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1. 发明申请

WO2005025555A2 ARYL ANILINE BETA-2 ADRENERGIC RECEPTOR AGONISTS 审中-公开
公开(公告)号：WO2005025555A2
公开(公告)日：2005-03-24
申请号：PCT/US2004/014168
申请日：2004-05-07
申请人： THERAVANCE, INC. , MORAN, Edmund, J. , JACOBSEN, John, R. , LEADBETTER, Michael, R. , NODWELL, Matthew, B. , TRAPP, Sean, G. , AGGEN, James, B. , CHURCH, Timothy, J.
发明人： MORAN, Edmund, J. , JACOBSEN, John, R. , LEADBETTER, Michael, R. , NODWELL, Matthew, B. , TRAPP, Sean, G. , AGGEN, James, B. , CHURCH, Timothy, J.
IPC分类号： A61K31/00
CPC分类号： A61K31/4706 , A61K31/136 , A61K31/277 , A61K31/325 , A61K31/33 , A61K31/343 , A61K31/35 , A61K31/36 , A61K31/381 , A61K31/385 , A61K31/405 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/47 , A61K31/4704 , A61K31/4709 , A61K31/58 , C07C213/04 , C07C215/34 , C07C215/60 , C07C217/84 , C07C229/38 , C07C233/43 , C07C317/36 , C07D213/75 , C07D215/227 , C07D215/26 , C07D231/22 , C07D239/38 , C07D239/42 , C07D239/47 , C07D239/69 , C07D277/46 , C07D311/80 , C07D321/10 , C07D401/12 , C07D409/12 , C07D413/12 , A61K2300/00
摘要： The invention provides novel β2 adrenergic receptor agonist compounds of formula (I): wherein R 1 - R 13 and w have any of the values described in the specification. The invention also provides combinations of such compounds and other therapeutic agents, pharmaceutical compositions comprising such compounds and combinations, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
摘要翻译：本发明提供式（I）的新型β2肾上腺素能受体激动剂化合物：其中R1-R13和w具有说明书中描述的任何值。本发明还提供了这些化合物和其它治疗剂的组合，包含这些化合物和组合的药物组合物，使用这些化合物治疗与β2肾上腺素能受体活性有关的疾病的方法，以及可用于制备这些化合物的方法和中间体。

2. 发明申请

WO1997023202A1 SUBTYPE-SELECTIVE NMDA RECEPTOR LIGANDS AND THE USE THEREOF 审中-公开
标题翻译：亚型选择性NMDA受体配体及其用途
公开(公告)号：WO1997023202A1
公开(公告)日：1997-07-03
申请号：PCT/US1996020086
申请日：1996-12-20
申请人： STATE OF OREGON, acting by and through THE OREGON STATE BOARD OF HIGHER EDUCATION, acting for and on behalf of THE OREGON HEALTH SCIENCES UNIVERSITYA ND THE UNIVERSITY OF OREGON, EUGENE OREGON , ACEA PHARMACEUTICALS, INC. , COCENSYS, INC. , CAI, Sui, Xiong , KEANA, John, F., W. , LAN, Nancy, C. , ARALDI, Gian, Luca , TAMIZ, Amir , ZHOU, Zhang-Lin , WOODWARD, Richard, M. , WHITTEMORE, Edward, R. , WEBER, Eckard
发明人： STATE OF OREGON, acting by and through THE OREGON STATE BOARD OF HIGHER EDUCATION, acting for and on behalf of THE OREGON HEALTH SCIENCES UNIVERSITYA ND THE UNIVERSITY OF OREGON, EUGENE OREGON , ACEA PHARMACEUTICALS, INC. , COCENSYS, INC.
IPC分类号： A61K31/13
CPC分类号： C07D207/08 , C07C45/74 , C07C211/27 , C07C215/34 , C07C215/52 , C07C215/54 , C07C217/16 , C07C233/11 , C07C233/22 , C07C235/34 , C07C255/41 , C07C2601/14 , C07D207/06 , C07D207/26 , C07D209/16 , C07D211/16 , C07D243/14 , C07C49/248
摘要： The invention relates to subtype-selective NMDA receptor ligands and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's diseae, Parkinson's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, chronic pain, glaucoma, CMV retinitis, urinary incontinence and inducing anesthesia, as well as for enhancing cognition, treating or preventing opiate tolerance, treating or preventing aminoglycoside antibiotic induced hearing loss, and treating opiate withdrawal.
摘要翻译：本发明涉及亚型选择性NMDA受体配体及其用于治疗或预防与中风，缺血，CNS创伤，低血糖和手术相关的神经元丧失的用途，以及治疗神经变性疾病，包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病，帕金森病和唐氏综合征，治疗或预防兴奋性氨基酸过度刺激的不良后果，治疗焦虑症，精神病，抽搐，慢性疼痛，青光眼，CMV视网膜炎，尿失禁和诱导麻醉，以及增强认知，治疗或预防阿片剂耐受，治疗或预防氨基糖苷类抗生素诱发的听力损失，以及治疗阿片剂戒断。

