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1. 发明授权

US11045562B2 Radiolabelled mGluR2/3 PET ligands 有权
公开(公告)号：US11045562B2
公开(公告)日：2021-06-29
申请号：US16061674
申请日：2016-12-16
申请人： Janssen Pharmaceutica NV
发明人： José Ignacio Andrés-Gil , Michiel Luc Maria Van Gool , Guy Maurits R Bormans , Joost Verbeek
IPC分类号： A61K49/04 , A61K51/04 , C07B59/00 , C07D487/04 , C07D241/50 , C07D253/08
摘要： The present invention relates to novel, radiolabeled mGluR2/3 ligands, selective versus other mGlu receptors which are useful for imaging and quantifying the metabotropic glutamate receptor mGlu2 and 3 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a mammal, in vitro or in vivo and to precursors of said compounds.

2. 发明授权

US10745404B2 Process for the synthesis of E1 activating enzyme inhibitors 有权
公开(公告)号：US10745404B2
公开(公告)日：2020-08-18
申请号：US15713293
申请日：2017-09-22
申请人： Millennium Pharmaceuticals, Inc.
发明人： Ian Armitage , Eric L. Elliott , Marianne Langston , Steven P. Langston , Quentin J. McCubbin , Hiro Mizutani , Matthew Stirling , Lei Zhu
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , C07C215/44 , C07C217/52 , C07C219/24 , C07D211/96 , C07D213/89 , C07D241/50 , C07D295/22 , C07D471/08 , C07C315/04 , C07C317/50 , C07D305/08
摘要： The present invention provides processes and synthetic intermediate (Ia) for the synthesis of 4-substituted ((1S, 2S, 4R)-2-hydroxy-4-{7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentyl)methyl sulfamates. These sulfamate compounds are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity.

3. 发明申请

US20200157076A1 ACLY INHIBITORS AND USES THEREOF 审中-公开
公开(公告)号：US20200157076A1
公开(公告)日：2020-05-21
申请号：US16684644
申请日：2019-11-15
申请人： Nimbus Artemis, Inc.
发明人： Silvana Marcel Leit de Moradei , Kevin Kreutter , H. James Harwood , Eric Therrien
IPC分类号： C07D401/12 , C07D209/08 , C07D491/107 , C07D487/04 , C07D295/26 , C07D205/04 , C07D211/96 , C07D207/48 , C07D217/08 , C07D417/04 , C07D241/04 , C07D241/50 , C07D403/06 , C07D403/04 , C07D409/12 , C07D401/04 , C07D401/14 , C07D403/10 , C07D239/92
摘要： The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.

4. 发明授权

US10377769B2 Benzopiperazine compositions as BET bromodomain inhibitors 有权
公开(公告)号：US10377769B2
公开(公告)日：2019-08-13
申请号：US16029166
申请日：2018-07-06
申请人： FORMA Therapeutics, Inc.
发明人： Kenneth W. Bair , Torsten Herbertz , Goss S. Kauffman , Katherine J. Kayser-Bricker , George P. Luke , Matthew W. Martin , David S. Millan , Shawn E. R. Schiller , Adam C. Talbot , Mark J. Tebbe
IPC分类号： C07D498/04 , C07D403/12 , C07D401/14 , C07D405/14 , C07D413/14 , A61K31/4985 , A61K31/53 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D241/42 , C07D417/10 , C07D241/50 , C07D417/14 , C07D451/04 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/048 , C07D495/04 , A61K45/06 , A61K31/498 , A61K31/5025 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/506 , A61K31/517 , A61K31/55 , A61K31/553
摘要： The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I): wherein X, Y, Z, R1, R2, R4 and R7 are defined herein.

5. 发明申请

US20180079755A1 PROCESS FOR THE SYNTHESIS OF E1 ACTIVATING ENZYME INHIBITORS 审中-公开
公开(公告)号：US20180079755A1
公开(公告)日：2018-03-22
申请号：US15713293
申请日：2017-09-22
申请人： Millennium Pharmaceuticals, Inc.
发明人： Ian Armitage , Eric L. Elliott , Marianne Langston , Steven P. Langston , Quentin J. McCubbin , Hiro Mizutani , Matthew Stirling , Lei Zhu
IPC分类号： C07D487/04 , C07D241/50 , C07C317/50 , C07D211/96 , C07D213/89 , C07D295/22 , C07D305/08 , C07D471/08 , C07C215/44 , C07C315/04 , C07C219/24 , C07C217/52
摘要： The present invention provides processes and synthetic intermediates for the synthesis of 4-substituted ((4S, 2S, 4R)-2-hydroxy-4-{7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentyl)methyl sulfamates, which are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity.

