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1. 发明授权

US06960586B2 Imidazole derivatives, process for their preparation and their use 失效
标题翻译：咪唑衍生物，其制备方法及其应用
公开(公告)号：US06960586B2
公开(公告)日：2005-11-01
申请号：US10416998
申请日：2001-11-19
申请人： Akihiro Tasaka , Nobuyuki Matsunaga , Akio Ojida , Masami Kusaka
发明人： Akihiro Tasaka , Nobuyuki Matsunaga , Akio Ojida , Masami Kusaka
IPC分类号： A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00 , C07D233/54 , C07D401/06 , C07D403/06 , A01N43/58 , A01N43/42 , A01N43/60 , A61K31/495 , A61K31/50
CPC分类号： C07D403/06 , C07D401/06 , Y02P20/55
摘要： The present invention provides a compound having a steroid C17,20-lyase inhibitory activity, which is useful as a prophylactic or therapeutic agent of prostatism and tumor such as breast cancer and the like.A compound represented by the formula: wherein R is a hydrogen atom or a protecting group, R1 is a lower alkyl group or a cyclic alkyl group, and ring A and ring B are each an optionally substituted 5-membered or 6-membered ring having an amide bond in the ring, or a salt thereof.
摘要翻译：本发明提供具有类固醇C 17-20半胱氨酸酶抑制活性的化合物，其可用作前列腺素和肿瘤如乳腺癌等的预防或治疗剂。由下式表示的化合物：其中R是氢原子或保护基，R 1是低级烷基或环状烷基，并且环A和环B各自为任选取代的5 环或其中具有酰胺键的六元环或其盐。

2. 发明授权

US06716863B2 Heterocyclic compounds their production and use 失效
标题翻译：杂环化合物的生产和使用
公开(公告)号：US06716863B2
公开(公告)日：2004-04-06
申请号：US09889974
申请日：2001-07-24
申请人： Akihiro Tasaka , Takenori Hitaka , Etsuya Matsutani
发明人： Akihiro Tasaka , Takenori Hitaka , Etsuya Matsutani
IPC分类号： A61K31422
CPC分类号： C07D413/12 , C07D263/32
摘要： A compound represented by the formula: wherein m is 1 or 2, R1 is a halogen or an optionally halogenated C1-2 alkyl; one of R2 and R3 is a hydrogen atom and the other is a group represented by the formula: wherein n is 3 or 4; R4 is a C1-4 alkyl group substituted by 1 or 2 hydroxy groups, or a salt thereof shows tyrosine kinase-inhibiting activity.
摘要翻译：由下式表示的化合物：其中m为1或2，R 1为卤素或任选卤代的C 1-2烷基; R 2和R 3之一是氢原子，另一个是由下式表示的基团：其中n是3或4; R 4是被1或2个羟基取代的C 1-4烷基，或其盐表示酪氨酸激酶抑制活性。

3. 发明授权

US06649643B1 Imidazol-4-ylmehanols and their use as inhibitors of steroid C17-20 lyase 有权
标题翻译：咪唑-4-基甲醇及其作为甾体C17-20裂解酶的抑制剂的用途
公开(公告)号：US06649643B1
公开(公告)日：2003-11-18
申请号：US10110599
申请日：2002-04-12
申请人： Akihiro Tasaka , Akio Ojida , Tomohiro Kaku , Masami Kusaka , Masuo Yamaoka
发明人： Akihiro Tasaka , Akio Ojida , Tomohiro Kaku , Masami Kusaka , Masuo Yamaoka
IPC分类号： A61K314164
CPC分类号： C07D233/64 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/12 , Y02P20/55
摘要： Imidazol-4-ylmethanols and their uses for preventing and treating primary tumors, metastasis and recurrence of tumors, various symptoms accompanying tumors, prostatic hypertrophy, virilism, hirsutism, male pattern alopecia, precocious puberty, endometriosis, uterine myoma, mastopathy and polycystic ovary syndrome are disclosed.
摘要翻译：咪唑-4-基甲醇及其用于预防和治疗原发性肿瘤，肿瘤转移和复发，伴随肿瘤的各种症状，前列腺肥大，病毒性，多毛症，男性脱发，早熟青春期，子宫内膜异位症，子宫肌瘤，乳腺病和多囊卵巢综合征被披露。

