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1. 发明授权

US5714613A Method of producing 2-naphthamide derivative, and compounds for producing 2-naphthamide derivative 失效
标题翻译： 2-萘甲酰胺衍生物的制造方法以及2-萘甲酰胺衍生物的制造方法
公开(公告)号：US5714613A
公开(公告)日：1998-02-03
申请号：US657545
申请日：1996-06-04
申请人： Hiroshi Ikawa , Masato Nishimura
发明人： Hiroshi Ikawa , Masato Nishimura
IPC分类号： C07D213/30 , C07D319/08 , C07D401/12 , C07D405/12 , C07D211/06
CPC分类号： C07D213/30 , C07D319/08 , C07D401/12 , C07D405/12
摘要： A method of producing a 2-naphthamide derivative of formula (I) that can be employed as an antiallergic agent or an agent for curing allergosis, and compounds for producing the 2-naphthamide derivative are provided: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an unsubstituted or substituted aromatic hydrocarbon group, or an unsubstituted or substituted aromatic heterocyclic group; R.sup.3 is an acyl group, an alkoxylcarbonyl group, a substituted carbamoyl group, or an unsubstituted or substituted alkyl group.
摘要翻译：提供了可用作抗过敏剂或用于治疗过敏原的药剂的式（I）的2-萘甲酰胺衍生物的方法和用于制备2-萘甲酰胺衍生物的化合物：其中R1和 R2各自独立地为未取代或取代的芳族烃基，或未取代或取代的芳族杂环基; R3是酰基，烷氧基羰基，取代的氨基甲酰基或未取代或取代的烷基。

2. 发明授权

US6060602A Compounds for producing 2-naphthamide derivative 失效
标题翻译：用于生产2-萘甲酰胺衍生物的化合物
公开(公告)号：US6060602A
公开(公告)日：2000-05-09
申请号：US216852
申请日：1998-12-21
申请人： Hiroshi Ikawa , Masato Nishimura
发明人： Hiroshi Ikawa , Masato Nishimura
IPC分类号： C07D213/30 , C07D319/08 , C07D401/12 , C07D405/12
CPC分类号： C07D213/30 , C07D319/08 , C07D401/12 , C07D405/12
摘要： A method of producing a 2-naphthamide derivative of formula (I) that can be employed as an antiallergic agent or an agent for curing allergosis, and compounds for producing the 2-naphthamide derivative are provided: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an unsubstituted or substituted aromatic hydrocarbon group, or an unsubstituted or substituted aromatic heterocyclic group; R.sup.3 is an acyl group, an alkoxylcarbonyl group, a substituted carbamoyl group, or an unsubstituted or substituted alkyl group.
摘要翻译：提供了可用作抗过敏剂或用于治疗过敏原的药剂的式（I）的2-萘甲酰胺衍生物的制备方法以及用于制备2-萘甲酰胺衍生物的化合物：其中R1和R2各自独立地为未取代的或取代的芳族烃基，或未取代或取代的芳族杂环基; R3是酰基，烷氧基羰基，取代的氨基甲酰基或未取代或取代的烷基。

3. 发明授权

US06812252B2 Acylsulfonamide derivatives 失效
标题翻译：酰基磺酰胺衍生物
公开(公告)号：US06812252B2
公开(公告)日：2004-11-02
申请号：US10335868
申请日：2003-01-03
申请人： Hiroshi Ikawa , Masato Nishimura , Keiji Okada , Takashi Nakamura , Kazuhiro Kojima , Hideki Kosono
发明人： Hiroshi Ikawa , Masato Nishimura , Keiji Okada , Takashi Nakamura , Kazuhiro Kojima , Hideki Kosono
IPC分类号： A61K3118
CPC分类号： C07C311/51 , A61K31/18
摘要： The present invention provides new acylsulfonamide derivatives such as 4-(3-trifluoromethyl)phenylethynyl-N-(2-(5-ketohexanoylamino)sulfonylphenyl)benzamide, 4-(3-trifluoromethyl)phenylethynyl-N-(2-(2-propyloxyacetylamino)sulfonylphenyl)benzamide or analogues thereof. These acylsulfonamide derivatives have a hypoglycemic effect equal to or superior to the effects of the conventional hypoglycemic agents and they are free from the side effects unlike the glitazone compounds.
摘要翻译：本发明提供新的酰基磺酰胺衍生物，例如4-（3-三氟甲基）苯基乙炔基-N-（2-（5-酮基己酰氨基）磺酰基苯基）苯甲酰胺，4-（3-三氟甲基）苯基乙炔基-N-（2-（2-丙氧基乙酰氨基）磺酰苯基）苯甲酰胺或其类似物。这些酰基磺酰胺衍生物具有等于或优于常规降血糖剂的效果的降血糖作用，并且它们与格列酮类化合物不同，没有副作用。

