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1. 发明申请

WO2010117084A1 NOVEL ISOQUINOLINE DERIVATIVES 审中-公开
标题翻译：新型异喹啉衍生物
公开(公告)号：WO2010117084A1
公开(公告)日：2010-10-14
申请号：PCT/JP2010/056635
申请日：2010-04-07
申请人： BANYU PHARMACEUTICAL CO.,LTD. , SUGIMOTO, Yuichi , SATOH, Atsushi , NISHIMURA, Teruyuki
发明人： SUGIMOTO, Yuichi , SATOH, Atsushi , NISHIMURA, Teruyuki
IPC分类号： C07D217/24 , A61K31/472 , A61K31/4725 , A61P3/04 , A61P3/06 , A61P3/10 , A61P43/00 , C07D401/12
CPC分类号： C07D217/24 , C07D401/12
摘要： The present invention relates to a compound represented by a formula (I): wherein: R is independently from each other a lower alkyl group and the like, X is an oxygen atom or a sulfur atom, Y is a lower alkylene group having 1 to 6 carbon atoms, R 1 is a phenyl group and the like which may be substituted by a halogen atom and the like, and any CH 2 in the following: (I-1) may be substituted by a lower alkyl group, and R 2 is a phenyl group or a pyridinyl group which may be substituted by a lower alkyl group and the like, m is 0, 1, 2 or 3, and n is 0 or 1, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及由式（I）表示的化合物：其中：R彼此独立地为低级烷基等，X为氧原子或硫原子，Y为低级亚烷基，具有1〜 6个碳原子，R 1是可以被卤素原子等取代的苯基等，以下的任何CH 2：（I-1）可以被低级烷基取代，R 2是苯基基团或可以被低级烷基等取代的吡啶基，m为0,1,2或3，n为0或1，或其药学上可接受的盐。

2. 发明申请

WO2010104195A1 NOVEL ISOINDOLIN-1-ONE DERIVATIVE 审中-公开
公开(公告)号：WO2010104195A1
公开(公告)日：2010-09-16
申请号：PCT/JP2010/054288
申请日：2010-03-09
申请人： BANYU PHARMACEUTICAL CO.,LTD. , ARAKAWA, Keisuke , NISHIMURA, Teruyuki , SUGIMOTO, Yuichi , TAKAHASHI, Hiroyuki , SHIMAMURA, Tadashi
发明人： ARAKAWA, Keisuke , NISHIMURA, Teruyuki , SUGIMOTO, Yuichi , TAKAHASHI, Hiroyuki , SHIMAMURA, Tadashi
IPC分类号： C07D401/12 , A61K31/428 , A61K31/4439 , A61K31/497 , A61K31/506 , A61P3/04 , A61P3/06 , A61P3/10 , A61P43/00 , C07D417/12
CPC分类号： C07D401/12 , C07D417/12
摘要： The present invention relates to a compound represented by formula (I): (wherein R 1 , R 2 , R 3 and R 4 each independently represent a hydrogen or halogen atom; R 5 and R 6 each independently represent a hydrogen atom or lower alkyl or together represent oxo; X represents C(O) or the like; Y represents an oxygen atom or the like; Z represents a hydrogen atom or the like; R represents 5- or 6-membered heteroaryl having 1-3 hetero atoms selected from the group consisting of nitrogen, sulfur and oxygen atoms, contained within a ring, or the like) or to a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及由式（I）表示的化合物：（其中R 1，R 2，R 3和R 4各自独立地表示氢或卤素原子; R 5和R 6各自独立地表示氢原子或低级烷基或一起代表氧代; X表示C（O）等; Y表示氧原子等; Z表示氢原子等; R表示具有1-3个选自氮原子的杂原子的5-或6-元杂芳基，硫和氧原子，包含在环内等）或其药学上可接受的盐。

