专利检索 ipc:"C07C323/40" 第 1 页

1.

发明申请
KETONE INHIBITORS OF LYSINE GINGIPAIN 有权

公开(公告)号：US20210053908A1

公开(公告)日：2021-02-25

申请号：US16899376

申请日：2020-06-11

申请人： CORTEXYME, INC.

发明人： Andrei W. Konradi , Robert A. Galemmo, JR. , Stephen S. Dominy , Casey C. Lynch , Leslie J. Holsinger

IPC分类号： C07C233/62 , C07D213/82 , C07D239/34 , C07D239/36 , C07D413/12 , C07D257/04 , C07D261/12 , C07D213/70 , C07C317/28 , C07C233/78 , C07C235/10 , C07C235/50 , C07B59/00 , C07C237/42 , C07D401/12 , C07C381/00 , C07C323/42 , C07D213/65 , C07D213/68 , C07D239/38 , C07C247/18 , C07F5/02 , A61P31/04 , A61P25/00 , A61K31/165 , A61K31/167 , A61K31/41 , A61K31/42 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/505 , A61K31/513 , A61K31/655 , A61K45/06 , C07C245/08 , C07C247/16 , C07C323/40 , C07D213/81

摘要： The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.

2.

发明授权
Ketone inhibitors of lysine gingipain 有权

公开(公告)号：US10730826B2

公开(公告)日：2020-08-04

申请号：US16353786

申请日：2019-03-14

申请人： CORTEXYME, INC.

发明人： Andrei W. Konradi , Robert A. Galemmo, Jr. , Stephen S. Dominy , Casey C. Lynch , Leslie J. Holsinger

IPC分类号： C07C233/62 , C07D213/82 , C07D239/34 , C07D239/36 , C07D413/12 , C07D257/04 , C07D261/12 , C07D213/70 , C07C317/28 , C07C233/78 , C07C235/10 , C07C235/50 , C07B59/00 , C07C237/42 , C07D401/12 , C07C381/00 , C07C323/42 , C07D213/65 , C07D213/68 , C07D239/38 , C07C247/18 , C07F5/02 , A61P31/04 , A61P25/00 , A61K31/165 , A61K31/167 , A61K31/41 , A61K31/42 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/505 , A61K31/513 , A61K31/655 , A61K45/06 , C07C245/08 , C07C247/16 , C07C323/40 , C07D213/81

摘要： The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.

3.

发明授权
Industrial process for the preparation of (5S, 10S)-10-benzyl-16-methyl-11, 14, 18-trioxo-15, 17, 19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium(E)-3-carboxyacrylate salt 有权

公开(公告)号：US10399936B2

公开(公告)日：2019-09-03

申请号：US15767966

申请日：2016-10-14

申请人： PHARMALEADS

发明人： Herve Poras , Loic Lefebvre , Xinjun Zhao , Luca Gamberoni , Sabrina De Rosa , Rosario Velardi

IPC分类号： C07C323/25 , C07C319/02 , C07C319/22 , C07C319/24 , C07C319/28 , C07C327/32 , B01J19/18 , C07D215/26 , C07C323/40

摘要： The present invention relates to an industrial process for the preparation of (5S,10S)-10-benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (E)-3-carboxyacrylate salt of following formula (I): wherein X is fumarate. This process comprises the following successive key steps: a kinetic resolution, formation of disulfide compound, peptide coupling, and anion exchange reaction to obtain the desired product of formula (I).

4.

