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1. 发明申请

US20100292206A1 HETEROCYCLIC COMPOUND 有权
标题翻译：杂环化合物
公开(公告)号：US20100292206A1
公开(公告)日：2010-11-18
申请号：US12738486
申请日：2008-10-17
申请人： Shizuo Kasai , Tomohiro Kaku , Masahiro Kamaura
发明人： Shizuo Kasai , Tomohiro Kaku , Masahiro Kamaura
IPC分类号： A61K31/4427 , C07D205/04 , A61K31/397 , C07D401/06 , C07D413/06 , C07D417/06 , C07D513/04 , C07D211/22 , A61K31/445 , C07D207/00 , A61K31/40 , A61P3/10
CPC分类号： C07D417/04 , C07D205/04 , C07D207/08 , C07D207/12 , C07D211/22 , C07D211/44 , C07D211/46 , C07D211/78 , C07D211/88 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D413/04 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/08 , C07D417/10 , C07D471/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
摘要翻译：本发明涉及其中每个符号如说明书中所定义的。本发明的化合物具有优异的RBP4降低作用，可用作预防或治疗由增加的RBP4介导的疾病和病症的药物。

2. 发明授权

US08586571B2 Heterocyclic compound 有权
标题翻译：杂环化合物
公开(公告)号：US08586571B2
公开(公告)日：2013-11-19
申请号：US12738486
申请日：2008-10-17
申请人： Shizuo Kasai , Tomohiro Kaku , Masahiro Kamaura
发明人： Shizuo Kasai , Tomohiro Kaku , Masahiro Kamaura
IPC分类号： C07D205/04 , C07D205/08 , C07D205/00 , C07D211/22 , C07D211/44 , C07D211/46 , C07D211/78 , C07D211/88 , C07D413/10 , C07D413/12 , C07D413/06 , C07D417/06 , C07D417/08 , C07D417/10 , C07D471/04 , C07D495/04 , C07D513/04 , C07D401/06 , A61K31/4427 , A61K31/397 , A61K31/445 , A61K31/40 , A61P3/10
CPC分类号： C07D417/04 , C07D205/04 , C07D207/08 , C07D207/12 , C07D211/22 , C07D211/44 , C07D211/46 , C07D211/78 , C07D211/88 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D413/04 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/08 , C07D417/10 , C07D471/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
摘要翻译：本发明涉及其中每个符号如说明书中所定义的。本发明的化合物具有优异的RBP4降低作用，可用作预防或治疗由增加的RBP4介导的疾病和病症的药物。

3. 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。

4. 发明申请

US20090062258A1 FUSED PYRIMIDINE DERIVATIVE AND USE THEREOF 审中-公开
标题翻译：熔融吡嗪衍生物及其用途
公开(公告)号：US20090062258A1
公开(公告)日：2009-03-05
申请号：US11815403
申请日：2006-02-02
申请人： Kazumasa Hamamura , Tsuneo Oda , Tomohiro Kaku , Tomohiro Suzaki
发明人： Kazumasa Hamamura , Tsuneo Oda , Tomohiro Kaku , Tomohiro Suzaki
IPC分类号： A61K31/55 , C07D239/70 , A61K31/519 , C07D495/04
CPC分类号： C07D495/04 , C07D487/04 , C07D495/14 , C07D513/04 , C07D519/00
摘要： The present invention provides a compound represented by the formula (I) and a salt thereof wherein: ring A is a 5-membered aromatic heterocycle optionally having substituent(s); R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s); W is an oxygen atom or a sulfur atom; X1 and X2 may be the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s) or a heterocyclic group, or, X1 and X2 in combination, optionally, form an oxygen atom, a sulfur atom or ═NR2; ring B is an aromatic ring optionally further having substituent(s); Y is a bond, C1-6 alkylene C2-6 alkenylene or C2-6 alkynylene, optionally having substituent(s); and Z is —SOnR3 or —COR4, which are useful as a pharmaceutical agent having GnRH antagonistic action.
摘要翻译：本发明提供由式（I）表示的化合物及其盐，其中：环A为任选具有取代基的5元芳族杂环; R1是氢原子或任选具有取代基的烃基; W是氧原子或硫原子; X1和X2可以相同或不同，各自为氢原子，任选具有取代基的烃基或杂环基，或者X1和X2组合，任选地形成氧原子，硫原子或 - NR2; 环B是任选进一步具有取代基的芳环; Y是键，任选具有取代基的C 1-6亚烷基C 2-6亚烯基或C 2-6亚炔基; Z为-SO n R 3或-COR 4，其可用作具有GnRH拮抗作用的药剂。