4. 发明授权

US5616711A Methods of producing aminobutene derivatives 失效
标题翻译：生产氨基丁衍生物的方法
公开(公告)号：US5616711A
公开(公告)日：1997-04-01
申请号：US102819
申请日：1993-08-06
申请人： Hiroshi Ikawa , Hajime Matsumoto , Masakatsu Matsumoto , Yasuo Sekine , Masato Nishimura , Akihiko Hosoda
发明人： Hiroshi Ikawa , Hajime Matsumoto , Masakatsu Matsumoto , Yasuo Sekine , Masato Nishimura , Akihiko Hosoda
IPC分类号： C07C215/24 , C07D213/64 , C07D307/38 , C07D309/10 , C07D405/12 , C07D407/12 , C07C233/00 , C07D211/36 , C07D211/68 , C07D217/22
CPC分类号： C07D213/64 , C07C215/24 , C07D307/38 , C07D309/10 , C07D405/12 , C07D407/12
摘要： A method of producing an aminobutene derivative of formula (I) by allowing a butenol derivative of formula (II) to react with an amide derivative of formula (III) is disclosed. The aminobutene derivative of formula (I) can be deprotected to produce an aminobutene derivative of formula (I-1) or an aminobutene derivative of formula (I-2): ##STR1## The aminobutene derivative of formula (I-A) can also be deprotected to produce the aminobutene derivative of formula (I-B). Any or all of the above aminobutene derivatives are useful as intermediates for producing anti-ulcer drugs, and anti-ulcer drugs having an inhibitory effect on gastric acid secretion based on the antagonism against histamine H.sub.2 receptor.
摘要翻译：公开了通过使式（II）的丁烯醇衍生物与式（III）的酰胺衍生物反应来制备式（I）的氨基丁衍生物的方法。式（I）的氨基丁衍生物可以去保护以产生式（I-1）的氨基丁衍生物或式（I-2）的氨基丁衍生物：IA）也可以被去保护以产生式（IB）。任何或所有上述氨基丁衍生物可用作制备抗溃疡药物的中间体，以及基于对组胺H 2受体的拮抗作用对胃酸分泌具有抑制作用的抗溃疡药物。

5. 发明授权

US06555584B1 Acylsulfonamide derivative 失效
标题翻译：酰基磺酰胺衍生物
公开(公告)号：US06555584B1
公开(公告)日：2003-04-29
申请号：US09606191
申请日：2000-06-29
申请人： Hiroshi Ikawa , Masato Nishimura , Keiji Okada , Takashi Nakamura
发明人： Hiroshi Ikawa , Masato Nishimura , Keiji Okada , Takashi Nakamura
IPC分类号： A61K3118
CPC分类号： C07C311/58 , C07C311/51 , C07C311/53 , C07C2601/14
摘要： This invention provides a novel acylsulfonamide derivative which can be used as an ACC activity inhibitor effective for the treatment of visceral fat syndrome that becomes the risk-factor of diseases of adult people such as myocardial infarction, cerebral infarction and diabetes. Particularly, it relates to an acylsulfonamide derivative represented by a general formula 1 wherein R1 is substituted/unsubstituted C2-C12 alkyl or alkoxy group or substituted/unsubstituted C2-C12 alkenyl or alkynyl group, R2 is hydrogen atom, hydroxyl group, mercapto group, substituted/unsubstituted C1-C6 alkoxy or alkylthio group, nitro group, halogen atom, trichloromethyl group, trifluoromethyl group or cyano group, R3 is substituted/unsubstituted C1-C20 alkyl or alkoxy group, substituted/unsubstituted C2-C20 alkenyl or alkynyl group, substituted/unsubstituted aromatic hydrocarbon or aromatic heterocyclic group, substituted amino group, substituted/unsubstituted C2-C20 alkenyloxy or alkynyloxy group or R4O— (wherein R4 is substituted/unsubstituted aromatic hydrocarbon or aromatic heterocyclic group), Y is —CH═CH—, —N═CH—, —CH═N—, sulfur or oxygen, and ring A is aromatic hydrocarbon, aromatic heterocyclic ring or cyclic alkyl group.
摘要翻译：本发明提供一种新的酰基磺酰胺衍生物，其可用作ACC成分抑制剂，其有效治疗成为心肌梗死，脑梗死和糖尿病等成人疾病的风险因素的内脏脂肪综合征。特别涉及由通式1表示的酰基磺酰胺衍生物，其中R1为取代/未取代的C2-C12烷基或烷氧基或取代/未取代的C2-C12烯基或炔基，R2为氢原子，羟基，巯基，取代/未取代的C1-C6 烷氧基或烷硫基，硝基，卤素原子，三氯甲基，三氟甲基或氰基，R 3是取代/未取代的C 1 -C 20烷基或烷氧基，取代/未取代的C 2 -C 20烯基或炔基，取代/未取代的芳烃或芳香族杂环基，取代氨基，取代/未取代的C 2〜C 20烯氧基或炔氧基或R 4 O- （其中R 4为取代/未取代的芳族烃或芳族杂环基），Y为-CH = CH-，-N = CH-，-CH = N-，硫或氧，环A为芳族烃，芳族杂环或环状烷基。

