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51. 发明专利

TW200911817A 多環鳥嘌呤衍生物及其使用方法 POLYCYCLIC GUANINE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
简体标题：多环鸟嘌呤衍生物及其使用方法 POLYCYCLIC GUANINE DERIVATIVES AND METHODS OF USE THEREOF
公开(公告)号：TW200911817A
公开(公告)日：2009-03-16
申请号：TW097122895
申请日：2008-06-19
申请人：美國先靈大藥廠 SCHERING CORPORATION , 奧爾伯尼分子研究公司 ALBANY MOLECULAR RESEARCH, INC.
发明人：迪恩突珊 TULSHIAN, DEEN , 茱利爾斯J 瑪塔希 MATASI, JULIUS J. , 麥可F 希茲尼克 CZARNIECKI, MICHAEL F. , 威廉B 吉斯 GEISS, WILLIAM B. , 葛瑞哥里S 馬汀 MARTIN, GREGORY S. , 凡杜克李 LE, VAN-DUC , 詹姆士C 哈伯二世 HABER, JAMES C. JR. , 史蒂芬妮妮可庫克 COOKE, STEPHANIE NICOLE
IPC分类号： C07D , A61K , A61P
CPC分类号： C07D487/14
摘要：本發明係關於多環鳥嘌呤衍生物,包含該多環鳥嘌呤衍生物之組合物,及使用該多環鳥嘌呤衍生物以治療疼痛或炎性疾病之方法。
简体摘要：本发明系关于多环鸟嘌呤衍生物,包含该多环鸟嘌呤衍生物之组合物,及使用该多环鸟嘌呤衍生物以治疗疼痛或炎性疾病之方法。

52. 发明专利

TWI478920B 芳基、雜芳基和雜環取代的四氫異喹啉及其用途失效
简体标题：芳基、杂芳基和杂环取代的四氢异喹啉及其用途
公开(公告)号：TWI478920B
公开(公告)日：2015-04-01
申请号：TW099115160
申请日：2010-05-12
申请人：奧爾伯尼分子研究公司 , ALBANY MOLECULAR RESEARCH, INC.
发明人：劉爽 , LIU, SHUANG , 莫里諾布魯斯F , MOLINO, BRUCE F. , 拿克洛卡斯沃姆 , NACRO, KASSOUM
IPC分类号： C07D471/04 , A61K31/472
CPC分类号： C07D401/04 , C07D217/02 , C07D217/12 , C07D217/14 , C07D413/04 , C07D471/04

53. 发明专利

TW200902516A 作為聚葡糖合成抑制劑之噠酮衍生物 PYRIDAZINONE DERIVATIVES USEFUL AS GLUCAN SYNTHASE INHIBITORS 审中-公开
简体标题：作为聚葡糖合成抑制剂之哒酮衍生物 PYRIDAZINONE DERIVATIVES USEFUL AS GLUCAN SYNTHASE INHIBITORS
公开(公告)号：TW200902516A
公开(公告)日：2009-01-16
申请号：TW097108919
申请日：2008-03-13
申请人：美國先靈大藥廠 SCHERING CORPORATION , 奧爾伯尼分子研究公司 ALBANY MOLECULAR RESEARCH, INC.
发明人：寶林C 丁 TING, PAULINE C. , 羅伯G 艾斯蘭安 ASLANIAN, ROBERT G. , 寇佳華 CAO, JIANHUA , 大衛伍錫金 KIM, DAVID WON-SHIK , 關若澤 KUANG, RONGZE , 周剛 ZHOU, GANG , 羅伯傑森希爾 HERR, ROBERT JASON , 安卓約翰茲克 ZYCH, ANDREW JOHN , 楊金海 YANG, JINHAI , 吳希平 WU, HEPING , 尼可拉斯朱恩 ZORN, NICOLAS
IPC分类号： C07D , A61K , A61P
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D487/08 , C07D515/22
摘要：在本發明之許多具體實施例中,其係提供經取代之噠酮化合物作為聚葡糖合成抑制劑,製備此種化合物之方法,包含一或多種此種化合物之醫藥,製備包含一或多種此種化合物或一或多種此種化合物伴隨著其他抗真菌劑之醫藥配方之方法,及使用此種化合物或醫藥組合物治療、預防、抑制或改善一或多種與聚葡糖合成有關聯之真菌感染之方法。
简体摘要：在本发明之许多具体实施例中,其系提供经取代之哒酮化合物作为聚葡糖合成抑制剂,制备此种化合物之方法,包含一或多种此种化合物之医药,制备包含一或多种此种化合物或一或多种此种化合物伴随着其他抗真菌剂之医药配方之方法,及使用此种化合物或医药组合物治疗、预防、抑制或改善一或多种与聚葡糖合成有关联之真菌感染之方法。