3. 发明申请

WO2011147311A1 羟基丙二醇类衍生物、其制备方法和其药物组合物与用途审中-公开
公开(公告)号：WO2011147311A1
公开(公告)日：2011-12-01
申请号：PCT/CN2011/074633
申请日：2011-05-25
申请人：中国医学科学院药物研究所 , 韩伟娟 , 周婉琪 , 李志永 , 张翼 , 陈晓光 , 尹大力
发明人：韩伟娟 , 周婉琪 , 李志永 , 张翼 , 陈晓光 , 尹大力
IPC分类号： C07D263/32 , C07D309/04 , C07D309/06 , C07C215/28 , A61K31/137 , A61K31/351 , A61K31/40 , A61P37/02 , A61P37/06
CPC分类号： C07D309/06 , C07C215/34 , C07C2601/14 , C07C2602/10 , C07D263/32 , C07D309/04

4. 发明申请

WO98045249A1 2-AMINOPROPANE-1,3-DIOL COMPOUNDS, MEDICINAL USE THEREOF, AND INTERMEDIATES IN SYNTHESIZING THE SAME 审中-公开
标题翻译： 2-氨基丙-1,3-二醇化合物，其医药用途及其合成中间体
公开(公告)号：WO98045249A1
公开(公告)日：1998-10-15
申请号：PCT/JP1998/001571
申请日：1998-04-03
IPC分类号： A61K31/00 , A61K31/13 , A61K31/135 , A61P37/00 , A61P37/06 , C07C20060101 , C07C215/00 , C07C215/10 , C07C215/34 , C07C223/00 , C07C223/02 , C07C225/08 , C07C225/16 , C07F7/18
CPC分类号： C07C225/16 , C07C215/34 , C07C223/02 , C07F7/1804
摘要： Compounds represented by general formula (I), pharmaceutically acceptable acid addition salts thereof, or hydrates of the same; drugs containing these compounds; medicinal compositions containing these compounds together with pharmaceutically acceptable carriers; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)-propane-1,3-diol optionally protected at the amino and/or hydroxy group or salts thereof, each useful as an intermediate in synthesizing the above compounds. In said formula, R , R , R and R represent each hydrogen or acyl. Because of having little toxicity, high safety and excellent immunosuppressive effects, these compounds are useful as preventives or depressants for rejection reactions in organ or bone marrow transplantations and preventives or remedies for various autoimmune diseases, various allergic diseases, etc.
摘要翻译：由通式（I）表示的化合物，其药学上可接受的酸加成盐或其水合物; 含有这些化合物的药物; 含有这些化合物与药学上可接受的载体的药物组合物; 和2-氨基-2-（2-（4-（1-羟基-5-苯基戊基）苯基）乙基）丙烷-1,3-二醇或2-氨基-2-（2-（4-甲酰基苯基）乙基）任选在氨基和/或羟基保护的丙烷-1,3-二醇或其盐，各自用作合成上述化合物的中间体。在所述式中，R 1，R 2，R 3和R 4各自代表氢或酰基。由于毒性小，安全性高，免疫抑制效果好，这些化合物可用作器官或骨髓移植排斥反应的预防剂或抑制剂，各种自身免疫性疾病，各种过敏性疾病等的预防措施或治疗方法。

