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1. 发明申请

US20180072746A1 DE NOVO SYNTHESIS OF BACTERIOCHLORINS 审中-公开
公开(公告)号：US20180072746A1
公开(公告)日：2018-03-15
申请号：US15817973
申请日：2017-11-20
申请人： North Carolina State University
发明人： Han-Je Kim , Jonathan S. Lindsey
IPC分类号： C07D487/22 , C09B47/00 , G01N21/64 , C07D207/335
CPC分类号： C07D487/22 , A61K31/555 , C07D207/335 , C09B47/00 , G01N21/6486
摘要： A method of making a bacteriochlorin is carried out by condensing a pair of compounds of Formula II to produce the bacteriochlorin, wherein R is an acetal or aldehyde group. The condensing may be carried out in an organic solvent, preferably in the presence of an acid. The bacteriochlorins are useful for a variety of purposes such as active agents in photodynamic therapy, luminescent compounds in flow cytometry, solar cells, light harvesting arrays, and molecular memory devices.

2. 发明授权

US09884832B2 Inhibitors targeting drug-resistant influenza A 有权
公开(公告)号：US09884832B2
公开(公告)日：2018-02-06
申请号：US14363116
申请日：2012-12-06
申请人： The Trustees of The University of Pennsylvania
发明人： William F. DeGrado , Jizhou Wang , Jun Wang , Hyunil Jo , Belgin Canturk
IPC分类号： C07D413/04 , A61K31/422 , C07D271/06 , C07D207/335 , A61K31/417 , A61K45/06 , C07C215/50 , A61K31/137 , A61K31/155 , A61K31/15 , C07C211/38 , C07C271/28 , A61K31/27 , C07C255/58 , A61K31/26 , C07D257/04 , A61K31/41 , A61K31/4245 , C07D213/38 , A61K31/4402 , C07D233/88 , A61K31/505 , C07D261/08 , A61K31/5377 , C07C211/27 , C07C211/49 , C07C217/58 , C07C219/28 , C07C233/43 , C07C235/20 , C07C237/30 , C07C255/24 , C07C317/32 , C07C323/32
CPC分类号： C07D271/06 , A61K31/137 , A61K31/15 , A61K31/155 , A61K31/26 , A61K31/27 , A61K31/41 , A61K31/417 , A61K31/422 , A61K31/4245 , A61K31/4402 , A61K31/505 , A61K31/5377 , A61K45/06 , C07C211/27 , C07C211/38 , C07C211/49 , C07C215/50 , C07C217/58 , C07C219/28 , C07C233/43 , C07C235/20 , C07C237/30 , C07C255/24 , C07C255/58 , C07C271/28 , C07C317/32 , C07C323/32 , C07C2601/02 , C07C2603/74 , C07D207/335 , C07D213/38 , C07D233/88 , C07D257/04 , C07D261/08 , C07D413/04
摘要： Provided are compounds according to formula (Ia) or (Ib) as described herein, that are capable of modulating the activity of influenza viruses (e.g., influenza A virus), for example, via interaction with the M2 transmembrane protein, and other similar viroporins. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds according to according to formulas (Ia′) or (Ib), as described herein.

