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1. 发明公开

US20230167070A1 MODULATORS OF TREX1 审中-公开
公开(公告)号：US20230167070A1
公开(公告)日：2023-06-01
申请号：US17922388
申请日：2021-04-30
申请人： Constellation Pharmaceuticals, Inc.
发明人： Julian R. Levell , Jonathan E. Wilson , Aaron Coffin , Kennedy Taveras
IPC分类号： C07D239/14 , A61P35/00
CPC分类号： C07D239/14 , A61P35/00
摘要： Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

2. 发明申请

US20180319743A1 TETRALIN AND INDANE DERIVATIVES AND USES THEREOF 审中-公开
公开(公告)号：US20180319743A1
公开(公告)日：2018-11-08
申请号：US16033169
申请日：2018-07-11
申请人： Roche Palo Alto LLC
发明人： Robert Greenhouse , Ralph New Harris, III , Saul Jaime-Figueroa , James M. Kress , David Bruce Repke , Russell Stephen Stabler
IPC分类号： C07C317/32 , C07D233/58 , C07D277/82 , C07D239/42 , C07D239/14 , C07D235/06 , C07D233/90 , C07D233/88 , C07D233/84 , C07D233/64 , C07D233/54 , C07D233/48 , C07D233/34 , C07D233/20 , C07D231/18 , C07D209/30 , C07D207/36 , C07D207/34 , C07D207/325 , C07D207/16 , C07C317/44 , C07D233/44
CPC分类号： C07C317/32 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07D207/16 , C07D207/325 , C07D207/34 , C07D207/36 , C07D209/30 , C07D231/18 , C07D233/20 , C07D233/34 , C07D233/44 , C07D233/48 , C07D233/54 , C07D233/58 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/06 , C07D239/14 , C07D239/42 , C07D277/82
摘要： The applicaton discloses pharmaceutical compounds of formula I useful for treating CNS diseases wherein m, s, R1R5, R6 and R7 are as defined herein.

3. 发明申请

US20180044299A1 SYNTHESIS OF CYCLOCREATINE AND ANALOGS THEREOF 审中-公开
公开(公告)号：US20180044299A1
公开(公告)日：2018-02-15
申请号：US15556657
申请日：2016-03-11
申请人： Lumos Pharma, Inc.
发明人： William R. Cantrell, JR. , William E. Bauta
IPC分类号： C07D239/14 , C07C279/14 , C07C277/02 , C07C279/12
CPC分类号： C07D239/14 , A61K31/4172 , C07C277/02 , C07C279/12 , C07C279/14
摘要： Provided herein is a process an intermediates for the preparation of a compound of formula (I): or a pharmaceutically acceptable salt thereof, using cyanamide in the reaction.

4. 发明申请

US20170050924A1 INHIBITORS OF CREATINE TRANSPORT AND USES THEREOF 审中-公开
标题翻译：运输运输的抑制剂及其用途
公开(公告)号：US20170050924A1
公开(公告)日：2017-02-23
申请号：US15307178
申请日：2015-04-30
申请人： Rgenix, Inc.
发明人： Eduardo J. MARTINEZ , Sohail F. TAVAZONE
IPC分类号： C07C279/14 , C07D233/46 , A61K31/4168 , C07D239/14 , A61K31/505 , C07D233/52 , C07D253/06 , A61K31/53 , A61K31/155 , C07D213/74 , A61K31/4402 , C07C275/70 , C07D207/16 , A61K31/40 , C07D205/08 , A61K31/397 , C07D401/04 , A61K31/4427 , C07H19/06 , A61K31/7068 , A61K45/06
CPC分类号： C07C279/14 , A61K31/00 , A61K31/155 , A61K31/337 , A61K31/397 , A61K31/40 , A61K31/4168 , A61K31/4402 , A61K31/4427 , A61K31/505 , A61K31/53 , A61K31/704 , A61K31/7068 , A61K31/7105 , A61K45/06 , C07B2200/05 , C07C257/14 , C07C259/14 , C07C275/70 , C07C279/16 , C07C279/26 , C07C279/36 , C07C281/16 , C07C281/18 , C07C309/15 , C07C313/34 , C07C2601/02 , C07C2601/04 , C07D205/04 , C07D205/08 , C07D207/16 , C07D207/22 , C07D213/74 , C07D213/76 , C07D231/12 , C07D233/26 , C07D233/46 , C07D233/52 , C07D233/64 , C07D233/88 , C07D239/06 , C07D239/14 , C07D249/08 , C07D249/14 , C07D253/06 , C07D257/08 , C07D295/32 , C07D401/04 , C07D405/04 , C07D487/04 , C07F9/097 , C07F9/2458 , C07F9/3808 , C07F9/4006 , C07F9/48 , C07F9/568 , C07F9/572 , C07F9/6506 , C07H19/06 , A61K2300/00
摘要： This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.
摘要翻译：本发明涉及抑制肌酸转运和/或肌酸激酶的化合物，包括这些化合物的药物组合物，以及利用这些化合物和组合物治疗癌症的方法。

