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公开(公告)号:US10550149B2
公开(公告)日:2020-02-04
申请号:US16022578
申请日:2018-06-28
发明人: Ronald M. Evans , Michael Downes
IPC分类号: A61K31/5377 , C07K5/062 , C07D309/04 , C07D407/12 , C07D271/12 , C07D295/13 , C07D213/40 , C07D213/64 , C07D307/68 , C07D309/06 , C07D231/12 , C07D333/24 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/10 , C07D417/12 , C07C233/87 , C07D205/04 , C07D209/34 , C07D295/155 , C07D213/56 , C07D305/06 , C07D307/54 , C07D307/81 , C07D307/83 , C07C255/57 , C07C259/06 , C07C233/73 , C07C235/42 , C07C235/48 , C07C235/84 , C07C237/32 , C07C317/44 , C07C233/75 , C07D333/38
摘要: Provided herein are deuterated compounds and compositions useful in increasing PPARδ activity. The compounds have a formula where L5 comprises at least one deuterium. Exemplary species include The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
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公开(公告)号:US10253007B2
公开(公告)日:2019-04-09
申请号:US15038264
申请日:2014-11-21
发明人: Wei Zhou , Yunrong Jing , Yongfeng Wang , Guocheng Wang
IPC分类号: A61K31/337 , C07D305/14 , C07D405/12 , C07C271/22 , C07C233/87
摘要: The present invention provides taxanes compounds with a formula (I) or formula (II) structure, a method for preparing the compounds, as well as the use of the compositions containing the compounds, pharmaceutically acceptable salts and solvates thereof as active ingredients in manufacturing oral antitumor medicaments, In formula (I), R1 is —COR6, —COOR6 or —CONR7aR7b; R2 is a C1-C6 alkyl, a C1-C6 alkenyl, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; R3 is —OR6, —OCOOR6, —OCOSR6 or —OCONR7aR7b; R4 is —OR6, —OCOOR6, —OCOSR6, —OCONR7aR7b or H; wherein, R6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; R7a and R7b are respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group. In formula (II), R1 is —COR6 or —COOR6; R2 is an aromatic group; R3 is —OR6; wherein, R6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group.
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公开(公告)号:US20170320828A1
公开(公告)日:2017-11-09
申请号:US15495670
申请日:2017-04-24
发明人: Wenjin Yang , Che-Hong Chen , Daria Mochly-Rosen
IPC分类号: C07D213/82 , C07D413/12 , C07C233/66 , C07C233/73 , C07D405/12 , C07D403/12 , C07D401/12 , C07D317/58 , C07D213/89 , C07D213/81 , C07C317/32 , C07C311/40 , C07C311/29 , C07C311/17 , C07C311/16 , C07C237/32 , C07C235/60 , C07C235/48 , C07C233/87 , C07C233/78 , C07D417/12 , C07C2601/02 , C07C2601/04 , C07C2601/08
CPC分类号: C07D213/82 , C07C233/66 , C07C233/73 , C07C233/78 , C07C233/87 , C07C235/48 , C07C235/60 , C07C237/32 , C07C311/16 , C07C311/17 , C07C311/29 , C07C311/40 , C07C317/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/81 , C07D213/89 , C07D317/58 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要: The present disclosure provides compounds of formula (I) that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity, and methods of preparing these compounds.
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公开(公告)号:US09670162B2
公开(公告)日:2017-06-06
申请号:US14774071
申请日:2014-03-13
发明人: Wenjin Yang , Che-Hong Chen , Daria Mochly-Rosen
IPC分类号: C07D213/82 , A61K31/44 , C07D213/81 , C07D401/12 , C07D405/12 , C07C311/16 , C07C311/17 , C07C311/29 , C07C311/40 , C07C317/32 , C07C233/66 , C07C233/73 , C07C233/78 , C07C233/87 , C07C235/60 , C07C237/32 , C07C235/48 , C07D213/89 , C07D317/58 , C07D403/12 , C07D413/12 , C07D417/12
CPC分类号: C07D213/82 , C07C233/66 , C07C233/73 , C07C233/78 , C07C233/87 , C07C235/48 , C07C235/60 , C07C237/32 , C07C311/16 , C07C311/17 , C07C311/29 , C07C311/40 , C07C317/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/81 , C07D213/89 , C07D317/58 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要: The present disclosure provides compounds of formula (I) that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity, and methods of preparing these compounds.
