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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

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。

3. 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。

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

US06194419B1 Nitrogen-containing heterocyclic compounds, their production and use 失效
标题翻译：含氮杂环化合物，其生产和使用
公开(公告)号：US06194419B1
公开(公告)日：2001-02-27
申请号：US09147616
申请日：1999-02-02
申请人： Shuichi Furuya , Toshihiro Imaeda , Satoshi Sasaki
发明人： Shuichi Furuya , Toshihiro Imaeda , Satoshi Sasaki
IPC分类号： A61K31519
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。

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. 发明申请

US20090169610A1 Liposome Preparation 审中-公开
标题翻译：脂质体制备
公开(公告)号：US20090169610A1
公开(公告)日：2009-07-02
申请号：US12223517
申请日：2007-02-02
申请人： Noboru Yamazaki , Sei Yoshida , Masuo Yamaoka , Akira Hori , Shigeya Kakimoto , Shuichi Furuya
发明人： Noboru Yamazaki , Sei Yoshida , Masuo Yamaoka , Akira Hori , Shigeya Kakimoto , Shuichi Furuya
IPC分类号： A61K9/127 , A61K39/395
CPC分类号： A61K9/1271 , A61K9/1272 , A61K31/282 , A61K31/337 , A61K31/513 , A61K31/537 , A61K31/573 , A61K31/7068 , A61K47/6911
摘要： The present invention provides cancer treatment preparations of excellent targetability. The sugar chain-modified liposomes of the present invention, which contain an aromatase inhibitor, anti-androgenic agent, lyase inhibitor, GnRH agonist, GnRH antagonist, anti-angiogenic agent, tyrosine kinase inhibitor, serine-threonine kinase inhibitor, antibody having an anticancer activity, ansamitocin, capecitabine, celmoleukin, docetaxel hydrate, gemcitabine hydrochloride, oxaliplatin, prednisolone, tegafur-uracil mixtures, zinostatin stimalamer or arsenic trioxide may be used as cancer treatment preparations having an excellent targetability.
摘要翻译：本发明提供了具有优异目标性的癌症治疗制剂。含有芳香酶抑制剂，抗雄激素剂，裂解酶抑制剂，GnRH激动剂，GnRH拮抗剂，抗血管生成剂，酪氨酸激酶抑制剂，丝氨酸 - 苏氨酸激酶抑制剂，抗癌剂的本发明糖链修饰脂质体活性，安曲霉素，卡培他滨，纤维白蛋白，多西紫杉醇水合物，盐酸吉西他滨，奥沙利铂，泼尼松龙，替加氟 - 尿嘧啶混合物，维生素D抑制素或三氧化二砷可用作具有优异靶向性的癌症治疗制剂。

8. 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。

9. 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。

10. 发明授权

US4873127A Method of making heat transfer tube 失效
标题翻译：制作传热管的方法
公开(公告)号：US4873127A
公开(公告)日：1989-10-10
申请号：US211084
申请日：1988-06-21
申请人： Kagetoshi Onodera , Tatsuya Koizumi , Toshiyuki Kato , Junji Sotani , Masauki Momo , Shuichi Furuya
发明人： Kagetoshi Onodera , Tatsuya Koizumi , Toshiyuki Kato , Junji Sotani , Masauki Momo , Shuichi Furuya
IPC分类号： B23K1/00 , F28F21/08
CPC分类号： F28F21/085 , B23K1/0012 , F28F21/082
摘要： A heat transfer tube comprising an inner tube formed of copper or steel, an intermediate layer having a uniform thickness, mounted on the outer periphery of the inner tube and formed of a low melting point metal such as solder, tin or lead and an outer tube of lead or lead alloy mounted on the intermediate layer on the inner tube and metallurgically bonded with the intermediate layer when the low melting point metal is melted.
摘要翻译：一种传热管，包括由铜或钢形成的内管，具有均匀厚度的中间层，安装在内管的外周上，由诸如焊料，锡或铅的低熔点金属形成，外管的铅或铅合金安装在内管的中间层上，并在低熔点金属熔化时与中间层冶金结合。

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