07D271/04 , A01N43/713 , A01N43/82
摘要： The present invention relates to compounds Formula (I) wherein Q, R2, R3 and R4 are as defined herein. The invention further relates to compositions comprising said compounds, and methods of controlling weeds using said compounds and/or compositions.

7. 发明申请

WO2021094505A1 HERBICIDAL COMPOUNDS 审中-公开
公开(公告)号：WO2021094505A1
公开(公告)日：2021-05-20
申请号：PCT/EP2020/081995
申请日：2020-11-13
申请人： SYNGENTA CROP PROTECTION AG
发明人： BURTON, Paul, Matthew , RAJAN, Ramya , EMERY, Katie , MITCHELL, Glynn , BURNS, David , MCGRANAGHAN, Andrea
IPC分类号： C07D257/04 , C07D271/04 , A01N43/713 , A01N43/82
摘要： The present invention relates to compounds Formula (I) wherein Q, R2, R3 and R4 are as defined herein. The invention further relates to compositions comprising said compounds, and methods of controlling weeds using said compounds and/or compositions.

8. 发明申请

WO2017191000A1 AROMATIC SULFONAMIDE DERIVATIVES 审中-公开
标题翻译：芳香族磺酰胺衍生物
公开(公告)号：WO2017191000A1
公开(公告)日：2017-11-09
申请号：PCT/EP2017/059882
申请日：2017-04-26
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： WERNER, Stefan , MESCH, Stefanie , CLEVE, Arwed , BRÄUER, Nico , HERBERT, Simon, Anthony , KOCH, Markus , DAHLLÖF, Henrik , OSMERS, Maren , HARDAKER, Elizabeth , LISHCHYNSKYI, Anton
IPC分类号： C07D213/85 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D233/16 , C07D233/61 , C07D233/64 , C07D233/68 , C07D401/04 , C07D235/06 , C07C311/40 , C07D403/04 , C07D237/08 , C07D405/04 , C07D239/26 , C07D405/06 , C07D239/34 , C07D239/42 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/14 , C07D471/04 , C07D261/08 , C07D271/06 , C07D207/333 , C07D207/416 , C07D213/40 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/74 , C07D231/38 , C07D231/56 , C07D239/30 , C07D249/06 , C07D249/18 , C07D249/20 , C07D263/32 , C07D271/04 , C07D275/02 , C07D277/26 , C07D277/34 , C07D277/56 , C07D213/60 , A61K31/41 , A61P35/00 , A61P37/00 , A61P25/02 , A61P25/28 , A61P25/16
摘要： Substituted aromatic sulfonamides of formula (I) pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.
摘要翻译：式（I）的取代的芳族磺酰胺药物组合物和包含所述化合物的组合以及所述化合物在制备用于治疗或预防疾病的药物组合物中的用途

9. 发明申请

WO2007016095A3 CYCLOOXYGENASE-2 SELECTIVE INHIBITOR COMPOUNDS COMPRISING NITRIC OXIDE ENHANCING GROUPS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：包含氮氧化物增强组合物的CYCLOOXYGENASE-2选择性抑制剂化合物，组合物和使用方法
公开(公告)号：WO2007016095A3
公开(公告)日：2008-02-28
申请号：PCT/US2006028856
申请日：2006-07-26
申请人： NITROMED INC , GARVEY DAVID S
发明人： GARVEY DAVID S
IPC分类号： C07C229/42 , A61K31/04 , A61K31/136 , A61K31/4245 , A61P1/04 , A61P7/02 , A61P9/14 , A61P25/28 , A61P29/00 , A61P35/00 , C07C271/02 , C07D271/04 , C07D271/08 , C07D273/00 , C07D413/04
CPC分类号： C07C229/42
摘要： The invention describes compositions and kits comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor comprising at least one nitric oxide enhancing group, or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor comprising at least one nitric oxide enhancing group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating inflammation, pain and fever; (b) treating gastrointestinal disorders and/or improving the gastrointestinal properties of COX-2 selective inhibitors; (c) facilitating wound healing; (d) treating renal and/or respiratory toxicities; (e) treating disorders resulting from elevated levels of cyclooxygenase-2; (f) improving the cardiovascular profile of COX-2 selective inhibitors; (g) treating diseases resulting from oxidative stress; (h) treating endothelial dysfunctions; (j) treating diseases caused by endothelial dysfunctions; (k) treating inflammatory disease states and/or disorders; (1) treating ophthalmic disorders; and (m) treating peripheral vascular diseases. The cyclooxygenase 2 selective inhibitors of the invention are 2(2-((2-chloro-6-fluorophenyl) amino)5-methylphenyl)acetic acid derivatives comprising at least one nitric oxide enhancing group. The nitric oxide enhancing groups are nitroxides and/or heterocyclic nitric oxide donors.
摘要翻译：本发明描述了包含至少一种包含至少一种一氧化氮增强基团的环氧合酶2（COX-2）选择性抑制剂或其药学上可接受的盐的组合物和试剂盒，以及包含至少一种环氧合酶2（COX-2）选择性抑制剂包括至少一种一氧化氮增强基团和任选的至少一种一氧化氮增强化合物和/或至少一种治疗剂。本发明还提供了（a）治疗炎症，疼痛和发烧的方法; （b）治疗胃肠道疾病和/或改善COX-2选择性抑制剂的胃肠性质; （c）促进伤口愈合; （d）治疗肾脏和/或呼吸毒性; （e）治疗由环氧合酶-2水平升高引起的疾病; （f）改善COX-2选择性抑制剂的心血管状态; （g）治疗由氧化应激引起的疾病; （h）治疗内皮功能障碍; （j）治疗由内皮功能障碍引起的疾病; （k）治疗炎性疾病状态和/或病症; （1）治疗眼科疾病; 和（m）治疗外周血管疾病。本发明的环氧合酶2选择性抑制剂是包含至少一种一氧化氮增强基团的2（2 - （（2-氯-6-氟苯基）氨基）5-甲基苯基）乙酸衍生物。一氧化氮增强基团是氮氧化物和/或杂环一氧化氮供体。

10. 发明申请

WO99040089A1 BENZOTHIADIAZOLES AND DERIVATIVES 审中-公开
标题翻译：苯并噻唑和衍生物
公开(公告)号：WO99040089A1
公开(公告)日：1999-08-12
申请号：PCT/EP1999/000622
申请日：1999-02-01
IPC分类号： A61K31/437 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61P1/04 , A61P1/06 , A61P1/14 , A61P3/04 , A61P11/06 , A61P15/00 , A61P15/06 , A61P15/08 , A61P17/00 , A61P19/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P25/32 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D207/00 , C07D239/00 , C07D239/72 , C07D241/36 , C07D271/04 , C07D285/06 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D473/34 , C07D475/10 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , A61K31/505 , C07D417/04
CPC分类号： C07D403/12 , C07D413/12 , C07D417/12 , C07D473/34 , C07D487/04
摘要： The invention provides a compound of formula (I) wherein X, R1, R2 and Het are as defined in the description, and a process for preparing them. The compounds of formula (I) are useful as pharmaceuticals.
摘要翻译：本发明提供式（I）化合物，其中X，R1，R2和Het如说明书中所定义，及其制备方法。式（I）的化合物可用作药物。

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