发明申请
Compositions and methods for the treatment of disease associated with Trp-p8 expression 有权
标题翻译：用于治疗与Trp-p8表达相关的疾病的组合物和方法

公开(公告)号：US20050054651A1

公开(公告)日：2005-03-10

申请号：US10923413

申请日：2004-08-20

申请人： Sateesh Natarajan , Ofir Moreno , Thomas Graddis , David Duncan , Reiner Laus , Feng Chen

发明人： Sateesh Natarajan , Ofir Moreno , Thomas Graddis , David Duncan , Reiner Laus , Feng Chen

IPC分类号： A61K31/498 , A61K31/517 , A61K45/06 , C07C311/20 , C07C311/37 , C07C323/40 , C07C323/44 , C07C333/06 , C07D207/06 , C07D207/09 , C07D207/32 , C07D207/325 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/48 , C07D213/40 , C07D215/04 , C07D215/08 , C07D215/46 , C07D217/06 , C07D231/12 , C07D231/14 , C07D231/56 , C07D235/18 , C07D235/26 , C07D239/42 , C07D241/18 , C07D241/44 , C07D251/54 , C07D263/34 , C07D263/56 , C07D263/57 , C07D279/12 , C07D295/096 , C07D295/135 , C07D295/26 , C07D307/52 , C07D317/66 , C07D333/34 , C07D401/04 , C07D405/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D471/04 , C07D487/04 , C07D493/08 , C07D495/04 , C07D513/04 , G01N33/68

CPC分类号： C07C233/60 , A61K31/498 , A61K31/517 , A61K45/06 , C07C233/58 , C07C243/36 , C07C243/38 , C07C311/20 , C07C311/37 , C07C323/40 , C07C323/44 , C07C333/06 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D207/06 , C07D207/09 , C07D207/325 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/20 , C07D209/48 , C07D211/06 , C07D213/40 , C07D215/04 , C07D215/08 , C07D215/46 , C07D217/06 , C07D223/04 , C07D231/12 , C07D231/14 , C07D231/56 , C07D235/18 , C07D235/26 , C07D239/42 , C07D241/18 , C07D241/44 , C07D241/54 , C07D251/54 , C07D263/34 , C07D263/57 , C07D279/12 , C07D295/096 , C07D295/135 , C07D295/155 , C07D295/26 , C07D307/52 , C07D311/16 , C07D317/66 , C07D333/34 , C07D401/04 , C07D403/14 , C07D405/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D471/04 , C07D487/04 , C07D493/08 , C07D495/04 , C07D513/04 , G01N33/5011 , G01N33/6872 , G01N2500/10 , A61K2300/00

摘要： Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

摘要翻译： 提供的是小分子Trp-p8调节剂，包括Trp-p8激动剂和Trp-p8拮抗剂，以及包含小分子Trp-p8激动剂的组合物以及用于鉴定和表征新型小分子Trp-p8调节剂的方法和方法降低Trp-p8表达细胞的生存力和/或抑制Trp-p8表达细胞的生长，用于激活Trp-p8介导的阳离子流入的方法，用于刺激细胞凋亡和/或坏死的方法以及用于治疗疾病的相关方法，包括癌症如肺，乳腺，结肠癌和/或前列腺癌以及与Trp-p8表达相关的其它疾病，例如良性前列腺增生。

5.

发明授权
Polyethylene glycol modified ceramide lipids and liposome uses thereof 失效
标题翻译：聚乙二醇改性的神经酰胺脂质及其脂质体用途

公开(公告)号：US5820873A

公开(公告)日：1998-10-13

申请号：US486214

申请日：1995-06-07

申请人： Lewis S. L. Choi , Thomas D. Madden , Murray S. Webb

发明人： Lewis S. L. Choi , Thomas D. Madden , Murray S. Webb

IPC分类号： G01N33/544 , A61K9/127 , A61K47/48 , B01J13/02 , C07C233/18 , C07C233/36 , C07C271/20 , C07C323/40 , C07F9/09 , C08G65/32 , C08G65/329 , A61K39/00 , A61K39/395 , A61K45/00

CPC分类号： A61K9/1272 , A61K47/48215 , C08G65/329 , Y10S424/812 , Y10S514/885

摘要： The present invention provides a novel class of polyethylene glycol modified ceramide lipids. The lipids can be used to form liposomes optionally containing various biological agents or drugs, such as anti-cancer agents. In addition, methods of use for the liposomes are provided.

