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1. 发明公开

US20240277701A1 PYRUVATE KINASE ACTIVATORS FOR USE IN THERAPY 审中-公开
公开(公告)号：US20240277701A1
公开(公告)日：2024-08-22
申请号：US18368709
申请日：2023-09-15
申请人： Agios Pharmaceuticals, Inc.
发明人： Shin-San Michael Su , Lenny Dang
IPC分类号： A61K31/496 , A61K31/415 , A61K31/4406 , A61K31/47 , A61K31/4965 , A61K31/497 , A61K31/535 , A61P7/06 , C07C13/04 , C07C307/10 , C07D205/04 , C07D213/81 , C07D215/14 , C07D235/06 , C07D241/04 , C07D241/20 , C07D271/12 , C07D295/192 , C07D307/14 , C07D333/24 , C07D401/12 , C07D405/12 , C07D417/12
CPC分类号： A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/535 , A61P7/06 , C07C307/10 , C07D205/04 , C07D213/81 , C07D215/14 , C07D235/06 , C07D241/04 , C07D241/20 , C07D271/12 , C07D295/192 , C07D333/24 , C07D401/12 , C07D405/12 , C07D417/12 , A61K31/415 , A61K31/4406 , A61K31/47 , C07C13/04 , C07D307/14
摘要： Described herein are methods for using compounds that activate pyruvate kinase.

2. 发明授权

US09732052B2 Processes and intermediates for making sweet taste enhancers 有权
公开(公告)号：US09732052B2
公开(公告)日：2017-08-15
申请号：US15184894
申请日：2016-06-16
申请人： Senomyx, Inc.
发明人： Catherine Tachdjian , Donald S. Karanewsky , Xiao-Qing Tang , Qing Chen , Peter Leeming , Tayyab Rashid , Daniel Levin
IPC分类号： C07D285/16 , C01B21/096 , C07C235/20 , C07C237/44 , C07C255/54 , C07C255/59 , C07C307/10 , C07C231/02 , C07C231/14 , C07C253/30 , C07C255/57 , C07C303/40
CPC分类号： C07D285/16 , C01B21/096 , C07C231/02 , C07C231/14 , C07C235/20 , C07C237/44 , C07C253/30 , C07C255/54 , C07C255/57 , C07C255/59 , C07C303/40 , C07C307/10
摘要： The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.

3. 发明申请

US20150175534A1 Alpha-7 NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS AND USES THEROF-I 审中-公开
标题翻译： α-7 NICOTINIC乙酰胆碱受体调节剂及其用途
公开(公告)号：US20150175534A1
公开(公告)日：2015-06-25
申请号：US14418695
申请日：2013-08-01
申请人： Merck Sharp & Dohme Corp.
发明人： Andrew Harvey , Thomas Avery , Dharam Paul , Justin Ripper , Belinda Huff , Rajinder Singh , Laurent Schaeffer , Christophe Joseph , Christophe Morice , Bruno Giethlen
IPC分类号： C07C311/37 , C07C311/08 , C07D261/14 , C07C303/36 , C07D213/74
CPC分类号： C07C311/37 , C07C211/53 , C07C217/82 , C07C303/36 , C07C307/10 , C07C311/08 , C07C311/30 , C07C311/39 , C07C311/48 , C07C311/49 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2602/50 , C07D213/74 , C07D231/38 , C07D233/72 , C07D237/20 , C07D239/42 , C07D239/47 , C07D241/20 , C07D261/14 , C07D277/42 , C07D295/135 , C07D305/08 , C07F9/58
摘要： The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (α7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of α7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases.
摘要翻译：本发明涉及式（I）化合物，其具有说明书中所述的取代基，其用于α7烟碱乙酰胆碱受体（α7nAChR）的阳性调节。本发明还涉及这些化合物在治疗或预防α7nAChR的阳性调节有益的广泛疾病中的用途，包括神经变性和神经精神疾病以及神经性疼痛和炎性疾病。

