公开(公告)号：US4978758A

公开(公告)日：1990-12-18

申请号：US355624

申请日：1989-05-23

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai ,  Ryoichi Unno ,  Hiroshi Ozawa ,  Masato Fukushima

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai ,  Ryoichi Unno ,  Hiroshi Ozawa ,  Masato Fukushima

IPC分类号： C07D311/24 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10

CPC分类号： C07D491/10 ,  C07D311/24 ,  C07D495/10

摘要： Hydantoin derivatives and salts thereof, intermediates therefor, process for the preparation thereof, and medicines containing the derivative, wherein said derivatives have the formula ##STR1## wherein one of V and W is hydrogen and the other is a halogenomethyl group, 1H-tetrazol-5-yl radical, --COOR group,in which R is hydrogen atom, an alkyl group, --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n is an integer of 1 to 113) or substituted phenyl, ##STR2## group, in which R.sub.1 and R.sub.2 are same or different independently, each is hydrogen atom, an alkyl group, substituted phenyl or --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n has the meaning as referred to) or R.sub.1 may form a heterocyclic ring together with R.sub.2 and nitrogen or oxygen atom, --CH.sub.2 OR.sub.3 group or ##STR3## group, in which R.sub.3 and R.sub.4 are same or different independently and each is hydrogen atom or an alkyl group,X is oxygen or sulfur atom, and Y and Z are same or different independently and each is hydrogen atom, a halogen atom, alkyl group, alkoxy group, alkylmercapto group, nitro radical or --NHR.sub.5 group, in which R.sub.5 is hydrogen atom or an acyl group.The derivatives and salts thereof are useful for the treatment of complications of diabetes.

公开(公告)号：US4985573A

公开(公告)日：1991-01-15

申请号：US355623

申请日：1989-05-23

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai ,  Ryoichi Unno ,  Hiroshi Ozawa ,  Masato Fukushima

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai ,  Ryoichi Unno ,  Hiroshi Ozawa ,  Masato Fukushima

IPC分类号： C07D311/24 ,  C07D491/10 ,  C07D495/10

CPC分类号： C07D491/10 ,  C07D311/24 ,  C07D495/10

摘要： Hydantoin derivatives and salts thereof, intermediates therefor, process for the preparation thereof, and medicines containing the derivative, wherein said derivatives have the formula ##STR1## wherein one of V and W is hydrogen and the other is a halogenomethyl group, 1H-tetrazol-5-yl radical, --COOR group, in which R is hydrogen atom, an alkyl group, --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n is an integer of 1 to 113) or substituted phenyl, ##STR2## in which R.sub.1 and R.sub.2 are same or different independently, each is hydrogen atom, an alkyl group, substituted phenyl or --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n has the meaning as referred to) or R.sub.1 may form a heterocyclic ring together with R.sub.2 and nitrogen or oxygen atom, ##STR3## in which R.sub.3 and R.sub.4 are same or different independently and each is hydrogen atom or an alkyl group,X is oxygen or sulfur atom, and Y and Z are same or different independently and each is hydrogen atom, a halogen atom, alkyl group, alkoxy group, alkylmercapto group, nitro radical or --NHR.sub.5 group, in which R.sub.5 is hydrogen atom or an acyl group.The derivatives and salts thereof are useful for the treatment of complications of diabetes.

摘要翻译： 乙内酰脲衍生物及其盐，其中间体，其制备方法和含有该衍生物的药物，其中所述衍生物具有式“IMAGE”，其中V和W之一是氢，另一个是卤代甲基，1H-四唑 - 其中R为氢原子，烷基， - （CH 2 CH 2 O）n CH 3基（n为1至113的整数）或取代的苯基，其中R 1和R 2相同的-COOR基团 或独立地不同，各自为氢原子，烷基，取代的苯基或 - （CH 2 CH 2 O）n CH 3基团（n具有所述的含义）或R 1可以与R 2和氮或氧原子一起形成杂环， 其中R3和R4独立地相同或不同，各自为氢原子或烷基，X为氧或硫原子，Y和Z独立地相同或不同，各自为氢原子，卤素原子，烷基，烷氧基 基团，烷基巯基，硝基或-NHR 5基团 ch R5是氢原子或酰基。 其衍生物和盐可​​用于治疗糖尿病并发症。