摘要翻译： 本发明提供了一类新型的聚乙二醇改性的神经酰胺脂质。脂质可用于形成任选地含有各种生物制剂或药物如抗癌剂的脂质体。此外，提供了脂质体的使用方法。

6.

发明授权
Ultraviolet ray-absorbing aromatic compound and polymeric composition containing the same 失效
标题翻译：紫外线吸收芳香族化合物和含有它们的聚合物组合物

公开(公告)号：US5532412A

公开(公告)日：1996-07-02

申请号：US304866

申请日：1994-09-13

申请人： Toshitsugu Matsuki , Toshihiro Santa

发明人： Toshitsugu Matsuki , Toshihiro Santa

IPC分类号： C07C235/64 , C07C235/66 , C07C323/40 , C07D209/56 , C07D209/80 , C07D209/88 , C07D235/02 , C07D307/91 , C08K5/00 , C08K5/20 , C08K5/375 , C08L77/00 , C08L77/10 , C08L101/00 , C09K3/00 , C07C233/65

CPC分类号： C07D209/80 , C07C235/64 , C07C235/66 , C07C323/40 , C07D209/88 , C07D307/91 , C08K5/005 , C08K5/20 , C08K5/375 , C07C2103/24

摘要： An aromatic o-hydroxyamide compound of the formula (I) ##STR1## wherein the formula: ##STR2## is a divalent aromatic group the formula: ##STR3## R.sup.1 =H, halogen, C.sub.1-10 alkyl group, or C.sub.1 -alkoxyl group, Ar.sub.1, Ar.sub.2, Ar.sub.3 =a divalent aromatic groups, X, Y=O or S, and n=0 or 1, has an excellent ultraviolet ray-absorption and heat-resistance and is useful for enhancing an ultraviolet ray-resistance of polymeric materials, for example, wholly aromatic polyamide fibers.

摘要翻译： 式（I）的芳族邻羟基酰胺化合物其中式：其中式为：下式的二价芳基：R 1 = H，卤素，C 1-10烷基或C 1 - 烷氧基，Ar 1，Ar 2，Ar 3 =二价芳基，X，Y = O或S，n = 0或1具有优异的紫外线吸收和耐热性，并且可用于增强聚合材料的抗紫外线性，例如全芳族聚酰胺纤维。

7.

发明授权
Phenylamidine and phenylguanidine derivatives and their use as anti-diabetic agents 失效
标题翻译：苯脒和苯胍衍生物及其作为抗糖尿病药的用途

公开(公告)号：US5373008A

公开(公告)日：1994-12-13

申请号：US9807

申请日：1993-01-27

申请人： Balasubramanian Gopalan

发明人： Balasubramanian Gopalan

IPC分类号： C07D295/12 , A61K31/155 , A61K31/40 , A61K31/4427 , A61K31/445 , A61K31/5375 , A61K31/5377 , A61P3/08 , A61P3/10 , C07C257/10 , C07C257/14 , C07C257/16 , C07C279/18 , C07C317/40 , C07C317/42 , C07C323/40 , C07C323/41 , C07C323/44 , C07D207/22 , C07D211/72 , C07D223/12 , C07D225/04 , C07D233/50 , C07D265/30 , C07D295/13 , C07D295/135 , C07D401/12 , C07D403/12 , C07D413/12 , A61K31/535 , A61K31/54 , C07D401/10 , C07D403/10 , C07D413/10 , C07D417/10

CPC分类号： C07D295/135 , C07C257/10 , C07C279/18 , C07D207/22 , C07D211/72 , C07D223/12 , C07D225/04 , C07D233/50 , C07D295/13 , C07D401/12 , C07C2101/14

摘要： Compounds of formula I ##STR1## and their salts in which n=0 or 1, R.sub.1 and R.sub.2 are each aliphatic or cycloalkyl or NR.sub.1 R.sub.2 is an optionally substituted heterocyclic ring, R.sub.3 is alkyl, cycloalkyl or optionally substituted amino, R.sub.5 is an aliphatic group, R.sub.6 is H, an optionally substituted aliphatic group or a cycloalkyl group, or R.sub.3 and R.sub.5 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached form a heterocyclic ring optionally substituted by alkyl and R.sub.7 is optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkoxycarbonyl, trifluoromethyl or cyano have utility as hypoglycemic agents.