4. 发明授权

US08802720B2 Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals 有权
标题翻译：酰氨基取代的稠环戊烷羧酸衍生物及其作为药物的用途
公开(公告)号：US08802720B2
公开(公告)日：2014-08-12
申请号：US13867293
申请日：2013-04-22
申请人： SANOFI
发明人： Matthias Schaefer , Josef Pernerstorfer , Dieter Kadereit , Hartmut Strobel , Werngard Czechtizky , L. Charlie Chen , Alena Safarova , Aleksandra Weichsel , Marcel Patek
IPC分类号： A61K31/381 , A61K31/44 , C07D333/38 , C07D213/82
CPC分类号： C07C235/54 , A61K31/196 , A61K31/216 , A61K31/277 , A61K31/381 , A61K31/439 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/495 , A61K31/4965 , C07C231/02 , C07C235/62 , C07C235/84 , C07C237/38 , C07C255/54 , C07C255/57 , C07C255/58 , C07C307/10 , C07C309/73 , C07C311/08 , C07C315/04 , C07C317/22 , C07C317/46 , C07C319/12 , C07C319/20 , C07C321/26 , C07C323/12 , C07C323/19 , C07C323/42 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D207/08 , C07D207/09 , C07D207/263 , C07D209/12 , C07D209/44 , C07D211/22 , C07D213/30 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D221/04 , C07D231/12 , C07D233/54 , C07D233/64 , C07D233/84 , C07D235/12 , C07D235/18 , C07D241/38 , C07D249/06 , C07D261/04 , C07D261/20 , C07D263/32 , C07D271/08 , C07D277/24 , C07D277/56 , C07D285/06 , C07D295/08 , C07D295/20 , C07D305/06 , C07D307/12 , C07D309/06 , C07D319/06 , C07D319/12 , C07D319/20 , C07D333/16 , C07D333/38 , C07D333/56 , C07D333/78 , C07D413/04 , C07D417/04 , C07D453/02 , C07D471/08
摘要： The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I化合物，其中A，Y，Z，R 3至R 6，R 20至R 22和R 50具有权利要求中所示的含义，它们是有价值的药物活性化合物。具体来说，它们是由溶血磷脂酸（LPA）激活的内皮分化基因受体2（Edg-2，EDG2）的抑制剂，也被称为LPA1受体，可用于治疗动脉粥样硬化，心肌的疾病梗死和心力衰竭。本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。

5. 发明申请

US20120264790A1 ACYLAMINO-SUBSTITUTED CYCLIC CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译： ACYLAMINO取代的环状羧酸衍生物及其作为药物的用途
公开(公告)号：US20120264790A1
公开(公告)日：2012-10-18
申请号：US13461264
申请日：2012-05-01
申请人： Josef PERNERSTORFER , Heinz-Werner KLEEMANN , Matthias SCHAEFER , Alena SAFAROVA , Marcel PATEK
发明人： Josef PERNERSTORFER , Heinz-Werner KLEEMANN , Matthias SCHAEFER , Alena SAFAROVA , Marcel PATEK
IPC分类号： C07C61/40 , C07D231/12 , A61K31/415 , C07D213/82 , A61K31/44 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P7/02 , A61P29/00 , A61P19/02 , A61P13/12 , A61P11/00 , A61P11/06 , A61P37/00 , A61P37/08 , A61P35/04 , A61P3/00 , A61P17/06 , A61P25/00 , A61P17/04 , A61P27/02 , A61P25/18 , A61P25/28 , A61P5/00 , A61P5/16 , A61P17/02 , A61P35/00 , A61K31/196
CPC分类号： C07C235/54 , C07C231/00 , C07C231/02 , C07C235/42 , C07C235/84 , C07C255/50 , C07C255/54 , C07C255/57 , C07C307/10 , C07C317/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/22 , C07C2602/50 , C07D213/16 , C07D213/64 , C07D213/69 , C07D213/81 , C07D213/82 , C07D231/12 , C07D231/18 , C07D305/04 , C07D305/06 , C07D305/08 , C07D309/04 , C07D309/08 , C07D309/14 , C07D313/04 , C07D317/06 , C07D317/68 , C07D317/72 , C07D333/16 , C07D333/32 , C07D335/02 , C07D335/14 , C07D335/18 , C07D493/10
摘要： The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I化合物，其中A，Y，Z，R20至R22和R50具有权利要求中所示的含义，它们是有价值的药物活性化合物。具体来说，它们是由溶血磷脂酸（LPA）激活的内皮分化基因受体2（Edg-2，EDG2）的抑制剂，也被称为LPA1受体，可用于治疗动脉粥样硬化，心肌的疾病梗死和心力衰竭。本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。