6. 发明授权

US5917046A Method for producing 2-naphthamide derivative, and compounds for producing 2-naphthamide derivative 失效
标题翻译： 2-萘甲酰胺衍生物的制造方法以及2-萘甲酰胺衍生物的制造方法
公开(公告)号：US5917046A
公开(公告)日：1999-06-29
申请号：US868149
申请日：1997-06-03
申请人： Hiroshi Ikawa , Masato Nishimura
发明人： Hiroshi Ikawa , Masato Nishimura
IPC分类号： C07D213/30 , C07D319/08 , C07D401/12 , C07D405/12 , C07D401/10
CPC分类号： C07D213/30 , C07D319/08 , C07D401/12 , C07D405/12
摘要： A method of producing a 2-naphthamide derivative of formula (I) that can be employed as an antiallergic agent or an agent for curing allergosis, and compounds for producing the 2-naphthamide derivative are provided: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an unsubstituted or substituted aromatic hydrocarbon group, or an unsubstituted or substituted aromatic heterocyclic group; R.sup.3 is an acyl group, an alkoxylcarbonyl group, a substituted carbamoyl group, or an unsubstituted or substituted alkyl group.
摘要翻译：提供了可用作抗过敏剂或用于治疗过敏原的药剂的式（I）的2-萘甲酰胺衍生物的制备方法以及用于制备2-萘甲酰胺衍生物的化合物：其中R1和R2各自独立地为未取代的或取代的芳族烃基，或未取代或取代的芳族杂环基; R3是酰基，烷氧基羰基，取代的氨基甲酰基或未取代或取代的烷基。

7. 发明授权

US5276150A 1,4-dihydropyridine derivatives 失效
标题翻译： 1,4-二氢吡啶衍生物
公开(公告)号：US5276150A
公开(公告)日：1994-01-04
申请号：US850201
申请日：1992-03-12
申请人： Hiroshi Ikawa , Akiyoshi Kadoiri , Nobuo Kobayashi , Yasuko Konagai , Yasuo Sekine
发明人： Hiroshi Ikawa , Akiyoshi Kadoiri , Nobuo Kobayashi , Yasuko Konagai , Yasuo Sekine
IPC分类号： C07D211/90 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D473/04 , C07D473/08 , C07D521/00 , C07D217/18 , C07D417/04 , C07D419/04
CPC分类号： C07D231/12 , C07D211/90 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D473/04 , C07D473/08
摘要： 1,4-dihydropyridine derivatives of formula (I): ##STR1## wherein Ar.sup.1 and Ar.sup.2 each represent an unsubstituted or substituted aromatic hydrocarbon or aromatic heterocyclic group; and R.sup.1 represents --CO.sub.2 R.sup.2, --SO.sub.2 R.sup.3, --COR.sup.4, --CON(R.sup.5).sub.2, --CH--or --NO.sub.2 in which R.sup.2 is hydrogen, a straight chain, branched chain or cyclic saturated hydrocarbon group, which may have a substituent or a straight chain, branched chain or cyclic unsaturated hydrocarbon group having 2 to 10 carbon atoms, which may have a substituent, R.sup.3 is an alkyl group having 1 to 4 carbon atoms, R.sup.4 is an alkyl group having 1 to 4 carbon atoms or a phenyl group; and R.sup.5 is an alkyl group having 1 to 4 carbon atoms.
摘要翻译：式（I）的1,4-二氢吡啶衍生物：其中Ar 1和Ar 2各自表示未取代或取代的芳族烃或芳族杂环基; 和R 1表示可以具有取代基的直链，支链或环状饱和烃基的-CO 2 R 2，-SO 2 R 3，-COR 4，-CON（R 5）2，-CH或-NO 2，可以具有取代基的碳原子数为2〜10的直链，支链或支链或环状不饱和烃基，R3为碳原子数1〜4的烷基，R4为碳原子数1〜4的烷基或苯基 ; R5为碳原子数为1〜4的烷基。

