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1. 发明授权

US08178681B2 3-carbamoyl-2-pyridone derivatives 有权
标题翻译： 3-氨基甲酰基-2-吡啶酮衍生物
公开(公告)号：US08178681B2
公开(公告)日：2012-05-15
申请号：US11628804
申请日：2005-10-28
申请人： Natsuki Ishizuka , Yoshiharu Hiramatsu , Yasuhiko Fujii , Yoshikazu Fukui
发明人： Natsuki Ishizuka , Yoshiharu Hiramatsu , Yasuhiko Fujii , Yoshikazu Fukui
IPC分类号： C07D221/04 , C07D213/62 , A61K31/54 , A61K31/435
CPC分类号： C07D213/82
摘要： The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1 is optionally substituted C1-C8 alkyl and the like; R2 is C1-C6 alkyl; R3 is C1-C6 alkyl and the like; or R2 and R3 taken together with may form an optionally substituted 5 to 10 membered non-aromatic carbon ring; R4 is hydrogen and the like; G is a group selected from the groups shown by the formula an the like: wherein R5 is hydrogen and the like; X1 is a single bond and the like; X2 is optionally substituted C1-C8 alkylene that may be replaced by one or two groups of —O—, or —N(R6)—, wherein R6 is hydrogen and the like, and the like; X3 is a single bond and the like; a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
摘要翻译：本发明提供对大麻素受体具有激动作用的化合物，其由式（I）表示：其中R 1为任选取代的C 1 -C 8烷基等; R2是C1-C6烷基; R3是C1-C6烷基等; 或者R 2和R 3与相邻碳原子一起可以形成任选取代的5至10元非芳族碳环; R4是氢等; G是选自下式的基团：其中R5是氢等; X1是单键等; X2是任选取代的C1-C8亚烷基，其可以被一个或两个-O-或-N（R 6） - 基团取代，其中R 6是氢等; X3是单键等; 药学上可接受的盐或其溶剂合物，以及药物组合物，特应性皮炎治疗剂和抗瘙痒剂，特别是用于口服和外用的抗瘙痒剂，其各自含有所述化合物作为活性成分。

2. 发明申请

US20080103139A1 3-Carbamoyl-2-Pyridone Derivative 有权
标题翻译： 3-氨基甲酰基-2-吡啶酮衍生物
公开(公告)号：US20080103139A1
公开(公告)日：2008-05-01
申请号：US11628804
申请日：2005-10-28
申请人： Natsuki Ishizuka , Takashi Sasatani , Yoshiharu Hiramatsu , Masanao Inagaki , Masahide Odan , Hiroshi Hashizume , Susumu Mitsumori , Yasuhiko Fujii , Yoshikazu Fukui , Hideaki Watanabe , Jun Sato
发明人： Natsuki Ishizuka , Takashi Sasatani , Yoshiharu Hiramatsu , Masanao Inagaki , Masahide Odan , Hiroshi Hashizume , Susumu Mitsumori , Yasuhiko Fujii , Yoshikazu Fukui , Hideaki Watanabe , Jun Sato
IPC分类号： A61K31/5377 , C07D221/04 , A61K31/435 , C07D211/84 , A61K31/4412 , A61P17/00 , C07D401/12 , A61K31/496 , A61K31/506 , C07D413/12
CPC分类号： C07D213/82
摘要： The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1 is optionally substituted C1-C8 alkyl and the like; R2 is C1-C6 alkyl; R3 is C1-C6 alkyl and the like; or R2 and R3 taken together with may form an optionally substituted 5 to 10 membered non-aromatic carbon ring; R4 is hydrogen and the like; G is a group selected from the groups shown by the formula an the like: wherein R5 is hydrogen and the like; X1 is a single bond and the like; X2 is optionally substituted C1-C8 alkylene that may be replaced by one or two groups of —O—, or —N(R6)—, wherein R6 is hydrogen and the like, and the like; X3 is a single bond and the like; a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
摘要翻译：本发明提供对大麻素受体具有激动作用的化合物，其由式（I）表示：其中R 1是任选取代的C 1 -C 8烷基等; R 2是C 1 -C 6烷基; R 3是C 1 -C 6烷基等; 或R 2和R 3与相邻碳原子一起可以形成任选取代的5至10元非芳族碳环; R 4是氢等; G为选自下式的基团：其中R 5为氢等; X 1是单键等; X 2是任选取代的C 1 -C 8亚烷基，其可以被一个或两个-O-或-N（R 6） - 基团取代，其中R 0 > 6是氢等; X 3是单键等; 其药学上可接受的盐或溶剂合物，以及药物组合物，特应性皮炎治疗剂和抗瘙痒剂，特别是用于口服和外用的抗瘙痒剂，其各自含有所述化合物作为活性成分。