6. 发明申请

US20110245494A1 PROCESSES AND INTERMEDIATES FOR MAKING SWEET TASTE ENHANCERS 有权
标题翻译：制作甜味剂增强剂的方法和中间体
公开(公告)号：US20110245494A1
公开(公告)日：2011-10-06
申请号：US13056843
申请日：2009-07-29
申请人： Catherine Tachdjian , Donald S. Karanewsky , Xiao-Qing Tang , Qing Chen , Peter Leeming , Tayyab Rashid , Daniel Levin
发明人： Catherine Tachdjian , Donald S. Karanewsky , Xiao-Qing Tang , Qing Chen , Peter Leeming , Tayyab Rashid , Daniel Levin
IPC分类号： C07D285/16 , C07C255/60 , C07C381/00 , C07C237/44 , C07C229/40 , C07C231/06 , C07C231/02 , C07C253/30 , C07C255/58
CPC分类号： C07D285/16 , C01B21/096 , C07C231/02 , C07C231/14 , C07C235/20 , C07C237/44 , C07C253/30 , C07C255/54 , C07C255/57 , C07C255/59 , C07C303/40 , C07C307/10
摘要： The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.
摘要翻译：本发明包括用于制备具有结构式（I）的化合物的方法/方法和中间体：其中X是烷基，取代的烷基，烯基，取代的烯基，杂烷基，取代的杂烷基，杂烯基或取代的杂烯基。

7. 发明授权

US08017650B2 2,3,4,5-tetrahydroxy-6-sulfooxy hexanoic acid, pharmaceutically acceptable salts and equilibrium forms thereof, processes for their preparation, pharmaceutical compositions comprising such compounds and their medical use 失效
标题翻译： 2,3,4,5-四羟基-6-磺氧基己酸，其药学上可接受的盐和平衡形式，其制备方法，包含这些化合物的药物组合物及其医疗用途
公开(公告)号：US08017650B2
公开(公告)日：2011-09-13
申请号：US12093785
申请日：2006-11-15
申请人： Jorge Ruas Da Silva , Ana Maria Staack Reis Machado , Joaquim Alberto Barros Pereira , Joao Carlos Ramos Damil , Carlos Alberto Casimiro Caixado , Augusto Eugenio Pardal Filipe
发明人： Jorge Ruas Da Silva , Ana Maria Staack Reis Machado , Joaquim Alberto Barros Pereira , Joao Carlos Ramos Damil , Carlos Alberto Casimiro Caixado , Augusto Eugenio Pardal Filipe
IPC分类号： A61K31/255 , C07C305/10
CPC分类号： C07C307/10
摘要： The invention relates to novel compounds of general formula I wherein M represents hydrogen, or a metallic cation, preferably an alkaline metal, or alkaline-earth metal, and n is equal to 1, 2 or 3. The present invention also comprises compounds of general formula I in their equilibrium forms, including lactonic forms, their enantiomers in pure form, or in an enriched form in one of the optical isomers, racemic mixtures, diastereomers and solvates thereof. The present invention further relates to processes for the preparation of compounds of general formula I, to pharmaceutical compositions comprising compounds of general formula I as only active ingredient, or in association with other active ingredients. Another aspect of the invention is the use of compounds of general formula I for the treatment of dyslipidemia, associated, or not, to other metabolic disorders, such as glucose intolerance syndrome and type 1 or 2 diabetes mellitus, by means of isolated administration or combined with other substances.
摘要翻译：本发明涉及通式I的新化合物，其中M表示氢，或金属阳离子，优选碱金属或碱土金属，n等于1,2或3.本发明还包括一般化合物其平衡形式的式I，包括内酯形式，其纯形式的对映异构体，或其中一种旋光异构体，外消旋混合物，非对映异构体和溶剂合物中的富集形式。本发明还涉及制备通式I化合物的方法，其包含通式I化合物作为活性成分或与其它活性成分结合的药物组合物。本发明的另一方面是通过分离给药或组合使用通式I的化合物来治疗与其它代谢紊乱如葡萄糖不耐受综合征和1型或2型糖尿病有关的血脂异常与其他物质。

