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公开(公告)号：US5026835A
公开(公告)日：1991-06-25
申请号：US447512
申请日：1989-12-07
申请人： Tohru Ueda , Takuma Sasaki , Akira Matsuda , Takanori Miyashita , Shinji Sakata , Keiji Yamagami , Akihiro Fujii
发明人： Tohru Ueda , Takuma Sasaki , Akira Matsuda , Takanori Miyashita , Shinji Sakata , Keiji Yamagami , Akihiro Fujii
IPC分类号： C07H19/06
CPC分类号： C07H19/06
摘要： Pyrimidine 2'-deoxy-2'-methylidene nucleoside compounds: ##STR1## wherein R.sup.1 represents amino, hydroxy, silylamino, silyloxy, acylamino or acyloxy; R.sup.2 represents hydrogen, halogen, a lower alkyl, a lower alkenyl, a lower alkynyl or haloalkyl; R.sup.3 and R.sup.4 represent the same or different hydrogen, silyl, acyl or aminoacyl, or a pharmaceutically acceptable salt or hydrate thereof, except that R.sup.1 is amino or hydroxy, and both of R.sup.3 and R.sup.4 are hydrogen.Said compounds possess excellent antitumor and antiviral activities, thus providing novel anticancer and antiviral agent.
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公开(公告)号：US5705630A
公开(公告)日：1998-01-06
申请号：US818656
申请日：1992-01-07
申请人： Tohru Ueda , Takuma Sasaki , Akira Matsuda , Keiji Yamagami , Akihiro Fujii
发明人： Tohru Ueda , Takuma Sasaki , Akira Matsuda , Keiji Yamagami , Akihiro Fujii
IPC分类号： C07H19/06 , C07H19/10 , C07H19/073
摘要： 2'-Methylidenepyrimidine nucleoside compounds of the general formula: ##STR1## wherein R.sup.1 stands for amino or hydroxy group; R.sup.2 stands for a halogen or a lower alkyl when R.sup.1 is amino or R.sup.2 stands for an alkyl having 2 to 4 carbon atoms, an alkynyl having 2 to 4 carbon atoms or a haloalkyl when R.sup.1 is hydroxy group; and R.sup.3 stands for hydrogen or a phosphoric acid residue, or salts thereof, anticancer compositions containing one or more of these compounds and methods for production of these compounds. Said compounds and salts thereof exhibit noticeable antitumor activities and are useful as anticancer agents.
摘要翻译： 2'-亚甲基嘧啶核苷化合物，其通式如下：其中R1代表氨基或羟基; 当R 1为氨基或R 2表示具有2至4个碳原子的烷基，具有2至4个碳原子的炔基或R 1为羟基时的卤代烷基时，R 2表示卤素或低级烷基; R3表示氢或磷酸残基或其盐，含有这些化合物中的一种或多种的抗癌组合物及其制备方法。 所述化合物及其盐具有显着的抗肿瘤活性，可用作抗癌剂。
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3.发明授权2'methylidenepyrimidine nucleoside compounds, their use and method for production thereof 失效二亚甲基嘧啶核苷化合物，其用途及其制备方法
公开(公告)号：US5401726A
公开(公告)日：1995-03-28
申请号：US44039
申请日：1993-04-08
申请人： Tohru Ueda , Takuma Sasaki , Akira Matsuda , Keiji Yamagami , Akihiro Fujii
发明人： Tohru Ueda , Takuma Sasaki , Akira Matsuda , Keiji Yamagami , Akihiro Fujii
摘要： 2'-Methylidenepyrimidine nucleoside compounds of the general formula: ##STR1## wherein R.sup.1 stands for amino or hydroxy group; R.sup.2 stands for a halogen or a lower alkyl when R.sup.1 is amino or R.sup.2 stands for an alkyl having 2 to 4 carbon atoms, an alkynyl having 2 to 4 carbon atoms or a haloalkyl when R.sup.1 is hydroxy group; and R.sup.3 stands for hydrogen or a phosphoric acid residue, or salts thereof, compositions containing one or more of these compounds and methods for production of these compounds are disclosed.Said compounds and salts thereof exhibit noticeable antitumor activities.