54. 发明申请

WO2012099952A2 BENZOFURO[3,2-C] PYRIDINES AND RELATED ANALOGS AS SEROTONIN SUB-TYPE 6 (5-HT6) MODULATORS FOR THE TREATMENT OF OBESITY, METABOLIC SYNDROME, COGNITION AND SCHIZOPHRENIA 审中-公开
标题翻译：苯并呋喃[3,2-C]吡啶和相关模拟物作为用于治疗肥胖，代谢综合征，认知和感染的硒酸亚型6型（5-HT6）调节剂
公开(公告)号：WO2012099952A2
公开(公告)日：2012-07-26
申请号：PCT/US2012/021708
申请日：2012-01-18
申请人： ALBANY MOLECULAR RESEARCH, INC. , GUZZO, Peter, R. , HENDERSON, Alan, J. , ISHERWOOD, Matthew , LEE, Chong, Yew , GHOSH, Animesh , ZHAO, He, River
发明人： GUZZO, Peter, R. , HENDERSON, Alan, J. , ISHERWOOD, Matthew , LEE, Chong, Yew , GHOSH, Animesh , ZHAO, He, River
IPC分类号： C07D491/04 , C07D307/91 , A61K31/4741 , A61P25/00
CPC分类号： C07D491/048 , C07D307/91 , C07D491/08 , C07D491/18
摘要： The present invention relates to benzofuro[3,2-c]pyridine and azepine analogs as serotonin sub-type 6 (5-HT6) modulators, pharmaceutical compositions including these compounds, methods of preparation, and use thereof. These compounds are useful in the treatment of central nervous system disorders including obesity, metabolic syndrome, cognition, schizophrenia, attention deficit hyperactivity disorder, bipolar disorder, rare and orphan diseases, and sleep disorders. The subject compounds have the structure of formula (I) with the substituents being described herein.
摘要翻译：本发明涉及作为血清素亚型6（5-HT6）调节剂的苯并呋喃并[3,2-c]吡啶和吖庚因类似物，包括这些化合物的药物组合物，其制备方法和用途。这些化合物可用于治疗中枢神经系统疾病，包括肥胖，代谢综合征，认知，精神分裂症，注意缺陷多动障碍，双相情感障碍，罕见和孤儿疾病以及睡眠障碍。本发明化合物具有式（I）的结构，其中取代基在本文中描述。

55. 发明申请

WO2012088038A2 PIPERAZINONE-SUBSTITUTED TETRAHYDRO-CARBOLINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USES THEREOF 审中-公开
标题翻译：哌嗪酮取代的四氢咔唑MCH-1拮抗剂，制备方法及其用途
公开(公告)号：WO2012088038A2
公开(公告)日：2012-06-28
申请号：PCT/US2011/066027
申请日：2011-12-20
申请人： ALBANY MOLECULAR RESEARCH, INC. , SURMAN, Matthew, D. , GUZZO, Peter, R.
发明人： SURMAN, Matthew, D. , GUZZO, Peter, R.
IPC分类号： C07D471/04 , C07D403/04 , A61K31/4738 , A61P3/00 , A61P25/00
CPC分类号： C07D471/04
摘要： The present invention relates to piperazinone-substituted tetrahydro- carboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.
摘要翻译：本发明涉及式（I）的哌嗪酮取代的四氢咔啉衍生物：具有本文所述的取代基，其为黑素浓缩激素（MCH-1）受体拮抗剂。本发明还涉及包含这些化合物的药物组合物，以及其制备方法和用途。

