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31. 发明申请

US20050215528A1 Gnrh agonist combination drugs 审中-公开
标题翻译： Gnrh激动剂联合药物
公开(公告)号：US20050215528A1
公开(公告)日：2005-09-29
申请号：US10486095
申请日：2002-08-08
申请人： Shuichi Furuya , Masami Kusaka
发明人： Shuichi Furuya , Masami Kusaka
IPC分类号： A61K9/50 , A61K9/52 , A61K31/352 , A61K31/36 , A61K31/4025 , A61K31/42 , A61K31/4535 , A61K31/506 , A61K31/58 , A61K31/663 , A61K38/00 , A61K45/06 , A61P3/14 , A61P5/06 , A61P9/00 , A61P13/08 , A61P15/00 , A61P15/08 , A61P15/12 , A61P19/00 , A61P19/08 , A61P25/22 , A61P25/28 , A61P35/00 , A61P35/04 , A61P43/00 , C07K7/06 , C07K7/64 , A61K31/675 , A61K31/40 , A61K31/445
CPC分类号： A61K45/06 , A61K31/4535 , A61K31/58 , A61K2300/00
摘要： In the field of pharmaceuticals, it is intended to provide drugs whereby the preventive and therapeutic effects of a GnRH agonist on various diseases can be enhanced and QOL can be improved. More specifically, combination of drugs characterized in that the GnRH agonist is combined with a chemical selected from among SERM, SARM, sex hormone synthesis inhibitors, receptor-type tyrosine kinase inhibitors, bone metabolism regulators, drugs for immunotherapy, cytokine/chemokine inhibitors and endothelin receptor antagonists. Owing to these combinations, excellent effects of enhancing the preventive and therapeutic effects of the GnRH agonist on various diseases and relieving side effects can be established. Furthermore, QOL can be improved thereby.
摘要翻译：在药物领域中，旨在提供药物，由此可以增强GnRH激动剂对各种疾病的预防和治疗作用，并且可以改善生活质量。更具体地，药物组合的特征在于GnRH激动剂与选自SERM，SARM，性激素合成抑制剂，受体型酪氨酸激酶抑制剂，骨代谢调节剂，免疫治疗药物，细胞因子/趋化因子抑制剂和内皮素的化学物质组合受体拮抗剂。由于这些组合，可以提供增强GnRH激动剂对各种疾病和缓解副作用的预防和治疗效果的优异效果。此外，可以改善生活质量。

32. 发明授权

US06413972B1 Nitrogen-containing heterocyclic compounds, their production and use 有权
标题翻译：含氮杂环化合物，其生产和使用
公开(公告)号：US06413972B1
公开(公告)日：2002-07-02
申请号：US09711139
申请日：2000-11-14
申请人： Shuichi Furuya , Toshihiro Imaeda , Satoshi Sasaki
发明人： Shuichi Furuya , Toshihiro Imaeda , Satoshi Sasaki
IPC分类号： C07D48704
CPC分类号： C07D487/04 , A61K31/506
摘要： A compound of the formula: wherein one of A and D is N and the other is C, or both are N; B is N or C; m is 0-3; R1, R2 and R3 each is (i) H or (ii) a group bound via C, N, O or S; R4 is a group bound via C; R5 is H or a group bound via C or O; R6 is H or a group bound via C; R7 is a homo- or hetero-cyclic group which may be substituted; or a salt thereof possesses excellent gonadotropin-releasing hormone antagonizing activity, and is useful as a prophylactic or therapeutic agent for sex hormone-dependent diseases, and so forth.
摘要翻译：下式的化合物：其中A和D中的一个为N，另一个为C，或两者均为N; B是N或C; m为0-3; R1，R2和R3各自为（i）H或（ii）通过C，N，O或S键合的基团; R4是通过C键合的基团; R5是H或通过C或O键合的基团; R6是H或通过C键合的基团; R7是可以被取代的同 - 或异环 - 基团; 或其盐具有优异的促性腺激素释放激素拮抗活性，并且可用作性激素依赖性疾病的预防或治疗剂等。

33. 发明申请

US20100286063A1 GNRH agonist combination drugs 审中-公开
标题翻译： GNRH激动剂联合药物
公开(公告)号：US20100286063A1
公开(公告)日：2010-11-11
申请号：US12662866
申请日：2010-05-07
申请人： Shuichi Furuya , Masami Kusaka
发明人： Shuichi Furuya , Masami Kusaka
IPC分类号： A61K38/08 , A61P35/00
CPC分类号： A61K45/06 , A61K31/4535 , A61K31/58 , A61K2300/00
摘要： In the field of pharmaceuticals, it is intended to provide drugs whereby the preventive and therapeutic effects of a GnRH agonist on various diseases can be enhanced and QOL can be improved. More specifically, combination of drugs characterized in that the GnRH agonist is combined with a chemical selected from among SERM, SARM, sex hormone synthesis inhibitors, receptor-type tyrosine kinase inhibitors, bone metabolism regulators, drugs for immunotherapy, cytokine/chemokine inhibitors and endothelin receptor antagonists. Owing to these combinations, excellent effects of enhancing the preventive and therapeutic effects of the GnRH agonist on various diseases and relieving side effects can be established. Furthermore, QOL can be improved thereby.
摘要翻译：在药物领域中，旨在提供药物，由此可以增强GnRH激动剂对各种疾病的预防和治疗作用，并且可以改善生活质量。更具体地，药物组合的特征在于GnRH激动剂与选自SERM，SARM，性激素合成抑制剂，受体型酪氨酸激酶抑制剂，骨代谢调节剂，免疫治疗药物，细胞因子/趋化因子抑制剂和内皮素的化学物质组合受体拮抗剂。由于这些组合，可以提供增强GnRH激动剂对各种疾病和缓解副作用的预防和治疗效果的优异效果。此外，可以改善生活质量。