8. 发明授权

US06339089B2 Pyrimidine nucleus-containing compound and a medicament containing the same for a blood oxygen partial pressure amelioration, and a method for preparing the same 失效
标题翻译：含有嘧啶核的化合物和含有其的用于血氧分压改善的药物及其制备方法
公开(公告)号：US06339089B2
公开(公告)日：2002-01-15
申请号：US09132706
申请日：1998-08-12
申请人： Yoshiharu Nakashima , Takashi Fujita , Michiyo Hizuka , Hiroshi Ikawa , Toru Hiruma
发明人： Yoshiharu Nakashima , Takashi Fujita , Michiyo Hizuka , Hiroshi Ikawa , Toru Hiruma
IPC分类号： C07D23995
CPC分类号： C07D401/12 , C07D239/95 , C07D405/12 , C07D409/12 , C07D495/04
摘要： A pyrimidine nucleus-containing compound represented by the formula (I): wherein ring A represents the ring of the formula (a): in which R1 is a nitro group, an amino group, a substituted amino group or a halogen atom, or the ring of the formula (b): in which R1′ is the group such as an alkyl group or an alkenyl group; R2 to R5 independently represent the group such as an alkyl group or an alkenyl group; with the proviso that at least one of R2 to R5 is an alkenyl group, or acid addition salts thereof.
摘要翻译：由式（I）表示的含嘧啶核的化合物：其中环A表示式（a）的环：其中R 1为硝基，氨基，取代的氨基或卤素原子，或式（b）的环：其中R1'为烷基或烯基等基团; R2至R5独立地表示烷基或烯基等基团; 条件是R2至R5中的至少一个为烯基，或其酸加成盐。

9. 发明授权

US5859244A 1,4-dihydropyridine derivatives and methods of producing the same 失效
标题翻译： 1,4-二氢吡啶衍生物及其制备方法
公开(公告)号：US5859244A
公开(公告)日：1999-01-12
申请号：US855500
申请日：1997-05-13
申请人： Hiroshi Ikawa , Akiyoshi Kadoiri , Yasuko Konagai , Tetsuaki Yamaura , Noriko Kase
发明人： Hiroshi Ikawa , Akiyoshi Kadoiri , Yasuko Konagai , Tetsuaki Yamaura , Noriko Kase
IPC分类号： A61K31/435 , A61K31/4422 , A61K31/4427 , A61K31/495 , A61P7/02 , A61P9/08 , A61P9/12 , A61P11/08 , A61P25/28 , A61P29/00 , A61P37/08 , C07D211/90 , C07D213/82 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12 , C07D473/08 , C07F7/10 , C07D213/12 , C07D401/04 , C07D403/04
CPC分类号： C07D401/06 , C07D211/90 , C07D213/82 , C07D401/12
摘要： 1,4-dihydropyridine derivatives and optically active 1,4-dihydropyridine derivatives with the following formula, having vasodilating activity based on calcium antagonism, and PAF antaognism, and methods of producing the same are disclosed: ##STR1## wherein (*) indicates a chiral center in the case of the optically active 1,4-dihydropyridine derivatives.
摘要翻译：公开了具有下式的1,4-二氢吡啶衍生物和光学活性的1,4-二氢吡啶衍生物，其具有基于钙拮抗作用的血管舒张活性和PAF抗体，其制备方法：其中（*）表示在光学活性的1,4-二氢吡啶衍生物的情况下手性中心。

10. 发明授权

US4672068A Antihypertensive 1,4-dihydropyridines having a conjugated ester 失效
标题翻译：具有共轭酯的抗高血压1,4-二氢吡啶类
公开(公告)号：US4672068A
公开(公告)日：1987-06-09
申请号：US727692
申请日：1985-04-26
申请人： Teruo Kutsuma , Hiroshi Ikawa , Yoshiaki Sato
发明人： Teruo Kutsuma , Hiroshi Ikawa , Yoshiaki Sato
IPC分类号： C07D211/90 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , A61K31/455
CPC分类号： C07D401/04 , C07D211/90 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12
摘要： 1,4-dihydropyridine derivatives represented by the following general formula, ##STR1## in which R.sup.3 is a combination of an unsaturated straight chain hydrocarbon group or derivative thereof connected by a single bond with an unsaturated hydrocarbon group or derivative thereof so that the unsaturated carbon atoms of the two groups are in conjugated relationship. These compounds have a hypotensive action the effective time of which is long, which makes the blood pressure descend slowly, and the toxicity of which is low.
摘要翻译：由以下通式表示的1,4-二氢吡啶衍生物，其中R3是通过单键与不饱和烃基或其衍生物连接的不饱和直链烃基或其衍生物的组合，使得不饱和碳两组原子呈共轭关系。这些化合物具有降血压作用，其有效时间长，这使得血压下降缓慢，其毒性低。

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