6. 发明授权

US09512111B2 N-sulfonylated tetrahydroquinolines and related bicyclic compounds for inhibition of RORγ activity and the treatment of disease 有权
标题翻译： N-磺酰化四氢喹啉和相关双环化合物，用于抑制RORγ活性和治疗疾病
公开(公告)号：US09512111B2
公开(公告)日：2016-12-06
申请号：US13883419
申请日：2011-11-08
申请人： Gary D. Glick , Peter L. Toogood , Arthur G. Romero , Chad A. Van Huis , Thomas D. Aicher , Carl Kaub , Matthew N. Mattson , William D. Thomas , Karin A. Stein , Erik Krogh-Jespersen , Zhan Wang
发明人： Gary D. Glick , Peter L. Toogood , Arthur G. Romero , Chad A. Van Huis , Thomas D. Aicher , Carl Kaub , Matthew N. Mattson , William D. Thomas , Karin A. Stein , Erik Krogh-Jespersen , Zhan Wang
IPC分类号： C07D413/06 , C07D209/08 , C07D209/34 , C07D215/58 , C07D231/56 , C07D241/50 , C07D265/36 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12 , C07D471/04
CPC分类号： C07D413/06 , C07D209/08 , C07D209/34 , C07D215/58 , C07D231/56 , C07D241/50 , C07D265/36 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The invention provides tetrahydroquinoline and related compounds, pharmaceutical compositions, methods of inhibiting RORγ activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydroquinoline and related compounds are provided.
摘要翻译：本发明提供了四氢喹啉及其相关化合物，药物组合物，抑制RORγ活性的方法，减少受试者中IL-17的量，以及使用这些四氢喹啉及相关化合物治疗免疫疾病和炎症性疾病。

7. 发明授权

US08901302B2 Pyrazino[2,3-D]isoxazole derivative which is useful as a production intermediate of pyrazine carboxamide derivative 有权
标题翻译：吡嗪并[2,3-D]异恶唑衍生物，其可用作吡嗪甲酰胺衍生物的生产中间体
公开(公告)号：US08901302B2
公开(公告)日：2014-12-02
申请号：US13886483
申请日：2013-05-03
申请人： FUJIFILM Corporation , Toyama Chemical Co., Ltd.
发明人： Kouki Nakamura , Takeshi Murakami , Hiroyuki Naitou , Naoyuki Hanaki , Katsuyuki Watanabe
IPC分类号： C07D241/50 , C07C239/18 , C07D498/04 , C07C251/38 , C07C255/23 , C07C237/06 , C07D261/18 , C07C255/29 , C07D241/18 , C07D241/24
CPC分类号： C07D241/24 , C07C237/06 , C07C239/18 , C07C251/38 , C07C255/23 , C07C255/29 , C07D241/18 , C07D261/18 , C07D498/04
摘要： The object of the present invention is to provide a compound which is useful as a production intermediate of pyrazine carboxamide derivative such as 6-fluoro-3-hydroxy-2-pyrazine carboxamide. The present invention provides a pyrazino[2,3-d]isoxazole derivative represented by the formula (I): wherein X represents a halogen atom, a hydroxyl group or a sulfamoyloxy group, and Y represents —C(═O)R or —CN; wherein R represents a hydrogen atom, an alkoxy group an aryloxy group, an alkyl group, an aryl group or an amino group.
摘要翻译：本发明的目的是提供一种可用作吡嗪甲酰胺衍生物如6-氟-3-羟基-2-吡嗪甲酰胺的制备中间体的化合物。本发明提供由式（I）表示的吡嗪并[2,3-d]异恶唑衍生物：其中X表示卤素原子，羟基或氨磺酰氧基，Y表示-C（= O）R或 - CN; 其中R表示氢原子，烷氧基，芳氧基，烷基，芳基或氨基。

8. 发明申请

US20110046112A1 NOVEL BICYCLIC SULFONAMIDE DERIVATIVES WHICH ARE L-CPT1 INHIBITORS 失效
标题翻译： L-CPT1抑制剂的新型双酚磺酰胺衍生物
公开(公告)号：US20110046112A1
公开(公告)日：2011-02-24
申请号：US12941374
申请日：2010-11-08
申请人： Jean Ackermann , Konrad Bleicher , Simona M. Ceccarelli , Odile Chomienne , Patrizio Mattei , Ulrike Obst Sander
发明人： Jean Ackermann , Konrad Bleicher , Simona M. Ceccarelli , Odile Chomienne , Patrizio Mattei , Ulrike Obst Sander
IPC分类号： A61K31/553 , C07D265/36 , C07D413/12 , C07D241/50 , C07D263/56 , C07D267/14 , C07D267/22 , C07D279/16 , C07D265/16 , A61K31/538 , A61K31/498 , A61K31/423 , A61K31/4439 , A61K31/395 , A61K31/5415 , A61P3/10
CPC分类号： C07D265/36 , C07D241/42 , C07D263/56 , C07D265/14 , C07D267/14 , C07D279/16 , C07D413/12 , C07D417/12 , C07D491/04
摘要： The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型杂双环衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6，V，W，X和Y如说明书和权利要求书中所定义，以及生理上可接受的盐及其酯。这些化合物抑制L-CPT1，可用作药物。