5. 发明申请

US20160264566A1 ANTI-ALPHAVBETA1 INTEGRIN INHIBITORS AND METHODS OF USE 审中-公开
标题翻译：抗ALPHAVBETA1 INTEGRIN抑制剂及其使用方法
公开(公告)号：US20160264566A1
公开(公告)日：2016-09-15
申请号：US15067124
申请日：2016-03-10
申请人： The Regents of the University of California
发明人： William F. DeGrado , Dean Sheppard , Hyunil Jo , Nilgun Isik Reed , Youzhi Tang , Joel McIntosh
IPC分类号： C07D417/12 , C07D249/06 , C07C279/14 , C07D471/04 , C07D233/50 , C07D217/24 , C07D263/32 , C07D277/30 , C07D401/12 , C07D239/14 , C07D413/12 , C07D403/12 , C07D271/02 , C07D285/04 , G01N33/68 , C07D213/74
CPC分类号： C07D417/12 , C07C279/14 , C07D213/74 , C07D217/24 , C07D233/50 , C07D239/14 , C07D249/06 , C07D263/32 , C07D271/02 , C07D277/30 , C07D285/04 , C07D401/12 , C07D403/12 , C07D413/12 , C07D471/04 , G01N33/573 , G01N33/6863 , G01N2333/7055
摘要： Provided herein, inter alia, are methods and compositions for inhibiting αvβ1 integrin and for treating fibrosis.
摘要翻译：本文提供了用于抑制αvβ1整联蛋白和治疗纤维化的方法和组合物。

6. 发明申请

US20150038523A1 INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING ALPHA-V-BETA-3 有权
标题翻译：用于指定递送至表达ALPHA-V-BETA-3的细胞的整合拮抗剂
公开(公告)号：US20150038523A1
公开(公告)日：2015-02-05
申请号：US14374680
申请日：2013-01-22
申请人： Hoffmann-La Roche Inc.
发明人： Robert Alan Goodnow, Jr. , Matthew Michael Hamilton , Agnieszka Kowalczyk , Achyutharao Sidduri
IPC分类号： C07D277/593 , C07D417/12 , C07C237/52 , C07D239/14 , C07D207/452
CPC分类号： C07D277/593 , A61K47/545 , A61K47/549 , A61K47/60 , C07C237/52 , C07C327/32 , C07D207/452 , C07D239/14 , C07D417/12
摘要： The invention relates to compounds of formula (I): wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-integrin antagonists to target cells expressing alpha-V-beta-3.
摘要翻译：本发明涉及式（I）的化合物：其中R 1，R 2和n在详细描述和权利要求书中定义。特别地，本发明涉及用于制备和递送缀合部分的式（I）化合物，所述共轭部分例如小分子，肽，核酸，荧光部分和与α-V-β- 整合素拮抗剂靶向表达α-V-β-3的细胞。