摘要翻译： 式I的化合物及其盐，其中n = 0或1，R 1和R 2各自为脂族或环烷基或NR 1 R 2为任选取代的杂环，R 3为烷基，环烷基或任选取代的氨基，R 5为脂族基团 R 6为H，任意取代的脂族基或环烷基，或者R 3和R 5与它们所连接的氮原子和碳原子一起形成任选取代的杂环或R 5和R 6与它们所连接的氮一起形成任选被烷基取代的杂环，并且R 7是任选取代的烷基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷氧基羰基，三氟甲基或氰基，可用作降血糖剂。

8.

发明授权
Tricyclic compounds and intermediates thereof 失效
标题翻译：三环化合物及其中间体

公开(公告)号：US5340807A

公开(公告)日：1994-08-23

申请号：US989906

申请日：1992-12-11

申请人： Toshiaki Kumazawa , Masashi Yanase , Hiroyuki Harakawa , Hiroyuki Obase , Shoji Oda , Shiro Shirakura , Koji Yamada , Kazuhiro Kubo

发明人： Toshiaki Kumazawa , Masashi Yanase , Hiroyuki Harakawa , Hiroyuki Obase , Shoji Oda , Shiro Shirakura , Koji Yamada , Kazuhiro Kubo

IPC分类号： A61K31/335 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/215 , A61K31/235 , A61K31/275 , A61K31/38 , A61K31/435 , A61K31/44 , A61K31/55 , A61P3/06 , A61P9/10 , A61P43/00 , C07C233/65 , C07C235/46 , C07C235/48 , C07C237/40 , C07C323/40 , C07C323/62 , C07C327/26 , C07C331/08 , C07D221/16 , C07D223/20 , C07D233/58 , C07D313/12 , C07D337/12 , C07D471/04 , C07D491/04 , C07D491/044 , C07D495/04 , A01N43/46 , C07D273/02 , C07D313/06

CPC分类号： C07D491/04 , C07C233/65 , C07D223/20 , C07D313/12 , C07D337/12 , C07C2103/32 , Y10S514/824

摘要： Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6 alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 --O, CH.sub.2 --(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.

摘要翻译： 公开了由式（I）表示的三环化合物：其中R 1，R 2，R 3和R 4各自独立地表示氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基， C 1-6烷基氨基，卤代C 1-6烷基，卤代C 1-6烷氧基，卤素，硝基，氰基，羧基，C 1-6烷氧基羰基，羟甲基，CR 9 R 10 CO 2 R 11（其中R 9，R 10和R 11各自独立地表示氢或C 1-6烷基）或CONR 12 R 13（其中R 12和R 13各自独立地表示氢或C 1-6烷基）; R5表示氢或C1-6烷基; R 6，R 7和R 8各自独立地表示氢，C 1-6烷基，羟基，C 1-6烷氧基，C 1-6烷酰氧基，C 1-6烷硫基，氰硫基或卤素; X表示CH或N; Y1-Y2表示CH2-O，CH2-（O）n，（其中n表示0,1或2），CH2CH2，CH = CH或CON（R14）（其中R14表示氢或C1-6烷基）和Z 表示氧或硫，或其药学上可接受的盐。该化合物具有酰基辅酶A：胆固醇酰基转移酶抑制活性，因此预期对高脂血症和动脉硬化具有预防和治疗作用。