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1. 发明授权

US08383839B2 Heterocyclidene acetamide derivative 失效
标题翻译：杂环亚乙酰胺衍生物
公开(公告)号：US08383839B2
公开(公告)日：2013-02-26
申请号：US13008456
申请日：2011-01-18
申请人： Hideharu Uchida , Naoto Kosuga , Tsutomu Satoh , Daido Hotta , Tomoyuki Kamino , Yoshitaka Maeda , Ken-ichi Amano , Yasushige Akada
发明人： Hideharu Uchida , Naoto Kosuga , Tsutomu Satoh , Daido Hotta , Tomoyuki Kamino , Yoshitaka Maeda , Ken-ichi Amano , Yasushige Akada
IPC分类号： C07D313/00 , C07D309/00
CPC分类号： C07D405/12 , C07D215/14 , C07D215/38 , C07D313/08 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： A compound represented by formula (I′): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q′ represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.
摘要翻译：由式（I'）表示的化合物：其中m，n和p各自表示0〜2; q表示0或1; R1表示卤素，烃基，杂环基，烷氧基，烷氧基羰基，氨磺酰基，CN基，NO 2基等; R 2表示卤素，氨基，烃基，芳香族杂环基或氧代基; X 1表示O，-NR 3 - 或-S（O） R 2; X 2表示亚甲基，O，-NR 3 - 或-S（O）r - ; Q'表示杂芳基，杂芳基烷基，取代的芳基或芳烷基; 环或杂芳环;波浪线表示E-异构体或Z-异构体），化合物的盐或化合物或其盐的溶剂合物。药物组合物和瞬时受体电位型I（TRPV1）受体拮抗剂各自含有化合物，化合物的盐和化合物或其盐的溶剂合物中的至少一种作为活性成分。

2. 发明授权

US06956046B2 4-hydroxypiperidine derivatives having analgesic activity 失效
标题翻译：具有止痛活性的4-羟基哌啶衍生物
公开(公告)号：US06956046B2
公开(公告)日：2005-10-18
申请号：US10478845
申请日：2002-05-17
申请人： Ichiro Yamamoto , Kazuyuki Matsuura , Kazuhiro Suzuki , Kazuo Kato , Yasushige Akada , Hidenori Mochizuki , Akihito Shimoi
发明人： Ichiro Yamamoto , Kazuyuki Matsuura , Kazuhiro Suzuki , Kazuo Kato , Yasushige Akada , Hidenori Mochizuki , Akihito Shimoi
IPC分类号： A61P29/00 , C07D211/48 , C07D401/12 , A61K31/44 , A61K31/4412
CPC分类号： C07D401/12 , C07D211/48
摘要： A compound represented by the following Formula (I): (wherein A represents oxygen atom or —NR3— (R3 represents hydrogen atom or lower alkyl group); R1 represents nitro group, lower alkoxycarbonyl group, carbamoyl group unsubstituted or mono- or di-substituted by lower alkyl group, unprotected or protected hydroxyl group, unprotected or protected carboxyl group, lower alkyl group substituted by unprotected or protected hydroxyl group, or tetrazolyl group; and R2 represents hydrogen atom, cyano group or lower alkylsulfonyl group, provided that when A is —NR3—, it is excluded that R1 represents unprotected or protected hydroxyl group or lower alkyl group substituted by unprotected or protected hydroxyl group) or its salt, and method for producing the compound, and a pharmaceutical composition containing the compound as active ingredient.
摘要翻译：由下式（I）表示的化合物：其中A表示氧原子或-NR 3 - （R 3表示氢原子或低级烷基） SUP> 1表示硝基，低级烷氧基羰基，未取代的或被低级烷基单取代或未被保护或被保护的羟基，未被保护或保护的羧基，未被保护或被保护的羟基取代的低级烷基的氨基甲酰基羟基或四唑基; R 2表示氢原子，氰基或低级烷基磺酰基，条件是当A是-NR 3 - 时，排除R 代表未被保护或保护的羟基或被未保护或被保护的羟基取代的低级烷基）或其盐，以及制备该化合物的方法，以及含有该化合物作为活性成分的药物组合物。