7. 发明授权

US08716226B2 3,5 phenyl-substituted beta amino acid derivatives as integrin antagonists 有权
标题翻译： 3,5-苯基取代的β氨基酸衍生物作为整联蛋白拮抗剂
公开(公告)号：US08716226B2
公开(公告)日：2014-05-06
申请号：US13944319
申请日：2013-07-17
申请人： Saint Louis University
发明人： Peter Ruminski , David Griggs
IPC分类号： A61K38/36
CPC分类号： C07D239/14
摘要： Disclosed herein are novel pharmaceutical agents which are useful as integrin receptor antagonists that mediate the pathologic processes of angiogenesis and fibrosis and as such are useful in pharmaceutical compositions and in methods for treating conditions mediated by these integrins by inhibiting or antagonizing these integrins. The novel pharmaceutical agents include those of the formula: wherein X is bromo or iodo, or pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods and intermediates useful for making the pharmaceutical agents and methods of using the pharmaceutical agents are also provided.
摘要翻译：本文公开了可用作介导血管生成和纤维化的病理过程的整联蛋白受体拮抗剂的新型药剂，因此可用于药物组合物和通过抑制或拮抗这些整联蛋白来治疗由这些整联蛋白介导的病症的方法。新型药剂包括下式的那些：其中X是溴或碘，或其药学上可接受的盐。还提供了包含这种药剂的药物组合物，试剂盒和制品。还提供了可用于制备药剂的方法和中间体以及使用药剂的方法。

8. 发明授权

US08129543B2 Cyclic guanidine ionic liquid 有权
标题翻译：环状胍离子液体
公开(公告)号：US08129543B2
公开(公告)日：2012-03-06
申请号：US12529590
申请日：2008-02-26
申请人： Atsushi Kawada , Aya Tashiro , Toshihiro Kumagai
发明人： Atsushi Kawada , Aya Tashiro , Toshihiro Kumagai
IPC分类号： C07D403/02
CPC分类号： H01M10/0568 , C07D233/44 , C07D233/48 , C07D239/12 , C07D239/14 , C07D401/04 , C07D403/04 , C07D417/04 , H01G9/038 , H01G9/2013 , H01G9/2031 , H01G9/2059 , H01G11/58 , H01G11/62 , H01M14/005 , Y02E10/542 , Y02E60/13 , Y02P70/521
摘要： Disclosed is an ionic liquid which is stable over a wide potential range and exhibits a high ionic conductivity. The ionic liquid comprises a cyclic guanidine salt represented by the following formula (1): wherein R1 and R2 each is independently an alkyl group or an alkoxyalkyl group, X is a methylene group, an oxygen atom, a sulfur atom, or R3N; R3 is an alkyl group, an alkoxyalkyl group, or an acyl group; l, m, and n each is an integer in the range of 1-6; Y− is a monovalent anion such as (R4SO2)2N−, R4SO3−, R4COO−, BF4−, PF6−, NO3−, (CN)2N−, (CHO)2N−, NCS−, R4OSO3−, R4SO2S−, and a halogen ion. The ionic liquid is useful for a variety of electrolytes, particularly for electrolytes of electrochemical cells.
摘要翻译：公开了一种离子液体，其在宽电势范围内是稳定的并且表现出高离子导电性。离子液体包含由下式（1）表示的环状胍盐：其中R1和R2各自独立地为烷基或烷氧基烷基，X为亚甲基，氧原子，硫原子或R3N; R3是烷基，烷氧基烷基或酰基; l，m和n分别为1-6的整数; Y-是一价阴离子如（R4SO2）2N-，R4SO3-，R4COO-，BF4-，PF6-，NO3-，（CN）2N-，（CHO）2N-，NCS-，R4OSO3-，R4SO2S-，和卤素离子。离子液体可用于各种电解质，特别是用于电化学电池的电解质。