9. 发明授权

US07115600B2 Histamine-3 receptor modulators 失效
标题翻译：组胺-3受体调节剂
公开(公告)号：US07115600B2
公开(公告)日：2006-10-03
申请号：US11045968
申请日：2005-01-28
申请人： Travis T. Wager , Ramalakshmi Y. Chandrasekaran
发明人： Travis T. Wager , Ramalakshmi Y. Chandrasekaran
IPC分类号： A61K31/496 , A61K31/541 , A61K31/4995 , C07D241/50 , C07D403/10 , C07D417/10
CPC分类号： C07D295/096 , C07D207/04 , C07D207/06 , C07D213/30 , C07D215/227 , C07D231/12 , C07D239/26 , C07D239/34 , C07D271/06 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D471/10 , C07D487/04
摘要： This invention is directed to a compound of the formula I as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by modulating histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above.
摘要翻译：本发明涉及本文定义的式I化合物或其药学上可接受的盐; 含有式I化合物的药物组合物，治疗可以通过调节组胺H3受体治疗的病症或病症的方法，所述方法包括向需要这种治疗的哺乳动物施用如上所述的式I化合物，以及治疗选自抑郁症，情绪障碍，精神分裂症，焦虑症，阿尔茨海默氏病，注意力缺陷多动障碍（ADHD），精神障碍，睡眠障碍，肥胖，眩晕，癫痫，过敏反应，过敏引起的气道反应，过敏性鼻炎，鼻充血，过敏充血，充血，低血压，心血管疾病，胃肠道疾病，胃肠道过度运动和运动不足及酸性分泌，该方法包括向需要这种治疗的哺乳动物施用如上所述的式I化合物。

10. 发明申请

US20050256000A1 Quinoxalin-2-one derivatives, compositions which protect useful plants and comprise these derivatives, and processes for their preparation and their use 审中-公开
标题翻译：喹喔啉-2-酮衍生物，保护有用植物并包含这些衍生物的组合物，及其制备方法及其用途
公开(公告)号：US20050256000A1
公开(公告)日：2005-11-17
申请号：US11127016
申请日：2005-05-11
申请人： Wolfgang Schaper , Lothar Willms , Christopher Rosinger , Erwin Hacker , Eckhard Rose , Dirk Schmutzler
发明人： Wolfgang Schaper , Lothar Willms , Christopher Rosinger , Erwin Hacker , Eckhard Rose , Dirk Schmutzler
IPC分类号： A01N25/32 , A01N43/60 , A01N43/78 , A01N43/80 , A01N43/82 , C07D241/50 , C07D241/52 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/14 , C07D241/36
CPC分类号： C07D401/04 , A01N25/32 , A01N43/60 , A01N43/78 , A01N43/80 , A01N43/82 , C07D241/52 , C07D401/06 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/14 , A01N61/00 , A01N43/56 , A01N2300/00
摘要： Compounds of the formula (I) and salts thereof in which X is O or S; (Y)n=n substituents Y, n is 0, 1, 2, 3 or 4, R1 is H, OH, NH2, (C1-C4)-alkylamino, di-[(C1-C4)-alkyl]amino or optionally substituted (C1-C10)-alkyl, (C3-C10)-alkenyl, (C3-C10)-alkynyl or (C1-C10)-alkoxy, (C3-C10)-cycloalkyl, (C4-C10)-cycloalkenyl, aryl or heterocyclyl, R2 is H or optionally substituted (C1-C10)-alkyl, (C3-C10)-alkenyl, (C3-C10)-alkynyl, (C3-C10)-cycloalkyl, (C4-C10)-cycloalkenyl, aryl or heterocyclyl, where the radicals Y are as defined in claim 1 are suitable for use as safeners for crop plants or useful plants against the phytotoxic actions of agrochemicals such as pesticides in these plants.
摘要翻译：式（I）化合物及其盐，其中X为O或S; （Y）n n = n取代基Y，n为0,1,2,3或4，R 1为H，OH，NH 2 ，（C 1 -C 4 -C 4 - ） - 烷基氨基，二 - [（C 1 -C 4 - - 烷基]氨基或任选取代的（C 1 -C 10 - ） - 烷基，（C 3 -C 10 - ）） - 烯基，（C 3 -C 10） - 炔基或（C 1 -C 10 - ） - 炔基或（C 1 -C 10） - 烷氧基，（C 3 -C 10） - 环烷基，（C 4 -C 10 - ） - 环烯基，芳基或杂环基，R 2是H或任选取代的（C 1 -C 10 - ） - 烷基，（C 3 < （C 3 -C 10） - 炔基，（C 3 -C 10） - 烯基，（C 3 -C 10 - ） - 炔基，（C 3 -C 10） C 1 -C 10 - 环烷基，（C 1-4 -C 10 - ）环烯基，芳基或杂环基，其中基团Y如所定义权利要求1中适用于农作物植物或有用植物的安全剂，以防止这些植物中农药如农药的植物毒性作用。

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