34. 发明申请

US20090048273A1 PREMATURE OVULATION PREVENTIVE AGENT 审中-公开
标题翻译：预处理预防剂
公开(公告)号：US20090048273A1
公开(公告)日：2009-02-19
申请号：US11996269
申请日：2006-07-21
申请人： Shuichi Furuya , Masami Kusaka
发明人： Shuichi Furuya , Masami Kusaka
IPC分类号： C07D495/04 , A61K31/519 , A61P15/08
CPC分类号： A61K31/519 , A61K9/2059 , C07D495/04
摘要： The present invention provides a premature ovulation inhibitor for use in in vitro fertilization or embryo transfer process, which contains a nonpeptidic compound having a gonadotropin releasing hormone antagonistic action. The premature ovulation inhibitor for use in in vitro fertilization or embryo transfer process of the present invention is low toxic, permits oral administration, and has a superior inhibitory effect on premature ovulation in in vitro fertilization or embryo transfer process.
摘要翻译：本发明提供了用于体外受精或胚胎移植过程的早产儿排卵抑制剂，其包含具有促性腺激素释放激素拮抗作用的非肽化合物。用于本发明的体外受精或胚胎移植过程的早产儿排卵抑制剂是低毒性的，允许口服给药，并且对体外受精或胚胎移植过程中的过早排卵具有优异的抑制作用。

35. 发明申请

US20070179097A1 GnRH agonist combination drugs 审中-公开
标题翻译： GnRH激动剂联合药物
公开(公告)号：US20070179097A1
公开(公告)日：2007-08-02
申请号：US11727549
申请日：2007-03-27
申请人： Shuichi Furuya , Masami Kusaka
发明人： Shuichi Furuya , Masami Kusaka
IPC分类号： A61K38/09
CPC分类号： A61K45/06 , A61K31/4535 , A61K31/58 , A61K2300/00
摘要： In the field of pharmaceuticals, it is intended to provide drugs whereby the preventive and therapeutic effects of a GnRH agonist on various diseases can be enhanced and QOL can be improved. More specifically, combination of drugs characterized in that the GnRH agonist is combined with a chemical selected from among SERM, SARM, sex hormone synthesis inhibitors, receptor-type tyrosine kinase inhibitors, bone metabolism regulators, drugs for immunotherapy, cytokine/chemokine inhibitors and endothelin receptor antagonists. Owing to these combinations, excellent effects of enhancing the preventive and therapeutic effects of the GnRH agonist on various diseases and relieving side effects can be established. Furthermore, QOL can be improved thereby.
摘要翻译：在药物领域中，旨在提供药物，由此可以增强GnRH激动剂对各种疾病的预防和治疗作用，并且可以改善生活质量。更具体地，药物组合的特征在于GnRH激动剂与选自SERM，SARM，性激素合成抑制剂，受体型酪氨酸激酶抑制剂，骨代谢调节剂，免疫治疗药物，细胞因子/趋化因子抑制剂和内皮素的化学物质组合受体拮抗剂。由于这些组合，可以提供增强GnRH激动剂对各种疾病和缓解副作用的预防和治疗效果的优异效果。此外，可以改善生活质量。

36. 发明申请

US20050250793A1 Preventives/remedies for hot flash 审中-公开
标题翻译：预防/治疗热闪光
公开(公告)号：US20050250793A1
公开(公告)日：2005-11-10
申请号：US10511050
申请日：2003-04-10
申请人： Masami Kusaka , Shuichi Furuya
发明人： Masami Kusaka , Shuichi Furuya
IPC分类号： A61K31/519 , A61P5/24 , A61P15/12 , A61P43/00 , C07D487/04 , C07D495/04 , A61K31/4743
CPC分类号： C07D487/04 , A61K31/519 , C07D495/04
摘要： It is intended to provide a preventing or treating agent for hot flash which comprises a nonpeptidic compound having gonadotropin releasing hormone antagonistic activity, in particular, a preventing or treating agent for hot flash which comprises a nonpeptidic compound having gonadotropin releasing hormone antagonistic activity, wherein said compound is capable of entering the brain.
摘要翻译：本发明旨在提供一种包含具有促性腺激素释放激素拮抗活性的非肽类化合物，特别是包含具有促性腺激素释放激素拮抗活性的非肽类化合物的预防或治疗热闪光的预防或治疗剂的热闪光防治剂，其中所述化合物能够进入大脑。