公开(公告)号：US5001240A

公开(公告)日：1991-03-19

申请号：US507608

申请日：1990-04-12

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai

IPC分类号： C07D311/24 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10

CPC分类号： C07D491/10 ,  C07D311/24 ,  C07D495/10

摘要： Hydantoin derivatives and salts thereof, intermediates therefor, process for the preparation thereof, and medicines containing the derivatives, wherein said derivatives have the formula ##STR1## wherein one of V and W is hydrogen and the other is a halogenomethyl group, 1H-tetrazol-5-yl radical, --COOR group,in which R is hydrogen atom, an alkyl group, --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n is an integer of 1 to 113) or substituted phenyl, ##STR2## group, in which R.sub.1 and R.sub.2 are same or different independently, each is hydrogen atom, an alkyl group, substituted phenyl or --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n has the meaning as referred to) or R.sub.1 may form a heterocyclic ring together with R.sub.2 and nitrogen or oxygen atom, --CH.sub.2 OR.sub.3 group or ##STR3## group, in which R.sub.3 and R.sub.4 are same or different independently and each is hydrogen atom or an alkyl group,X is oxygen or sulfur atom, and Y and Z are same or different independently and each is hydrogen atom, a halogen atom, alkyl group, alkoxy group, alkylmercapto group, nitro radical or --NHR.sub.5 group, in which R.sub.5 is hydrogen atom or an acyl group.The derivatives and salts thereof are useful for the treatment of complications of diabetes.

公开(公告)号：US4861792A

公开(公告)日：1989-08-29

申请号：US90729

申请日：1987-08-28

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai ,  Ryoichi Unno ,  Hiroshi Ozawa ,  Masato Fukushima

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai ,  Ryoichi Unno ,  Hiroshi Ozawa ,  Masato Fukushima

IPC分类号： C07D311/24 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10

CPC分类号： C07D491/10 ,  C07D311/24 ,  C07D495/10

摘要： Hydantoin derivatives and salts thereof, intermediates therefor, process for the preparation thereof, and medicines containing the derivative, wherein said derivatives have the formula ##STR1## wherein one of V and W is hydrogen and the other is a halogenomethyl group, 1H-tetrazol-5-yl radical, --COOR group,in which R is hydrogen atom, an alkyl group, --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n is an integer of 1 to 113) or substituted phenyl, ##STR2## in which R.sub.1 and R.sub.2 are same or different independently, each is hydrogen atom, an alkyl group, substituted phenyl or --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n has the meaning as referred to) or R.sub.1 may form a heterocyclic ring together with R.sub.2 and nitrogen or oxygen atom, ##STR3## in which R.sub.2 and R.sub.4 are same or different independently and each is hydrogen atom or an alkyl group,X is oxygen or sulfur atom, and Y and Z are same or different independently and each is hydrogen atom, a halogen atom, alkyl group, alkoxy group, alkylmercapto group, nitro radical or --NHR.sub.5 group, in which R.sub.5 is hydrogen atom or an acyl group.The derivatives and salts thereof are useful for the treatment of complications of diabetes.

公开(公告)号：US5447946A

公开(公告)日：1995-09-05

申请号：US311005

申请日：1994-09-23

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai ,  Ryoichi Unno ,  Hiroshi Ozawa ,  Masato Fukushima

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai ,  Ryoichi Unno ,  Hiroshi Ozawa ,  Masato Fukushima

IPC分类号： C07D311/24 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10 ,  A61K31/415 ,  C07D405/02

CPC分类号： C07D491/10 ,  C07D311/24 ,  C07D495/10

摘要： Hydantoin derivatives and salts thereof, intermediates therefor, process for the preparation thereof, and medicines containing the derivative, wherein said derivatives have the formula ##STR1## wherein one of V and W is hydrogen and the other is a halogenomethyl group, 1H-tetrazol-5-yl radical, --COOR group,in which R is hydrogen atom, an alkyl group, --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n is an integer of 1 to 113) or substituted phenyl, ##STR2## in which R.sub.1 and R.sub.2 are same or different independently, each is hydrogen atom, an alkyl group, substituted phenyl or --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n has the meaning as referred to) or R.sub.1 may form a heterocyclic ring together with R.sub.2 and nitogen or oxygen atom,--CH.sub.2 OH.sub.3 group or ##STR3## group, in which R.sub.3 and R.sub.4 are same or different independently and each is hydrogen atom or an alkyl group,X is oxygen or sulfur atom, and Y and Z are same or different independently and each is hydrogen atom, a halogen atom, alkyl group, alkoxy group, alkylmercapto group, nitro radical or --NHR.sub.5 group, in which R.sub.5 is hydrogen atom or an acyl group.The derivatives and salts thereof are useful for the treatment of complications of diabetes.