5. 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。

6. 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。

7. 发明授权

US07067537B2 Substituted thiazole derivatives bearing 3-pyridyl groups, process for preparing the same and use thereof 失效
标题翻译：带有3-吡啶基的取代噻唑衍生物，其制备方法及其应用
公开(公告)号：US07067537B2
公开(公告)日：2006-06-27
申请号：US10433910
申请日：2001-12-07
申请人： Noritaka Kuroda , Yoshi Nara , Shohei Hashiguchi , Akihiro Tasaka , Masami Kusaka , Masuo Yamaoka , Tomohiro Kaku
发明人： Noritaka Kuroda , Yoshi Nara , Shohei Hashiguchi , Akihiro Tasaka , Masami Kusaka , Masuo Yamaoka , Tomohiro Kaku
IPC分类号： A01N43/40 , A61K31/44
CPC分类号： C07D417/04 , A61K31/4439 , A61K31/4545 , A61K31/4725 , C07D417/14
摘要： The present invention provides a pharmaceutical composition having a steroid C17,20-lyase inhibitory activity, which is useful as a prophylactic or therapeutic agent of prostatism, tumor such as breast cancer and the like, more particularly, a steroid C17,20-lyase inhibitor containing a compound represented by the formula: wherein A1 is an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, one of A2 and A3 is a hydrogen atom, a halogen atom, a C1-4 aliphatic hydrocarbon group optionally having substituents or an optionally esterified carboxyl group, the other of A2 and A3 is an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, and at least one of A1, A2 and A3 is a 3-pyridyl group optionally having substituents, or a salt thereof or a prodrug thereof.
摘要翻译：本发明提供了具有类固醇C 17-20半胱氨酸酶抑制活性的药物组合物，其可用作前列腺症的预防或治疗剂，诸如乳腺癌等肿瘤，更具体地，含有由下式表示的化合物的类固醇C 17-20重量酶抑制剂：其中A 1是任选具有取代基的芳族烃基或任选具有取代基的杂环基， A 2和A 3之一是氢原子，卤素原子，任选具有取代基的C 1-4烷基脂族烃基或任选地酯化的羧基，A 2和A 3中的另一个是任选具有取代基的芳族烃基或任选具有取代基的杂环基，并且A < SUP> 1，A 2和A 3是任选具有取代基的3-吡啶基，或其盐或前药其中。

8. 发明申请

US20060032148A1 Method of manufacturing polishing slurry for use in precise polishing process 审中-公开
标题翻译：制造用于精密抛光工艺的抛光浆料的方法
公开(公告)号：US20060032148A1
公开(公告)日：2006-02-16
申请号：US11192364
申请日：2005-07-29
申请人： Takaharu Kunugi , Tomohiro Kaku , Takanori Sasakura
发明人： Takaharu Kunugi , Tomohiro Kaku , Takanori Sasakura
IPC分类号： C09K3/14 , B24D3/02 , C09C1/68
CPC分类号： C09G1/02
摘要： An abrasive and a dispersion medium are introduced into a dispersing machine to uniformly disperse the abrasive. The liquid to be processed after dispersion is centrifugally classified by a centrifugal classifier to remove heavy particles which will cause scratches. Chemicals are added to the liquid to be processed after classification to make adjustments on a variety of properties such as the concentration, pH, and the like. The polishing slurry after adjustment for a desired composition is filtered by a filter to remove debris therefrom. The filter may have a mesh size large enough to allow particles of the abrasive to pass therethrough.
摘要翻译：将研磨剂和分散介质引入分散机以均匀地分散研磨剂。分散后待处理的液体通过离心分级机离心分级，以除去会引起刮伤的重质颗粒。在分级后将化学品加入到待处理的液体中以对各种性质如浓度，pH等进行调整。调整所需组合物后的抛光浆料用过滤器过滤以从中除去碎屑。过滤器可以具有足够大的筛网尺寸，以允许研磨剂的颗粒通过。