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公开(公告)号:US09510592B2
公开(公告)日:2016-12-06
申请号:US14880651
申请日:2015-10-12
申请人: Dow AgroSciences LLC
发明人: William C. Lo , James E. Hunter , Gerald B. Watson , Akshay Patny , Pravin S. Iyer , Joshodeep Boruwa
IPC分类号: A01N59/26 , A61K31/166 , A01N59/02 , C07C243/38 , A01N59/00 , A61K31/277 , C07C255/42 , C07C233/87 , A61K33/42 , A01C1/06 , A01N37/44 , A01N37/18 , A01N43/20 , A01N43/36 , A01N43/40 , A01N43/54 , A01N43/60 , A01N43/84 , A61K31/38 , A61K31/4015 , A61K31/44 , A61K31/4965 , A61K31/505 , A61K31/5375 , C07D207/27 , C07D213/56 , C07D239/26 , C07D241/12 , C07D295/10 , C07D331/04 , C07C327/42 , C07C233/78 , C07C255/19 , A01N37/20 , A01N37/28 , A01N41/10 , A01N43/08 , A01N43/16 , A01N43/38 , A01N43/653 , A01N43/78 , A01N43/82 , A01N47/32 , A01N53/00 , A01N37/10 , A01N37/34 , A01N37/46 , A01N43/50 , A01N25/08 , A01N33/04 , A01N43/58 , C07C63/70 , C07C211/29 , C07C233/59 , C07C255/57 , C07C335/14 , C07D209/50 , C07D211/58 , C07D213/61 , C07D233/64 , C07D237/32 , C07D249/08 , C07D271/10 , C07D277/30 , C07D277/64 , C07D295/192 , C07D307/16 , C07D309/14 , C07D401/10 , C07C63/74 , C07C233/66 , C07C255/66 , C07C327/56
CPC分类号: C07C63/70 , A01N25/08 , A01N33/04 , A01N37/10 , A01N37/18 , A01N37/20 , A01N37/28 , A01N37/30 , A01N37/34 , A01N37/44 , A01N37/46 , A01N41/10 , A01N43/08 , A01N43/16 , A01N43/20 , A01N43/36 , A01N43/38 , A01N43/40 , A01N43/50 , A01N43/54 , A01N43/58 , A01N43/60 , A01N43/653 , A01N43/78 , A01N43/82 , A01N43/84 , A01N47/12 , A01N47/28 , A01N47/32 , A01N53/00 , A01N59/02 , A61K31/38 , A61K31/4015 , A61K31/44 , A61K31/4965 , A61K31/505 , A61K31/5375 , C07C63/74 , C07C211/29 , C07C211/42 , C07C233/12 , C07C233/15 , C07C233/59 , C07C233/64 , C07C233/65 , C07C233/66 , C07C233/78 , C07C237/52 , C07C239/20 , C07C243/36 , C07C243/38 , C07C255/19 , C07C255/50 , C07C255/57 , C07C255/66 , C07C271/14 , C07C275/24 , C07C317/44 , C07C327/42 , C07C327/48 , C07C327/56 , C07C335/02 , C07C335/14 , C07C2601/02 , C07C2602/46 , C07D207/26 , C07D207/27 , C07D209/08 , C07D209/48 , C07D209/50 , C07D211/58 , C07D213/40 , C07D213/56 , C07D213/61 , C07D213/74 , C07D233/64 , C07D237/32 , C07D239/26 , C07D241/12 , C07D249/08 , C07D249/14 , C07D271/10 , C07D277/28 , C07D277/30 , C07D277/64 , C07D295/10 , C07D295/108 , C07D295/192 , C07D307/06 , C07D307/16 , C07D307/52 , C07D309/14 , C07D331/04 , C07D401/10 , C07D405/04
摘要: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
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公开(公告)号:US20160023991A1
公开(公告)日:2016-01-28
申请号:US14874008
申请日:2015-10-02
发明人: Ronald M. Evans , Michael Downes , Thomas J. Baiga , Joseph P. Noel , Emi Kanakubo Embler , Weiwei Fan , John F.W. Keana , Mark G. Bock , Arthur F. Kluge , Mike A. Patane
IPC分类号: C07C233/87 , C07C259/06 , C07D213/56 , C07D405/04 , C07D307/54 , C07D333/24 , C07D295/13 , C07C237/48 , C07D231/12
CPC分类号: C07C233/87 , A61K31/164 , A61K31/341 , A61K31/381 , A61K31/4025 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/44 , A61K31/5377 , C07C233/73 , C07C235/42 , C07C235/48 , C07C235/84 , C07C237/22 , C07C237/32 , C07C237/48 , C07C255/57 , C07C259/06 , C07C317/44 , C07C2601/02 , C07D207/04 , C07D209/34 , C07D213/56 , C07D231/12 , C07D271/12 , C07D295/13 , C07D305/06 , C07D307/54 , C07D307/83 , C07D309/06 , C07D333/24 , C07D405/04 , C07D405/10 , C07D405/12 , C07D407/12 , C07D413/04 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/10 , C07D417/12
摘要: Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
摘要翻译: 本文提供了可用于增加PPARδ活性的化合物和组合物。 本文提供的化合物和组合物可用于治疗PPARδ相关疾病(例如肌肉疾病,血管疾病,脱髓鞘疾病和代谢疾病)。
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公开(公告)号:US09139515B2
公开(公告)日:2015-09-22
申请号:US14236999
申请日:2012-08-16
申请人: Petrus Johannes Hermsen , Peter Hans Ermann , Peter Hans Riebel , Michael Wolberg , Andreas Hendrikus Maria De Vries
发明人: Petrus Johannes Hermsen , Peter Hans Ermann , Peter Hans Riebel , Michael Wolberg , Andreas Hendrikus Maria De Vries
IPC分类号: C07C233/51 , C07C231/02 , C07C235/26 , C07C269/04 , C07C271/16 , C07C213/02 , C07C215/28 , C07C231/12 , C07C233/73 , C07C233/87
CPC分类号: C07C233/51 , C07C213/02 , C07C215/28 , C07C231/12 , C07C233/73 , C07C233/87 , C07C269/04 , C07C271/16
摘要: This invention relates to a novel process for the synthesis of R-biphenylalaninol and to intermediate compounds that are formed in the process according to the invention, i.e. novel intermediates useful in the synthesis of R-biphenylalaninol. The invention also relates to R-biphenylalaninol, The process according to the invention, the intermediates to of R-biphenylalaninol and of R-biphenylalaninol are all useful in the synthesis of pharmaceutically active compounds.