3. 发明授权

US07494987B2 Agent for treating respiratory diseases containing 4-hydroxypiperidine derivative as active ingredient 失效
标题翻译：用于治疗含有4-羟基哌啶衍生物作为活性成分的呼吸系统疾病的药剂
公开(公告)号：US07494987B2
公开(公告)日：2009-02-24
申请号：US10536459
申请日：2003-11-25
申请人： Yasushige Akada , Kazuyuki Matsuura
发明人： Yasushige Akada , Kazuyuki Matsuura
IPC分类号： A61K31/397 , C07D205/04
CPC分类号： A61K31/397 , A61K31/40 , A61K31/445 , C07D205/04 , C07D207/12 , C07D211/42 , C07D211/48
摘要： An agent for preventing/treating respiratory diseases contains, as an active ingredient, a compound represented by following Formula (I): wherein A is a group represented by L-W [wherein L is a bond or CH2; and W is O, SOn (wherein n is 0 to 2), or —NR7— (wherein R7 is hydrogen or lower alkyl)]; each of G1 and G2 is (CH2)r (wherein r is 0 to 2), provided that when n is 1, G1 and G2 may be bridged by lower alkylene; Y is a lower alkylene or (substituted) benzylidene; Z is a bond or O, provided that when Z is a bond, Y may form a 5- or 6-membered ring with carbon on the benzene ring; R1 is, for example, NO2, a lower alkoxycarbonyl, (substituted) carbamoyl, (protected) hydroxyl group, (protected) carboxyl, or (protected) N-hydroxycarbamoyl; each of R2 and R3 is hydrogen, halogen, (halogenated) lower alkyl, (halogenated) lower alkoxy or NO2; each of R4 and R5 is, for example, hydrogen, halogen, (halogenated) lower alkyl, (halogenated) lower alkoxy, CN, or lower alkylsulfonyl; and R6 is hydrogen or lower alkyl, a salt thereof or a solvate of them. It has excellent antitussive activity when used as an agent for preventing/treating respiratory diseases such as lung cancer, common cold syndrome, pulmonary tuberculosis, pneumonia, acute bronchitis or chronic bronchitis.
摘要翻译：作为预防/治疗呼吸系统疾病的药剂含有作为活性成分的下述式（I）表示的化合物，其中，A为由L-W表示的基团，[其中L为键或CH2; W为O，SO n（n为0〜2）或-NR 7 - （其中，R 7为氢或低级烷基）]。 G1和G2各自为（CH 2）r（其中r为0至2），条件是当n为1时，G 1和G 2可以被低级亚烷基桥连; Y是低级亚烷基或（取代的）亚苄基; Z是键或O，条件是当Z为键时，Y可以在苯环上与碳形成5-或6-元环; R1是例如NO2，低级烷氧基羰基，（取代的）氨基甲酰基，（被保护的）羟基，（被保护的）羧基或（保护的）N-羟基氨基甲酰基; R2和R3各自为氢，卤素，（卤代）低级烷基，（卤代）低级烷氧基或NO2; R4和R5各自为例如氢，卤素，（卤代）低级烷基，（卤代）低级烷氧基，CN或低级烷基磺酰基; R6是氢或低级烷基，它们的盐或它们的溶剂合物。用作预防/治疗肺癌，普通感冒综合征，肺结核，肺炎，急性支气管炎或慢性支气管炎等呼吸系统疾病的药剂时，具有优异的镇咳活性。

4. 发明授权

US6040331A Nerve cell protective agents 失效
标题翻译：神经细胞保护剂
公开(公告)号：US6040331A
公开(公告)日：2000-03-21
申请号：US11260
申请日：1998-01-30
申请人： Ichiro Yamamoto , Manabu Itoh , Masato Shimojo , Yasunobu Yumiya , Takafumi Mukaihira , Yasushige Akada
发明人： Ichiro Yamamoto , Manabu Itoh , Masato Shimojo , Yasunobu Yumiya , Takafumi Mukaihira , Yasushige Akada
IPC分类号： C07D209/90 , C07D401/04 , C07D491/06 , A61K31/40 , A61K31/425 , C07D403/00 , C07D417/00
CPC分类号： C07D401/04 , C07D209/90 , C07D491/06
摘要： The invention provides novel benzindole derivatives, processes for producing them, as well as a neuroprotective agent, an agent to prevent or treat diseases involving the degeneration, retraction or death of neurons, and an analgesic, each containing the benzindole derivatives as an active ingredient. ##STR1##
摘要翻译： PCT No.PCT / JP97 / 01828 Sec。 371日期1998年1月30日 102（e）1998年1月30日PCT PCT 1997年5月29日PCT公布。出版物WO97 / 45410 PCT 日期1997年12月4日本发明提供新颖的苯并吲哚衍生物，其制备方法以及神经保护剂，预防或治疗涉及神经元变性，缩回或死亡的疾病的试剂，以及各自含有苯并吲哚衍生物作为活性成分。