摘要翻译： 乙内酰脲衍生物及其盐，其中间体，其制备方法和含有该衍生物的药物，其中所述衍生物具有下式的化合物：其中V和W之一是氢，另一个是卤代甲基，1H-四唑 - 其中R为氢原子，烷基， - （CH 2 CH 2 O）n CH 3基（n为1至113的整数）或取代的苯基，其中R 1和R 2相同的-COOR基团 或独立地不同，各自为氢原子，烷基，取代的苯基或 - （CH 2 CH 2 O）n CH 3基（n具有所述的含义）或R 1可以与R 2和硝基或氧原子一起形成杂环，-CH 2 OH 3基 或基，其中R3和R4独立地相同或不同，各自为氢原子或烷基，X为氧或硫原子，Y和Z各自独立地相同或不同，各自为氢原子，卤素 原子，烷基，烷氧基，烷基巯基，硝基 或-NHR 5基团，其中R 5是氢原子或酰基。 其衍生物和盐可​​用于治疗糖尿病并发症。

公开(公告)号：US4985574A

公开(公告)日：1991-01-15

申请号：US440135

申请日：1989-11-22

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai ,  Ryoichi Unno ,  Hiroshi Ozawa ,  Masato Fukushima

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai ,  Ryoichi Unno ,  Hiroshi Ozawa ,  Masato Fukushima

IPC分类号： C07D311/24 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10

CPC分类号： C07D491/10 ,  C07D311/24 ,  C07D495/10

摘要： Hydantoin derivatives and salts thereof, intermediates therefor, process for the preparation thereof, and medicines containing the derivative, wherein said derivatives have the formula ##STR1## wherein one of V and W is hydrogen and the other is a halogenomethyl group, 1H-tetrazol-5-yl radical, --COOR group, in which R is hydrogen atom, an alkyl group, --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n is an integer of 1 to 113) or substituted phenyl, ##STR2## in which R.sub.1 and R.sub.2 are same or different independently, each is hydrogen atom, an alkyl group, substituted phenyl or --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n has the meaning as referred to) or R.sub.1 may form a heterocyclic ring together with R.sub.2 and nitogen or oxygen atom, ##STR3## in which R.sub.3 and R.sub.4 are same or different independently and each is hydrogen atom or an alkyl group,X is oxygen or sulfur atom, and Y and Z are same or different independently and each is hydrogen atom, a halogen atom, alkyl group, alkoxy group, alkylmercapto group, nitro radical or --NHR.sub.5 group, in which R.sub.5 is hydrogen atom or an acyl group.The derivatives and salts thereof are useful for the treatment of complications of diabetes.

公开(公告)号：US5171865A

公开(公告)日：1992-12-15

申请号：US664686

申请日：1991-03-05

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Kenji Miura ,  Toshinao Usui ,  Ryoichi Unno ,  Takuji Kakigami ,  Kiichi Sawai

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Kenji Miura ,  Toshinao Usui ,  Ryoichi Unno ,  Takuji Kakigami ,  Kiichi Sawai

IPC分类号： C07C59/68 ,  C07D311/24

CPC分类号： C07D311/24 ,  C07C59/68

摘要： A process for the preparation of optically active 4-oxo-1-benzopyran-2-carboxylic acid derivatives of the formula ##STR1## wherein X and Y are hydrogen atom, halogen atom or alkyl group, and R.sub.1 is hydrogen atom or alkyl group,intermediates thereof, as well as a process for the preparation of the intermediates.

摘要翻译： 制备下式的光学活性4-氧代-1-苯并吡喃-2-羧酸衍生物的方法，其中X和Y是氢原子，卤素原子或烷基，R 1是氢原子或烷基， 其中间体，以及制备中间体的方法。

公开(公告)号：US5036080A

公开(公告)日：1991-07-30

申请号：US331329

申请日：1989-03-31

申请人： Masayasu Kurono ,  Toshinao Usui ,  Kenji Miura ,  Yasuaki Kondo ,  Kiichi Sawai

发明人： Masayasu Kurono ,  Toshinao Usui ,  Kenji Miura ,  Yasuaki Kondo ,  Kiichi Sawai

IPC分类号： C07D405/04 ,  A61K31/415 ,  A61K31/4188 ,  A61P3/08 ,  A61P3/10 ,  A61P13/02 ,  A61P15/00 ,  A61P25/02 ,  A61P27/02 ,  A61P43/00 ,  C07D491/10 ,  C07D491/107

CPC分类号： C07D491/10

摘要： Hydantoin derivatives of the formula ##STR1## wherein Ra and Rb are same or different, each being hydrogen atom, alkanoyl, substituted or none-substituted aroyl, heteroaroyl, alkoxycarbonyl, substituted or none-substituted aralkoxycarbonyl, aryloxycarbonyl, N-alkylcarbamoyl, N,N-dialkylcarbamoyl, substituted or none-substituted N-aralkylcarbamoyl, alkoxyalkyl, 1-(acyloxy)-alkyl, alkylmercapto, substituted or none-substituted arylmercapto, alkylsulfinyl, substituted or none-substituted arylsulfinyl, alkylsulfonyl or substituted or none-substituted arylsulfonyl, but both of Ra and Rb do not concurrently mean hydrogen atom,a process for the preparation of the derivatives, and use thereof as an agent for preventing and curing chronic complications due to diabetes.

