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1. 发明授权

US10011574B2 Glutaminase inhibitors and method of use 有权
公开(公告)号：US10011574B2
公开(公告)日：2018-07-03
申请号：US14646239
申请日：2013-11-21
申请人： AGIOS PHARMACEUTICALS, INC.
发明人： Rene M. Lemieux , Janeta Popovici-Muller , Francesco G. Salituro , Jeffrey O. Saunders , Jeremy Travins , Shunqi Yan
IPC分类号： C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02 , C07D401/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D421/00 , C07D513/00 , C07D285/14 , C07D285/08 , A61K31/44 , A61K31/41 , C07D285/135 , C07D417/14 , C07D285/12 , C07D417/12 , C07D471/04
CPC分类号： C07D285/135 , C07D285/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.

2. 发明授权

US09944638B2 Indoles as respiratory syncytial virus antiviral agents 有权
公开(公告)号：US09944638B2
公开(公告)日：2018-04-17
申请号：US15136769
申请日：2016-04-22
申请人： Janssen Sciences Ireland UC
发明人： Ludwig Paul Cooymans , Samuël Dominique Demin , Lili Hu , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Abdellah Tahri , Sandrine Marie Helene Vendeville
IPC分类号： C07D471/04 , C07D403/06 , C07D513/02 , C07D515/02 , A61K31/437 , A61P31/12 , C07D209/10 , C07D209/12 , C07D235/26
CPC分类号： C07D471/04 , C07D209/10 , C07D209/12 , C07D235/26 , C07D403/06
摘要： Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.

3. 发明授权

US09555022B2 Substituted triazolopyridines 有权
标题翻译：取代三唑并吡啶类
公开(公告)号：US09555022B2
公开(公告)日：2017-01-31
申请号：US13704859
申请日：2011-06-14
申请人： Volker Schulze , Dirk Kosemund , Hartmut Schirok , Benjamin Bader , Philip Lienau , Antje Margret Wengner , Hans Briem , Simon Holton , Gerhard Siemeister , Stefan Prechtl , Marcus Koppitz , Detlef Stöckigt , Olaf Prien
发明人： Volker Schulze , Dirk Kosemund , Hartmut Schirok , Benjamin Bader , Philip Lienau , Antje Margret Wengner , Hans Briem , Simon Holton , Gerhard Siemeister , Stefan Prechtl , Marcus Koppitz , Detlef Stöckigt , Olaf Prien
IPC分类号： C07D513/02 , C07D515/02 , C07D249/08 , A61K31/44 , A61K31/437 , A61K45/06 , C07D471/04 , C07D519/00 , A61K31/167 , A61K31/277 , A61K31/282 , A61K31/337 , A61K31/427 , A61K31/428 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/565 , A61K31/675 , A61K31/69 , A61K31/704 , A61K31/7048 , A61K33/24 , A61K38/14 , A61K39/395 , C07D491/08 , C07D491/107
CPC分类号： A61K31/437 , A61K31/167 , A61K31/277 , A61K31/282 , A61K31/337 , A61K31/427 , A61K31/428 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/565 , A61K31/675 , A61K31/69 , A61K31/704 , A61K31/7048 , A61K33/24 , A61K38/14 , A61K39/395 , A61K45/06 , C07D471/04 , C07D491/08 , C07D491/107 , C07D519/00 , A61K2300/00
摘要： The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds.
摘要翻译：本发明涉及通式（I）的取代三唑并吡啶化合物：其中R1，R2，R3，R4和R5如说明书和权利要求书中所述，涉及制备所述化合物的方法，药物组合物和组合包括所述化合物，用于制备用于治疗或预防不受控制的细胞生长，增殖和/或存活的疾病的药物组合物以及使用中间体化合物来制备所述化合物的用途。