5. 发明申请

WO01096278A3 A NOVEL PROCESS FOR PREPARING SALMETEROL 审中-公开
标题翻译：制备沙利度醇的新方法
公开(公告)号：WO01096278A3
公开(公告)日：2002-03-21
申请号：PCT/GB2001/002624
申请日：2001-06-13
IPC分类号： C07D319/08 , C07B61/00 , C07C213/00 , C07C213/08 , C07C215/34 , C07C217/10 , C07C225/16 , C07C213/02
CPC分类号： C07C213/08 , C07B2200/07 , C07C215/34 , C07C225/16 , Y02P20/55 , C07C217/10
摘要： Accordingly, the present invention provides a process for the preparation of a compound of formula (I) or a single enantiomer thereof, or a salt or a solvate thereof, wherein W is a chiral auxiliary or hydrogen and P and P are each independently selected from hydrogen or a protecting group, which comprises: a) treatment of a compound of formula (II), or a salt or a solvate thereof, wherein W is a chiral auxiliary and P and P are each independently selected from hydrogen or a protecting group, with a compound of formula (III); b) treatment of the resulting product with a reducing agent; c) if required, deprotection to yield the compound of formula (I), or a salt or solvate thereof. In particular there is provided a process for producing a substantially pure single enantiomer of salmeterol.
摘要翻译：因此，本发明提供了制备式（I）化合物或其单一对映异构体或其盐或溶剂合物的方法，其中W是手性助剂或氢，P 1和P 2 其各自独立地选自氢或保护基，其包括：a）处理式（II）化合物或其盐或溶剂合物，其中W是手性助剂，P 1和P 2 各自独立地选自氢或保护基，与式（III）的化合物反应; b）用还原剂处理所得产物; c）如果需要，脱保护得到式（I）化合物或其盐或溶剂合物。特别地，提供了生产沙美特罗基本上纯的单一对映异构体的方法。

6. 发明申请

WO0196278A2 A NOVEL PROCESS FOR PREPARING SALMETEROL 审中-公开
标题翻译：制备沙利度醇的新方法
公开(公告)号：WO0196278A2
公开(公告)日：2001-12-20
申请号：PCT/GB0102624
申请日：2001-06-13
申请人： GLAXO GROUP LTD , PROCOPIOU PANAYIOTIS ALEXANDRO
发明人： PROCOPIOU PANAYIOTIS ALEXANDRO
IPC分类号： C07D319/08 , C07B61/00 , C07C213/00 , C07C213/08 , C07C215/34 , C07C217/10 , C07C225/16 , C07C213/02
CPC分类号： C07C213/08 , C07B2200/07 , C07C215/34 , C07C225/16 , Y02P20/55 , C07C217/10
摘要： Accordingly, the present invention provides a process for the preparation of a compound of formula (I) or a single enantiomer thereof, or a salt or a solvate thereof, wherein W is a chiral auxiliary or hydrogen and P and P are each independently selected from hydrogen or a protecting group, which comprises: a) treatment of a compound of formula (II), or a salt or a solvate thereof, wherein W is a chiral auxiliary and P and P are each independently selected from hydrogen or a protecting group, with a compound of formula (III); b) treatment of the resulting product with a reducing agent; c) if required, deprotection to yield the compound of formula (I), or a salt or solvate thereof. In particular there is provided a process for producing a substantially pure single enantiomer of salmeterol.
摘要翻译：因此，本发明提供了制备式（I）化合物或其单一对映异构体或其盐或溶剂合物的方法，其中W是手性助剂或氢，P 1和P 2 其各自独立地选自氢或保护基，其包括：a）处理式（II）化合物或其盐或溶剂合物，其中W是手性助剂，P 1和P 2 各自独立地选自氢或保护基，与式（III）的化合物反应; b）用还原剂处理所得产物; c）如果需要，脱保护得到式（I）化合物或其盐或溶剂合物。特别地，提供了生产沙美特罗基本上纯的单一对映异构体的方法。