公开(公告)号：US5164391A

公开(公告)日：1992-11-17

申请号：US582039

申请日：1990-09-13

申请人： Masayasu Kurono ,  Ryoichi Unno ,  Hiromoto Kimura ,  Noboru Tomiya ,  Kiichi Sawai ,  Kenji Miura ,  Toshinao Usui ,  Yasuaki Kondo ,  Yukiya Tanaka ,  Shigeyoshi Nakamura ,  Tsunemasa Suzuki ,  Motohide Hayashi

发明人： Masayasu Kurono ,  Ryoichi Unno ,  Hiromoto Kimura ,  Noboru Tomiya ,  Kiichi Sawai ,  Kenji Miura ,  Toshinao Usui ,  Yasuaki Kondo ,  Yukiya Tanaka ,  Shigeyoshi Nakamura ,  Tsunemasa Suzuki ,  Motohide Hayashi

IPC分类号： C07D491/10 ,  C07D491/107 ,  C07D495/10

CPC分类号： C07D491/10 ,  C07D495/10

摘要： The invention relates to a hydantoin derivative, salt thereof, process for the preparation thereof, and medicine containing the derivative. The derivative is represented by the formula ##STR1## wherein M is --CONH--NHR.sup.1 group, --CONH--OR.sup.2 group, ##STR2## in which R.sup.1 is hydrogen atom, an alkyl group, an alkenyl group, a phenyl radical, a substituted phenyl group, a naphthyl radical, a substituted naphthyl group, a pyridyl radical, a furyl radical or a thienyl radical, R.sup.2 is a hydrogen atom, an alkyl group, a phenyl radical or a substituted phenyl group, R.sup.3 and R.sup.4 are the same or different independently, each being a phenyl radical, or an aralkyl group, or R.sup.3 may form a substituted or non-substituted C.sub.5-6 saturated heterocyclic ring together with R.sup.4 and a possible nitrogen or oxygen atom, R.sup.5 forms a substituted or non-substituted saturated heterocyclic ring together with R.sup.6 and a possible nitrogen or oxygen atom, R.sup.7 is a nitroxy radical or a heteroaryl group, .sub.m and .sub.n are an integer of 2 to 5, Q is a hydrogen atom or ##STR3## in which R.sup.8 and R.sup.9 are the same or different independently, each being a substituted or non-substituted alkyl group, or R.sup.8 may form a substituted or non-substituted C.sub.5-6 saturated heterocyclic ring together with R.sup.9 and a possible nitrogen or oxygen atom, .sub.r is an integer of 2 to 5, T and X are the same or different independently, each being a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or an alkylmercapto group, and Z is an oxygen or sulfur atom.The derivatives and salts thereof are useful for the treatment of complications of diabetes and circulatory diseases.

公开(公告)号：US4740517A

公开(公告)日：1988-04-26

申请号：US835823

申请日：1986-03-03

申请人： Masayasu Kurono ,  Takuji Yamaguchi ,  Toshinao Usui ,  Masato Fukushima ,  Kuniharu Mizuno ,  Akira Matsubara

发明人： Masayasu Kurono ,  Takuji Yamaguchi ,  Toshinao Usui ,  Masato Fukushima ,  Kuniharu Mizuno ,  Akira Matsubara

IPC分类号： A61K31/415 ,  A61K31/425 ,  A61P3/08 ,  A61P3/10 ,  A61P25/02 ,  A61P43/00 ,  C07D335/00 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10 ,  C07D513/10 ,  C12N9/99

CPC分类号： C07D491/10 ,  C07D495/10 ,  C07D513/10

摘要： A spiro-3-heteroazolidine compound and agents comprising that compound which have special utility as an antidiabetic composition and as a substance to inhibit aldose reductase enzyme activity.

摘要翻译： 螺-3-异恶唑烷化合物和包含具有作为抗糖尿病组合物的特殊用途的化合物和抑制醛糖还原酶活性的物质的药剂。