56. 发明申请

WO2011003007A1 AZABICYCLOALKANE-INDOLE AND AZABICYCLOALKANE-PYRROLO-PYRIDINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF 审中-公开
标题翻译：丙氨酸环糊精和亚氨基环丙基 - 吡咯烷 - 吡啶MCH-1拮抗剂，其制备方法及其用途
公开(公告)号：WO2011003007A1
公开(公告)日：2011-01-06
申请号：PCT/US2010/040803
申请日：2010-07-01
申请人： ALBANY MOLECULAR RESEARCH, INC.
发明人： GUZZO, Peter, R. , SURMAN, Matthew, David , HENDERSON, Alan, John , HADDEN, Mark , FREEMAN, Emily, Elizabeth
IPC分类号： A61K31/50
CPC分类号： C07D471/22
摘要： Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
摘要翻译：公开了新的MCH-1受体拮抗剂。这些化合物用于治疗各种疾病，包括肥胖症，焦虑症，抑郁症，非酒精性脂肪性肝病和精神疾病。制备这些化合物的方法也在本发明中描述。

57. 发明申请

WO2003078646A2 AZA-THIOXANTHENONES WITH ANTITUMOR ACTIVITY 审中-公开
标题翻译：具有抗肿瘤活性的AZA-噻吗酮
公开(公告)号：WO2003078646A2
公开(公告)日：2003-09-25
申请号：PCT/US2003/007581
申请日：2003-03-11
申请人： ALBANY MOLECULAR RESEARCH, INC.
发明人： HAYDAR, Simon, N.
IPC分类号： C12Q
CPC分类号： C07D495/04 , C07D335/16
摘要： The present invention relates to a group of aza-thioxanthenone compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-thioxanthenone compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.
摘要翻译：本发明涉及一组具有抗肿瘤活性的氮杂 - 噻吨酮化合物及其制备方法。还公开了含有氮杂 - 噻吨酮化合物的组合物和用本发明化合物治疗哺乳动物肿瘤和癌症的方法。

58. 发明申请

WO2003022805A3 HETEROCYCLE SUBSTITUTED PURINES AS ANTIPROLIFERATIVE AGENTS 审中-公开
公开(公告)号：WO2003022805A3
公开(公告)日：2003-03-20
申请号：PCT/US2002/028730
申请日：2002-09-09
申请人： ALBANY MOLECULAR RESEARCH, INC.
发明人： TROVA, Michael, Peter
IPC分类号： C07D473/16
摘要： The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures (I) and (II) with Y, V, A, R 1 , R 2 , R 3 , R 4 , R 7 , and n 1 defined herein.

59. 发明申请

WO1997042950A1 METHOD FOR TREATING COCAINE AND AMPHETAMINE DEPENDENCY 审中-公开
标题翻译：用于处理咖啡因和安非他明依赖的方法
公开(公告)号：WO1997042950A1
公开(公告)日：1997-11-20
申请号：PCT/US1997008273
申请日：1997-05-14
申请人： ALBANY MOLECULAR RESEARCH, INC. , ARCHER, David +em
发明人： ALBANY MOLECULAR RESEARCH, INC. , ARCHER, David +em , ARCHER, Sydney +di
IPC分类号： A61K31/44
CPC分类号： A61K31/439 , Y10S514/812
摘要： The present invention relates to methods for treating cocaine and amphetamine dependency. The method involves administering to a patient in need of such treatment an effective amount of a compound of the formula, defined herein, or a pharmaceutically acceptable acid-addition salt thereof. Discomforting side effects can be minimized by optionally administering naltrexone, naloxone, or a mixture thereof during the early phases of treatment.
摘要翻译：本发明涉及治疗可卡因和苯丙胺依赖的方法。该方法涉及向需要这种治疗的患者施用有效量的本文所定义的式的化合物或其药学上可接受的酸加成盐。通过在治疗的早期阶段任选地施用纳曲酮，纳洛酮或其混合物，可以使不适的副作用最小化。