4. 发明授权

US09540366B2 Ring-fused heterocyclic compound 有权
标题翻译：环稠合杂环化合物
公开(公告)号：US09540366B2
公开(公告)日：2017-01-10
申请号：US14418253
申请日：2013-07-31
申请人： Kyowa Hakko Kirin Co., Ltd.
发明人： Takayuki Furuta , Takashi Sawada , Tomohiro Danjo , Takahiro Nakajima , Noriaki Uesaka
IPC分类号： C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02 , A61K31/44 , C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/5377
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/5377
摘要： The ring-fused heterocyclic compound or a pharmaceutically acceptable salt thereof according to the present invention has a T-type calcium channel regulatory effect, and is useful, for example, as a medicament for treating and/or preventing pruritus. The present invention provides a ring-fused heterocyclic compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof and the like which has a T-type calcium channel regulatory effect and is useful as a therapeutic and/or preventive agent for pruritus, and the like. [wherein, R1 represents optionally substituted lower alkyl and the like, R2 represents optionally substituted lower alkyl and the like, R3 represents the formula (II): (wherein, n represents 0 or 1, R3a represents a hydrogen atom and the like, R3b represents a hydrogen atom and the like, and R3c represents a hydrogen atom and the like) and the like, Q represents a hydrogen atom and the like, and W1 represents a nitrogen atom and the like, W2 represents a nitrogen atom and the like].
摘要翻译：根据本发明的环稠合杂环化合物或其药学上可接受的盐具有T型钙通道调节作用，并且可用作例如用于治疗和/或预防瘙痒的药物。本发明提供由以下通式（I）表示的环稠合杂环化合物或其药学上可接受的盐等具有T型钙通道调节作用，可用作治疗和/或预防剂瘙痒等。 [其中，R 1表示任选取代的低级烷基等，R 2表示任意取代的低级烷基等，R 3表示式（II）：（其中，n表示0或1，R 3a表示氢原子，类似物，R 3b表示氢原子等，R 3c表示氢原子等）等，Q表示氢原子等，W 1表示氮原子等，W 2 表示氮原子等]

5. 发明授权

US09457084B2 Use of EP4 receptor antagonists in the treatment of IL-23 mediated diseases 有权
标题翻译：使用EP4受体拮抗剂治疗IL-23介导的疾病
公开(公告)号：US09457084B2
公开(公告)日：2016-10-04
申请号：US13580323
申请日：2011-02-22
申请人： Kiyoshi Kanazawa , Kazuhiko Nonomura , Takako Okumura , Shinichi Koizumi
发明人： Kiyoshi Kanazawa , Kazuhiko Nonomura , Takako Okumura , Shinichi Koizumi
IPC分类号： A01N43/42 , A61K31/44 , A01N37/12 , A01N47/28 , A61K31/17 , C07D513/02 , C07D515/02 , C07D211/72 , A61K45/06 , A61K31/38 , A61K31/437 , A61K31/4412 , A61K31/443
CPC分类号： A61K45/06 , A61K31/38 , A61K31/437 , A61K31/44 , A61K31/4412 , A61K31/443 , A61K2300/00
摘要： This invention relates to a compound with EP4 antagonistic activity, or a pharmaceutically acceptable salt with EP4 receptor antagonistic activities, which is useful in the treatment of immune disease or allergy. This invention also relates to a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof with EP4 receptor antagonistic activities, which is useful in the treatment of immune disease or allergy. This invention also relates to a pharmaceutical composition for the treatment of immune disease or allergy which comprises a therapeutically effective amount of a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof. Further this invention relates to a method for the treatment of immune disease or allergy in an animal subject including a mammalian subject, which comprises administering to the animal subject including a mammalian subject a compound of the formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof.