3. 发明申请

US20090030014A1 Indole Derivative Having Pgd2 Receptor Antagonist Activity 有权
标题翻译：具有Pgd2受体拮抗剂活性的吲哚衍生物
公开(公告)号：US20090030014A1
公开(公告)日：2009-01-29
申请号：US11989138
申请日：2006-07-20
申请人： Akira Kugimiya , Michitaka Shichijo , Yoshiharu Hiramatsu , Natsuki Ishizuka
发明人： Akira Kugimiya , Michitaka Shichijo , Yoshiharu Hiramatsu , Natsuki Ishizuka
IPC分类号： A61K31/496 , C07D487/00 , C07D401/02 , A61K31/4439 , A61P25/28 , A61K31/404 , A61K31/454 , C07D403/02
CPC分类号： C07D403/04 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention creates an indole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.A compound of the generic formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is C2-C4 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is independently C1-C4 alkyl etc.; R9 is carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译：本发明产生具有DP受体拮抗活性的吲哚衍生物和包含所述化合物作为活性成分的药物组合物，还有用于治疗过敏性疾病的治疗剂。通式（I）的化合物，其中环A是芳族碳环等; 环B为3〜8元含氮非芳族杂环等; R1，R2，R3，R4和R5独立地是氢原子或卤素原子等; R6是C2-C4烷氧基等; R7独立地为卤素原子等; R8独立地为C1-C4烷基等。 R9是羧基等。 Y是单键等; M是磺酰基等。 L1，L2和L3是任选含有一个或两个杂原子等的单键或亚烷基; n为0等 q为0等; 其药学上可接受的盐或水合物。

4. 发明授权

US07956082B2 Indole derivative having PGD2 receptor antagonist activity 有权
标题翻译：具有PGD2受体拮抗剂活性的吲哚衍生物
公开(公告)号：US07956082B2
公开(公告)日：2011-06-07
申请号：US11989138
申请日：2006-07-20
申请人： Akira Kugimiya , Michitaka Shichijo , Yoshiharu Hiramatsu , Natsuki Ishizuka
发明人： Akira Kugimiya , Michitaka Shichijo , Yoshiharu Hiramatsu , Natsuki Ishizuka
IPC分类号： A61K31/496 , A61K31/4439 , A61K31/404 , A61K31/454 , A61P25/28 , C07D487/00 , C07D401/02 , C07D403/02
CPC分类号： C07D403/04 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention creates an indole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.A compound of the generic formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is C2-C4 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is independently C1-C4 alkyl etc.; R9 is carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.;a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译：本发明产生具有DP受体拮抗活性的吲哚衍生物和包含所述化合物作为活性成分的药物组合物，还有用于治疗过敏性疾病的治疗剂。通式（I）的化合物，其中环A是芳族碳环等; 环B为3〜8元含氮非芳族杂环等; R1，R2，R3，R4和R5独立地是氢原子或卤素原子等; R6是C2-C4烷氧基等; R7独立地为卤素原子等; R8独立地为C1-C4烷基等。 R9是羧基等。 Y是单键等; M是磺酰基等。 L1，L2和L3是任选含有一个或两个杂原子等的单键或亚烷基; n为0等 q为0等; 其药学上可接受的盐或水合物。

5. 发明申请

US20050171143A1 Compound exhibiting pgd 2 receptor antagonism 失效
标题翻译：化合物表现出pgd 2受体拮抗作用
公开(公告)号：US20050171143A1
公开(公告)日：2005-08-04
申请号：US10514317
申请日：2003-05-15
申请人： Norihiko Tanimoto , Yoshiharu Hiramatsu , Susumu Mitsumori , Masanao Inagaki
发明人： Norihiko Tanimoto , Yoshiharu Hiramatsu , Susumu Mitsumori , Masanao Inagaki
IPC分类号： A61K31/403 , A61K31/405 , A61K31/407 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61P11/06 , A61P37/08 , A61P43/00 , C07D209/14 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D409/12 , C07D409/14 , C07D471/04 , C07D471/02 , A61K31/4745 , A61K31/416
CPC分类号： C07D209/80 , A61K31/403 , A61K31/405 , A61K31/407 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4709 , C07D209/14 , C07D231/56 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D409/12 , C07D409/14 , C07D471/04 , Y02A50/423
摘要： A compound having CRTH2 receptor antagonism, represented by the following formula (I). The compound is useful for the treatment of allergic diseases having a relation to eosinophils and the like. A compound of the formula (I): wherein a group represented by the formula: is a group represented by the formula: and the like, R1 is carboxy and the like, R3 is —(CH2)n-N(—Y)—SO2-Ar and the like, the other symbols are as defined in claim 1.
摘要翻译：具有CRTH2受体拮抗作用的化合物，由下式（I）表示。该化合物可用于治疗与嗜酸性粒细胞等有关的过敏性疾病。式（I）的化合物：其中由下式表示的基团是由下式表示的基团：等等，R 1是羧基等，R 3， / SUP>是 - （CH 2）nN（-Y）-SO 2 -Ar等，其它符号如权利要求1中所定义。