4. 发明授权

US5677464A Production of optically active triazole compounds and their intermediates 失效
标题翻译：光学活性三唑化合物及其中间体的制备
公开(公告)号：US5677464A
公开(公告)日：1997-10-14
申请号：US453968
申请日：1995-05-30
申请人： Katsumi Itoh , Akihiro Tasaka , Hiroshi Hosono
发明人： Katsumi Itoh , Akihiro Tasaka , Hiroshi Hosono
IPC分类号： C07C45/67 , C07C49/82 , C07D233/32 , C07D233/70 , C07D249/12 , C07D521/00 , C07F7/18
CPC分类号： C07D231/12 , C07C45/673 , C07C49/82 , C07D233/32 , C07D233/56 , C07D233/70 , C07D249/08 , C07D249/12 , C07F7/1856
摘要： A compound of the formula (V): ##STR1## wherein Ar' is a halogenated phenyl group, R is a hydrocarbon residue having a functional group at the .alpha.-carbon, R.sup.3' is an optionally substituted aliphatic or aromatic hydrocarbon residue or an optionally substituted aromatic heterocyclic group, Y and Z are, the same or different, a nitrogen atom or a methine group optionally substituted with a lower alkyl group, and (R) and (S) represent configurations, which is an optically active intermediate for production of optically active triazole compounds (I): ##STR2## wherein the symbols have the same meanings as defined above, and methods of preparing the compounds (V) and (I).
摘要翻译：式（V）的化合物：其中Ar'是卤代苯基，R是在α-碳上具有官能团的烃残基，R3'是任选取代的脂族或芳族烃残基或任选取代的芳族杂环基，Y和Z相同或不同，任选被低级烷基取代的氮原子或次甲基，和（R）和（S）表示构型，其为光学活性中间体用于制备光学活性三唑化合物（I）：其中符号具有与上述相同的含义，以及制备化合物（V）和（I）的方法。

5. 发明授权

US5008454A Propanediol derivatives, their production and use 失效
标题翻译：丙二醇衍生物，其生产和使用
公开(公告)号：US5008454A
公开(公告)日：1991-04-16
申请号：US492330
申请日：1990-03-12
申请人： Keizo Inoue , Hiroaki Nomura , Akihiro Tasaka
发明人： Keizo Inoue , Hiroaki Nomura , Akihiro Tasaka
IPC分类号： C07D213/20 , C07D213/80 , C07D277/22
CPC分类号： C07D213/20 , C07D213/80 , C07D277/22
摘要： Novel compounds having the formula:R.sup.1 --OCH.sub.2 CH.sub.2 CH.sub.2 O--(CH.sub.2).sub.n --R.sup.2wherein R.sup.1 stands for a higher alkyl group; R.sup.2 stands for a primary to tertiary amino group or a quaternary ammonium group; and n denotes an integer of 3 to 10; and salts thereof, have excellent anti-tumor action and therefore are useful as anti-tumor agents.

6. 发明授权

US06518257B1 1-substituted phenyl-1-(1h-imidazol-4-yl) alcohols, process for producing the same and use thereof 有权
标题翻译： 1-取代的苯基-1-（1h-咪唑-4-基）醇，其制备方法及其用途
公开(公告)号：US06518257B1
公开(公告)日：2003-02-11
申请号：US10111136
申请日：2002-04-18
申请人： Akihiro Tasaka , Tomohiro Kaku , Masami Kusaka
发明人： Akihiro Tasaka , Tomohiro Kaku , Masami Kusaka
IPC分类号： A61K314164
CPC分类号： C07D233/64 , Y02P20/55
摘要： To provide a composition having a steroid C17,20-lyase inhibitory activity and useful as an agent for the prophylaxis or treatment of prostatism and tumors such as breast cancer. A compound represented by the formula: wherein R is a hydrogen atom or a protecting group, R1 is a lower alkyl group or a cyclic hydrocarbon group, R2 is an aromatic hydrocarbon group optionally having substituents or an aromatic heterocyclic group optionally having substituents, R3 is a hydrocarbon group optionally having substituents, a hydroxyl group optionally having substituents, a thiol group optionally having substituents, an amino group optionally having substituents, an acyl group or a halogen atom, and n is an integer of 0 to 4, and a salt thereof have a steroid C17,20-lyase inhibitory activity, and are useful as an agent for the pophylaxis or treatment of prostatism and tumors such as beast cancer and the like.
摘要翻译：提供具有类固醇C17,20裂解酶抑制活性并可用作预防或治疗前列腺症和肿瘤如乳腺癌的药剂的组合物。由下式表示的化合物：其中R是氢原子或保护基，R 1是低级烷基或环状烃基，R 2是任选具有取代基的芳族烃基或任选具有取代基的芳族杂环基，R 3是任选具有取代基的烃基，任选具有取代基的羟基，任选具有取代基的硫醇基，任选具有取代基的氨基，酰基或卤素原子，n表示0〜4的整数，及其盐具有类固醇C17,20裂解酶抑制活性，并且可用作预防或治疗前列腺症和肿瘤如兽癌等的药剂。

