公开(公告)号：US20240174614A1

公开(公告)日：2024-05-30

申请号：US18341613

申请日：2023-06-26

申请人： Aldeyra Therapeutics, Inc.

发明人： Thomas A. Jordan ,  John E. Dowling ,  John Clifford Chabala

IPC分类号： C07D215/38 ,  A61K31/41 ,  A61K31/423 ,  A61K31/426 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/47 ,  A61K31/4706 ,  C07C215/68 ,  C07C229/56 ,  C07C229/60 ,  C07D261/06 ,  C07D275/00 ,  C07D277/40 ,  C07D277/56 ,  C07D333/04

CPC分类号： C07D215/38 ,  A61K31/41 ,  A61K31/423 ,  A61K31/426 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/47 ,  A61K31/4706 ,  C07C215/68 ,  C07C229/56 ,  C07C229/60 ,  C07D261/06 ,  C07D275/00 ,  C07D277/40 ,  C07D277/56 ,  C07D333/04

摘要： Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed

公开(公告)号：US11724987B2

公开(公告)日：2023-08-15

申请号：US17164556

申请日：2021-02-01

申请人： Aldeyra Therapeutics, Inc.

发明人： Thomas A. Jordan ,  John E. Dowling ,  John Clifford Chabala

IPC分类号： A61K31/4418 ,  A61K31/41 ,  A61K31/423 ,  C07D215/38 ,  A61K31/44 ,  A61K31/426 ,  A61K31/435 ,  A61K31/4706 ,  C07C215/68 ,  C07C229/60 ,  C07D277/40 ,  C07D277/56 ,  C07D261/06 ,  C07D275/00 ,  C07D333/04 ,  C07C229/56 ,  A61K31/47

CPC分类号： C07D215/38 ,  A61K31/41 ,  A61K31/423 ,  A61K31/426 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/47 ,  A61K31/4706 ,  C07C215/68 ,  C07C229/56 ,  C07C229/60 ,  C07D261/06 ,  C07D275/00 ,  C07D277/40 ,  C07D277/56 ,  C07D333/04

摘要： Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed.

公开(公告)号：US20180118662A1

公开(公告)日：2018-05-03

申请号：US15794530

申请日：2017-10-26

申请人： NUFORMIX LIMITED

发明人： Joanne HOLLAND ,  Christopher FRAMPTON

IPC分类号： C07C233/55 ,  C07C65/05 ,  C07C235/38 ,  C07C229/60 ,  C07C275/02 ,  C07C65/10 ,  C07C65/03 ,  C07D213/82 ,  C07D275/06 ,  C07C229/56

CPC分类号： C07C233/55 ,  C07B2200/13 ,  C07C65/03 ,  C07C65/05 ,  C07C65/10 ,  C07C229/56 ,  C07C229/60 ,  C07C235/38 ,  C07C275/02 ,  C07D213/82 ,  C07D275/06

摘要： New tranilast complexes and new tranilast cocrystals are disclosed. These include a 1:1 tranilast nicotinamide complex, a 1:1 tranilast nicotinamide cocrystal, a 1:1 tranilast saccharin complex, a 1:1 tranilast saccharin cocrystal, a 1:1 tranilast gentisic acid complex, a 1:1 tranilast gentisic acid cocrystal, a 1:1 tranilast salicylic acid complex, a 1:1 tranilast salicylic acid cocrystal, a 1:1 tranilast urea complex, a 1:1 tranilast urea cocrystal, a 1:1 tranilast 4-aminobenzoic acid complex, a 1:1 tranilast 4-aminobenzoic acid cocrystal, a 1:1 tranilast 2,4-dihydroxybenzoic acid complex and a 1:1 tranilast 2,4-dihydroxybenzoic acid cocrystal. Also disclosed are pharmaceutical compositions containing a tranilast complex or cocrystal of the invention and a pharmaceutically acceptable carrier. Methods of treatment using the tranilast complexes and cocrystals as well as the pharmaceutical compositions are disclosed.