3. 发明申请

WO2010056496A1 AZEPINONE DERIVATIVES 审中-公开
标题翻译： AZEPINONE衍生物
公开(公告)号：WO2010056496A1
公开(公告)日：2010-05-20
申请号：PCT/US2009/062006
申请日：2009-10-26
申请人： MERCK SHARP & DOHME CORP. , BANYU PHARMACEUTICAL CO., LTD. , OKAMOTO, Osamu , SASAKI, Yasuhiro , WATANABE, Hitomi , JONA, Hideki , DYKSTRA, Kevin, D.
发明人： OKAMOTO, Osamu , SASAKI, Yasuhiro , WATANABE, Hitomi , JONA, Hideki , DYKSTRA, Kevin, D.
IPC分类号： C07K5/00 , A61K38/00 , C07D255/04
CPC分类号： C07D223/16 , C07D401/12 , C07D417/12 , C07K5/06026
摘要： The present invention relates to a compound represented by formula (I): wherein R 1 represents a hydrogen atom or the like; R 2 and R 3 represent a hydrogen atom or the like; R 4 is a group represented by (II) R 5 represents a phenyl group which may be substituted with a halogen or the like; m is an integer of from 1 to 3; and p is an integer of from 0 to 4; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及由式（I）表示的化合物：其中R1表示氢原子等; R2和R3表示氢原子等; R4是由（II）表示的基团，R5表示可以被卤素等取代的苯基; m为1〜3的整数，且p为0至4的整数; 或其药学上可接受的盐。

4. 发明申请

WO2008070016A2 INHIBITORS OF AKT ACTIVITY 审中-公开
公开(公告)号：WO2008070016A2
公开(公告)日：2008-06-12
申请号：PCT/US2007/024722
申请日：2007-12-03
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , KELLY, Michael, J. , LAYTON, Mark, E. , LIQUORI, Michael, E. , OGINO, Yoshio , ONOZAKI, Yu , SANDERSON, Philip, E. , WANG, Jiabing
发明人： KELLY, Michael, J. , LAYTON, Mark, E. , LIQUORI, Michael, E. , OGINO, Yoshio , ONOZAKI, Yu , SANDERSON, Philip, E. , WANG, Jiabing
CPC分类号： C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D407/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/14
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

5. 发明申请

WO2005061501A2 PROCESS FOR PREPARING HEXAHYDROPYRIMIDO[1,2-A]AZEPINE-2-CARBOXYLATES AND RELATED COMPOUNDS 审中-公开
标题翻译：制备十六氢二咪唑[1,2-A]亚甲基-2-羧酸酯及相关化合物的方法
公开(公告)号：WO2005061501A2
公开(公告)日：2005-07-07
申请号：PCT/US2004/041115
申请日：2004-12-08
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , ASKIN, David , CONLON, David , LEE, Jaemoon , PIPIK, Brenda , ZHONG, Yong-Li , KOHMURA, Yoshinori
发明人： ASKIN, David , CONLON, David , LEE, Jaemoon , PIPIK, Brenda , ZHONG, Yong-Li , KOHMURA, Yoshinori
IPC分类号： C07D487/00
CPC分类号： C07F9/6561 , C07C251/60 , C07C255/26 , C07C259/14 , C07D239/557 , C07D487/04
摘要： Processes for preparing 10-amino-3-hydroxy-4-oxo-4,6,7,8,9,10-hexahydropyrimido[1,2-a]azepine-2-carboxylates and related compounds are disclosed. The preparation of carboxamide derivatives from these carboxylates is also disclosed. The carboxamides are HIV integrase inhibitors and are useful for treating HIV infection and AIDS.
摘要翻译：公开了制备10-氨基-3-羟基-4-氧代-4,6,7,8,9,10-六氢嘧啶并[1,2-a]吖庚因-2-羧酸酯和相关化合物的方法。还公开了从这些羧酸盐制备羧酰胺衍生物。甲酰胺是HIV整合酶抑制剂，可用于治疗艾滋病毒感染和艾滋病。