3. 发明授权

US09850225B2 Compounds useful as immunomodulators 有权
公开(公告)号：US09850225B2
公开(公告)日：2017-12-26
申请号：US14681772
申请日：2015-04-08
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： Louis S. Chupak , Min Ding , Scott W. Martin , Xiaofan Zheng , Piyasena Hewawasam , Timothy P. Connolly , Ningning Xu , Kap-Sun Yeung , Juliang Zhu , David R. Langley , Paul Michael Scola
IPC分类号： C07D319/18 , A61K31/357 , C07D405/12 , A61K31/453 , C07D405/14 , A61K31/4545 , C07D217/16 , A61K31/472 , C07D413/12 , A61K31/5377 , C07D417/12 , A61K31/541 , A61K31/496 , A61K45/06 , C07C255/54 , C07D215/14 , C07D215/18 , C07D231/56 , C07D405/04 , C07D239/26 , C07D261/08 , C07D271/06 , C07D207/26 , C07D207/335 , C07D213/30 , C07C271/28 , C07C317/22 , C07C233/36 , C07C235/42 , C07C255/13 , A61K31/165 , A61K31/277 , A61K31/40 , A61K31/4015 , A61K31/416 , A61K31/4178 , A61K31/4245 , A61K31/427 , A61K31/4433 , A61K31/47 , A61K31/505
CPC分类号： C07D319/18 , A61K31/165 , A61K31/277 , A61K31/357 , A61K31/40 , A61K31/4015 , A61K31/416 , A61K31/4178 , A61K31/4245 , A61K31/427 , A61K31/4433 , A61K31/453 , A61K31/4545 , A61K31/47 , A61K31/472 , A61K31/496 , A61K31/505 , A61K31/5377 , A61K31/541 , A61K45/06 , C07C233/36 , C07C235/42 , C07C255/13 , C07C255/54 , C07C271/28 , C07C317/22 , C07D207/26 , C07D207/335 , C07D213/30 , C07D215/14 , C07D215/18 , C07D217/16 , C07D231/56 , C07D239/26 , C07D261/08 , C07D271/06 , C07D405/04 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , Y02A50/463 , A61K2300/00
摘要： The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.

4. 发明申请

US20170253596A2 SHIP1 MODULATORS AND METHODS RELATED THERETO 审中-公开
公开(公告)号：US20170253596A2
公开(公告)日：2017-09-07
申请号：US14772737
申请日：2014-02-27
申请人： Aquinox Pharmaceuticals (Canada) Inc.
发明人： Lloyd F. Mackenzie , Curtis Harwig , David Bogucki , Jeffery R. Raymond , Jeremy D. Pettigrew
IPC分类号： C07D473/34 , C07C215/42 , C07C233/23 , C07D207/335 , C07C311/04 , C07C225/10 , C07D207/06 , C07D213/38 , C07C233/74 , C07D231/12 , C07D249/08 , C07D233/60 , C07D209/08 , C07D317/46 , C07D295/096 , C07D213/64 , C07D239/34 , C07D241/18 , C07C255/31 , C07C275/24 , C07C279/08
CPC分类号： C07D473/34 , C07C35/21 , C07C35/32 , C07C59/46 , C07C62/32 , C07C215/42 , C07C215/50 , C07C215/52 , C07C225/10 , C07C233/18 , C07C233/23 , C07C233/60 , C07C233/74 , C07C235/30 , C07C235/44 , C07C235/46 , C07C235/48 , C07C255/31 , C07C261/04 , C07C275/10 , C07C275/24 , C07C275/34 , C07C279/08 , C07C291/04 , C07C311/04 , C07C335/10 , C07C2602/24 , C07C2603/14 , C07D207/06 , C07D207/08 , C07D207/335 , C07D207/416 , C07D209/08 , C07D213/04 , C07D213/30 , C07D213/36 , C07D213/38 , C07D213/64 , C07D213/81 , C07D213/82 , C07D231/12 , C07D233/60 , C07D233/72 , C07D235/06 , C07D235/14 , C07D239/34 , C07D241/18 , C07D241/28 , C07D249/08 , C07D295/096 , C07D307/68 , C07D317/46 , C07D317/58
摘要： Compounds of formula (I): where R1, R2, R3, R4a, R4b, R5, R6 and R7 are defined herein, or stereoisomers or pharmaceutically acceptable salts thereof, are described herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