37. 发明授权

US6136781A LH-RH receptor antagonists 失效
标题翻译： LH-RH受体拮抗剂
公开(公告)号：US6136781A
公开(公告)日：2000-10-24
申请号：US656244
申请日：1996-06-06
申请人： Chieko Kitada , Shuichi Furuya , Koichi Kato
发明人： Chieko Kitada , Shuichi Furuya , Koichi Kato
IPC分类号： A61K38/00 , C07K7/23 , C07K7/64 , A61K38/12
CPC分类号： C07K7/64 , C07K7/23 , A61K38/00 , Y10S424/813 , Y10S424/814
摘要： The LH-RH receptor antagonists containing cyclic pentapeptides or salts thereof and novel cyclic pentapeptide or salts thereof are provided.The LH-RH receptor antagonists of the present invention are effective as medicines for preventing and curing sex hormone-dependent cancers (e.g., prostatic cancer, uterine cancer, mammary cancer, pituitary tumor, etc.), prostatomegaly, endometriosis, hysteromyoma, puberty precox, amenorrheal syndromes, multilocular ovarian syndromes, comedo, etc. and are also effective as pregnancy controlling agents (e.g., contraceptives, etc.) and menstrual cycle controlling agents. Moreover, these are also useful in the livestock industry for the control of the estrus of animals and also for the improvement in the quality of meat and for the control of the growth of animals, as well as in the marine products industry as spawning promoters for fishes.
摘要翻译： PCT No.PCT / JP96 / 01140 Sec。 371日期：1996年6月6日 102（e）日期1996年6月6日PCT 1996年4月25日PCT公布。公开号WO96 / 34012PC。日期1996年10月31日提供含有环状五肽或其盐的新型环状五肽或其盐的LH-RH受体拮抗剂。本发明的LH-RH受体拮抗剂作为用于预防和治疗性激素依赖性癌症（例如前列腺癌，子宫癌，乳腺癌，垂体瘤等），前列腺肥大，子宫内膜异位症，子宫肌瘤，青春期precox的药物是有效的，闭经综合征，多腔卵巢综合征，喜剧等，并且作为妊娠控制剂（例如避孕药等）和月经周期控制剂也是有效的。此外，这些也可用于畜牧业控制动物发情，以及提高肉类质量和控制动物生长，以及在海产品产业中作为产卵促进剂鱼

38. 发明授权

US6004954A Condensed thiazine derivatives, their production and use thereof 失效
标题翻译：缩合噻嗪衍生物，其生产和使用
公开(公告)号：US6004954A
公开(公告)日：1999-12-21
申请号：US813986
申请日：1997-03-10
申请人： Shuichi Furuya , Seiichi Tanida , Yoshikazu Ohta
发明人： Shuichi Furuya , Seiichi Tanida , Yoshikazu Ohta
IPC分类号： C07D513/04 , A61K31/54
CPC分类号： C07D513/04
摘要： This invention relates to a compound of the following formula or a salt thereof, their production and use. ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen, a group bonding through a carbon atom, a group bonding through a nitrogen atom, a group bonding through an oxygen atom, or a group bonding through a sulfur atom; R.sup.3 represents hydrogen, halogen, a group bonding through a carbon atom, a group bonding through a nitrogen atom, a group bonding through an oxygen atom, or a group bonding through a sulfur atom; W represents an oxygen atom or sulfur atom; A represents a group forming a nitrogen-containing condensed ring at the 3,4- of a 1,4-thiazine ring; R.sup.1 and R.sup.2 may be combined to form a bivalent hydrocarbon group interrupted by one or more hetero atoms or an alkylene group. The above compound or a salt thereof not only has Th1 and Th2 cell function modulating activity but has splenocyte proliferation response, interleukin-5 production, and interferon-gamma production inhibitory activity and finds application as an effective therapeutic and/or prophylactic agent for allergic or autoimmune diseases or as an effective therapeutic and/or prophylactic agent for graft rejection or graft-vs-host disease.
摘要翻译：本发明涉及下式的化合物或其盐，其制备和用途。其中R1和R2独立地表示氢，通过碳原子键合的基团，通过氮原子键合的基团，通过氧原子键合的基团，或通过硫原子键合的基团; R3表示氢，卤素，通过碳原子键合的基团，通过氮原子键合的基团，通过氧原子键合的基团，或通过硫原子键合的基团; W表示氧原子或硫原子; A表示在1,4-噻嗪环的3,4-中形成含氮缩合环的基团; R1和R2可以组合形成被一个或多个杂原子或亚烷基间隔的二价烃基。上述化合物或其盐不仅具有Th1和Th2细胞功能调节活性，而且具有脾细胞增殖反应，白细胞介素-5产生和干扰素-γ产生抑制活性，并且被用作有效的治疗和/或预防药物用于过敏或自身免疫疾病或作为移植排斥或移植物抗宿主病的有效治疗和/或预防剂。

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