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1. 发明授权

US06297379B1 Thienopyrimidine compounds, their production and use 失效
标题翻译：噻吩并嘧啶化合物，其生产和使用
公开(公告)号：US06297379B1
公开(公告)日：2001-10-02
申请号：US09530495
申请日：2000-04-26
申请人： Shuichi Furuya , Nobuhiro Suzuki , Nobuo Choh , Yoshi Nara
发明人： Shuichi Furuya , Nobuhiro Suzuki , Nobuo Choh , Yoshi Nara
IPC分类号： C07D49504
CPC分类号： C07D495/04
摘要： A compound of formula (I) wherein R1 and R2 each is hydrogen, hydroxy, C1-4 alkoxy, C1-4 alkoxy-carbonyl or C1-4 alkyl which may be substituted; R3 is hydrogen, halogen, hydroxy or C1-4 alkoxy which may be substituted; or adjacent two R3 may form C1-4 alkylenedioxy; R4 is hydrogen or C1-4 alkyl; R6 is C1-4 alkyl which may be substituted or a group of the formula (A) wherein R5 is hydrogen of R4 and R5 may form heterocycle; and n is 0-5, or a salt thereof, has an excellent GnRH-antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases.
摘要翻译：其中R 1和R 2各自为氢，羟基，C 1-4烷氧基，C 1-4烷氧基 - 羰基或可被取代的C 1-4烷基的式（I）化合物; R3是氢，卤素，羟基或可被取代的C1-4烷氧基; 或相邻的两个R 3可以形成C 1-4亚烷基二氧基; R4是氢或C1-4烷基; R 6是可以被取代的C 1-4烷基或式（A）的基团，其中R 5是氢的R 4和R 5可以形成杂环; n为0-5或其盐具有优异的GnRH拮抗活性，可用于预防或治疗性激素依赖性疾病。

2. 发明授权

US06340686B1 Thienopyrimidine compounds, their production and use 有权
标题翻译：噻吩并嘧啶化合物，其生产和使用
公开(公告)号：US06340686B1
公开(公告)日：2002-01-22
申请号：US09571215
申请日：2000-05-16
申请人： Shuichi Furuya , Nobuhiro Suzuki , Nobuo Choh , Yoshi Nara
发明人： Shuichi Furuya , Nobuhiro Suzuki , Nobuo Choh , Yoshi Nara
IPC分类号： A61K31519
CPC分类号： C07D495/04
摘要： A compound of the formula: wherein R1 and R2 each is hydrogen, hydroxy, C1-4 alkoxy, C1-4 alkoxy-carbonyl or C1-4 alkyl which may be substituted; R3 is hydrogen, halogen, hydroxy or C1-4 alkoxy which may be substituted; or adjacent two R3 may form C1-4 alkylenedioxy; R4 is hydrogen or C1-4 alkyl; R6 is C1-4 alkyl which may be substituted or a group of the formula: wherein R5 is hydrogen or R4 and R5 may form heterocycle; and n is 0-5, or a salt thereof, has an excellent GnRH-antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases.
摘要翻译：下式化合物：其中R 1和R 2各自为氢，羟基，C 1-4烷氧基，C 1-4烷氧羰基或可被取代的C 1-4烷基; R3是氢，卤素，羟基或可被取代的C1-4烷氧基; 或相邻的两个R 3可以形成C 1-4亚烷基二氧基; R4是氢或C1-4烷基; R6是可以被取代的C1-4烷基或下式的基团：其中R5是氢或R4和R5可以形成杂环; 并且n为0-5或其盐具有优异的GnRH拮抗活性，并且可用于预防或治疗性激素依赖性疾病。

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

US6048863A Condensed-ring thiophene derivatives and thienopyrimidine derivatives, their production and use 失效
标题翻译：缩环噻吩衍生物和噻吩并嘧啶衍生物，其生产和使用
公开(公告)号：US6048863A
公开(公告)日：2000-04-11
申请号：US682442
申请日：1996-07-17
申请人： Shuichi Furuya , Nobuo Choh , Koichi Kato , Shuji Hinuma
发明人： Shuichi Furuya , Nobuo Choh , Koichi Kato , Shuji Hinuma
IPC分类号： A61K31/505 , C07D495/04
CPC分类号： C07D495/04
摘要： Thienopyrimidine derivatives of formula: ##STR1## The present thienopyrimidine derivatives are useful for treating mammals suffering from disorders related to gonadotropin realeasing hormone (GnRH).
摘要翻译：噻吩并嘧啶衍生物：本发明的噻吩并嘧啶衍生物可用于治疗患有与促性腺激素释放激素（GnRH）相关的疾病的哺乳动物。