5. 发明申请

US20110112071A1 NOVEL HETEROCYCLIDENE ACETAMIDE DERIVATIVE 失效
标题翻译：新型异喹喔啉乙酰胺衍生物
公开(公告)号：US20110112071A1
公开(公告)日：2011-05-12
申请号：US13008456
申请日：2011-01-18
申请人： Hideharu UCHIDA , Naoto Kosuga , Tsutomu Satoh , Daido Hotta , Tomoyuki Kamino , Yoshitaka Maeda , Ken-ichi Amano , Yasushige Akada
发明人： Hideharu UCHIDA , Naoto Kosuga , Tsutomu Satoh , Daido Hotta , Tomoyuki Kamino , Yoshitaka Maeda , Ken-ichi Amano , Yasushige Akada
IPC分类号： A61K31/55 , C07D407/12 , A61K31/357 , A61P19/02 , A61P11/06 , A61P13/06 , A61P25/06 , A61P17/06 , A61P3/04 , C07D311/76 , C07D313/08 , C07D405/12 , A61K31/4725 , A61K31/4709 , C07D417/12 , A61K31/428 , C07D413/14 , A61K31/5377 , A61K31/44 , A61K31/335 , C07D401/12
CPC分类号： C07D405/12 , C07D215/14 , C07D215/38 , C07D313/08 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： A compound represented by formula (I′): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q′ represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.
摘要翻译：由式（I'）表示的化合物：其中m，n和p各自表示0〜2; q表示0或1; R1表示卤素，烃基，杂环基，烷氧基，烷氧基羰基，氨磺酰基，CN基，NO 2基等; R 2表示卤素，氨基，烃基，芳香族杂环基或氧代基; X 1表示O，-NR 3 - 或-S（O） R 2; X 2表示亚甲基，O，-NR 3 - 或-S（O）r - ; Q'表示杂芳基，杂芳基烷基，取代的芳基或芳烷基; 环或杂芳环;波浪线表示E-异构体或Z-异构体），化合物的盐或化合物或其盐的溶剂合物。药物组合物和瞬时受体电位型I（TRPV1）受体拮抗剂各自含有化合物，化合物的盐和化合物或其盐的溶剂合物中的至少一种作为活性成分。

6. 发明授权

US07910751B2 Heterocyclidene acetamide derivative 有权
标题翻译：杂环亚乙酰胺衍生物
公开(公告)号：US07910751B2
公开(公告)日：2011-03-22
申请号：US11988659
申请日：2006-07-24
申请人： Hideharu Uchida , Naoto Kosuga , Tsutomu Satoh , Daido Hotta , Tomoyuki Kamino , Yoshitaka Maeda , Ken-ichi Amano , Yasushige Akada
发明人： Hideharu Uchida , Naoto Kosuga , Tsutomu Satoh , Daido Hotta , Tomoyuki Kamino , Yoshitaka Maeda , Ken-ichi Amano , Yasushige Akada
IPC分类号： C07D313/00 , C07D309/00
CPC分类号： C07D405/12 , C07D215/14 , C07D215/38 , C07D313/08 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： A compound represented by formula (I′): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q′ represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.
摘要翻译：由式（I'）表示的化合物：其中m，n和p各自表示0〜2; q表示0或1; R1表示卤素，烃基，杂环基，烷氧基，烷氧基羰基，氨磺酰基，CN基，NO 2基等; R 2表示卤素，氨基，烃基，芳香族杂环基或氧代基; X 1表示O，-NR 3 - 或-S（O） R 2; X 2表示亚甲基，O，-NR 3 - 或-S（O）r - ; Q'表示杂芳基，杂芳基烷基，取代的芳基或芳烷基; 环或杂芳环;波浪线表示E-异构体或Z-异构体），化合物的盐或化合物或其盐的溶剂合物。药物组合物和瞬时受体电位型I（TRPV1）受体拮抗剂各自含有化合物，化合物的盐和化合物或其盐的溶剂合物中的至少一种作为活性成分。

