公开(公告)号：US09956213B2

公开(公告)日：2018-05-01

申请号：US15603286

申请日：2017-05-23

申请人： DART NEUROSCIENCE (CAYMAN) LTD.

发明人： Jillian Basinger ,  Graeme Freestone ,  Varsha Gupta ,  Alan Kaplan ,  Chi Ching Mak ,  Benjamin Pratt ,  Vincent Santora ,  Dipanjan Sengupta ,  Lino Valdez

IPC分类号： C07D215/00 ,  A61K31/47 ,  A61K31/4375 ,  A61K31/4709 ,  C07D215/20 ,  C07D471/04 ,  C07D215/54 ,  C07D215/60 ,  C07D401/12 ,  C07D215/22

CPC分类号： A61K31/47 ,  A61K31/4375 ,  A61K31/4709 ,  C07D215/20 ,  C07D215/22 ,  C07D215/54 ,  C07D215/60 ,  C07D401/12 ,  C07D471/04

摘要： The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.

公开(公告)号：US09809589B2

公开(公告)日：2017-11-07

申请号：US14653933

申请日：2013-12-23

申请人： KBP BIOSCIENCES CO., LTD.

发明人： Chen Jiang ,  Aichen Wang ,  Dedong Zhang

IPC分类号： C07D471/04 ,  C07D215/20 ,  C07D215/60 ,  C07D215/48 ,  C07C255/50

CPC分类号： C07D471/04 ,  C07C255/50 ,  C07D215/20 ,  C07D215/48 ,  C07D215/60

摘要： The present invention belongs to the technical field of medicines, and relates to a crystal form of a compound used as a mineralocorticoid receptor antagonist and a preparation method therefor, and in particular, to a method for preparing a compound 2-chloro-4-[(3S,3aR)-3-cyclopentyl-7-(4-hydroxypiperidin-1-carbonyl)-3,3a,4,5-tetrahydro-2H-pyrazolo[3,4-f]quinolin-2-yl]benzonitrile of formula (1); a crystal form thereof, a preparation method for the crystal form, and the use of the crystal form in the preparation of drugs for the treatment and/or prevention of renal injury or cardiovascular diseases.

公开(公告)号：US20170312263A1

公开(公告)日：2017-11-02

申请号：US15603286

申请日：2017-05-23

申请人： DART NEUROSCIENCE (CAYMAN) LTD.

发明人： Jillian Basinger ,  Graeme Freestone ,  Varsha Gupta ,  Alan Kaplan ,  Chi Ching Mak ,  Benjamin Pratt ,  Vincent Santora ,  Dipanjan Sengupta ,  Lino Valdez

IPC分类号： A61K31/47 ,  C07D401/12 ,  C07D215/60 ,  C07D215/54 ,  C07D215/22 ,  C07D215/20 ,  A61K31/4709 ,  C07D471/04 ,  A61K31/4375

CPC分类号： A61K31/47 ,  A61K31/4375 ,  A61K31/4709 ,  C07D215/20 ,  C07D215/22 ,  C07D215/54 ,  C07D215/60 ,  C07D401/12 ,  C07D471/04

摘要： The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.

公开(公告)号：US20170305904A1

公开(公告)日：2017-10-26

申请号：US15589590

申请日：2017-05-08

申请人： The United States of America, as represented by the Secretary, Department of Health and Human Serv

发明人： Xue Zhi Zhao ,  Steven Smith ,  Mathieu Metifiot ,  Barry Johnson ,  Christophe Marchand ,  Stephen H. Hughes ,  Yves Pommier ,  Terrence R. Burke, JR.

IPC分类号： C07D471/04 ,  C07D215/60 ,  C07D215/58 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4704 ,  C07D491/147 ,  A61K31/4375

CPC分类号： C07D471/04 ,  A61K31/4375 ,  A61K31/4704 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D215/58 ,  C07D215/60 ,  C07D491/147 ,  A61K2300/00

摘要： A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is N, C(OH), or CH; Y is H or OH; each of Z1-Z5 is independently H or halogen; R4 is H, OH, NH2, NHR8, NR8R9 or R8; R5, R6, and R7 is each independently H, halogen, OR8, R8, NHR8, NR8R9, CO2R8, CONR8R9, SO2NR8R9, or R5 and R6 together with the carbon atoms to which R5 and R6 are attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; and R8 and R9 is each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or R8 and R9 together with the nitrogen to which R8 and R9 are attached form an optionally-substituted heterocycle.