6. 发明授权

US09370477B2 Dyeing composition comprising a fatty substance, a pyrazolopyridine oxidation base and a coupler 有权
标题翻译：包含脂肪物质，吡唑并吡啶氧化碱和偶合剂的染色组合物
公开(公告)号：US09370477B2
公开(公告)日：2016-06-21
申请号：US13994281
申请日：2011-12-14
申请人： Delphine Allard , Valérie Nicou
发明人： Delphine Allard , Valérie Nicou
IPC分类号： A61Q5/10 , C07D515/02 , A61K8/49 , C07D471/04 , A61K8/36
CPC分类号： A61K8/4946 , A61K8/31 , A61K8/342 , A61K8/36 , A61K8/375 , A61K8/494 , A61K2800/882 , A61Q5/10 , C07D471/04
摘要： A subject-matter of the present invention is a composition for dyeing keratinous fibers, in particular human keratinous fibers, such as the hair, comprising: —at least 25% by weight of at least one fatty substance not comprising a carboxylic acid functional group; —at least one aminopyrazolopyridine oxidation base chosen from the bases of formula (I), the bases of formula (II) and their addition salts, their solvates and the solvates of their salts: —at least one coupler; and —at least one oxidizing agent. The composition of the invention is suitable for use in oxidation dyeing and results in a coloration with shades which are varied, intense or chromatic, powerful, attractive, not very selective and highly resistant to the various assaults which the hair may be subjected to, such as shampooing operations, sweat, permanent reshapings and light. In particular, it makes it possible to obtain an optimized color result with a good power, a good dyeing capacity and a good equal depth.
摘要翻译：本发明的主题是用于染色角质纤维，特别是人角质纤维如头发的组合物，其包含：至少25重量％的至少一种不包含羧酸官能团的脂肪物质; - 选自式（I）的碱基，式（II）的碱基及其加成盐，它们的溶剂合物和它们的盐的溶剂化物中的至少一种氨基吡唑并吡啶氧化碱：至少一种成色剂; 和至少一种氧化剂。本发明的组合物适合用于氧化染色，并且可使色调变色，强烈或有色，强大，有吸引力，不是非常选择性和高度耐受头发可能受到的各种攻击，如作为洗发操作，汗水，永久重塑和光照。特别地，它可以获得具有良好的功率，良好的染色能力和良好的相等深度的优化的颜色结果。

7. 发明授权

US08921391B2 Selective EP4 receptor antagonistic substance for treatment of cancer 有权
标题翻译：用于治疗癌症的选择性EP4受体拮抗物质
公开(公告)号：US08921391B2
公开(公告)日：2014-12-30
申请号：US13265216
申请日：2010-04-22
申请人： Yukinori Take , Shinichi Koizumi , Takako Okumura , Kazuhiko Nonomura
发明人： Yukinori Take , Shinichi Koizumi , Takako Okumura , Kazuhiko Nonomura
IPC分类号： A01N43/42 , A61K31/44 , A01N43/40 , A01N37/12 , A01N37/44 , A61K31/195 , A01N47/28 , A61K31/17 , C07D513/02 , C07D515/02 , C07D211/72 , C07D211/84 , C07D213/56 , C07C273/00 , C07C275/00 , C07C239/00 , A61K31/192 , A61K31/437 , A61K31/4412
CPC分类号： C07D471/04 , A61K31/192 , A61K31/437 , A61K31/44 , A61K31/4412 , A61K45/06 , C07C235/60 , C07D213/82
摘要： This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.
摘要翻译：本发明提供了用于治疗导致癌症减少的癌症的药物。本发明涉及对前列腺素E2受体（EP4受体）具有抑制活性且由以下通式（I），（II），（III）或（IV）表示的化合物或其药学上可接受的盐或包含该化合物或盐的药物组合物，用于制备用于治疗癌症的药物。本发明涉及一种治疗癌症的方法，其包括将化合物或其药学上可接受的盐或包含该化合物或盐的药物组合物给予人或动物。化合物或其药学上可接受的盐或药物组合物可以与一种或多种第二活性剂组合使用。