摘要翻译: 本发明涉及一种用于合成R-联苯基苯丙醇和在本发明方法中形成的中间体化合物的新方法,即用于合成R-联苯丙氨醇的新型中间体。 本发明还涉及R-联苯基丙氨醇。根据本发明的方法,R-联苯基苯丙醇和R-联苯丙氨醇的中间体都可用于药物活性化合物的合成。
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公开(公告)号:US20050282900A1
公开(公告)日:2005-12-22
申请号:US11179729
申请日:2005-07-13
IPC分类号: A61P3/10 , A61K31/165 , A61K31/166 , A61K31/198 , A61K31/223 , A61K31/24 , A61P1/00 , A61P11/00 , A61P11/06 , A61P19/00 , A61P19/02 , A61P29/00 , A61P37/06 , C07B61/00 , C07C231/12 , C07C231/14 , C07C233/00 , C07C233/87
CPC分类号: C07C233/87 , A61K31/198
摘要: The present invention relates to a phenylalanine derivative of Formula (I) wherein X1 is a halogen atom, X2 is a halogen atom, Q is a CH2R— is a carboxyl group which may be esterified; or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明涉及式(I)的苯丙氨酸衍生物,其中X 1是卤原子,X 2是卤素原子,Q是CH 2 R-是可被酯化的羧基; 或其药学上可接受的盐。
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公开(公告)号:US20050215598A1
公开(公告)日:2005-09-29
申请号:US11130531
申请日:2005-05-17
申请人: Sarah Archibald , John Head , Graham Warrellow , John Porter
发明人: Sarah Archibald , John Head , Graham Warrellow , John Porter
IPC分类号: A61K31/195 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4439 , A61K31/455 , A61P29/00 , A61P37/02 , A61P43/00 , C07C233/87 , C07C235/60 , C07C237/30 , C07C323/62 , C07D213/61 , C07D213/81 , C07D403/12 , C07D213/46 , C07D43/02
CPC分类号: C07D213/81 , C07C233/87 , C07C235/60 , C07C237/30 , C07C323/62 , C07D213/61
摘要: Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; Ar is an optionally substituted aromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译: 描述了式(1)的苯丙氨酸衍生物:其中R是羧酸或其衍生物; L 1是连接原子或基团; Ar是任选取代的芳族基团; 及其盐,溶剂合物,水合物和N-氧化物。 该化合物能够抑制α4整联蛋白与其配体的结合,并且可用于预防和治疗免疫或炎症性疾病。
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公开(公告)号:US20050186176A1
公开(公告)日:2005-08-25
申请号:US11104173
申请日:2005-04-11
申请人: Andrea Leone-Bay , Sam Milstein , Donald Sarrubi , Harry Leipold
发明人: Andrea Leone-Bay , Sam Milstein , Donald Sarrubi , Harry Leipold
IPC分类号: A01N37/00 , A61K9/00 , A61K9/16 , A61K9/48 , A61K38/00 , A61K38/20 , A61K38/21 , A61K38/23 , A61K38/27 , A61K38/28 , A61K38/29 , A61K47/18 , A61K47/20 , A61K47/22 , A61K47/48 , C07C229/42 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/69 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , C07C235/82 , C07C237/12 , C07C237/20 , C07C237/36 , C07C237/40 , C07C237/42 , C07C243/38 , C07C259/06 , C07C271/28 , C07C271/54 , C07D209/48 , C07D211/62 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , C07D257/04 , C07D295/192 , C07D311/12 , C07D311/24 , C07D311/30 , A61K31/195 , A61K31/728 , A61K31/737 , A61K38/22
CPC分类号: C07D209/48 , A61K9/0019 , A61K9/0043 , A61K9/0056 , A61K9/1617 , A61K9/4858 , A61K31/727 , A61K38/212 , A61K38/23 , A61K38/27 , A61K38/29 , A61K47/18 , A61K47/183 , A61K47/20 , A61K47/22 , A61K47/541 , C07C229/42 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/69 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , C07C235/82 , C07C237/12 , C07C237/20 , C07C237/36 , C07C237/40 , C07C237/42 , C07C243/38 , C07C259/06 , C07C271/28 , C07C271/54 , C07D211/62 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , C07D257/04 , C07D295/192 , C07D311/12 , C07D311/24 , C07D311/30
摘要: Modified amino acid compounds useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
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