6. 发明授权

US09549915B2 Urea compounds and their use as enzyme inhibitors 有权
标题翻译：尿素化合物及其作为酶抑制剂的用途
公开(公告)号：US09549915B2
公开(公告)日：2017-01-24
申请号：US14416675
申请日：2013-07-24
申请人： BIAL-PORTELA & CA, S.A.
发明人： Carla Patricia da Costa Pereira Rosa , Rita Gusmao De Noronha , Laszlo Erno Kiss , Patricio Manuel Vieira Araujo Soares Da Silva , Domenico Russo , Jorge Bruno Reis Wahnon , William Maton
IPC分类号： C07D233/61 , C07D233/88 , A61K31/4178 , A61P31/00 , A61K31/4164 , C07C209/00 , C07C209/26 , A61K45/06 , C07D207/335 , C07C209/48
CPC分类号： C07D233/64 , A61K31/4164 , A61K45/06 , C07C209/00 , C07C209/26 , C07D207/335 , C07D233/61 , C07D233/88 , C07C211/35
摘要： A compound having the following structure: or a pharmaceutically acceptable salt or derivative thereof. The compound may be used in the treatment or prevention of a disorder selected from appetite regulation, obesity, metabolic disorders, cachexia, anorexia, pain, inflammation, neurotoxicity, neurotrauma, stroke, multiple sclerosis, spinal cord injury, Parkinson's disease, levodopa-induced dyskinesia, Huntington's disease, Gilles de la Tourette's syndrome, tardive dyskinesia, dystonia, amyotrophic lateral sclerosis, Alzheimer's disease, epilepsy, schizophrenia, anxiety, depression, insomnia, nausea, emesis, alcohol disorders, drug addictions such as opiates, nicotine, cocaine, alcohol and psychostimulants, hypertension, circulatory shock, myocardial reperfusion injury, atherosclerosis, asthma, glaucoma, retinopathy, cancer, inflammatory bowel disease, acute and chronic liver disease such as hepatitis and liver cirrhosis, arthritis and osteoporosis.
摘要翻译：具有以下结构的化合物或其药学上可接受的盐或衍生物。该化合物可用于治疗或预防选自食欲调节，肥胖症，代谢紊乱，恶病质，厌食，疼痛，炎症，神经毒性，神经损伤，中风，多发性硬化，脊髓损伤，帕金森病，左旋多巴诱导运动障碍，亨廷顿疾病，吉列斯·杜勒特综合征，迟发性运动障碍，肌张力障碍，肌萎缩性侧索硬化，阿尔茨海默病，癫痫，精神分裂症，焦虑，抑郁，失眠，恶心，呕吐，酒精失调，药物成瘾如阿片剂，尼古丁，可卡因，酒精和精神兴奋剂，高血压，循环休克，心肌再灌注损伤，动脉粥样硬化，哮喘，青光眼，视网膜病变，癌症，炎症性肠病，急性和慢性肝病如肝炎和肝硬化，关节炎和骨质疏松症。

