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1. 发明公开

EP2340242A4 COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS 审中-公开
标题翻译：化合物眼睛的疾病和病症的治疗
公开(公告)号：EP2340242A4
公开(公告)日：2012-04-04
申请号：EP09822658
申请日：2009-10-21
申请人： ACUCELA INC
发明人： SCOTT IAN L , KUKSA VLADIMIR A , HONG FENG , KUBOTA RYO , GAGE JENNIFER
IPC分类号： C07C311/33 , A61K31/167 , A61K31/18 , A61P27/02 , C07C237/20 , C07C311/08 , C07C311/36
CPC分类号： C07C233/25 , A61K31/167 , A61K31/18 , C07B59/001 , C07B2200/05 , C07C211/49 , C07C211/52 , C07C215/08 , C07C215/14 , C07C215/42 , C07C215/68 , C07C217/08 , C07C217/10 , C07C217/58 , C07C225/06 , C07C225/22 , C07C233/36 , C07C233/43 , C07C233/62 , C07C275/40 , C07C311/08 , C07C311/10 , C07C311/14 , C07C311/21 , C07C311/24 , C07C335/18 , C07C2601/08 , C07C2601/14 , C07D277/28

2. 发明公开

EP2385944A2 FLUORINE CONTAINING COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译： FLUOR含氮化合物及其使用方法
公开(公告)号：EP2385944A2
公开(公告)日：2011-11-16
申请号：EP10729595.8
申请日：2010-01-08
申请人： President and Fellows of Harvard College
发明人： RITTER, Tobias , BRASS, Laura , KEITH, Curtis , WATSON, Alan , GREENBLATT, David, J.
IPC分类号： C07D405/06 , C07D405/14 , C07D417/12 , C07D403/14
CPC分类号： C07D471/04 , C07B59/00 , C07B2200/05 , C07C59/72 , C07C63/72 , C07C69/63 , C07C69/736 , C07C69/76 , C07C211/27 , C07C211/29 , C07C211/31 , C07C211/32 , C07C211/40 , C07C211/42 , C07C215/42 , C07C217/10 , C07C217/18 , C07C217/20 , C07C217/48 , C07C217/74 , C07C225/16 , C07C225/20 , C07C229/34 , C07C229/36 , C07C233/15 , C07C237/04 , C07C237/10 , C07C243/18 , C07C243/34 , C07C255/41 , C07C271/44 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/10 , C07C2603/32 , C07C2603/88 , C07D223/28 , C07D249/12 , C07D267/20 , C07D313/12 , C07D333/20 , C07D471/08 , C07D471/14 , C07F9/65061
摘要： Fluorinated compounds and methods of making fluorinated compounds are described herein.
摘要翻译：氟化化合物及其制备氟化的化合物的方法描述英寸

3. 发明公开

EP1513825A4 ANTI TUBERCULAR DRUG: COMPOSITIONS AND METHODS 有权
标题翻译：抗菌素ARZNEIMITTEL：ZUSAMMENSETZUNGEN UND VERFAHREN
公开(公告)号：EP1513825A4
公开(公告)日：2011-01-05
申请号：EP03729047
申请日：2003-05-19
申请人： DEPT OF HEALTH AND HUMAN SERVICES , SEQUELLA INC
发明人： PROTOPOPOVA MARINA NIKOLAEVNA , LEE RICHARD EDWARD , SLAYDEN RICHARD ALLAN , BARRY III CLIFTON E , EINCK LEO
IPC分类号： C07D243/08 , A61K31/132 , A61K31/133 , A61K31/137 , A61K31/381 , A61K31/40 , A61K31/445 , A61K31/47 , A61K31/5375 , A61K31/55 , A61K31/551 , A61P1/04 , A61P31/00 , A61P31/04 , A61P31/06 , A61P31/10 , A61P31/12 , A61P33/00 , C07C209/50 , C07C211/09 , C07C211/27 , C07C211/29 , C07C211/34 , C07C211/35 , C07C211/42 , C07C213/08 , C07C215/14 , C07C215/30 , C07C215/60 , C07C217/08 , C07C217/10 , C07C217/58 , C07C217/60 , C07C217/62 , C07C217/84 , C07C319/20 , C07C323/25 , C07C323/47 , C07D211/46 , C07D223/14 , C07D295/12 , C07D333/20
CPC分类号： C07C323/25 , A61K31/132 , A61K31/133 , A61K31/137 , A61K31/40 , A61K31/445 , C07C211/27 , C07C211/29 , C07C211/34 , C07C211/35 , C07C211/42 , C07C215/14 , C07C215/30 , C07C215/60 , C07C217/08 , C07C217/10 , C07C217/58 , C07C217/60 , C07C217/62 , C07C323/47 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D211/46
摘要： Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.
摘要翻译：用于治疗感染因子，特别是结核病引起的疾病的方法和组合物。特别地，提供了包含用于治疗感染性疾病的取代的乙二胺的方法和组合物。在一个实施方案中，这些方法和组合物用于治疗分枝杆菌感染，包括但不限于结核病。