8. 发明授权

US07906042B2 Branched surfactant having fluoroalkyl group and hydrocarbon group 有权
标题翻译：具有氟代烷基和烃基的支化表面活性剂
公开(公告)号：US07906042B2
公开(公告)日：2011-03-15
申请号：US12696694
申请日：2010-01-29
申请人： Takabumi Nagai , Kazuhisa Fujii
发明人： Takabumi Nagai , Kazuhisa Fujii
IPC分类号： B01F1/00
CPC分类号： B01F17/0057 , C07C305/06 , C07C307/10 , C07C309/17 , C11D1/004
摘要： The present invention relates to a surfactant represented by Formula (I): wherein Rf represents a fluoroalkyl group which may have an ether bond; Rh represents an alkyl group; r represents 1 or 0; when r=0, Z1 and Z2 represent (CH2)n1—(X1)p1— and —(X2)q1—, respectively; and when r=1, Z1 and Z2 represent (CH2Y)p2—CH2— and —(CH2Y)q2—, respectively, wherein X1 and X2 may be the same or different and each represents a divalent linking group, p1 represents 0 or 1, q1 represents 0 or 1, n1 represents an integer of 1-10; Y represents O, S or NR, wherein R represents a hydrogen atom, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, or t-butyl; p2 and q2 each represent 0 or 1 but are not 0 at the same time; and M represents a hydrogen atom, alkali metal, ½ alkaline earth metal or ammonium.
摘要翻译：本发明涉及由式（I）表示的表面活性剂：其中Rf表示可具有醚键的氟烷基; Rh表示烷基; r表示1或0; 当r = 0时，Z1和Z2分别表示（CH2）n1-（X1）p1和 - （X2）q1; 并且当r = 1时，Z 1和Z 2分别表示（CH 2 Y）p2-CH2-和 - （CH2Y）q2-，其中X1和X2可以相同或不同，并且各自表示二价连接基团，p1表示0或1 q1表示0或1，n1表示1〜10的整数， Y表示O，S或NR，其中R表示氢原子，甲基，乙基，正丙基，异丙基，正丁基，异丁基，仲丁基或叔丁基; p2和q2各自表示0或1，但不同时为0; M表示氢原子，碱金属，½碱土金属或铵。

9. 发明授权

US07524969B2 Malonyl-CoA decarboxylase inhibitors useful as metabolic modulators 失效
标题翻译：用作代谢调节剂的丙二酰辅酶A脱羧酶抑制剂
公开(公告)号：US07524969B2
公开(公告)日：2009-04-28
申请号：US10466923
申请日：2002-01-22
申请人： Thomas Arrhenius , Mi Chen , Jie Fei Chang , Yujin Huang , Alex Michael Nadzan , Richard Julius Penuliar , David Mark Wallace , Lin Zhang , Gary D. Lopaschuk , Jason R. Dyck
发明人： Thomas Arrhenius , Mi Chen , Jie Fei Chang , Yujin Huang , Alex Michael Nadzan , Richard Julius Penuliar , David Mark Wallace , Lin Zhang , Gary D. Lopaschuk , Jason R. Dyck
IPC分类号： C07D277/00
CPC分类号： C07D233/64 , A61K31/16 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/42 , A61K31/44 , A61K31/5375 , C07C33/48 , C07C215/24 , C07C233/22 , C07C307/10 , C07C323/14 , C07D239/42 , C07D261/04 , C07D261/08 , C07D277/46 , C07D277/48 , C07D277/52 , C07D285/135 , C07D307/46 , C07D401/12 , C07D413/06 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/08 , C07F9/6539
摘要： The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD). In particular, the invention relates to compounds and compositions and the methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the inhibition of malonyl-coenzyme A decarboxylase.
摘要翻译：本发明涉及新型化合物（I），其前药和药学上可接受的盐以及含有这样的化合物的药物组合物，其可用于治疗某些代谢疾病和通过抑制酶丙二酰辅酶A脱羧酶（丙二酰 - CoA脱羧酶，MCD）。特别地，本发明涉及通过抑制丙二酰辅酶A脱羧酶来预防，治疗和治疗心血管疾病，糖尿病，酸中毒，癌症和肥胖的化合物和组合物和方法。