7. 发明授权

US07141598B2 Imidazole derivatives, production method thereof and use thereof 有权
标题翻译：咪唑衍生物及其制备方法及用途
公开(公告)号：US07141598B2
公开(公告)日：2006-11-28
申请号：US10416986
申请日：2001-11-16
申请人： Akihiro Tasaka , Takenori Hitaka , Nobuyuki Matsunaga , Masami Kusaka
发明人： Akihiro Tasaka , Takenori Hitaka , Nobuyuki Matsunaga , Masami Kusaka
IPC分类号： A61K31/4184 , C07D235/02
CPC分类号： C07D233/64 , C07D471/04 , C07D487/04
摘要： The present invention provides a compound having a steroid C17,20-lyase-inhibitory activity and useful for the therapy and prophylaxis of tumor such as prostatism, breast cancer and the like, and a method for efficiently separating an optically active compound of this compound from a mixture of optical isomers thereof, a compound of the formula: wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof, and a method for obtaining an optically active compound by optically resolving a mixture of optical isomers by the use of a resolving agent such as tartranilic acid and the like.
摘要翻译：本发明提供了具有类固醇C 17,20 - 酶抑制活性并可用于治疗和预防诸如前列腺症，乳腺癌等肿瘤的化合物和有效分离的方法该化合物的旋光异构体的混合物的光学活性化合物，下式的化合物：其中每个符号如说明书中所定义，其盐或其前药，以及通过光学获得光学活性化合物的方法通过使用诸如格列硝酸等拆分剂来拆分光学异构体的混合物。

8. 发明授权

US07084149B2 Naphthalene derivatives, their production and use 失效
标题翻译：萘衍生物，其生产和使用
公开(公告)号：US07084149B2
公开(公告)日：2006-08-01
申请号：US10443379
申请日：2003-05-22
申请人： Akihiro Tasaka , Akio Ojida , Tomohiro Kaku , Masami Kusaka , Masuo Yamaoka
发明人： Akihiro Tasaka , Akio Ojida , Tomohiro Kaku , Masami Kusaka , Masuo Yamaoka
IPC分类号： A61K31/44 , C07D213/30 , A61P35/00
CPC分类号： C07D213/30 , C07D233/64 , C07D263/32 , C07D277/24 , C07D401/06
摘要： A composition containing a compound of the formula: wherein A is a nitrogen-containing heterocyclic group which may be substituted, R1 is a hydrogen atom, hydrocarbon group which may be substituted, or monocyclic aromatic heterocyclic group which may be substituted, R2 is a hydrogen atom or a lower alkyl group which may be substituted, R3, R4, R5, R6, R7, R8 and R9 are independently a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxy group which may be substituted, a thiol group which may be substituted, an amino group which may be substituted, an acyl group or a halogen atom, a salt thereof or a prodrug thereof has steroid C17,20-lyase inhibitory activity, and are useful for preventing and treating a mammal suffering from, for example, primary cancer of malignant tumor, its metastasis and recurrence thereof.
摘要翻译：含有下式化合物的组合物：其中A为可被取代的含氮杂环基，R 1为氢原子，可被取代的烃基或单环芳族杂环基，其中， R 2可以被取代，R 2是氢原子或可被取代的低级烷基，R 3，R 4，R 4， > 5，R 6，R 7，R 8和R 9独立地是氢可以被取代的烃基，可被取代的羟基，可被取代的硫醇基，可被取代的氨基，酰基或卤素原子，其盐或其前药具有类固醇C 17,20 - 酶抑制活性，可用于预防和治疗患有例如恶性肿瘤原发性癌症，其转移和复发的哺乳动物。