摘要翻译： 2'-亚甲基嘧啶核苷化合物，其通式如下：其中R1代表氨基或羟基; 当R 1为氨基或R 2表示具有2至4个碳原子的烷基，具有2至4个碳原子的炔基或R 1为羟基时的卤代烷基时，R 2表示卤素或低级烷基; R3代表氢或磷酸残基，或其盐，含有这些化合物中的一种或多种的组合物和这些化合物的制备方法。 所述化合物及其盐具有显着的抗肿瘤活性。
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公开(公告)号：US06451825B1
公开(公告)日：2002-09-17
申请号：US09791648
申请日：2001-02-26
IPC分类号： A61K31445
CPC分类号： A61K45/00 , A61K31/00 , A61K31/437 , A61K31/4409 , A61K31/4545 , A61K31/496 , A61K31/551
摘要： A Rho kinase inhibitor is provided as a novel pharmaceutical agent, particularly as a therapeutic agent of hypertension, a therapeutic agent of angina pectoris, a suppressive agent of cerebrovascular contraction, a therapeutic agent of asthma, a therapeutic agent of peripheral circulation disorder, a prophylactic agent of immature birth, a therapeutic agent of arteriosclerosis, an anti-cancer drug, an anti-inflammatory agent, an immunosuppressant, a therapeutic agent of autoimmune disease, an anti-AIDS drug, a contraceptive, a prophylactic agent of digestive tract infection, a therapeutic agent of osteoporosis, a therapeutic agent of retinopathy and a brain function improving drug. In addition, the Rho kinase inhibitor is provided as a reagent and a diagnostic.
摘要翻译： 提供Rho激酶抑制剂作为新型药剂，特别是高血压治疗剂，心绞痛治疗剂，脑血管收缩抑制剂，哮喘治疗剂，外周循环障碍治疗剂，预防性药物 不成熟的药剂，动脉硬化治疗剂，抗癌药，抗炎剂，免疫抑制剂，自身免疫性疾病的治疗剂，抗艾滋病药，避孕药，消化道感染的预防剂， 骨质疏松症治疗剂，视网膜病变治疗剂和脑功能改善药物。 另外，提供Rho激酶抑制剂作为试剂和诊断。
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公开(公告)号：US06906061B2
公开(公告)日：2005-06-14
申请号：US10208100
申请日：2002-07-31
IPC分类号： A61K31/16 , A61K31/00 , A61K31/437 , A61K31/4409 , A61K31/4545 , A61K31/496 , A61K31/551 , A61K45/00 , G01N33/48 , A61K31/47 , C07D401/12
CPC分类号： A61K45/00 , A61K31/00 , A61K31/437 , A61K31/4409 , A61K31/4545 , A61K31/496 , A61K31/551
摘要： A Rho kinase inhibitor is provided as a novel pharmaceutical agent, particularly as a therapeutic agent of hypertension, a therapeutic agent of angina pectoris, a suppressive agent of cerebrovascular contraction, a therapeutic agent of asthma, a therapeutic agent of peripheral circulation disorder, a prophylactic agent of immature birth, a therapeutic agent of arteriosclerosis, an anti-cancer drug, an anti-inflammatory agent, an immunosuppressant, a therapeutic agent of autoimmune disease, an anti-AIDS drug, a contraceptive, a prophylactic agent of digestive tract infection, a therapeutic agent of osteoporosis, a therapeutic agent of retinopathy and a brain function improving drug. In addition, the Rho kinase inhibitor is provided as a reagent and a diagnostic.