公开(公告)号：US20180105485A1

公开(公告)日：2018-04-19

申请号：US15842032

申请日：2017-12-14

申请人： ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI

发明人： Ming-Ming ZHOU ,  Michael OHLMEYER ,  Adam VINCEK ,  Nilesh ZAWARE

IPC分类号： C07C225/20 ,  C07C237/40 ,  A61K31/5375 ,  A61K31/517 ,  A61K31/498 ,  A61K31/4965 ,  C07C229/68 ,  C07C229/48 ,  A61K31/4468 ,  A61K31/4409 ,  A61K31/4406 ,  A61K31/277 ,  C07C255/58 ,  A61K31/18 ,  C07C311/38 ,  A61K31/196 ,  C07C229/56 ,  C07C237/30 ,  A61K31/245 ,  C07C229/60 ,  C07D249/04 ,  C07D295/16 ,  C07D235/26 ,  C07D209/08 ,  C07D239/74 ,  C07D241/42 ,  C07D217/02 ,  C07D215/06 ,  C07D241/20 ,  C07D211/58 ,  C07D213/74 ,  C07D295/21 ,  C07D209/40 ,  C07D249/06 ,  C07D215/38 ,  C07D213/76 ,  C07D213/75 ,  A61K31/47 ,  A61K31/4402 ,  A61K31/44 ,  A61K31/4192 ,  A61K31/4184 ,  A61K31/404 ,  A61K31/195 ,  A61K31/166 ,  A61K31/136 ,  A61K45/06

CPC分类号： C07C225/20 ,  A61K31/136 ,  A61K31/166 ,  A61K31/18 ,  A61K31/195 ,  A61K31/196 ,  A61K31/245 ,  A61K31/277 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4468 ,  A61K31/47 ,  A61K31/4965 ,  A61K31/498 ,  A61K31/517 ,  A61K31/5375 ,  A61K45/06 ,  C07C229/48 ,  C07C229/56 ,  C07C229/60 ,  C07C229/68 ,  C07C237/30 ,  C07C237/40 ,  C07C255/58 ,  C07C311/38 ,  C07D209/08 ,  C07D209/40 ,  C07D211/58 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D215/06 ,  C07D215/38 ,  C07D217/02 ,  C07D235/26 ,  C07D239/74 ,  C07D241/20 ,  C07D241/42 ,  C07D249/04 ,  C07D249/06 ,  C07D295/16 ,  C07D295/21 ,  A61K2300/00

摘要： Cyclic vinylogous amides of Formula I are disclosed The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain.

公开(公告)号：US09932445B2

公开(公告)日：2018-04-03

申请号：US15076810

申请日：2016-03-22

申请人： Government of the United States, as represented by the Secretary of the Air Force

发明人： Loon-Seng Tan ,  David Huabin Wang ,  Richard A. Vaia

IPC分类号： C07C315/04 ,  C08G73/10 ,  C08G73/14 ,  C08G69/32 ,  C07C317/44 ,  C07C315/00 ,  C07C229/56

CPC分类号： C08G73/1085 ,  C07C229/56 ,  C07C315/00 ,  C07C315/04 ,  C07C317/18 ,  C07C317/40 ,  C07C317/44 ,  C08G69/32 ,  C08G69/42 ,  C08G73/1039 ,  C08G73/1042 ,  C08G73/1067 ,  C08G73/1071 ,  C08G73/14

摘要： New diamine monomers bearing sulfone terminated pendant groups, as well as methods for making the same, are provided. The diamine monomers are useful toward making polyamide, polyimide, and poly(amide-imide) polymers and copolymers, which possess hygromorphic properties and demonstrate humidity driven motility.

公开(公告)号：US09856214B2

公开(公告)日：2018-01-02

申请号：US15036211

申请日：2014-11-14

申请人： THE WISTAR INSTITUTE OF ANATOMY AND BIOLOGY

发明人： Troy E. Messick ,  Garry R. Smith ,  Allen B. Reitz ,  Paul M. Lieberman ,  Mark E. McDonnell ,  Yan Zhang ,  Venkata Velvadapu