4. 发明公开

EP2076124A2 STYRENYL DERIVATIVE COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS 审中-公开
标题翻译： STYRENYLDERIVATVERBINDUNGEN疾病和痛苦眼科的治疗
公开(公告)号：EP2076124A2
公开(公告)日：2009-07-08
申请号：EP08746483.0
申请日：2008-04-21
申请人： Acucela, Inc.
发明人： SCOTT, Ian, Leslie , KUKSA, Vladimir, Aleksandrovich , GALL, Anna , ORME, Mark, W. , GAGE, Jennifer , LITTLE, Thomas, L., Jr. , JIANG, Qin , ROSSITER, Lana, Michele , MCGEE, Kevin, F., Jr. , KUBOTA, Ryo
IPC分类号： A01N33/02 , A61K31/135
CPC分类号： A61K31/5375 , A61K31/137 , A61K31/145 , A61K31/167 , A61K31/40 , A61K31/4453 , A61K31/495 , C07C211/27 , C07C211/28 , C07C211/29 , C07C215/08 , C07C215/30 , C07C215/42 , C07C215/46 , C07C217/10 , C07C217/16 , C07C217/18 , C07C217/48 , C07C217/54 , C07C217/62 , C07C217/72 , C07C225/06 , C07C225/18 , C07C233/05 , C07C237/04 , C07C317/28 , C07C323/25 , C07C323/32 , C07C323/33 , C07C2602/14 , C07C2602/16 , C07D207/06 , C07D211/14 , C07D295/03
摘要： The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

5. 发明公开

EP1930308A1 Pharmaceutical agents for the treatment of cerebral amyloidosis 失效
标题翻译： Pharmazutische Wirkstoffe zur Behandlung von Hirnamyloidose
公开(公告)号：EP1930308A1
公开(公告)日：2008-06-11
申请号：EP07021294.9
申请日：1998-05-19
申请人： NYMOX CORPORATION
发明人： Averback, Paul , Ghanbari, Hossein , Beheshti, Iraj , Morse, David
IPC分类号： C07C43/164 , A61K31/08 , C07C43/174 , C07C217/10 , C07D211/90 , C07D295/02 , C07D295/08 , C07D473/04 , A61K31/495 , A61K31/44 , A61K31/52
CPC分类号： C07D295/03 , C07C43/164 , C07C43/1745 , C07C211/28 , C07C217/10 , C07D211/90 , C07D295/088 , C07D473/04
摘要： The invention relates to a compound of the following general formula (III):

wherein:
R 1 and R 2 each are one or more independent substituents selected from the group consisting of hydrogen, C1-C5 alkyl, C2-C5 alkenyl, C3-C5 cycloalkyl, C1-C5 alkoxy, C2-C5 alkynyl, halogen, C1-C5 haloalkyl, alkylamino, phenyl, nitro and carboxyl;
R 3 is selected from the group consisting of amino, C1-C5 substituted amino and CH 2 ;
n and m are independently an integer of from 0-5;

or a pharmaceutically acceptable salt of such compound;
a compound of the following general formula (IV):

wherein:
R 1 and R 2 each are one or more independent substituents selected from the group consisting of hydrogen, C1-C5 alkyl, C2-C5 alkenyl, C3-C5 cycloalkyl, C1-C5 alkoxy, C2-C5 alkynyl, halogen, C1-C5 haloalkyl, alkylamino, phenyl, nitro and ca rboxyl;
R 3 and R 4 each are independent and selected from the group consisting of hydrogen and C1-C5 alkyl;
n is an integer of from 1 to 5;