公开(公告)号：US09233957B2

公开(公告)日：2016-01-12

申请号：US14123043

申请日：2012-06-11

申请人： Coo-Min Chung ,  Choon-Ho Ryu ,  Yoon-Kyeong Lee ,  Jin-Sook Moon ,  Hye-Sung Lee ,  Seon-Jeong Lee ,  Kyung-Seok Oh

发明人： Coo-Min Chung ,  Choon-Ho Ryu ,  Yoon-Kyeong Lee ,  Jin-Sook Moon ,  Hye-Sung Lee ,  Seon-Jeong Lee ,  Kyung-Seok Oh

IPC分类号： C07D207/34 ,  C07D213/81 ,  C07D213/89 ,  C07D215/48 ,  C07D215/60 ,  C07D417/04 ,  C07D333/38 ,  C07D261/10 ,  C07D307/56 ,  C07D261/18 ,  C07D307/68 ,  C07D401/04 ,  C07D413/04 ,  C07D413/12

CPC分类号： C07D417/04 ,  C07D207/34 ,  C07D213/81 ,  C07D213/89 ,  C07D215/48 ,  C07D215/60 ,  C07D261/10 ,  C07D261/18 ,  C07D307/56 ,  C07D307/68 ,  C07D333/38 ,  C07D401/04 ,  C07D413/04 ,  C07D413/12

摘要： Provided are a novel derivative of 5-carbamoyl adamantan-2-yl amide of Formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof for inhibiting the activity of 11β-hydroxystreroid dehydrogenase type 1 (11b-HSD1) or for preventing and/or treating various diseases mediated by 11β-hydroxystreroid dehydrogenase type 1.

摘要翻译： 提供式（I）的5-氨基甲酰基金刚烷-2-基酰胺或其药学上可接受的盐的新型衍生物及其用于抑制11型β-葡萄糖醛酸脱氢酶1型（11b-HSD1）的活性的药物用途， 或用于预防和/或治疗由11型β-羟化神经元脱氢酶1介导的各种疾病。

公开(公告)号：US20150336950A1

公开(公告)日：2015-11-26

申请号：US14653933

申请日：2013-12-23

申请人： KBP BIOSCIENCES CO., LTD.

发明人： Chen JIANG ,  Aichen WANG ,  Dedong ZHANG

IPC分类号： C07D471/04 ,  C07C255/50 ,  C07D215/48 ,  C07D215/20 ,  C07D215/60

CPC分类号： C07D471/04 ,  C07C255/50 ,  C07D215/20 ,  C07D215/48 ,  C07D215/60

摘要： The present invention belongs to the technical field of medicines, and relates to a crystal form of a compound used as a mineralocorticoid receptor antagonist and a preparation method therefor, and in particular, to a method for preparing a compound 2-chloro-4-[(3S,3aR)-3-cyclopentyl-7-(4-hydroxypiperidin-1-carbonyl)-3,3a,4,5-tetrahydro-2H-pyrazolo[3,4-f]quinolin-2-yl]benzonitrile of formula (1); a crystal form thereof, a preparation method for the crystal form, and the use of the crystal form in the preparation of drugs for the treatment and/or prevention of renal injury or cardiovascular diseases.

摘要翻译： 本发明属于药物技术领域，涉及用作盐皮质激素受体拮抗剂的化合物的结晶形式及其制备方法，特别涉及2-氯-4- [ （3S，3aR）-3-环戊基-7-（4-羟基哌啶-1-羰基）-3,3a，4,5-四氢-2H-吡唑并[3,4-f]喹啉-2-基]苄腈 公式1）; 其晶体形式，晶体形式的制备方法，以及晶体形式在制备用于治疗和/或预防肾损伤或心血管疾病的药物中的用途。

公开(公告)号：US20150336897A1

公开(公告)日：2015-11-26

申请号：US14817329

申请日：2015-08-04

申请人： Nivalis Therapeutics, Inc.

发明人： Xicheng Sun ,  Jian Qiu ,  Adam Stout

IPC分类号： C07D215/20 ,  C07D401/10 ,  C07D401/04 ,  C07D215/42 ,  C07D409/04 ,  C07D417/10 ,  C07D409/14 ,  C07D215/46 ,  C07D215/60 ,  C07D413/10

CPC分类号： C07D215/20 ,  A61K31/47 ,  A61K31/4706 ,  A61K31/4709 ,  C07D215/00 ,  C07D215/42 ,  C07D215/46 ,  C07D215/54 ,  C07D215/60 ,  C07D401/04 ,  C07D401/10 ,  C07D409/04 ,  C07D409/14 ,  C07D413/10 ,  C07D417/10

摘要： The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

摘要翻译： 本发明涉及可用作S-亚硝基谷胱甘肽还原酶（GSNOR）抑制剂的新型喹啉化合物，包含这些化合物的药物组合物及其制备和使用方法。

公开(公告)号：US09139528B2

公开(公告)日：2015-09-22

申请号：US14540216

申请日：2014-11-13

申请人： N30 Pharmaceuticals, Inc.