6. 发明申请

WO2004093785A2 RHESUS MONKEY BOMBESIN RECEPTOR SUBTYPE-3 (BRS-3), NUCLEOTIDES ENCODING SAME, AND USES THEREOF 审中-公开
标题翻译： RHESUS MONKEY BOMBESIN受体亚型3（BRS-3），编码它们的核苷酸及其用途
公开(公告)号：WO2004093785A2
公开(公告)日：2004-11-04
申请号：PCT/US2004/011473
申请日：2004-04-14
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , TAN, Carina, P. , HOWARD, Andrew, D. , SANO, Hideki
发明人： TAN, Carina, P. , HOWARD, Andrew, D. , SANO, Hideki
IPC分类号： A61K
CPC分类号： C07K14/70571 , C07K14/723 , G01N2333/70571
摘要： A rhesus monkey bombesin receptor subtype-3 has been isolated, cloned and sequenced. This receptor is characteristic of the G-protein family of receptors. Isolated rhesus monkey bombesin receptor subtype-3 may be used to screen and identify novel bombesin receptor modulators that may contribute to the regulation of endocrine processes, metabolism, or the cell cycle. Such compounds may be used in the treatment of conditions that result from deregulated expression of bombesin receptor subtype-3.
摘要翻译：已经分离，克隆和测序了恒河猴铃蟾肽受体亚型3。该受体是G-蛋白家族受体的特征。分离的恒河猴铃蟾肽受体亚型-3可用于筛选和鉴定可能有助于调节内分泌过程，代谢或细胞周期的新型bombesin受体调节剂。这些化合物可用于治疗由bombesin受体亚型-3的失调表达引起的病症。

7. 发明申请

WO2004009015A2 COMBINATION THERAPY FOR THE TREATMENT OF OBESITY 审中-公开
标题翻译：治疗肥胖的组合疗法
公开(公告)号：WO2004009015A2
公开(公告)日：2004-01-29
申请号：PCT/US2003/022077
申请日：2003-07-14
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , MACNEIL, Douglas, J. , MCINTYRE, James, H. , VAN DER PLOEG, Leonardus, H. T. , ISHIHARA, Akane
发明人： MACNEIL, Douglas, J. , MCINTYRE, James, H. , VAN DER PLOEG, Leonardus, H. T. , ISHIHARA, Akane
IPC分类号： A61K
CPC分类号： A61K31/155 , A61K31/353 , A61K31/438 , A61K31/4747 , A61K31/506
摘要： The present invention relates to compositions comprising a NPY5 antagonist of formula I or II and an anti-obesity agent, useful for the treatment and prevention of diabetes, obesity and obesity-related disorders. The present invention further relates to methods of treating or preventing obesity and obesity-related disorder in a subject in need thereof by administering a composition of the present invention. The present invention further provides for pharmaceutical compositions, medicaments, and kits useful in carrying out these methods.
摘要翻译：本发明涉及包含式I或II的NPY5拮抗剂和抗肥胖剂的组合物，其可用于治疗和预防糖尿病，肥胖症和肥胖相关疾病。本发明还涉及通过给予本发明的组合物来治疗或预防有需要的受试者中的肥胖和肥胖相关疾病的方法。本发明进一步提供可用于实施这些方法的药物组合物，药物和试剂盒。