IPC分类号： A61K31/405 ,  A61K31/41 ,  A61K31/42 ,  C07D209/42 ,  C07D401/00 ,  C07D403/00 ,  C07D207/327 ,  C07C229/56 ,  C07C255/54 ,  C07C255/55 ,  C07C211/27 ,  C07C217/84 ,  C07C233/11 ,  C07C233/64 ,  C07C233/65 ,  C07C235/58 ,  C07C311/08 ,  C07C311/16 ,  C07C311/17 ,  C07C317/14 ,  C07D235/06 ,  C07D403/10 ,  C07D239/26 ,  C07D409/10 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D209/08 ,  C07D295/155 ,  C07D213/55 ,  C07C53/18 ,  C07C63/66 ,  C07C65/19 ,  C07C65/28 ,  C07C229/64 ,  C07C317/44 ,  C07D207/08 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D211/70 ,  C07D213/64 ,  C07D213/74 ,  C07D215/14 ,  C07D231/12 ,  C07D249/06 ,  C07D277/30 ,  C07D307/79 ,  C07D333/54 ,  C07D401/04 ,  C07D401/10

CPC分类号： C07D207/327 ,  C07C53/18 ,  C07C63/66 ,  C07C65/19 ,  C07C65/28 ,  C07C211/27 ,  C07C217/84 ,  C07C229/56 ,  C07C229/64 ,  C07C233/11 ,  C07C233/64 ,  C07C233/65 ,  C07C235/58 ,  C07C255/54 ,  C07C255/55 ,  C07C311/08 ,  C07C311/16 ,  C07C311/17 ,  C07C317/14 ,  C07C317/44 ,  C07C2601/02 ,  C07D207/08 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D209/08 ,  C07D211/70 ,  C07D213/55 ,  C07D213/64 ,  C07D213/74 ,  C07D215/14 ,  C07D231/12 ,  C07D235/06 ,  C07D239/26 ,  C07D249/06 ,  C07D277/30 ,  C07D295/155 ,  C07D307/79 ,  C07D333/54 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10 ,  C07D409/10 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04

摘要： The invention provides EBNA1 inhibitors, and pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by EBNA1 activity such as, but not limited to, cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and/or rheumatoid arthritis. The compounds and compositions of the invention are further useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. The compounds and compositions of the invention are further useful for the treatment of diseases caused by lytic EBV infection.

公开(公告)号：US20170283447A1

公开(公告)日：2017-10-05

申请号：US15508114

申请日：2015-09-03

申请人： YEDA RESEARCH AND DEVELOPMENT CO. LTD.

发明人： David MILSTEIN ,  Peng HU ,  Eran FOGLER ,  Jai Anand Garg Narayana RAO

IPC分类号： C07F15/00 ,  C07C67/40 ,  C07C29/149 ,  C07D241/08 ,  C07D207/16 ,  C07C231/08 ,  C07C213/00 ,  C07C249/02 ,  C07C227/02 ,  B01J31/24 ,  C07C231/10

CPC分类号： C07F15/0046 ,  B01J31/24 ,  B01J31/2404 ,  B01J31/28 ,  B01J2231/641 ,  B01J2231/763 ,  B01J2531/0244 ,  B01J2531/821 ,  C07C29/149 ,  C07C67/00 ,  C07C67/40 ,  C07C209/00 ,  C07C209/50 ,  C07C213/00 ,  C07C227/02 ,  C07C231/02 ,  C07C231/08 ,  C07C231/10 ,  C07C249/02 ,  C07C2601/14 ,  C07D207/16 ,  C07D241/08 ,  C07C69/24 ,  C07C69/78 ,  C07C69/92 ,  C07C69/708 ,  C07C69/63 ,  C07C31/125 ,  C07C31/08 ,  C07C35/08 ,  C07C31/12 ,  C07C31/20 ,  C07C31/38 ,  C07C33/22 ,  C07C33/20 ,  C07C233/36 ,  C07C237/08 ,  C07C211/10 ,  C07C215/08 ,  C07C229/08 ,  C07C229/12 ,  C07C229/56 ,  C07C233/11 ,  C07C229/14 ,  C07C233/05 ,  C07C211/03 ,  C07C229/36

摘要： The present invention relates to novel Ruthenium complexes of formulae A1-A4 and their use, inter alia, for (1) dehydrogenative coupling of alcohols to esters; (2) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones), or polyesters); (3) preparing amides from alcohols and amines—(including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or polymerization of amino alcohols and/or forming cyclic dipeptides from p-aminoalcohols; (4) hydrogenation of amides (including cyclic dipeptides, polypeptides and polyamides) to alcohols and amines; (5) hydrogenation of organic carbonates (including polycarbonates) to alcohols or hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (6) dehydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e., synthesis of amides from esters and amines); (8) acylation of alcohols using esters; (9) coupling of alcohols with water and a base to form carboxylic acids; and (10) preparation of amino acids or their salts by coupling of amino alcohols with water and a base. The present, invention further relates to the use of certain known Ruthenium complexes for the preparation of amino acids or their salts from amino alcohols.