7. 发明授权

US09346832B2 Gold complexes for use in the treatment of cancer 有权
标题翻译：用于治疗癌症的金配合物
公开(公告)号：US09346832B2
公开(公告)日：2016-05-24
申请号：US13704894
申请日：2011-06-14
申请人： Orde Quentin Munro , Kate Julie Akerman , Piers Akerman
发明人： Orde Quentin Munro , Kate Julie Akerman , Piers Akerman
IPC分类号： C07F1/12 , A61K31/28 , C01G7/00 , C07C209/16 , C07C213/02 , C07D401/12 , C07D487/22 , C07C209/68 , C07C209/86 , C07C213/06 , C07D207/335
CPC分类号： C07F1/12 , C01G7/00 , C07C209/16 , C07C209/68 , C07C209/86 , C07C213/02 , C07C213/06 , C07D207/335 , C07D401/12 , C07D487/22 , C07C211/15 , C07C217/42
摘要： The invention provides compounds of the Formula (I), in which W is independently selected from W1, W2, W3, W4, W5, or W represents a pair of substituents independently selected from H, alkyl, aryl or amide in which the amide is optionally part of a linking chain, and the Zn—Zn′ bonds (n=4-17; n′=n+1) are optionally of any whole or partial bond order, Y is Y1 or Y represents a pair of substituents independently selected from H, C1-C6 alkyl, Z5 or Z6 aryl, or Y is optionally a bridging structure that may comprise one or more C1-C6 amide, C1-C6 ether, or C1-C6 ester groups, R—R39 are independently selected from no substituent, a lone pair of electrons, H, halogen, C5-C6 aryl, C1-C12 alkyl, amine, C1-C6 alkylamine, C1-C6 amide, nitro, cyano, carboxyl, C1-C6 ester, phosphane, thiol, C1-C6 thioether, OR40, and suitable pairs of adjacent R groups (R—R39) may optionally together form part of a C5 or C6 aryl ring, a Z5 or Z6 ring, R40 is independently selected from H, C1-C6 alkyl, Z5 or Z6 aryl, C1-C6 ester, poly(—C2O—), amine, and C1-C6 alkylamine, Z—Z24 are independently selected from C, N, P, O, and S, and X− is a pharmaceutically acceptable anion, for the treatment of cancer.
摘要翻译：本发明提供式（I）化合物，其中W独立地选自W 1，W 2，W 3，W 4，W 5或W表示独立地选自H，烷基，芳基或酰胺的一对取代基，其中酰胺是任选地部分连接链，Zn-Zn'键（n = 4-17; n'= n + 1）任选地具有任何全部或部分键合顺序，Y是Y1或Y表示独立选择的一对取代基由H，C 1 -C 6烷基，Z 5或Z 6芳基，或Y任选是可以包含一个或多个C 1 -C 6酰胺，C 1 -C 6醚或C 1 -C 6酯基团的桥连结构，R-R 39独立地选自无取代基，孤对电子，H，卤素，C5-C6芳基，C1-C12烷基，胺，C1-C6烷基胺，C1-C6酰胺，硝基，氰基，羧基，C1-C6酯， C1-C6硫醚，OR40和适当的相邻R基团（R-R39）可以任选地一起形成C5或C6芳基环，Z5或Z6环的一部分，R40独立地选自H，C1-C6烷基， Z5 或Z6芳基，C1-C6酯，聚（-C2O-），胺和C1-C6烷基胺，Z-Z24独立地选自C，N，P，O和S，X-是药学上可接受的阴离子，用于治疗癌症。

8. 发明授权

US09221755B2 Ethers, secondary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto 有权
标题翻译：醚，仲胺及其衍生物作为可用于治疗与其有关的疾病的5-HT2A 5-羟色胺受体的调节剂
公开(公告)号：US09221755B2
公开(公告)日：2015-12-29
申请号：US14182994
申请日：2014-02-18
申请人： Arena Pharmaceuticals, Inc.
发明人： Bradley Teegarden , Dennis Chapman , Marc Decaire , Peter I. Dosa , Konrad Feichtinger , Honnappa Jayakumar , Thuy-Anh Tran , Sonja Strah-Pleynet , Jay Xu
IPC分类号： C07D231/12 , C07D401/12 , C07D403/12 , C07D207/34 , C07D413/12 , C07D405/12 , C07D207/335 , C07D417/12
CPC分类号： C07D231/12 , A61K31/415 , C07D207/335 , C07D207/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：本发明涉及某些调节5-HT2A 5-羟色胺受体活性的式（Ia）化合物及其药物组合物。化合物及其药物组合物涉及可用于治疗血小板聚集，冠状动脉疾病，心肌梗死，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法，精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症精神分裂症和相关疾病，睡眠障碍，睡眠障碍，糖尿病性精神病，精神病，精神病，相关疾病，进行性多灶性脑白质病等。本发明还涉及与单独或一起施用的其它药剂组合治疗5-HT2A 5-羟色胺受体相关疾病的方法。