6. 发明授权

US06399788B1 Process for producing benzothiophenecarboxylic acid amide derivatives 失效
标题翻译：苯并噻吩羧酸酰胺衍生物的制备方法
公开(公告)号：US06399788B1
公开(公告)日：2002-06-04
申请号：US09647353
申请日：2000-09-29
申请人： Tsunetoshi Honma , Yoshiharu Hiramatsu , Tetsuo Okada , Makoto Kakinuma
发明人： Tsunetoshi Honma , Yoshiharu Hiramatsu , Tetsuo Okada , Makoto Kakinuma
IPC分类号： C07D33364
CPC分类号： C07D333/68 , C07C213/02 , C07C2602/42 , C07C215/42
摘要： A process for preparing a compound having PGD2 antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.
摘要翻译：一种制备由式（I）表示的具有PGD 2拮抗作用的化合物或其药学上可接受的盐或水合物的方法，该方法包括使式（II）或其盐的氨基醇与式（III）的化合物反应）或其反应性衍生物，在2,2,6,6-四甲基哌啶-1-氧基存在下用卤代含氧酸氧化产物，在Wittig反应条件下使产物与叶立德反应，并任选地使产物脱保护。

7. 发明授权

US07105564B1 Pharmaceutical composition comprising a dual antagonist against PGD2/TXA2 receptors having a [2.2.1] or [3.1.1] bicyclic skeleton 失效
标题翻译：药物组合物包含针对具有[2.2.1]或[3.1.1]双环骨架的PGD2 / TXA2受体的双重拮抗剂
公开(公告)号：US07105564B1
公开(公告)日：2006-09-12
申请号：US09936161
申请日：2000-03-02
申请人： Tsunetoshi Honma , Yoshiharu Hiramatsu , Akinori Arimura
发明人： Tsunetoshi Honma , Yoshiharu Hiramatsu , Akinori Arimura
IPC分类号： A61P11/00 , A61K31/40 , A61K31/47 , A61K31/44 , A61K31/425
CPC分类号： C07D207/323 , A61K31/00 , A61K31/201 , A61K31/381 , A61K31/40 , A61K31/402 , A61K31/4025 , A61K31/404 , A61K31/4155 , A61K31/4178 , A61K31/4188 , A61K31/422 , A61K31/423 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/4402 , A61K31/4725 , C07C311/21 , C07C317/44 , C07C323/62 , C07C2602/42 , C07D207/48 , C07D209/08 , C07D213/75 , C07D277/46 , C07D277/52 , C07D307/68 , C07D307/84 , C07D333/34 , C07D333/38 , C07D333/54 , C07D333/68 , C07D333/76 , C07D333/78 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/06 , C07D495/04
摘要： The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them.A compound of the formula (I): wherein R1 is —CH2—CH═CH—CH2—CH2—CH2—COOR2 or —CH═CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(═O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.
摘要翻译：本发明提供了对凝血恶烷A2受体和前列腺素D 2受体具有双重拮抗活性的新型化合物和包含它们的药物组合物。式（I）的化合物：其中R 1是-CH 2 CH-CH 2 CH 2 -CH 2 -CH 2 CH 2 -COOR 2或-CH-CH-CH 2 -CH 2 - （CH 2 CH 2 CH 2 CH 2 CH 2） CH 2 -COOR 2 O 2; R 2是氢或烷基; m为0或1; p为0或1; X 1和X 3各自独立地是任选取代的芳基或任选取代的杂芳基; X 2是一个键，-CH 2 - ， - S - ， - SO 2 - ， - CH 2 ，-O-CH 2 - ， - CH 2 -S-，-S-CH 2 - 等 ; X 4是-CH 2 - ， - CH 2 -CH 2 - ， - C（ - O） - 或类似物对血栓素A 2 O 2受体和前列腺素D 2受体具有双重拮抗活性。