7. 发明申请

WO2006117339A1 MANNICHBASE AUF RESORCIN-BASIS 审中-公开
标题翻译：曼尼希间苯二酚为主
公开(公告)号：WO2006117339A1
公开(公告)日：2006-11-09
申请号：PCT/EP2006/061917
申请日：2006-04-28
申请人： SIKA TECHNOLOGY AG , GERBER, Ulrich
发明人： GERBER, Ulrich
IPC分类号： C08G14/06 , C07C215/34 , C08L63/00 , C08L75/00
CPC分类号： C08G14/06 , C07C215/34 , C08G18/3237 , C08G59/623 , C08G2190/00 , C09J163/00 , C09J175/12
摘要： Die vorliegende Erfindung betrifft Mannichbasen, welche aus Resorcin, Formaldehyd, sowie Triethylentetramin und/oder Tetraethylenpentamin herstellbar sind. Weiterhin wird ein Verfahren zu deren Herstellung und deren Verwendung als Härter für Amin-reaktive Verbindungen offenbart. Besonders geeignet haben sich die Mannichbasen als Härterkomponente in Klebstoffen.
摘要翻译：本发明涉及为Mannich其可以由间苯二酚，甲醛和三亚乙基四胺和/或四亚乙基五来制备碱。此外，它们的制备和它们的用途的处理被公开为用于胺反应性化合物的固化剂。的曼尼希碱作为固化在粘合剂组分已被证明特别适合的。

8. 发明申请

WO2005042473A1 IMPROVED PROCESS FOR THE MANUFACTURE OF CITALOPRAM HYDROBROMIDE 审中-公开
标题翻译：改进氢氯化铬制造工艺
公开(公告)号：WO2005042473A1
公开(公告)日：2005-05-12
申请号：PCT/IB2003/004757
申请日：2003-10-28
申请人： WOCKHARDT LIMITED , JAWEED MUKARRAM, Siddiqui, Mohammed , BHARGAV, Krishnaji, Upadhye , MISHRA, Krishna, Gopalji , FAROOQUI, Mohammed, Ismail
发明人： JAWEED MUKARRAM, Siddiqui, Mohammed , BHARGAV, Krishnaji, Upadhye , MISHRA, Krishna, Gopalji , FAROOQUI, Mohammed, Ismail
IPC分类号： C07C255/00
CPC分类号： C07D307/87 , C07C215/34
摘要： The present invention describes an improved process for the preparation of extremely pure 1-(4'-Fluorophenyl)-1-(3-dimethylaminopropyl)-5-phthalanecarbonitrile and its bromide salt (citalopram hydrobromide), which is a well known antidepressant. Other aspect of the invention are isolation of crystalline (4-Bromo-2-hydroxymethyl)phenyl-(4-fluorophenyl)-3-(dimethylaminopropyl)methanol (Bromodiol) and conversion of desmethylcitalopram which is formed during the cyanide exchange reaction, to Citalopram by heating with a mixture of formaldhyde and formic acid in chloroform. The resulting citalopram is conventionally purified using extraction methodology.
摘要翻译：本发明描述了制备极纯的1-（4'-氟苯基）-1-（3-二甲基氨基丙基）-5-邻苯二甲腈及其溴化物盐（西酞普兰氢溴酸盐）的改进方法，其是众所周知的抗抑郁药。本发明的另一方面是将氰化物交换反应期间形成的结晶（4-溴-2-羟甲基）苯基 - （4-氟苯基）-3-（二甲基氨基丙基）甲醇（溴二醇）和去甲西酞普兰转化为西酞普兰通过用氯仿中的甲醛和甲酸的混合物加热。所得西酞普兰通常使用提取方法纯化。