7. 发明申请

US20060040985A1 Therapeutic agent for treating respiratory diseases containing 4-hydroxypiperidine derivative as active ingredient 失效
标题翻译：用于治疗含有4-羟基哌啶衍生物作为活性成分的呼吸系统疾病的治疗剂
公开(公告)号：US20060040985A1
公开(公告)日：2006-02-23
申请号：US10536459
申请日：2003-11-25
申请人： Yasushige Akada , Kazuyuki Matsuura
发明人： Yasushige Akada , Kazuyuki Matsuura
IPC分类号： A61K31/445 , C07D211/54
CPC分类号： A61K31/397 , A61K31/40 , A61K31/445 , C07D205/04 , C07D207/12 , C07D211/42 , C07D211/48
摘要： An agent for preventing/treating respiratory diseases contains, as an active ingredient, a compound represented by following Formula (I): wherein A is a group represented by L-W [wherein L is a bond or CH2; and W is O, SOn (wherein n is 0 to 2), or —NR7— (wherein R7 is hydrogen or lower alkyl)]; each of G1 and G2 is (CH2)r (wherein r is 0 to 2), provided that when n is 1, G1 and G2 may be bridged by lower alkylene; Y is a lower alkylene or (substituted) benzylidene; Z is a bond or O, provided that when Z is a bond, Y may form a 5- or 6-membered ring with carbon on the benzene ring; R1 is, for example, NO2, a lower alkoxycarbonyl, (substituted) carbamoyl, (protected) hydroxyl group, (protected) carboxyl, or (protected) N-hydroxycarbamoyl; each of R2 and R3 is hydrogen, halogen, (halogenated) lower alkyl, (halogenated) lower alkoxy or NO2; each of R4 and R5 is, for example, hydrogen, halogen, (halogenated) lower alkyl, (halogenated) lower alkoxy, CN, or lower alkylsulfonyl; and R6 is hydrogen or lower alkyl, a salt thereof or a solvate of them. It has excellent antitussive activity when used as an agent for preventing/treating respiratory diseases such as lung cancer, common cold syndrome, pulmonary tuberculosis, pneumonia, acute bronchitis or chronic bronchitis.
摘要翻译：作为预防/治疗呼吸系统疾病的药剂含有作为活性成分的下述式（I）表示的化合物：其中，A为L-W所示的基团，[其中L为键或CH 2“ 且W为O，SO n（其中n为0至2）或-NR 7 - （其中R 7为氢或低级烷基）]。 G 1和G 2各自为（CH 2 2）r（其中r为0至2），条件是当n为1时， G 1和G 2可以被低级亚烷基桥连; Y是低级亚烷基或（取代的）亚苄基; Z是键或O，条件是当Z为键时，Y可以在苯环上与碳形成5-或6-元环; 低级烷氧基羰基，（取代的）氨基甲酰基，（保护的）羟基，（被保护的）羧基或（被保护的）N- 羟基氨基甲酰基; R 2和R 3各自为氢，卤素，（卤代）低级烷基，（卤代）低级烷氧基或NO 2。 R 4和R 5各自为例如氢，卤素，（卤代）低级烷基，（卤代）低级烷氧基，CN或低级烷基磺酰基; R 6是氢或低级烷基，它们的盐或它们的溶剂合物。用作预防/治疗肺癌，普通感冒综合征，肺结核，肺炎，急性支气管炎或慢性支气管炎等呼吸系统疾病的药剂时，具有优异的镇咳活性。

