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1. 发明申请

US20050222174A1 Thienopyrimidines, process for preparing the same and use thereof 有权
标题翻译：噻吩并嘧啶，其制备方法及其用途
公开(公告)号：US20050222174A1
公开(公告)日：2005-10-06
申请号：US10502903
申请日：2003-01-29
申请人： Shuichi Furuya , Takashi Imada , Takenori Hitaka , Kazuhiro Miwa , Masami Kusaka , Nobuhiro Suzuki
发明人： Shuichi Furuya , Takashi Imada , Takenori Hitaka , Kazuhiro Miwa , Masami Kusaka , Nobuhiro Suzuki
IPC分类号： A61P5/08 , A61P5/24 , A61P13/08 , A61P15/00 , A61P15/08 , A61P17/10 , A61P17/14 , A61P25/28 , A61P35/00 , A61P35/04 , A61P43/00 , C07D495/04 , A61K31/519 , C07D498/02
CPC分类号： C07D495/04
摘要： The present invention provides a thienopyrimidine compound, represented by the formula [wherein, R1 is C1-4 alkyl, R2 is (1) phenyl optionally having a substituent such as amino, mono C1-4 alkylamino and di C1-4 alkylamino, or (2) a heterocyclic group optionally having a substituent such as amino, mono C1-4 alkylamino and di C1-4 alkylamino and the like, R3 is a hydrogen atom or C1-4 alkyl, R4 is C1-4 alkyl optionally having a substituent such as C1-4 alkoxy-carbonyl, carboxyl, mono C1-4 alkylamino and N—C1-4 alkyl-N—C7-10 aralkylamino and the like] or a salt thereof, which has antagonistic action for gonadotropin-releasing hormone.
摘要翻译：本发明提供由式[其中R 1为C 1-4烷基，R 2为（1）表示的噻吩并嘧啶化合物为（1 ）任选具有取代基的苯基，例如氨基，单C 1-4烷基氨基和二-C 1-4烷基氨基，或（2）任选具有取代基的杂环基作为氨基，单C 1-4烷基氨基和二C 1-4烷基氨基等，R 3是氢原子或C < C 1-4烷基，R 4是任选具有取代基的C 1-4烷基，例如C 1-4烷基，烷氧基羰基，羧基，单C 1-4烷基氨基和NC 1-4烷基-NC 7-10芳烷基氨基等]或其盐对促性腺激素释放激素具有拮抗作用。

2. 发明授权

US07569570B2 Thienopyrimidines, process for preparing the same and use thereof 有权
标题翻译：噻吩并嘧啶，其制备方法及其用途
公开(公告)号：US07569570B2
公开(公告)日：2009-08-04
申请号：US10502903
申请日：2003-01-29
申请人： Shuichi Furuya , Takashi Imada , Takenori Hitaka , Kazuhiro Miwa , Masami Kusaka , Nobuhiro Suzuki
发明人： Shuichi Furuya , Takashi Imada , Takenori Hitaka , Kazuhiro Miwa , Masami Kusaka , Nobuhiro Suzuki
IPC分类号： A61K31/519 , C07D495/04
CPC分类号： C07D495/04
摘要： The present invention provides a thienopyrimidine compound, represented by the formula [wherein, R1 is C1-4 alkyl, R2 is (1) phenyl optionally having a substituent such as amino, mono C1-4 alkylamino and di C1-4 alkylamino, or (2) a heterocyclic group optionally having a substituent such as amino, mono C1-4 alkylamino and di C1-4 alkylamino and the like, R3 is a hydrogen atom or C1-4 alkyl, R4 is C1-4 alkyl optionally having a substituent such as C1-4 alkoxy-carbonyl, carboxyl, mono C1-4 alkylamino and N—C1-4 alkyl-N—C7-10 aralkylamino and the like] or a salt thereof, which has antagonistic action for gonadotropin-releasing hormone.
摘要翻译：本发明提供由式[其中，R 1为C 1-4烷基，R 2为（1）任选具有取代基的苯基，例如氨基，单C 1-4烷基氨基和二C 1-4烷基氨基的噻吩并嘧啶化合物或（ 2）任选具有取代基的杂环基，例如氨基，单C 1-4烷基氨基和二C 1-4烷基氨基等，R 3是氢原子或C 1-4烷基，R 4是任选具有取代基的C 1-4烷基作为对促性腺激素释放激素具有拮抗作用的C 1-4烷氧基 - 羰基，羧基，单C 1-4烷基氨基和N-C 1-4烷基-N C 7-10芳烷基氨基等]或其盐。