9. 发明申请

WO1994008943A1 2-AMINO-1,3-PROPANEDIOL COMPOUND AND IMMUNOSUPPRESSANT 审中-公开
标题翻译： 2-氨基-1,3-丙二醇化合物和免疫抑制剂
公开(公告)号：WO1994008943A1
公开(公告)日：1994-04-28
申请号：PCT/JP1993001515
申请日：1993-10-18
申请人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. , TAITO CO., LTD. , FUJITA, Tetsuro , SASAKI, Shigeo , YONETA, Masahiko , MISHINA, Tadashi , ADACHI, Kunitomo , CHIBA, Kenji
发明人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. , TAITO CO., LTD.
IPC分类号： C07C215/10
CPC分类号： C07D207/325 , C07C215/10 , C07C215/18 , C07C215/20 , C07C215/24 , C07C215/26 , C07C215/28 , C07C215/34 , C07C215/42 , C07C215/54 , C07C215/56 , C07C215/68 , C07C217/28 , C07C217/30 , C07C217/34 , C07C217/48 , C07C217/52 , C07C217/64 , C07C217/72 , C07C217/76 , C07C219/06 , C07C219/24 , C07C219/30 , C07C225/04 , C07C225/06 , C07C225/10 , C07C225/14 , C07C225/16 , C07C229/22 , C07C229/38 , C07C229/46 , C07C233/18 , C07C233/31 , C07C233/35 , C07C233/36 , C07C233/41 , C07C233/43 , C07C233/47 , C07C237/06 , C07C237/24 , C07C237/30 , C07C251/38 , C07C271/20 , C07C271/24 , C07C271/28 , C07C323/25 , C07C323/30 , C07C323/32 , C07C323/34 , C07C323/41 , C07C2601/08 , C07C2601/14 , C07D207/06 , C07D207/09 , C07D207/335 , C07D211/14 , C07D211/26 , C07D213/38 , C07D213/40 , C07D231/12 , C07D233/56 , C07D233/64 , C07D237/08 , C07D239/26 , C07D241/12 , C07D249/08 , C07D261/08 , C07D263/32 , C07D265/30 , C07D275/02 , C07D277/28 , C07D279/12 , C07D295/13 , C07D295/135 , C07D307/52 , C07D309/32 , C07D317/28 , C07D333/20
摘要： A 2-amino-1,3-propanediol compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, and an immunosuppressant containing the same as the active ingredient. In said formula R represents optionally substituted linear or branched carbon chain, optionally substituted aryl or optionally substituted cycloalkyl; and R , R , R and R , which may be the same or different from one another, represent each hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl. The compound is immunodepressant and useful as an inhibitor against rejection in organ or bone marrow transplantation, as a preventive or remedy for autoimmune diseases and so forth, or a reagent in the medical and pharmaceutical fields.
摘要翻译：由通式（I）表示的2-氨基-1,3-丙二醇化合物或其药学上可接受的盐，和含有该活性成分的免疫抑制剂。在所述式中，R代表任选取代的直链或支链碳链，任选取代的芳基或任选取代的环烷基; 和R 2，R 3，R 4和R 5彼此可以相同或不同，表示每个氢，烷基，芳烷基，酰基或烷氧基羰基。该化合物是免疫抑制剂，可用作作为器官或骨髓移植排斥反应的抑制剂，作为自身免疫疾病等的预防或补救剂，或医药领域的试剂。

10. 发明申请

WO2017070052A1 COMPOSITIONS AND METHODS OF REGULATING CANCER RELATED DISORDERS AND DISEASES 审中-公开
标题翻译：调节癌症相关病症和疾病的组合物和方法
公开(公告)号：WO2017070052A1
公开(公告)日：2017-04-27
申请号：PCT/US2016/057377
申请日：2016-10-17
申请人： ONCO THERAPIES LLC
发明人： VASHISHTHA, Anshu , VASHISHTHA, Malini
IPC分类号： C07D417/10 , A61K31/165 , A61P35/00
CPC分类号： A61K31/165 , C07C211/27 , C07C211/30 , C07C215/32 , C07C215/34 , C07C215/52 , C07C215/60 , C07C215/76 , C07C215/86 , C07C217/94 , C07C233/43
摘要： Provided herein are naphthylic derivative compounds, or pharmaceutically acceptable salts thereof, that are useful for inhibiting cancers. Also provided herein are methods of using effective amounts of said compounds, optionally with pharmaceutical carriers, for the treatment of cancers within human subjects.
摘要翻译：本文提供可用于抑制癌症的萘基衍生化合物或其药学上可接受的盐。本文还提供了使用有效量的所述化合物，任选与药物载体一起用于治疗人类受试者内的癌症的方法。

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