or a pharmaceutically acceptable salt of such compound;
a compound of the following general formula (V):

wherein:
R 1 and R 2 each are one or more independent substituents selected from the group consisting of hydrogen, C1-C5 alkyl, C2-C5 alkenyl, C3-C5 cycloalkyl, C1-C5 alkoxy, C2-C5 alkynyl, halogen, C1-C5 haloalkyl, alkylamino, phenyl, nitro and carboxyl;
R 3 is selected from hydrogen and C1-C5 alkyl;
R 4 is selected from hydrogen and C1-C5 alkyl;
n is an integer of from 1 to 5 inclusive;
or a pharmaceutically acceptable salt of such compound; and
a compound of the following general formula (VI):

wherein:
R 1 and R 2 each are one or more independent substituents selected from the group consisting of hydrogen, C1-C5 alkyl, C2-C5 alkenyl, C3-C5 cycloalkyl, C1-C5 alkoxy, C2-C5 alkynyl, halogen, C1-C5 haloalkyl, alkylamino, phenyl, nitro and carboxyl;
R3 and R4 each are independent and selected from hydrogen and C1-C5 alkyl;
n is an integer of from 1 to 5 inclusive;
or a pharmaceutically acceptable salt of such compound.
Also compositions comprising the compounds III-VI as well as uses of said compounds.
摘要翻译：本发明涉及以下通式（III）的化合物：其中：R 1和R 2各自为选自氢，C 1 -C 5烷基，C 2 -C 5烯基，C 3 -C 5中的一个或多个独立取代基环烷基，C 1 -C 5烷氧基，C 2 -C 5炔基，卤素，C 1 -C 5卤代烷基，烷基氨基，苯基，硝基和羧基; R 3选自氨基，C 1 -C 5取代的氨基和CH 2; n和m独立地为0-5的整数; 或该化合物的药学上可接受的盐; 下列通式（IV）的化合物：其中：R 1和R 2各自为一个或多个选自氢，C 1 -C 5烷基，C 2 -C 5烯基，C 3 -C 5环烷基，C 1 -C 5环烷基， C5烷氧基，C2-C5炔基，卤素，C1-C5卤代烷基，烷基氨基，苯基，硝基和羧基; R 3和R 4各自独立地选自氢和C 1 -C 5烷基; n为1〜5的整数，或该化合物的药学上可接受的盐; 下列通式（V）的化合物：其中：R 1和R 2各自为一个或多个选自氢，C 1 -C 5烷基，C 2 -C 5烯基，C 3 -C 5环烷基，C 1 -C 5环烷基， C5烷氧基，C2-C5炔基，卤素，C1-C5卤代烷基，烷基氨基，苯基，硝基和羧基; R 3选自氢和C 1 -C 5烷基; R 4选自氢和C 1 -C 5烷基; n为1〜5的整数，或该化合物的药学上可接受的盐; 和下列通式（VI）的化合物：其中：R 1和R 2各自为一个或多个选自氢，C 1 -C 5烷基，C 2 -C 5烯基，C 3 -C 5环烷基，C 1 -C 5环烷基 C 5烷氧基，C 2 -C 5炔基，卤素，C 1 -C 5卤代烷基，烷基氨基，苯基，硝基和羧基; R 3和R 4各自独立地选自氢和C 1 -C 5烷基; n为1〜5的整数，或该化合物的药学上可接受的盐。还包含化合物III-VI的组合物以及所述化合物的用途。