发明人： Xicheng Sun ,  Jian Qiu ,  Adam Stout

IPC分类号： A61K31/47 ,  C07D215/20 ,  C07D215/00 ,  C07D215/42 ,  C07D215/54 ,  C07D215/60 ,  C07D401/04 ,  C07D401/10 ,  C07D409/04 ,  C07D409/14 ,  C07D413/10 ,  C07D417/10

CPC分类号： C07D215/20 ,  A61K31/47 ,  A61K31/4706 ,  A61K31/4709 ,  C07D215/00 ,  C07D215/42 ,  C07D215/46 ,  C07D215/54 ,  C07D215/60 ,  C07D401/04 ,  C07D401/10 ,  C07D409/04 ,  C07D409/14 ,  C07D413/10 ,  C07D417/10

摘要： The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

摘要翻译： 本发明涉及可用作S-亚硝基谷胱甘肽还原酶（GSNOR）抑制剂的新型喹啉化合物，包含这些化合物的药物组合物及其制备和使用方法。

公开(公告)号：US20140329821A1

公开(公告)日：2014-11-06

申请号：US14326686

申请日：2014-07-09

申请人： N30 Pharmaeuticals, Inc.

发明人： Xicheng Sun ,  Jian Qiu ,  Adam Stout

IPC分类号： C07D417/10 ,  C07D241/42 ,  C07D239/26 ,  C07D215/20 ,  C07D413/10 ,  C07D401/10 ,  C07D409/04 ,  C07D409/14 ,  C07D401/04 ,  C07D253/10 ,  C07D215/60

CPC分类号： A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/498 ,  A61K31/517 ,  A61K31/53 ,  C07C65/105 ,  C07C65/17 ,  C07C65/24 ,  C07D213/79 ,  C07D215/06 ,  C07D215/20 ,  C07D215/60 ,  C07D217/04 ,  C07D217/16 ,  C07D237/24 ,  C07D239/26 ,  C07D239/28 ,  C07D239/34 ,  C07D239/74 ,  C07D241/24 ,  C07D241/42 ,  C07D249/18 ,  C07D253/10 ,  C07D257/04 ,  C07D295/155 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/10 ,  C07D417/10 ,  C12N9/0006 ,  C12N9/0065 ,  C12N9/99 ,  C12Y101/01284

摘要： The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

摘要翻译： 本发明涉及用作S-亚硝基谷胱甘肽还原酶（GSNOR）抑制剂的新型取代的双环芳族化合物，包含这些化合物的药物组合物及其制备和使用方法。

公开(公告)号：US20140315944A1

公开(公告)日：2014-10-23

申请号：US14204738

申请日：2014-03-11

申请人： DART NEUROSCIENCE, LLC

发明人： Jillian Basinger ,  James Breitenbucher ,  Graeme Freestone ,  Varsha Gupta ,  Alan Kaplan ,  Chi-Ching Mak ,  Benjamin Pratt ,  Vincent Santora ,  Dipanjan Sengupta ,  Lino Valdez

IPC分类号： C07D471/04 ,  C07D215/60 ,  C07D401/12 ,  C07D215/54

CPC分类号： A61K31/47 ,  A61K31/4375 ,  A61K31/4709 ,  C07D215/20 ,  C07D215/22 ,  C07D215/54 ,  C07D215/60 ,  C07D401/12 ,  C07D471/04

摘要： The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.

摘要翻译： 本发明提供式（I）的化学实体，其中R 1，R 2，R 3，Y和n具有本文所述的任何值和包含这些化学实体的组合物; 制作方法; 并在广泛的方法中使用，包括代谢和反应动力学研究，检测和成像技术以及放射性治疗; 选择性地抑制MAO和MAO-B的治疗，增强神经元可塑性，治疗神经障碍，提供神经保护，治疗与CNS病症相关的认知障碍，提高认知和运动训练的效率，提供神经复发和神经康复，增强 非人类动物训练方案的效率以及治疗周围疾病（包括肥胖，糖尿病和心脏代谢紊乱）及其相关并发症。