60. 发明申请

WO1997022344A1 PROCESS FOR PRODUCTION OF PIPERIDINE DERIVATIVES 审中-公开
标题翻译：生产哌啶衍生物的方法
公开(公告)号：WO1997022344A1
公开(公告)日：1997-06-26
申请号：PCT/US1996020769
申请日：1996-12-19
申请人： ALBANY MOLECULAR RESEARCH, INC.
发明人： ALBANY MOLECULAR RESEARCH, INC. , D'AMBRA, Thomas, E. , PILLING, Garry, M.
IPC分类号： A61K31/445
CPC分类号： C07D211/54 , C07D211/22 , C07D261/04
摘要： The present invention discloses processes for preparing piperidine derivative compounds of formulae (I) or (II) wherein n is 0 or 1; R is hydrogen or hydroxy; R is hydrogen; or, when n is 0, R and R taken together form a second bond between the carbon atoms bearing R and R , provided that when n is 1, R and R are each hydrogen; R is -COOH or -COOR ; R is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents. One process comprises providing a regioisomer of formula (III) wherein Z is -CG G G , (IV) or (V), m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR ; G , G , and G are the same or different and are selected from the group consisting of OR , SR , and NR R ; X is halogen, OR , SR , NR R , OSO2R , or NHSO2R ; R and R are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR , SR , and NR R ; and R , R , R , R , and R are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and converting the regioisomer to the piperidine derivative compound with a piperidine compound. Another process for producing piperidine derivative compounds comprises providing an alpha , alpha -disubstituted-methylbenzene derivative having formula (VI) wherein X is a halogen, trialkyl or triaryl tin, trialkyl or triaryl borate, trialkyl silicon, alkylhalo silicon, a substituted sulfonic ester, or substituents useful in organometallic coupling reactions and converting the alpha , alpha -disubstituted-methylbenzene derivative to the piperidine derivative compound with a piperidine compound. In yet another process, a 4-( alpha , alpha -disubstituted)-toluic acid derivative having formula (VII) wherein X is a halogen; an alkali metal oxide; a moiety having formula -OR ; a moiety having formula -SR ; or an amine; and R is selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety, is provided and converted to the piperidine derivative compound with a piperidine compound.
摘要翻译：本发明公开了制备其中n为0或1的式（I）或（II）的哌啶衍生物化合物的方法; R 1是氢或羟基; R 2是氢; 或者当n为0时，R 1和R 2一起形成带有R 1和R 2的碳原子之间的第二个键，条件是当n为1时，R 1和R 2 2是氢; R 3是-COOH或-COOR 4; R 4是烷基或芳基部分; A，B和D是它们的环的取代基，其各自可以不同或相同，并且选自氢，卤素，烷基，羟基，烷氧基和其它取代基。一种方法包括提供其中Z为-CG 1 G G 3，（IV）或（V）的式（III）的区域异构体，m为1至6的整数; Q和Y相同或不同，选自O，S和NR 5; G 1，G 2和G 3相同或不同，并且选自OR 8，SR 8和NR 8 R 9; X 3是卤素，OR 15，SR 15，NR 15 R 16，OSO 2 R 15或NHSO 2 R 15; R 6和R 7相同或不同，并且选自氢，烷基部分，芳基部分，OR 8，SR 8和NR 8 R 9 >; 并且R 5，R 8，R 9，R 15和R 16相同或不同，并且选自氢，烷基部分和芳基部分; 并用哌啶化合物转化为哌啶衍生物化合物。制备哌啶衍生物化合物的另一种方法包括提供具有式（Ⅵ）的α，α-二取代甲基苯衍生物，其中X 1是卤素，三烷基或三芳基锡，三烷基或三芳基硼酸盐，三烷基硅，烷基卤代硅，磺酸酯或可用于有机金属偶联反应的取代基，并将α，α-二取代甲基苯衍生物与哌啶化合物转化成哌啶衍生物化合物。在另一方法中，具有式（VII）的4-（α，α-二取代） - 甲苯衍生物，其中X 2是卤素; 碱金属氧化物; 具有式-OR 10的部分; 具有式-SR 10的部分; 或胺; 并且提供R 10选自氢，烷基部分和芳基部分，并用哌啶化合物转化成哌啶衍生物化合物。

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