3. 发明授权

US06329388B2 Thienopyridine compounds, their production and use 失效
标题翻译：噻吩并吡啶化合物，其生产和使用
公开(公告)号：US06329388B2
公开(公告)日：2001-12-11
申请号：US09736641
申请日：2000-12-14
申请人： Shuichi Furuya , Nobuo Choh , Nobuhiro Suzuki , Takashi Imada
发明人： Shuichi Furuya , Nobuo Choh , Nobuhiro Suzuki , Takashi Imada
IPC分类号： A61K31435
CPC分类号： C07D495/04
摘要： The compounds of the present invention possess excellent gonadotropin-releasing hormone antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases, e.g., sex hormone-dependent cancers (e.g., prostatic cancer, uterine cancer, breast cancer, pituitary tumor), prostatic hypertrophy, hysteromyoma, endometriosis, precocious puberty, amenorrhea syndrome, multilocular ovary syndrome, pimples etc, or as a pregnancy regulator (e.g., contraceptive), infertility remedy or menstruation regulator.
摘要翻译：本发明的化合物具有优异的促性腺激素释放激素拮抗活性，并且可用于预防或治疗性激素依赖性疾病，例如性激素依赖性癌症（例如前列腺癌，子宫癌，乳腺癌，垂体瘤），前列腺肥大，子宫肌瘤，子宫内膜异位症，早熟青春期，闭经综合征，多腔卵巢综合征，丘疹等，或作为妊娠调节剂（如避孕药），不育补救或月经调节剂。

4. 发明授权

US06262267B1 Thienopyridine compound 失效
标题翻译：噻吩并吡啶化合物
公开(公告)号：US06262267B1
公开(公告)日：2001-07-17
申请号：US09402206
申请日：1999-09-30
申请人： Shuichi Furuya , Nobuo Choh , Nobuhiro Suzuki , Takashi Imada
发明人： Shuichi Furuya , Nobuo Choh , Nobuhiro Suzuki , Takashi Imada
IPC分类号： C07D47104
CPC分类号： C07D495/04
摘要： The compound of the present invention possesses excellent gonadotropin-releasing hormone antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases, e,g., sex hormone-dependent cancers (e.g., prostatic cancer, uterine cancer, breast cancer, pituitary tumor), prostatic hypertrophy, hysteromyoma, endometriosis, precocious puberty, amenorrhea sydrome, multilocular ovary sydrome, pimples etc, or as a pregnancy regulator (e.g., contraceptive), infertility remedy or menstruation regulator.
摘要翻译：本发明的化合物具有优异的促性腺激素释放激素拮抗活性，并且可用于预防或治疗性激素依赖性疾病，例如性激素依赖性癌症（例如，前列腺癌，子宫癌，乳腺癌，垂体肿瘤），前列腺肥大，子宫肌瘤，子宫内膜异位症，早熟青春期，闭经症状，多腔卵巢综合征，丘疹等，或作为妊娠调节者（如避孕药），不育补救或月经调节剂。

5. 发明授权

US06297255B1 Thienopyridine compounds, their production and use 失效
标题翻译：噻吩并吡啶化合物，其生产和使用
公开(公告)号：US06297255B1
公开(公告)日：2001-10-02
申请号：US09420358
申请日：1999-10-18
申请人： Shuichi Furuya , Nobuo Choh , Nobuhiro Suzuki , Takashi Imada
发明人： Shuichi Furuya , Nobuo Choh , Nobuhiro Suzuki , Takashi Imada
IPC分类号： A61K31435
CPC分类号： C07D495/04
摘要： The compound of the present invention possesses excellent gonadotropin-releasing hormone antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases, e.g., sex hormone-dependent cancers (e.g., prostatic cancer, uterine cancer, breast cancer, pituitary tumor), prostatic hypertrophy, hysteromyoma, endometriosis, precocious puberty, amenorrhea syndrome, multilocular ovary syndrome, pimples etc. or as a pregnancy regulator (e.g., contraceptive), infertility remedy or menstruation regulator.
摘要翻译：本发明的化合物具有优异的促性腺激素释放激素拮抗活性，并且可用于预防或治疗性激素依赖性疾病，例如性激素依赖性癌症（例如前列腺癌，子宫癌，乳腺癌，垂体瘤），前列腺肥大，子宫肌瘤，子宫内膜异位症，早熟青春期，闭经综合征，多腔卵巢综合征，丘疹等，或作为妊娠调节者（如避孕药），不育补救或月经调节剂。