9. 发明授权

US07759339B2 Hydroxysteroid dehydrogenase inhibitors 失效
标题翻译：羟基类固醇脱氢酶抑制剂
公开(公告)号：US07759339B2
公开(公告)日：2010-07-20
申请号：US11392297
申请日：2006-03-28
申请人： Kathleen Aertgeerts , Nancy K. Brennan , Sheldon X. Cao , Edcon Chang , Andre A. Kiryanov , Yan Liu
发明人： Kathleen Aertgeerts , Nancy K. Brennan , Sheldon X. Cao , Edcon Chang , Andre A. Kiryanov , Yan Liu
IPC分类号： C07D241/04 , C07D295/00 , C07D413/12 , A61K31/496 , A61K31/445
CPC分类号： C07D241/38 , C07D207/48 , C07D209/08 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/38 , C07D211/54 , C07D211/58 , C07D211/62 , C07D211/76 , C07D211/96 , C07D213/70 , C07D213/74 , C07D215/04 , C07D215/42 , C07D215/58 , C07D217/02 , C07D217/06 , C07D217/08 , C07D217/22 , C07D217/24 , C07D231/18 , C07D231/56 , C07D233/42 , C07D235/26 , C07D239/14 , C07D241/08 , C07D241/50 , C07D261/10 , C07D265/36 , C07D271/12 , C07D277/56 , C07D277/58 , C07D277/62 , C07D279/16 , C07D285/14 , C07D285/16 , C07D295/26 , C07D307/68 , C07D307/79 , C07D333/62 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D413/04 , C07D471/08 , C07D487/04 , C07D487/08 , C07D491/10 , C07D513/04
摘要： Compounds, pharmaceutical compositions, kits and methods are provided for use with hydroxysteroid dehydrogenases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.
摘要翻译：提供化合物，药物组合物，试剂盒和方法用于含有选自以下的化合物的羟基类固醇脱氢酶：其中变量如本文所定义。

10. 发明申请

US20100160290A1 PHARMACEUTICAL COMPOSITION FOR TREATING ALZHEIMER'S DISEASE 有权
标题翻译：用于治疗阿尔茨海默病的药物组合物
公开(公告)号：US20100160290A1
公开(公告)日：2010-06-24
申请号：US12597470
申请日：2008-04-23
申请人： Naotake Kobayashi , Kazuo Ueda , Naohiro Itoh , Shinji Suzuki , Gaku Sakaguchi , Akira Kato , Akira Yukimasa , Akihiro Hori , Yuuji Kooriyama , Hidekazu Haraguchi , Ken Yasui , Yasuhiko Kanda
发明人： Naotake Kobayashi , Kazuo Ueda , Naohiro Itoh , Shinji Suzuki , Gaku Sakaguchi , Akira Kato , Akira Yukimasa , Akihiro Hori , Yuuji Kooriyama , Hidekazu Haraguchi , Ken Yasui , Yasuhiko Kanda
IPC分类号： A61K31/554 , C07D417/02 , A61K31/541 , C07D279/06 , C07D277/18 , A61K31/426 , C07D239/02 , A61K31/506 , C07D281/02 , A61P25/28
CPC分类号： C07D471/04 , A61K9/0019 , A61K9/1623 , A61K9/2018 , A61K31/426 , A61K31/506 , A61K31/535 , A61K31/54 , A61K31/541 , A61K31/554 , C07D239/14 , C07D265/08 , C07D277/18 , C07D279/06 , C07D281/02 , C07D285/36 , C07D295/155 , C07D295/192 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , A61K2300/00
摘要： A pharmaceutical composition for treating Alzheimer's disease containing a compound represented by the general formula (I); wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene, etc.; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b are each independently a hydrogen atom, halogen, hydroxy, etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 1 to 3; and R5 is a hydrogen atom, optionally substituted lower alkyl, etc.; its pharmaceutically acceptable salt, or a solvate thereof as an active ingredient.
摘要翻译：一种用于治疗含有由通式（I）表示的化合物的阿尔茨海默病的药物组合物; 其中环A是任选取代的碳环基团或任选取代的杂环基团; E为低级亚烷基等; X是S，O或NR1; R1是氢原子或低级烷基; R2a，R2b，R3a，R3b，R4a和R4b各自独立地为氢原子，卤素，羟基等; n和m各自独立地为0〜3的整数， n + m为1〜3的整数， R5为氢原子，任意取代的低级烷基等; 其药学上可接受的盐或其溶剂合物作为活性成分。

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