6. 发明授权

EP1096926B1 METHODS AND COMPOUNDS FOR TREATING DEPRESSION 有权
标题翻译： VERFAHREN UND VERBINDUNGEN ZUR BEHANDLUNG DER DEPRESSION
公开(公告)号：EP1096926B1
公开(公告)日：2007-02-28
申请号：EP99933987.2
申请日：1999-07-12
申请人： NPS PHARMACEUTICALS, INC.
发明人： MUELLER, Alan , MOE, Scott , BALANDRIN, Manuel
IPC分类号： A61K31/137 , A61P25/24
CPC分类号： C07C217/62 , A61K31/135 , A61K31/137 , A61K31/138 , A61K31/335 , A61K31/341 , A61K31/352 , A61K31/381 , A61K31/382 , A61K31/4462 , C07B2200/07 , C07C217/10 , C07C217/18
摘要： The present invention features compounds active at both the serotonin euptake site and the N-methyl-D-aspartate (NMDA) receptor and the use of such compounds for treating different disorders. Compounds having activity at the serotonin reuptake site and the NMDA receptor ('multi-active compounds') can be used to treat different types of disorders such as depression, obsessive-compulsive disorders (OCD), sleep disorders, sexual dysfunction, and eating disorders. Preferably, the multi-active compounds are used to treat depression.
摘要翻译：本发明具有在5-羟色胺再摄取位点和N-甲基-D-天冬氨酸（NMDA）受体两者都具有活性的化合物，以及这些化合物用于治疗不同疾病的用途。可以使用在5-羟色胺再摄取位点和NMDA受体（“多活性化合物”）具有活性的化合物治疗不同类型的障碍，例如抑郁症，强迫症（OCD），睡眠障碍，性功能障碍和饮食障碍。优选地，多活性化合物用于治疗抑郁症。

7. 发明公开

EP1578353A2 METHODS OF USE AND COMPOSITIONS FOR THE DIAGNOSIS AND TREATMENT OF INFECTIOUS DISEASE 有权
标题翻译： 4-羟基哌啶衍生物维尔维隆
公开(公告)号：EP1578353A2
公开(公告)日：2005-09-28
申请号：EP03726938.8
申请日：2003-05-19
申请人： Sequella, Inc.
发明人： PROTOPOPOVA, Marina, Nikolaevna , BOGATCHEVA, Elena
IPC分类号： A61K6/00
CPC分类号： C07C323/25 , A61K31/132 , A61K31/133 , A61K31/40 , A61K31/445 , C07C211/29 , C07C211/34 , C07C211/35 , C07C211/42 , C07C215/14 , C07C215/30 , C07C215/60 , C07C217/08 , C07C217/10 , C07C217/58 , C07C217/60 , C07C217/62 , C07C323/47 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D211/46 , Y02A50/479
摘要： Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.
摘要翻译：用于治疗感染因子，特别是结核病引起的疾病的方法和组合物。特别地，提供了包含用于治疗感染性疾病的取代二胺的方法和组合物。在一个实施方案中，这些方法和组合物用于治疗分枝杆菌感染，包括但不限于结核病。

8. 发明授权

EP0831799B1 COMPOUNDS ACTIVE AT A NOVEL SITE ON RECEPTOR-OPERATED CALCIUM CHANNELS USEFUL FOR TREATMENT OF NEUROLOGICAL DISORDERS 失效
标题翻译：化合物中的新的专对受体刺激的钙通道有效适用于神经疾病的治疗
公开(公告)号：EP0831799B1
公开(公告)日：2003-05-02
申请号：EP96918477.9
申请日：1996-06-07
申请人： NPS PHARMACEUTICALS, INC.
发明人： MUELLER, Alan, L. , MOE, Scott, T. , BALANDRIN, Manuel, F. , DELMAR, Eric, G. , VANWAGENEN, Bradford, C. , ARTMAN, Linda, D. , BARMORE, Robert, M. , SMITH, Daryl, L.
IPC分类号： A61K31/135 , A61K31/155 , A61K31/165 , A61K31/40 , A61K31/38 , A61K31/44 , A61K31/445
CPC分类号： C07D207/08 , A61K31/135 , A61K31/136 , A61K31/137 , A61K31/138 , A61K31/155 , A61K31/165 , A61K31/295 , A61K31/381 , A61K31/40 , A61K31/4409 , A61K31/4462 , A61K31/4465 , C07B2200/07 , C07C211/27 , C07C211/28 , C07C211/29 , C07C211/40 , C07C211/54 , C07C215/28 , C07C215/54 , C07C217/10 , C07C217/48 , C07C217/60 , C07C217/62 , C07C233/13 , C07C233/22 , C07C235/34 , C07C237/22 , C07C279/14 , C07C2601/08 , C07C2601/14 , C07D207/12 , C07D207/20 , C07D209/42 , C07D211/18 , C07D213/30 , C07D213/38 , C07D333/20
摘要： Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequency occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amytrophic lateral sclerosis (ALS).
摘要翻译：方法和组合物用于治疗患有神经疾病或病症，：如中风，头部创伤，脊髓损伤，癫痫，焦虑，或神经变性疾病的患者：如阿尔茨海默氏病，亨廷顿氏病，帕金森氏病，或肌萎缩性侧索硬化症（ALS），