8. 发明申请

WO2004002986A2 NOVEL BENZIMIDAZOLE DERIVATIVES 审中-公开
标题翻译：新型苯并咪唑衍生物
公开(公告)号：WO2004002986A2
公开(公告)日：2004-01-08
申请号：PCT/JP2003/008161
申请日：2003-06-26
申请人： BANYU PHARMACEUTICAL CO., LTD. , OTAKE, Norikazu , MORIYA, Minoru , OGINO, Yoshio , MATSUDA, Kenji , NAGAE, Yoshikazu , KANATANI, Akio , FUKAMI, Takehiro
发明人： OTAKE, Norikazu , MORIYA, Minoru , OGINO, Yoshio , MATSUDA, Kenji , NAGAE, Yoshikazu , KANATANI, Akio , FUKAMI, Takehiro
IPC分类号： C07D471/04
CPC分类号： C07D473/30 , C07D405/04 , C07D471/04 , C07D471/10 , C07D473/00 , C07D491/04
摘要： A compound of the formula (I): (wherein A, B, C and D are independently nitrogen or optionally substituted methine; E is nitrogen, methine or hydroxy substituted methine; n is 0 or 1; T, U, V and W are independently nitrogen or optionally substituted methine; X is - N(S0 2 R 4 )-, - N (COR 5 ) - or - CO-; Y is -C (R 6 ) (R 7 )_, -0- or -N (R 8 )_, provided that the compound (I) when E is nitrogen, n is 0, X is -CO-, and Y is - 0- is excluded) is useful as an agent for the treatment of various diseases related to NPY, for example cardiovascular disorders such as angina, acute or congestive heart failure, myocardial infarction, hypertension, nephropathy, electrolyte abnormality, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, memory impairment, sleep disorders, cognitive impairment, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorder, inflammatory diseases or glaucoma, and the like, also for example, atherosclerosis, hypogonadism, hyperandrogenism, polycystic ovary syndrome, hirsutism, gastro-intestinal motility disorder, obesity-related gastro-esophageal reflux, obesity hypoventilation (Pickwickian syndrome), sleep apnea, inflammation, systemic inflammation of the vasculature, osteoarthritis, insulin resistance, bronchoconstriction, alcohol preference, metabolic syndrome, Alzheimer's disease, cardiac hypertrophy, left ventricular hypertrophy, hypertriglyceridemia, low HDL cholesterol, cardiovascular disorders such as coronary heart disease (CHD), cerebrovascular disease, stroke, peripheral vascular disease, sudden death, gallbladder diseases, cancer (breast, endometrial, colon), breathlessness, hyperuricemia, impaired fertility, low back pain, and increased anesthetic risk.
摘要翻译：式（I）的化合物：其中A，B，C和D独立地为氮或任选取代的次甲基; E为氮，次甲基或羟基取代的次甲基; n为0或1; T，U，V和W为独立的氮或任选取代的次甲基; X是-N（SO 2 R 4） - ， - N（COR 5） - 或 - CO-; Y是-C（R 6）其中当E为氮时，化合物（I）为n，n为0，X为-CO-，Y为0〜 - 被排除）可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病如心绞痛，急性或充血性心力衰竭，心肌梗塞，高血压，肾病，电解质异常，血管痉挛，动脉硬化等，中枢神经系统疾病如贪食症，抑郁症，焦虑症，癫痫发作，癫痫症，痴呆症，酗酒，戒酒，药物戒断，昼夜节律紊乱，精神分裂症，记忆障碍，睡眠障碍，认知障碍等，代谢疾病如肥胖，糖尿病，激素异常，高胆固醇血症，高脂血症，痛风，脂肪肝等，生殖器官或生殖障碍如不育症，早产，性功能障碍等，胃肠疾病，呼吸系统疾病，炎性疾病或青光眼，以及例如动脉粥样硬化，性腺机能减退，雄激素过多症，多囊卵巢综合征，多毛症，胃肠动力障碍，肥胖相关的胃食管反流，肥胖低通气（皮克维克综合征），睡眠呼吸暂停，炎症，脉管系统的全身炎症，骨关节炎，胰岛素抵抗，支气管收缩，酒精偏爱，代谢综合征，阿尔茨海默病，心脏肥大，左心室肥大，高甘油三酯血症，低HDL胆固醇，心血管疾病如冠心病（CHD），脑血管疾病，中风，外周血管疾病，突发死亡，胆囊疾病，癌症（乳腺癌，子宫内膜癌，结肠癌）），呼吸困难，高尿酸血症，生育能力受损，腰痛，麻醉风险增加。