摘要翻译： 提供Rho激酶抑制剂作为新型药剂，特别是高血压治疗剂，心绞痛治疗剂，脑血管收缩抑制剂，哮喘治疗剂，外周循环障碍治疗剂，预防性药物 不成熟的药剂，动脉硬化治疗剂，抗癌药，抗炎剂，免疫抑制剂，自身免疫性疾病的治疗剂，抗艾滋病药，避孕药，消化道感染的预防剂， 骨质疏松症治疗剂，视网膜病变治疗剂和脑功能改善药物。 另外，提供Rho激酶抑制剂作为试剂和诊断。
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公开(公告)号：US5958944A
公开(公告)日：1999-09-28
申请号：US727669
申请日：1996-10-17
IPC分类号： A61P9/12 , C07D213/75 , C07D213/82 , C07D215/42 , C07D239/42 , C07D239/48 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D473/34 , C07D487/04 , A61K31/44 , A61K31/435 , C07D213/72
CPC分类号： C07D213/75 , C07D213/82 , C07D215/42 , C07D239/42 , C07D239/48 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D473/34 , C07D487/04
摘要： Benzamide compounds of the formula ##STR1## wherein each symbol is as defined in the specification, isomers thereof and pharmaceutically acceptable acid addition salts thereof. Pharmaceutical compositions comprising a therapeutically effective amount of this compound and a pharmaceutically acceptable additive, and therapeutic agents for hypertension, therapeutic agents for angina pectoris, therapeutic agent for asthma, therapeutic agents for renal and peripheral circulatory disturbances and inhibitor of cerebral vasospasm, which comprise this compound. The compound of the present invention has strong smooth muscle relaxing action, and shows hypotensive action and cerebral coronary vasodilating action like conventional calcium antagonists, as well as long-lasting renal and peripheral circulation improving action. Unlike calcium antagonists, it permits oral administration to suppress vascular contraction caused by various agonists, and is useful as a strong and long-acting agent for prophylaxis and treatment of circulatory diseases in coronary, cerebral, renal and peripheral arteries, as a therapeutic agent for hypertension, angina pectoris, and renal and peripheral circulation disorder, an inhibitor of cerebral vasospasm and the like. Moreover, the compound of the present invention is useful as a therapeutic agent for asthma.
摘要翻译： PCT No.PCT / JP95 / 00747 Sec。 371日期1996年10月17日第 102（e）日期1996年10月17日PCT提交1995年4月17日PCT公布。 WO95 / 28387 PCT出版物 日期1995年10月26日具有下式的苯甲酰胺化合物其中每个符号如说明书中所定义，其异构体和其药学上可接受的酸加成盐。 包含治疗有效量的该化合物和药学上可接受的添加剂的药物组合物，高血压治疗剂，心绞痛治疗剂，哮喘治疗剂，肾脏和周围循环障碍的治疗剂以及脑血管痉挛抑制剂，其包含该 复合。 本发明的化合物具有强烈的平滑肌松弛作用，并且显示降血压作用和像常规钙拮抗剂的脑冠状动脉血管舒张作用，以及持久的肾和外周循环改善作用。 与钙拮抗剂不同，它允许口服给药以抑制由各种激动剂引起的血管收缩，并且可用作预防和治疗冠状动脉，脑，肾和外周动脉中的循环系统疾病的强力和长效剂，作为治疗剂 高血压，心绞痛，肾和周围循环障碍，脑血管痉挛抑制剂等。 此外，本发明的化合物可用作哮喘的治疗剂。
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公开(公告)号：US5006520A
公开(公告)日：1991-04-09
申请号：US373296
申请日：1989-06-13
申请人： Takanori Oe , Hiroyuki Sueoka , Masao Hisadome , Keiji Yamagami
发明人： Takanori Oe , Hiroyuki Sueoka , Masao Hisadome , Keiji Yamagami
IPC分类号： C07D231/56 , C07D471/04
CPC分类号： C07D471/04 , C07D231/56
摘要： Novel fused pyrazole compounds of the general formula ##STR1## wherein all the symbols are as defined in the specification or its pharmaceutically acceptable salt which possesses a stimulating action on phagocytosis of leukocytes, a stimulating action on phagocytosis of macrophages, a restorative action on leukopenia, a stimulating action on non-specific resistance to infection, an antitumour action, an activating action on immune responses and the like, and thereof is of use as a pharmaceutical.