9. 发明公开

EP1132373A2 NEW DERIVATIVES OF 6-(4-PHENYLBUTOXY)HEXYLAMINE AND PROCESS FOR PRODUCING SALMETEROL 有权
标题翻译： DERIVATE DES 6-（4-苯基氧基）HEXYLAMINS UND VERFAHREN ZUR HERSTELLUNG VON SALMETEROL
公开(公告)号：EP1132373A2
公开(公告)日：2001-09-12
申请号：EP99969711.3
申请日：1999-09-20
申请人： VITA-INVEST, S.A.
发明人： BESSA BELLMUNT, Jordi , DALMASES BARJOAN, Pere , MARQUILLAS OLONDRIZ, Francisco
IPC分类号： C07C217/44 , C07C213/08 , C07D319/06
CPC分类号： C07D319/08 , C07C213/08 , C07C217/28 , C07C217/40 , C07C271/16 , Y02P20/55 , C07C217/10
摘要： The present invention refers to new derivatives of the 6-(4-phenylbutoxy)hexylamine of the general formula (I):
wherein:

R 1 is CHO or CHOR 3 OR 4 , where R 3 and R 4 independently are C 1 -C 6 alkyl, aralkyl, or they form 5 or 6 membered cyclic acetals; and
R 2 is H, benzyl or an alkyloxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl or acyl group;
and to a process for its obtention.
The invention also refers to a new process for obtaining Salmeterol or its pharmaceutically acceptable salts, characterised in that reaction of an organometallic compound of the general formula ( 13 ) is carried out in an inert solvent at low temperature with a synthetic intermediate of the general formula ( I ), wherein R 1 is CHO, and R 2 is an alkyloxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl or acyl group.
摘要翻译：本发明涉及通式（I）的6-（4-苯基丁氧基）己胺的新衍生物：其中：R1是CHO或CHOR3OR4，其中R3和R4独立地是C1-C6烷基，芳烷基或它们形成5或6元环状缩醛; R2为H，苄基或烷氧基羰基，芳氧基羰基，芳烷氧基羰基或酰基; 并为其获得一个进程。本发明还涉及一种获得沙美特罗或其药学上可接受的盐的新方法，其特征在于通式（13）的有机金属化合物在低温惰性溶剂中的反应与通式（I），其中R1是CHO，R2是烷氧基羰基，芳氧基羰基，芳烷氧基羰基或酰基。

10. 发明公开

EP0983222A1 PHARMACEUTICAL AGENTS FOR THE TREATMENT OF CEREBRAL AMYLOIDOSIS 失效
标题翻译：药剂脑淀粉样变治疗
公开(公告)号：EP0983222A1
公开(公告)日：2000-03-08
申请号：EP98923520.5
申请日：1998-05-19
申请人： NYMOX CORPORATION
发明人： AVERBACK, Paul , GHANBARI, Hossein , BEHESHTI, Iraj , MORSE, David
IPC分类号： C07C43/164 , A61K31/08 , C07C43/174 , C07C217/10 , C07D211/90 , C07D295/02 , C07D295/08 , C07D473/04 , A61K31/495 , A61K31/645 , A61K31/44 , A61K31/52
CPC分类号： C07D295/03 , C07C43/164 , C07C43/1745 , C07C211/28 , C07C217/10 , C07D211/90 , C07D295/088 , C07D473/04
摘要： Formation of cerebral amyloid associated with Alzheimer's disease can be treated or averted using medicaments that are effective in vivo in preventing disruption of dense microspheres (DMS) or in altering the disruption so as to (i) reduce the volume of tissue occupied by redistributed, transformed DMS protein material and its associated injury focus; (ii) reduce the persistence or duration of injury and inflammation associated with the disrupted DMS and redistributed transformed DMS protein material; and/or (iii) increase the digestion and removal of DMS material through the reticuloendothelial system.

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