8. 发明授权

US08742113B2 Furanone derivative 有权
标题翻译：呋喃酮衍生物
公开(公告)号：US08742113B2
公开(公告)日：2014-06-03
申请号：US14008488
申请日：2012-03-30
申请人： Takayuki Irie , Ayako Sawa , Masaaki Sawa , Tokiko Asami , Yoko Funakoshi , Chika Tanaka
发明人： Takayuki Irie , Ayako Sawa , Masaaki Sawa , Tokiko Asami , Yoko Funakoshi , Chika Tanaka
IPC分类号： C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4375 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/541 , C07D519/00
摘要： To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I): wherein A represents —COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and each independently represent a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic fused ring, or an optionally substituted amino group; or alternatively, R2 and R3, taken together with the nitrogen atom to which they are attached, may form an optionally substituted heterocycle or an optionally substituted heterocyclic fused ring; and R4 represents a hydrogen atom or a halogen atom; with the proviso that when A represents —COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.
摘要翻译：提供一种新颖的呋喃酮衍生物，以及包含该呋喃酮衍生物的药物。呋喃酮衍生物由式（I）表示：其中A表示-COOR 1或氢原子; R1表示氢原子，任选取代的烃基或任选取代的杂环; R2和R3相同或不同，并且各自独立地表示氢原子，任选取代的烃基，任选取代的苯基，任选取代的杂环，任选取代的杂环稠合环或任选取代的氨基; 或者R2和R3与它们所连接的氮原子一起可以形成任选取代的杂环或任选取代的杂环稠环; R4代表氢原子或卤原子; 条件是当A表示-COOR 1时，R2和R3不同时为任选取代的氨基，当A表示氢原子时，R 3表示氢原子。

9. 发明授权

US08722687B2 Imidazo [1,2-A]pyridine derivatives as FGFR kinase inhibitors for use in therapy 有权
标题翻译：咪唑并[1,2-A]吡啶衍生物作为FGFR激酶抑制剂用于治疗
公开(公告)号：US08722687B2
公开(公告)日：2014-05-13
申请号：US13264596
申请日：2010-04-15
申请人： Gordon Saxty , Valerio Berdini , Christopher William Murray , Eddy Jean Edgard Freyne , Yannick Aimé Eddy Ligny , Pascal Ghislain André Bonnet , Berthold Wroblowski , Alexandra Papanikos
发明人： Gordon Saxty , Valerio Berdini , Christopher William Murray , Eddy Jean Edgard Freyne , Yannick Aimé Eddy Ligny , Pascal Ghislain André Bonnet , Berthold Wroblowski , Alexandra Papanikos
IPC分类号： C07D239/42 , C07D401/04 , A61K31/44 , A01N43/42 , C07D513/02 , C07D515/02 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00
CPC分类号： C07D471/04
摘要： The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
摘要翻译：本发明涉及式（I）的新的双环杂环基衍生物，包含所述化合物的药物组合物和所述化合物在治疗疾病中的用途，例如，癌症。

10. 发明授权

US08680079B2 Tetrahydro-imidazo [1,5-A] pyridyin derivatives as aldosterone synthase inhibitors 失效
标题翻译：四氢 - 咪唑并[1,5-A]吡啶并衍生物作为醛固酮合酶抑制剂
公开(公告)号：US08680079B2
公开(公告)日：2014-03-25
申请号：US11597623
申请日：2005-05-27
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christoph Schumacher , Michael Quirmbach
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christoph Schumacher , Michael Quirmbach
IPC分类号： C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02 , C07D345/00 , C07D517/00
CPC分类号： C07D221/04 , C07D217/02 , C07D239/74 , C07D471/04
摘要： The application relates to novel heterocyclic compounds of the general formula (I) in which R, R1, R2, X, Y, Z and n have the meanings defined in the description, to a process for their preparation and to the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
摘要翻译：本申请涉及通式（I）的新型杂环化合物，其中R，R 1，R 2，X，Y，Z和n具有本说明书中定义的含义，其制备方法和这些化合物的用途作为药物，特别是作为醛固酮合酶抑制剂。

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