7. 发明授权

US5807869A Quinoline derivatives, their production and use 失效
标题翻译：喹啉衍生物，其生产和使用
公开(公告)号：US5807869A
公开(公告)日：1998-09-15
申请号：US779609
申请日：1997-01-07
申请人： Shuichi Furuya , Nobuo Choh , Satoshi Sasaki
发明人： Shuichi Furuya , Nobuo Choh , Satoshi Sasaki
IPC分类号： C07D215/56 , A61K31/47
CPC分类号： C07D215/56
摘要： The present quinoline derivatives and compositions having gonadotropin-releasing hormone antagonistic activity are useful as propylactics or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, uterine or cervical cancer, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, polycystic ovary syndrome and acne vulgaris; are effective as a fertility controlling agent in both sexes (e.g. a pregnancy controlling agent and a menstrual cycle controlling agent); can be used as a male or female contraceptive, as an ovulation-inducing agent; can be used as an infertility treating agent by using a rebound effect owing to a stoppage of administration thereof; and are useful for modulating estrous cycles in animals in the field of animal husbandry, as agents for improving the quality of edible meat or promoting the growth of animals, and as agents for promoting spawning in fish.
摘要翻译：本发明的喹诺酮衍生物和具有促性腺激素释放激素拮抗作用的组合物可用作预防或治疗若干激素依赖性疾病，例如性激素依赖性癌症（例如前列腺癌，子宫颈癌或宫颈癌，乳腺癌）的丙型或治疗剂癌症，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）有效; 可用作男性或女性避孕药，作为排卵诱导剂; 可以通过使用由于其施用停止而产生的反弹效应而用作不育处理剂; 可用于调节畜牧业动物的发情周期，作为改善食用肉质量或促进动物生长的药剂，以及用于促进鱼类产卵的药剂。

8. 发明授权

US06514988B1 Condensed-ring thiophene derivatives, their production and use 失效
标题翻译：缩环噻吩衍生物，其生产和使用
公开(公告)号：US06514988B1
公开(公告)日：2003-02-04
申请号：US09672777
申请日：2000-09-29
申请人： Shuichi Furuya , Nobuo Choh , Koichi Kato , Shuji Hinuma
发明人： Shuichi Furuya , Nobuo Choh , Koichi Kato , Shuji Hinuma
IPC分类号： A61K31437
CPC分类号： C07D495/04
摘要： A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or hetero 5 to 7 membered ring is effective as a propylactic or therapeutic agent 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, pplycystic 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); can be used as a contraceptive of male or female, as an ovulation-inducing agent of female; can be used 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 fro 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：促性腺激素释放激素拮抗组合物，其包含任选取代的稠合双环化合物，其由同质或杂的5至7元环和同质或异构的5至7元环组成，作为用于预防或治疗几种激素依赖性疾病，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，经前综合征，囊性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; 可作为男性或女性的避孕方法，作为女性的排卵诱导剂; 可以通过使用由于其施用停止而产生的反弹效应而用作不育处理剂; 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。

9. 发明授权

US5817819A Condensed-ring thiophene derivatives, their production and use 失效
标题翻译：缩环噻吩衍生物，其生产和使用
公开(公告)号：US5817819A
公开(公告)日：1998-10-06
申请号：US454304
申请日：1995-06-16
申请人： Shuichi Furuya , Nobuo Choh , Koichi Kato , Shuji Hinuma
发明人： Shuichi Furuya , Nobuo Choh , Koichi Kato , Shuji Hinuma
IPC分类号： A61K31/38 , A61K31/44 , A61K31/505 , A61K31/55 , A61P5/04 , C07D495/04
CPC分类号： C07D495/04
摘要： A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or hetero 5 to 7 membered ring is effective as a propylactic or therapeutic agent 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); can be used as a contraceptive of male or female, as an ovulation-inducing agent of female; can be used 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 fro 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 / JP95 / 00728 Sec。 371日期：1995年6月16日 102（e）日期1995年6月16日PCT提交1995年4月14日PCT公布。出版物WO95 / 28405 日期1995年10月26日发明促性腺激素释放激素拮抗组合物，其包含任选取代的稠合双环化合物，其由同质或杂的5至7元环和同质或异构的5至7元环组成，作为丙基或治疗用于预防或治疗几种激素依赖性疾病的药剂，例如性激素依赖性癌症（例如前列腺癌，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，早熟青春期，闭经，经前综合征，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; 可作为男性或女性的避孕方法，作为女性的排卵诱导剂; 可以通过使用由于其施用停止而产生的反弹效应而用作不育处理剂; 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。

10. 发明授权

US6087503A Quinoline derivatives, their production and use 失效
标题翻译：喹啉衍生物，其生产和使用
公开(公告)号：US6087503A
公开(公告)日：2000-07-11
申请号：US152514
申请日：1998-09-14
申请人： Shuichi Furuya , Nobuo Choh , Satoshi Sasaki
发明人： Shuichi Furuya , Nobuo Choh , Satoshi Sasaki
IPC分类号： C07D215/56
CPC分类号： C07D215/56
摘要： The present compounds are intermediates for the preparation of quinoline derivatives and compositions having gonadotropin-releasing hormone antagonistic activity useful as propylactics or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, uterine or cervical cancer, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, polycystic ovary syndrome and acne vulgaris; are effective as a fertility controlling agent in both sexes (e.g. a pregnancy controlling agent and a menstrual cycle controlling agent); can be used as a male or female contraceptive, as an ovulation-inducing agent; can be used as an infertility treating agent by using a rebound effect owing to a stoppage of administration thereof; and are useful for modulating estrous cycles in animals in the field of animal husbandry, as agents for improving the quality of edible meat or promoting the growth of animals, and as agents for promoting spawning in fish.
摘要翻译：本发明化合物是用于制备喹啉衍生物的中间体和具有促性腺激素释放激素拮抗活性的组合物，其用作预防或治疗若干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）有效; 可用作男性或女性避孕药，作为排卵诱导剂; 可以通过使用由于其施用停止而产生的反弹效应而用作不育处理剂; 可用于调节畜牧业动物的发情周期，作为改善食用肉质量或促进动物生长的药剂，以及用于促进鱼类产卵的药剂。

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