6. 发明授权

US06001850A Thienopyridine derivatives, their production and use 失效
标题翻译：噻吩并吡啶衍生物，其生产和使用
公开(公告)号：US06001850A
公开(公告)日：1999-12-14
申请号：US894318
申请日：1997-08-14
申请人： Shuichi Furuya , Hirokazu Matsumoto , Yoji Hayase , Nobuhiro Suzuki , Takashi Imada
发明人： Shuichi Furuya , Hirokazu Matsumoto , Yoji Hayase , Nobuhiro Suzuki , Takashi Imada
IPC分类号： C07D495/04 , A61K31/435
CPC分类号： C07D495/04
摘要： The present thienopyridine derivatives and composition having gonadotropin-releasing hormone antagonistic activity are useful as prophylactic or therapeutic agents for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, cancer of uterine cervix, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, polycystic ovary syndrome and acne vulgaris; is effective as a fertility controlling agent in both sexes (e.g. a pregnancy controlling agent and a menstrual cycle controlling agent); is useful as a contraceptive of male or female, as an ovulation-inducing agent of female; is useful as an infertility treating agent by using a rebound effect owing to a stoppage of administration thereof; is useful as modulating estrous cycles in animals in the field of animal husbandry, as an agent for improving the quality of edible meat or promoting the growth of animals; is useful as an agent of spawning promotion in fish.
摘要翻译： PCT No.PCT / JP97 / 01434 371日期1997年8月14日 102（e）日期1997年8月14日PCT 1997年4月24日PCT PCT。出版物WO97 / 41126 日期1997年11月6日目前具有促性腺激素释放激素拮抗活性的噻吩并吡啶衍生物和组合物可用作预防或治疗若干激素依赖性疾病的预防或治疗剂，例如性激素依赖性癌症（例如前列腺癌，癌症子宫颈癌，乳腺癌，垂体腺瘤），良性前列腺肥大，子宫肌瘤，子宫内膜异位症，早熟性青春期，闭经，经前期综合征，多囊卵巢综合征和寻常型痤疮; 作为两性生育调节剂（例如妊娠控制剂和月经周期控制剂）是有效的; 作为女性的排卵诱导剂作为男性或女性的避孕药具是有用的; 作为不孕症治疗剂，由于其施用停止而使用反弹效应是有用的; 可用作调整动物饲养领域的发情周期，作为提高食用肉质量或促进动物生长的药剂; 作为鱼类产卵促销的代理人是有用的。

7. 发明申请

US20050101657A1 Androgen receptor antagonists 审中-公开
标题翻译：雄激素受体拮抗剂
公开(公告)号：US20050101657A1
公开(公告)日：2005-05-12
申请号：US10499300
申请日：2002-12-26
申请人： Shuichi Furuya , Nobuyuki Matsunaga , Masami Kusaka , Takahito Hara , Junichi Miyazaki
发明人： Shuichi Furuya , Nobuyuki Matsunaga , Masami Kusaka , Takahito Hara , Junichi Miyazaki
IPC分类号： A61K31/00 , A61K31/40 , A61K45/06 , A61P13/08 , A61P35/00 , A61P43/00 , C07D207/32 , C07D207/333 , C07D207/337 , C07D207/34 , C07D207/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/06 , A61K31/401 , A61K31/4015 , A61K31/4025
CPC分类号： C07D207/333 , A61K9/0019 , A61K9/08 , A61K9/2018 , A61K31/00 , A61K31/40 , A61K45/06 , C07D207/32 , C07D207/337 , C07D207/34 , C07D207/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/06 , A61K2300/00
摘要： The present invention provides an androgen receptor antagonistic agent and a superior prophylactic or therapeutic agent for hormone-sensitive cancer, which contain a compound of the formula: wherein, R1 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom, R2 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom, R3 is a hydrogen atom, a hydrocarbon group which may have substituent(s), an acyl group or a heterocyclic group which may have substituent(s), R4 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom, and R5 is a cyclic group which may have substituent(s); or a salt thereof, or its prodrug.
摘要翻译：本发明提供了一种雄激素受体拮抗剂和用于激素敏感性癌症的优异的预防或治疗剂，其含有下式化合物：其中R 1是氢原子，通过碳原子，通过氮原子结合的基团，通过氧原子结合的基团或通过硫原子结合的基团，R 2是氢原子，通过碳原子键合的基团，通过氮原子结合的基团，通过氧原子结合的基团或通过硫原子结合的基团，R 3是氢原子，可以具有取代基的烃基，可以具有取代基的烃基，酰基或可具有取代基的杂环基，R 4是氢原子，通过碳原子结合的基团，通过氮原子结合的基团，通过氧结合的基团原子或通过硫原子结合的基团，R 5是可以具有取代基的环状基团 t（s）; 或其盐，或其前药。

8. 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。

9. 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。

10. 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。

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