8. 发明授权

US06346628B1 Process for preparing 5-hydroxybenzo [b] thiophene-3-carboxylic acid derivatives 失效
标题翻译：制备5-羟基苯并[b]噻吩-3-羧酸衍生物的方法
公开(公告)号：US06346628B1
公开(公告)日：2002-02-12
申请号：US09962189
申请日：2001-09-26
申请人： Tsunetoshi Honma , Yoshiharu Hiramatsu
发明人： Tsunetoshi Honma , Yoshiharu Hiramatsu
IPC分类号： C07D33356
CPC分类号： C07D333/68
摘要： Processes for producing compounds of the formula (VI) are disclosed. Benzothiophenecarboxylic acid derivatives of the formula (I), which are useful as starting materials for producing drugs, are disclosed. Particularly, disclosed is a process for preparing 5-dydroxybenzo[b]-thiophene-3-carboxylic acid derivatives of the formula (VI), which are specific PGD2 antagonists are also disclosed.
摘要翻译：公开了制备式（Ⅵ）化合物的方法。公开了可用作生产药物原料的式（I）的苯并噻吩羧酸衍生物。特别公开的是制备式（VI）的5-二羟基苯并[b] - 噻吩-3-羧酸衍生物的方法，其也是特异性PGD 2拮抗剂。

9. 发明授权

US6083974A Benzothiophenecarboxamide derivatives and PGD.sub.2 antagonists comprising them 有权
标题翻译：苯并噻吩甲酰胺衍生物和包含它们的PGD2拮抗剂
公开(公告)号：US6083974A
公开(公告)日：2000-07-04
申请号：US308176
申请日：1999-05-17
申请人： Tsunetoshi Honma , Yoshiharu Hiramatsu , Akinori Arimura
发明人： Tsunetoshi Honma , Yoshiharu Hiramatsu , Akinori Arimura
IPC分类号： A61K31/381 , A61P9/00 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D333/38 , C07D333/68 , C07D333/70 , A61K31/38 , C07D333/52 , C07D333/56
CPC分类号： C07D333/68 , C07D333/38
摘要： A compound, a pharmaceutically acceptable salt thereof, or a hydrate thereof having PGD.sub.2 -antagonistic activities, inhibitory activities against infiltration of eosinophils, and being useful as a drug for treating diseases, such as systemic mastocytosis and disorder of systemic mast cell activation, as well as tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, ischemic reperfusion injury, inflammation and atopic dermatitis, which is shown by the following formula (I): ##STR1## is provided
摘要翻译： PCT No.PCT / JP97 / 04527 Sec。 371日期1999年5月17日 102（e）日期1999年5月17日PCT 1997年12月10日PCT公布。第WO98 / 25919号公报日期1998年6月18日具有PGD2-拮抗活性的化合物，其药学上可接受的盐或其水合物，对嗜酸性粒细胞浸润的抑制活性，并且可用作治疗疾病的药物，例如全身性肥大细胞增多症和系统性and妄提供下列通式（I）所示的细胞活化以及气管收缩，哮喘，过敏性鼻炎，过敏性结膜炎，荨麻疹，缺血再灌注损伤，炎症和特应性皮炎。

10. 发明授权

US07214832B2 Processes for the preparation of bicyclic aminoalcohols 失效
标题翻译：制备双环氨基醇的方法
公开(公告)号：US07214832B2
公开(公告)日：2007-05-08
申请号：US10784930
申请日：2004-02-25
申请人： Tsunetoshi Honma , Yoshiharu Hiramatsu , Susumu Mitsumori
发明人： Tsunetoshi Honma , Yoshiharu Hiramatsu , Susumu Mitsumori
IPC分类号： C07C45/00
CPC分类号： C07F7/188 , C07B2200/07 , C07C67/343 , C07C213/00 , C07C213/02 , C07C215/42 , C07C249/08 , C07C2602/42 , C07D333/68 , C07D333/70 , C07F7/1804 , C07C69/716 , C07C251/44 , C07C251/50
摘要： The present invention provides a process for the preparation of a bicyclic aminoalcohol which comprises reacting a starting compound, nopinone (I), with XCH2COOR1 wherein X is halogen, and R1 is alkyl, in the presence of an additive and a base to produce a compound (II), converting it to oxime derivative (III), and reducing it with an aluminum hydride
摘要翻译：本发明提供一种双环氨基醇的制备方法，其包括使起始化合物，萘诺酮（I）与XCH 2 COOR 1其中X为卤素，和 R 1是在添加剂和碱的存在下的烷基，以制备化合物（II），将其转化为肟衍生物（III），并用氢化铝

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