9. 发明申请

US20150307426A9 INDENE DERIVATIVES AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译：作为药剂的INDENE衍生物
公开(公告)号：US20150307426A9
公开(公告)日：2015-10-29
申请号：US14162136
申请日：2014-01-23
申请人： Aquinox Pharmaceuticals Inc.
发明人： Jeffery R. Raymond , Kang Han , Yuanlin Zhou , Yuehua He , Bradley Noren , James Gee Ken Yee
IPC分类号： C07C35/32 , C07C213/00 , C07C247/14 , C07C315/00 , C07C51/083 , C07C51/347 , C07D317/70 , C07C35/14 , C07C215/42 , C07C62/34 , C07D213/30 , C07C233/21 , C07C279/08 , C07D295/096 , C07D233/64 , C07C213/08
CPC分类号： C07C35/32 , C07C35/14 , C07C35/21 , C07C51/083 , C07C51/347 , C07C62/34 , C07C69/013 , C07C213/00 , C07C213/08 , C07C215/42 , C07C233/18 , C07C233/21 , C07C233/72 , C07C247/14 , C07C279/08 , C07C311/04 , C07C315/00 , C07C2601/14 , C07C2602/08 , C07C2602/24 , C07D207/335 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/74 , C07D233/54 , C07D233/64 , C07D295/096 , C07D307/66 , C07D317/66 , C07D317/70 , Y10S514/825 , Y10S514/826 , Y10S514/863
摘要： Processes for making and using compounds of formula (I): wherein R1, R2, R3, R4a, R4b, R5 and R6 are defined herein, as well as other indene derivatives are disclosed herein. These compounds are disclosed as being useful in treating inflammatory conditions or diseases.
摘要翻译：制备和使用式（I）化合物的方法：其中R1，R2，R3，R4a，R4b，R5和R6如本文所定义，以及其它茚衍生物在本文中公开。这些化合物被公开用于治疗炎性疾病或疾病。

10. 发明申请

US20150291549A1 Compounds Useful as Immunomodulators 有权
标题翻译：可用作免疫调节剂的化合物
公开(公告)号：US20150291549A1
公开(公告)日：2015-10-15
申请号：US14681772
申请日：2015-04-08
申请人： Bristol-Myers Squibb Company
发明人： Louis S. Chupak , Min Ding , Scott W. Martin , Xiaofan Zheng , Piyasena Hewawasam , Timothy P. Connolly , Ningning Xu , Kap-Sun Yeung , Juliang Zhu , David R. Langley , Daniel J. Tenney , Paul Michael Scola
IPC分类号： C07D319/18 , C07D405/12 , A61K31/453 , C07D405/14 , A61K31/4545 , A61K45/06 , A61K31/472 , C07D413/12 , A61K31/5377 , C07D417/12 , A61K31/541 , A61K31/496 , A61K31/357 , C07D217/16
CPC分类号： C07D319/18 , A61K31/165 , A61K31/277 , A61K31/357 , A61K31/40 , A61K31/4015 , A61K31/416 , A61K31/4178 , A61K31/4245 , A61K31/427 , A61K31/4433 , A61K31/453 , A61K31/4545 , A61K31/47 , A61K31/472 , A61K31/496 , A61K31/505 , A61K31/5377 , A61K31/541 , A61K45/06 , C07C233/36 , C07C235/42 , C07C255/13 , C07C255/54 , C07C271/28 , C07C317/22 , C07D207/26 , C07D207/335 , C07D213/30 , C07D215/14 , C07D215/18 , C07D217/16 , C07D231/56 , C07D239/26 , C07D261/08 , C07D271/06 , C07D405/04 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , Y02A50/463 , A61K2300/00
摘要： The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.
摘要翻译：本公开一般涉及可用作免疫调节剂的化合物。本文提供的化合物，包含这些化合物的组合物及其使用方法。本公开还涉及包含至少一种根据本公开的化合物的药物组合物，其可用于治疗各种疾病，包括癌症和感染性疾病。

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