9. 发明申请

US20090270361A1 Substituted pyrazole derivatives and use thereof 审中-公开
标题翻译：取代的吡唑衍生物及其用途
公开(公告)号：US20090270361A1
公开(公告)日：2009-10-29
申请号：US12383502
申请日：2009-03-25
申请人： Mitsuhiro Ito , Naoki Tomita , Tomohiro Kaku , Tomohiko Suzaki
发明人： Mitsuhiro Ito , Naoki Tomita , Tomohiro Kaku , Tomohiko Suzaki
IPC分类号： A61K31/4155 , C07D231/12 , A61K31/415 , A61K31/4439 , C07D401/12 , C07D403/10 , A61P35/00
CPC分类号： C07D231/12 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/12 , C07D413/10 , C07D413/12 , C07D417/12
摘要： The present invention aims to provide a novel pyrazole derivative and a pharmaceutical agent containing the same. The present invention provides a compound represented by the formula (I′) wherein R1′ is (1) a hydrogen atom, (2) a group via a carbon atom, (3) a group via a nitrogen atom, (4) a group via an oxygen atom or (5) a group via a sulfur atom; R2′ is an aromatic ring group optionally having substituent(s); R3′ is (1) a hydrogen atom, (2) a group via a carbon atom, (3) a group via a nitrogen atom, (4) a group via an oxygen atom or (5) a group via a sulfur atom; R4′ is a cyanophenyl group optionally having substituent(s); X′ is (1) —Y′—CR5′R6′-Z′- wherein R5′ and R6′ are the same or different and each is a hydrogen atom, a group via a carbon atom, a group via a nitrogen atom, a group via an oxygen atom or a group via a sulfur atom, or —CR5′R6′— is —C(alkylidene)-; Y′ is a bond, —COCO—, —CONH—, —COCONH— or —O—; and Z′ is a bond, —CH2—, —CONH—, —O—, —OCH2—, —S—, —SO—, —SO2—, —CON(C6H5)— or (2) —CO(CONH)n— wherein n is 0 or 1, (3) —NHCO—, (4) —CONH—, (5) —O—, (6) —CH═CH— or (7) —O(C1-3 alkylene)O—; (excluding the compounds indicated to be excluded from the specification), or a salt thereof.
摘要翻译：本发明的目的在于提供一种新的吡唑衍生物和含有它们的药剂。本发明提供由式（I'）表示的化合物，其中R 1'为（1）氢原子，（2）通过碳原子的基团，（3）通过氮原子的基团，（4）通过氧原子或（5）经由硫原子的基团; R2'是任选具有取代基的芳环基团; R 3'为（1）氢原子，（2）经由碳原子的基团，（3）经由氮原子的基团，（4）经由氧原子的基团或（5）经由硫原子的基团; R4'是任选具有取代基的氰基苯基; X'为（1）-Y'-CR5'R6'-Z'-，其中R5'和R6'相同或不同，各自为氢原子，经由碳原子的基团，经由氮原子的基团，一个经由氧原子或一个经由硫原子的基团，或-CR 5'R 6' - 是-C（亚烷基） - ; Y'是键，-COCO - ， - CONH-，-COCONH-或-O-; 并且Z'为键，-CH 2 - ， - CONH - ， - O - ， - OCH 2 - ， - S - ， - SO - ， - SO 2 - ， - CON（C 6 H 5） - 或（2）-CO 其中n为0或1，（3）-NHCO-，（4）-CONH-，（5）-O-，（6）-CH-CH-或（7）-O（C1-3亚烷基） O-; （不包括表示从说明书中排除的化合物）或其盐。

10. 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。

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