8. 发明授权

US06642257B2 Agents for treating neuropathic pain 失效
标题翻译：用于治疗神经性疼痛的药剂
公开(公告)号：US06642257B2
公开(公告)日：2003-11-04
申请号：US09969644
申请日：2001-10-04
申请人： Ichiro Yamamoto , Manabu Itoh , Fumiaki Yamasaki , Yasushige Akada , Yutaka Miyazaki , Shinichi Ogawa
发明人： Ichiro Yamamoto , Manabu Itoh , Fumiaki Yamasaki , Yasushige Akada , Yutaka Miyazaki , Shinichi Ogawa
IPC分类号： A61K3144
CPC分类号： C07D405/06 , C07D211/48 , C07D407/06 , C07D409/06
摘要： The present invention relates to a compound represented by Formula (I) below: (wherein A represents, for example, phenyl group substituted by R1 and R2, or an unsubstituted furyl group or an unsubstitued thienyl group; R1 represents, for example, hydrogen atom, fluorine atom, chlorine atom, trifluoromethyl group, nitro group, cyano group or methyl group while R2 represents, for example, hydrogen atom; R3 represents, for example, hydrogen atom or methyl group; R4 represents, for example, hydrogen atom or methyl group; R5 represents ethoxy group or isopropoxy group; X represents group: —CH(OH)— or methylene group; and Z represents, for example, a single bond or methylene group unsubstituted or substituted by hydroxyl group), and its salts, and medicinal compositions containing, as their active ingredient, the above compound or its salts. The compound of this invention, which is orally applicable, is highly effective for treating neuroapthic pain while presenting with fewer side-effects than do the conventional analgesics.
摘要翻译：本发明涉及由下式（I）表示的化合物：其中A表示例如被R 1和R 2取代的苯基或未取代的呋喃基或未取代的噻吩基; 1表示例如氢原子，氟原子，氯原子，三氟甲基，硝基，氰基或甲基，而R 2表示例如氢原子; R 3表示例如氢原子或甲基; R 4表示例如氢原子或甲基; R 5表示乙氧基或异丙氧基; X表示基团：-CH（OH） - 或亚甲基; Z表示对于例如，未取代或被羟基取代的单键或亚甲基）及其盐，以及含有作为其活性成分的上述化合物或其盐的药物组合物。口服适用的本发明化合物对于治疗神经痛与非常有效，同时具有比常规止痛剂更少的副作用。

9. 发明申请

US20080287428A1 Novel Heterocyclidene Acetamide Derivative 有权
标题翻译：新型杂环亚乙基乙酰胺衍生物
公开(公告)号：US20080287428A1
公开(公告)日：2008-11-20
申请号：US11988659
申请日：2006-07-24
申请人： Hideharu Uchida , Naoto Kosuga , Tsutomu Satoh , Daido Hotta , Tomoyuki Kamino , Yoshitaka Maeda , Ken-ichi Amano , Yasushige Akada
发明人： Hideharu Uchida , Naoto Kosuga , Tsutomu Satoh , Daido Hotta , Tomoyuki Kamino , Yoshitaka Maeda , Ken-ichi Amano , Yasushige Akada
IPC分类号： A61K31/5383 , C07D405/02 , A61K31/4709 , C07D313/08 , A61K31/335 , C07D498/04
CPC分类号： C07D405/12 , C07D215/14 , C07D215/38 , C07D313/08 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： A compound represented by formula (I′): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q′ represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.
摘要翻译：由式（I'）表示的化合物：其中m，n和p各自表示0〜2; q表示0或1; R 1表示卤素，烃基，杂环基，烷氧基，烷氧基羰基，氨磺酰基，CN基，NO 2 2基等; R 2表示卤素，氨基，烃基，芳族杂环基或氧代基; X 1表示O，-NR 3 - 或-S（O）r - ; X 2， SUB>表示亚甲基，O，-NR 3 - 或-S（O）r - ; Q'表示杂芳基，杂芳基烷基，取代的芳基或芳烷基 ;环状部分表示芳基环或杂芳基环;波浪线表示E-异构体或Z-异构体），化合物的盐或化合物或其盐的溶剂合物。药物组合物和瞬时受体电位型I（TRPV1）受体拮抗剂各自含有化合物，化合物的盐和化合物或其盐的溶剂合物中的至少一种作为活性成分。

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