9. 发明申请

WO2002097394A2 RHESUS MONKEY, DOG AND FERRET MELANIN-CONCENTRATING HORMONE TYPE 2 RECEPTOR 审中-公开
标题翻译：鹿茸，OG OG AND ET TOR TOR TOR TOR TOR TOR TOR TOR TOR TOR TOR TOR TOR
公开(公告)号：WO2002097394A2
公开(公告)日：2002-12-05
申请号：PCT/US2002/016702
申请日：2002-05-28
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , TAN, Carina , SANO, Hideki
发明人： TAN, Carina , SANO, Hideki
IPC分类号： G01N
CPC分类号： C07K14/72 , G01N33/74 , G01N33/9406
摘要： The present invention identifies the presence of MCH-2R in the dog, ferret and rhesus monkey. MCH-2R is a G-protein coupled receptor that responds to MCH and is distinct from MCH-1R. MCH-2R polypeptide and nucleic acid sequences related to the dog, ferret, and rhesus monkey MCH-2R are described herein along with uses of such polypeptides and nucleic acids.
摘要翻译：本发明鉴定了狗，白鼬和恒河猴中MCH-2R的存在。 MCH-2R是对MCH反应的G蛋白偶联受体，不同于MCH-1R。本文中描述了与狗，白鼬和恒河猴MCH-2R相关的MCH-2R多肽和核酸序列以及这些多肽和核酸的用途。

10. 发明申请

WO1998025906A1 PROCESS FOR PRODUCING HALOGENATED HETEROARYL COMPOUNDS 审中-公开
标题翻译：生产羟基化合物的方法
公开(公告)号：WO1998025906A1
公开(公告)日：1998-06-18
申请号：PCT/JP1997004508
申请日：1997-12-09
申请人： BANYU PHARMACEUTICAL CO., LTD. , OKADA, Shigemitsu , USHIJIMA, Ryosuke , ISHIKAWA, Kiyofumi
发明人： BANYU PHARMACEUTICAL CO., LTD.
IPC分类号： C07D213/61
CPC分类号： C07D213/79 , C07D213/61 , C07D213/85 , C07D215/48 , C07D241/44
摘要： A process for producing compounds represented by general formula (II), wherein X represents halogeno; A , A , and A are the same or different and each represents carbon or nitrogen, provided that at least one of A , A , and A is nitrogen; and R , R , R and R are the same or different and each represents hydrogen, lower alkyl, cyano, carboxy, lower alkyloxycarbonyl, carbamoyl, halogeno, nitro, hydroxy, or lower aminoalkyl, provided that when R and R are adjacent substituents, the two can be bonded to each other to form a five- or six-membered ring optionally having on the ring one substituent selected from the group consisting of lower alkyl, nitryl, carboxy, lower alkyloxycarbonyl, carbamoyl, halogeno, nitro, hydroxy, and lower aminoalkyl, characterized by reacting a compound represented by general formula (I), wherein A , A , A , R , R , R , and R have the same meaning as the above, with a halogenated quaternary ammonium salt in the presence of phosphorus pentaoxide.
摘要翻译：一种制备由通式（II）表示的化合物的方法，其中X表示卤代; A 1，A 2和A 3相同或不同，各自表示碳或氮，条件是A 1，A 2和A 3中的至少一个为氮 ; R 1，R 2，R 3和R 4相同或不同，各自代表氢，低级烷基，氰基，羧基，低级烷氧基羰基，氨基甲酰基，卤代，硝基，羟基或低级氨基烷基，条件是当R 1和R 2是相邻的取代基时，两个可以彼此键合以形成任选地在环上具有一个选自下面的取代基的五元或六元环：低级烷基，硝基，羧基，低级烷氧基羰基，氨基甲酰基，卤代，硝基，羟基和低级氨基烷基，其特征在于使通式（I）表示的化合物，其中A 1，A 2，卤化季铵盐在五氧化二磷存在下，R 1，R 2，R 3和R 4具有与上述相同的含义。

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