10. 发明授权

US07411072B2 Tricyclic steroid hormone nuclear receptor modulators 有权
标题翻译：三环类固醇激素核受体调节剂
公开(公告)号：US07411072B2
公开(公告)日：2008-08-12
申请号：US10517010
申请日：2003-06-13
申请人： Michael Joseph Coghlan , Jonathan Edward Green , Timothy Alan Grese , Prabhakar Kondaji Jadhav , Donald Paul Matthews , Mitchell Irvin Steinberg , Kevin Robert Fales , Michael Gregory Bell
发明人： Michael Joseph Coghlan , Jonathan Edward Green , Timothy Alan Grese , Prabhakar Kondaji Jadhav , Donald Paul Matthews , Mitchell Irvin Steinberg , Kevin Robert Fales , Michael Gregory Bell
IPC分类号： A01N43/52 , C07D235/04
CPC分类号： C07D213/16 , C07C22/04 , C07C22/08 , C07C25/24 , C07C33/38 , C07C39/17 , C07C39/23 , C07C39/42 , C07C43/215 , C07C43/225 , C07C43/23 , C07C47/548 , C07C47/57 , C07C49/835 , C07C69/00 , C07C69/618 , C07C69/65 , C07C205/06 , C07C205/34 , C07C205/35 , C07C211/28 , C07C211/32 , C07C211/45 , C07C215/76 , C07C217/84 , C07C233/07 , C07C233/65 , C07C233/84 , C07C235/16 , C07C251/40 , C07C251/48 , C07C255/50 , C07C261/04 , C07C271/14 , C07C275/28 , C07C307/10 , C07C311/03 , C07C311/08 , C07C311/09 , C07C311/16 , C07C311/20 , C07C311/21 , C07C311/29 , C07C317/14 , C07C317/32 , C07C321/28 , C07C323/49 , C07C2601/02 , C07C2603/32 , C07C2603/40 , C07C2603/78 , C07C2603/86 , C07D209/08 , C07D209/34 , C07D211/96 , C07D213/06 , C07D213/73 , C07D213/76 , C07D213/81 , C07D221/16 , C07D223/20 , C07D231/12 , C07D231/18 , C07D233/26 , C07D233/68 , C07D233/84 , C07D235/26 , C07D241/12 , C07D241/20 , C07D261/08 , C07D261/10 , C07D263/52 , C07D263/56 , C07D263/58 , C07D277/60 , C07D295/088 , C07D295/26 , C07D313/12 , C07D333/78 , C07D333/80 , C07D337/12 , C07D401/06 , C07D405/06 , C07D409/04 , C07D471/04 , C07D471/06 , C07D487/04 , C07D491/044
摘要： The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation comprising administering to a patient in need thereof an effective amount of a compound of the formula: or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula I, including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula I.
摘要翻译：本发明涉及治疗对类固醇激素核受体调节敏感的病理学障碍的方法，其包括向有需要的患者施用有效量的下式化合物或其药学上可接受的盐。此外，本发明提供了新颖的式I的药物化合物，包括其药学上可接受的盐，以及包含式I化合物作为活性成分的药物组合物。

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