公开(公告)号：US20170158618A1

公开(公告)日：2017-06-08

申请号：US15336154

申请日：2016-10-27

申请人： NUFORMIX LIMITED

发明人： Joanne Holland ,  Christopher Frampton

IPC分类号： C07C233/55 ,  C07C229/56 ,  C07C275/02 ,  C07D275/06 ,  C07C65/03

CPC分类号： C07C233/55 ,  C07B2200/13 ,  C07C65/03 ,  C07C65/05 ,  C07C65/10 ,  C07C229/56 ,  C07C229/60 ,  C07C235/38 ,  C07C275/02 ,  C07D213/82 ,  C07D275/06

摘要： New tranilast complexes and new tranilast cocrystals are disclosed. These include a 1:1 tranilast nicotinamide complex, a 1:1 tranilast nicotinamide cocrystal, a 1:1 tranilast saccharin complex, a 1:1 tranilast saccharin cocrystal, a 1:1 tranilast gentisic acid complex, a 1:1 tranilast gentisic acid cocrystal, a 1:1 tranilast salicylic acid complex, a 1:1 tranilast salicylic acid cocrystal, a 1:1 tranilast urea complex, a 1:1 tranilast urea cocrystal, a 1:1 tranilast 4-aminobenzoic acid complex, a 1:1 tranilast 4-aminobenzoic acid cocrystal, a 1:1 tranilast 2,4-dihydroxybenzoic acid complex and a 1:1 tranilast 2,4-dihydroxybenzoic acid cocrystal. Also disclosed are pharmaceutical compositions containing a tranilast complex or cocrystal of the invention and a pharmaceutically acceptable carrier. Methods of treatment using the tranilast complexes and cocrystals as well as the pharmaceutical compositions are disclosed.

公开(公告)号：US09265759B2

公开(公告)日：2016-02-23

申请号：US14581462

申请日：2014-12-23

申请人： ALDEYRA THERAPEUTICS, INC.

发明人： Thomas A. Jordan ,  John E. Dowling ,  John Clifford Chabala

IPC分类号： A61K31/47 ,  A61K31/41 ,  A61K31/423 ,  A61K31/426 ,  A61K31/435 ,  A61K31/4706 ,  C07C215/68 ,  C07C229/56 ,  C07C229/60 ,  C07D215/38 ,  C07D277/40 ,  C07D277/56

CPC分类号： C07D215/38 ,  A61K31/41 ,  A61K31/423 ,  A61K31/426 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/47 ,  A61K31/4706 ,  C07C215/68 ,  C07C229/56 ,  C07C229/60 ,  C07D277/40 ,  C07D277/56

摘要： Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed.

公开(公告)号：US09102592B2

公开(公告)日：2015-08-11

申请号：US14471951

申请日：2014-08-28

申请人： MAPI PHARMA LTD.

发明人： Ehud Marom ,  Michael Mizhiritskii ,  Shai Rubnov

IPC分类号： C07D215/00 ,  C07D215/22 ,  C07C233/55 ,  C07C63/70 ,  C07C233/11 ,  C07D221/02 ,  C07C235/78 ,  C07C229/56

CPC分类号： C07C235/78 ,  C07C63/70 ,  C07C229/56 ,  C07C233/11 ,  C07C233/55 ,  C07D215/00 ,  C07D215/22

摘要： The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.

摘要翻译： 本发明涉及制备喹啉-3-甲酰胺衍生物的方法，例如5-氯-3-（乙基苯基氨基甲酰基）-1-甲基-2-氧代-1,2-二氢喹啉-4-醇酸钠（Laquinimod钠 ）。 本发明还涉及在这些方法中形成的中间体。