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公开(公告)号：US06218410B1
公开(公告)日：2001-04-17
申请号：US09242261
申请日：1999-04-19
IPC分类号： A61K31445
CPC分类号： A61K45/00 , A61K31/00 , A61K31/437 , A61K31/4409 , A61K31/4545 , A61K31/496 , A61K31/551
摘要： A Rho kinase inhibitor is provided as a novel pharmaceutical agent, particularly as a therapeutic agent of hypertension, a therapeutic agent of angina pectoris, a suppressive agent of cerebrovascular contraction, a therapeutic agent of asthma, a therapeutic agent of peripheral circulation disorder, a prophylactic agent of immature birth, a therapeutic agent of arteriosclerosis, an anti-cancer drug, an anti-inflammatory agent, an immunosuppressant, a therapeutic agent of autoimmune disease, an anti-AIDS drug, a contraceptive, a prophylactic agent of digestive tract infection, a therapeutic agent of osteoporosis, a therapeutic agent of retinopathy and a brain function improving drug. In addition, the Rho kinase inhibitor is provided as a reagent and a diagnostic.
摘要翻译： 提供Rho激酶抑制剂作为新型药剂，特别是高血压治疗剂，心绞痛治疗剂，脑血管收缩抑制剂，哮喘治疗剂，外周循环障碍治疗剂，预防性药物 不成熟的药剂，动脉硬化治疗剂，抗癌药，抗炎剂，免疫抑制剂，自身免疫性疾病的治疗剂，抗艾滋病药，避孕药，消化道感染的预防剂， 骨质疏松症治疗剂，视网膜病变治疗剂和脑功能改善药物。 另外，提供Rho激酶抑制剂作为试剂和诊断。
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公开(公告)号：US6156766A
公开(公告)日：2000-12-05
申请号：US252079
申请日：1999-02-18
IPC分类号： A61P9/12 , C07D213/75 , C07D213/82 , C07D215/42 , C07D239/42 , C07D239/48 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D473/34 , C07D487/04 , A61K31/437 , A61K31/519
CPC分类号： C07D213/75 , C07D213/82 , C07D215/42 , C07D239/42 , C07D239/48 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D473/34 , C07D487/04
摘要： Benzamide compounds of the formula ##STR1## wherein each symbol is defined in the specification, isomers thereof and pharmaceutically acceptable acid addition salts thereof. Pharmaceutical compositions comprising a therapeutically effective amount of this compound and a pharamaceutically acceptable additive, and therapeutic agents for hypertension, therapeutic agents for angina pectoris, therapeutic agent for asthma, therapeutic agents for renal and peripheral circulatory disturbances and inhibitor of cerebral vasospasm, which comprise this compound. The compound of the present invention has strong smooth muscle relaxing action, and shows hypertensive action and cerebral.cndot.coronary vasodilating action like conventional calcium antagonists, as well as long-lasting renal and peripheral circulation improving action. Unlike calcium antagonists, it permits oral administration to suppress vascular contraction caused by various agonists, and is useful as a strong and long-acting agent for prophylaxis and treatment of circulatory diseases in coronary, cerebral, renal and peripheral arteries, as a therapeutic agent for hypertension, angina pectoris, and renal and peripheral circulation disorder, an inhibitor of cerebral vasospasm and the like. Moreover, the compound of the present invention is useful as a therapeutic agent for asthma.
摘要翻译： 具有下式的苯甲酰胺化合物其中每个符号在说明书中定义，其异构体和其药学上可接受的酸加成盐。 包含治疗有效量的该化合物和药学上可接受的添加剂的药物组合物，高血压治疗剂，心绞痛治疗剂，哮喘治疗剂，肾脏和外周循环障碍治疗剂以及脑血管痉挛抑制剂，其包含 复合。 本发明的化合物具有强的平滑肌松弛作用，并且显示出与常规钙拮抗剂相似的高血压作用和脑血管舒张作用，以及持久的肾脏和外周循环改善作用。 与钙拮抗剂不同，它允许口服给药以抑制由各种激动剂引起的血管收缩，并且可用作预防和治疗冠状动脉，脑，肾和外周动脉中的循环系统疾病的强力和长效剂，作为治疗剂 高血压，心绞痛，肾和周围循环障碍，脑血管痉挛抑制剂等。 此外，本发明的化合物可用作哮喘的治疗剂。
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