9. 发明授权

US06573289B1 Naphthalene derivatives, their production and use 有权
标题翻译：萘衍生物，其生产和使用
公开(公告)号：US06573289B1
公开(公告)日：2003-06-03
申请号：US09673591
申请日：2000-10-18
申请人： Akihiro Tasaka , Akio Ojida , Tomohiro Kaku , Masami Kusaka , Masuo Yamaoka
发明人： Akihiro Tasaka , Akio Ojida , Tomohiro Kaku , Masami Kusaka , Masuo Yamaoka
IPC分类号： A61K31415
CPC分类号： C07D213/30 , C07D233/64 , C07D263/32 , C07D277/24 , C07D401/06
摘要： A composition containing a compound of the formula: wherein A is a nitrogen-containing heterocyclic group which may be substituted, R1 is a hydrogen atom, hydrocarbon group which may be substituted, or monocyclic aromatic heterocyclic group which may be substituted, R2 is a hydrogen atom or a lower alkyl group which may be substituted, R3, R4, R5, R6, R7, R8 and R9 are independently a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxy group which may be substituted, a thiol group which may be substituted, an amino group which may be substituted, an acyl group or a halogen atom, a salt thereof or a prodrug thereof has steroid C17,20-lyase inhibitory activity, and is useful for preventing and treating for example, primary cancer of malignant tumor, its metastasis and recurrence thereof.
摘要翻译：一种含有下式化合物的组合物：其中A为可被取代的含氮杂环基，R 1为氢原子，可被取代的烃基或可被取代的单环芳族杂环基，R 2为氢原子或可被取代的低级烷基，R 3，R 4，R 5，R 6，R 7，R 8和R 9分别是氢原子，可被取代的烃基，可被取代的羟基，硫醇基，可以被取代的氨基，酰基或卤素原子，其盐或其前药具有类固醇C17,20-裂解酶抑制活性，并且可用于预防和治疗例如原发性癌症恶性肿瘤，其转移和复发。

10. 发明授权

US06362206B1 Azole compounds, their production and use 失效
标题翻译：唑类化合物，其生产和使用
公开(公告)号：US06362206B1
公开(公告)日：2002-03-26
申请号：US09413876
申请日：1999-10-07
申请人： Katsumi Itoh , Kenji Okonogi , Akihiro Tasaka
发明人： Katsumi Itoh , Kenji Okonogi , Akihiro Tasaka
IPC分类号： A61K314192
CPC分类号： C07D231/12 , A01N43/653 , C07D233/56 , C07D249/08
摘要： The present invention provides an azole compound represented by the formula (I): wherein Ar is an optionally substituted phenyl group; R1 and R2, the same or different, are a hydrogen atom or a lower alkyl group, or R1 and R2 may combine together to form a lower alkylene group; R is a hydrogen atom or an acyl group; X is a nitrogen atom or a methine group; A is Y═Z (Y and Z, the same or different, are a nitrogen atom or a methine group optionally substituted with a lower alkyl group) or an ethylene group optionally substituted with a lower alkyl group; n is an integer from 0 to 2; and Az is an optionally substituted azolyl group, or its salt, which is useful for a prevention and therapy of a fungal infection of a mammal as a antifungal agent.
摘要翻译：本发明提供由式（I）表示的唑化合物：其中Ar为任选取代的苯基; R1和R2相同或不同，为氢原子或低级烷基，或者R1和R2可以结合在一起形成低级亚烷基; R是氢原子或酰基; X是氮原子或次甲基; A是Y = Z（Y和Z相同或不同，是任选被低级烷基取代的氮原子或次甲基）或任选被低级烷基取代的亚乙基; n为0〜2的整数; 并且Az是任选取代的唑基或其盐，其可用于预防和治疗作为抗真菌剂的哺乳动物的真菌感染。

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