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1.发明授权1-Phenyl isoquinoline-5-acetic acid compounds and analgesic compositions thereof 失效1-苯基异喹啉-5-乙酸化合物及其镇痛组合物
公开(公告)号：US4337256A
公开(公告)日：1982-06-29
申请号：US107613
申请日：1979-12-27
申请人： Yasushi Suzuki , Kunio Tsukamoto , Nobuyoshi Minami , Yukio Hasegawa , Michitaka Satoh , Norio Yamamoto , Katsuhiko Miyasaka , Takashi Mikami , Satoshi Funakoshi
发明人： Yasushi Suzuki , Kunio Tsukamoto , Nobuyoshi Minami , Yukio Hasegawa , Michitaka Satoh , Norio Yamamoto , Katsuhiko Miyasaka , Takashi Mikami , Satoshi Funakoshi
IPC分类号： C07D217/02 , A61K31/47 , A61K31/472 , A61P7/02 , A61P25/04 , A61P29/00 , A61P43/00 , C07C233/12 , C07D217/04 , C07D217/12 , C07D217/14 , C07D217/16 , C07D217/26
CPC分类号： C07C255/00 , C07D217/14 , C07D217/16 , C07D217/26
摘要： Novel isoquinoline derivatives of the general formula ##STR1## wherein R represents a lower alkyl group, a lower cycloalkyl group, or a group of the formula ##STR2## in which R.sup.2 represents a hydrogen atom, a halogen atom, a methyl group, a trifluoromethyl group, a methoxy group, a methylamino group or a dimethylami no group;R.sup.1 represents a hydrogen atom or a lower alkyl group; andY represents a carboxyl group, a cyano group, a carbamoyl group, a lower alkoxycarbonyl group or a lower alkylaminocarbonyl group;or a salt thereof; a process for the production thereof.The above compound is useful as an anti-inflammatory and analgesic agent.
摘要翻译： 新的通式为（I）的异喹啉衍生物其中R表示低级烷基，低级环烷基或下式的基团：
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公开(公告)号：US4230703A
公开(公告)日：1980-10-28
申请号：US891112
申请日：1978-03-28
申请人： Yasushi Suzuki , Kunio Tsukamoto , Nobuyoshi Minami , Yukio Hasegawa , Tadaharu Watanabe , Katsuhiko Miyasaka , Takashi Mikami , Satoshi Funakoshi
发明人： Yasushi Suzuki , Kunio Tsukamoto , Nobuyoshi Minami , Yukio Hasegawa , Tadaharu Watanabe , Katsuhiko Miyasaka , Takashi Mikami , Satoshi Funakoshi
IPC分类号： C07D223/20 , A61K31/55
CPC分类号： C07D223/20
摘要： Compounds of the general formula ##STR1## or their salts, esters or amide derivatives; and processes for their preparation. In the formula, R.sub.O represents hydrogen or lower alkyl, R.sub.2 represents hydrogen, halogen or nitro, R.sub.3 represents hydrogen or halogen, and R.sub.4 represents hydrogen or lower alkyl; and when R.sub.O is hydrogen, R.sub.2, R.sub.3 and R.sub.4 are all hydrogens and the group ##STR2## is present at the 2-position. These compounds exhibit superior analgesic and/or anti-inflammatory actions with little gastrointestinal troubles.
摘要翻译： 通式为“IMAGE”的化合物或其盐，酯或酰胺衍生物; 及其制备方法。 在该式中，RO表示氢或低级烷基，R2表示氢，卤素或硝基，R3表示氢或卤素，R4表示氢或低级烷基; 当RO为氢时，R2，R3和R4均为氢，组“IMAGE”存在于2位。 这些化合物表现出优异的止痛和/或抗炎作用，很少有胃肠道麻烦。
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公开(公告)号：US5082844A
公开(公告)日：1992-01-21
申请号：US539741
申请日：1990-06-18
申请人： Kikuo Yasuda , Kenyu Shibata , Nobuyoshi Minami , Toshimi Seki , Masafumi Shiraiwa , Tomio Nakao , Katsuhiko Miyasaka , Tsutomu Ishimori , Kotaro Gotanda , Takako Sasaki
发明人： Kikuo Yasuda , Kenyu Shibata , Nobuyoshi Minami , Toshimi Seki , Masafumi Shiraiwa , Tomio Nakao , Katsuhiko Miyasaka , Tsutomu Ishimori , Kotaro Gotanda , Takako Sasaki
IPC分类号： C07D237/04 , C07D401/12 , C07D403/12
CPC分类号： C07D401/12 , C07D237/04 , C07D403/12
摘要： A pyridazinone compound represented by the general formula ##STR1## wherein Ar is ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 may be identical or different, and each represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, a halogen atom, a cyano group or a nitro group, and R.sup.4 represents a hydrogen atom, a lower alkoxy group, or a lower alkyl group substituted by a lower alkoxy group or a carbamoyl group, and C* is an asymmetric carbon atom, or a salt thereof. This compound is useful for the treatment of diseases of the circulatory system.
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公开(公告)号：US5221674A
公开(公告)日：1993-06-22
申请号：US770288
申请日：1991-09-27
申请人： Kikuo Yasuda , Kenyu Shibata , Nobuyoshi Minami , Toshimi Seki , Masafumi Shiraiwa , Tomio Nakao , Katsuhiko Miyasaka , Tsutomu Ishimori , Kotaro Gotanda , Takako Sasaki
发明人： Kikuo Yasuda , Kenyu Shibata , Nobuyoshi Minami , Toshimi Seki , Masafumi Shiraiwa , Tomio Nakao , Katsuhiko Miyasaka , Tsutomu Ishimori , Kotaro Gotanda , Takako Sasaki
IPC分类号： C07D237/04 , C07D401/12 , C07D403/12
CPC分类号： C07D401/12 , C07D237/04 , C07D403/12
摘要： A pyridazinone compound represented by the general formula ##STR1## wherein Ar is ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 may be identical or different, and each represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, a halogen atom, a cyano group or a nitro group, and R.sup.4 represents a hydrogen atom, a lower alkoxy group, or a lower alkyl group substituted by a lower alkoxy group or a carbamoyl group, and C* is an assymmetric carbon atom,or a salt thereof. This compound is useful for the treatment of diseases of the circulatory system.
摘要翻译： 由通式（I）表示的哒嗪酮化合物，其中Ar是其中R 1，R 2和R 3可以相同或不同，并且各自表示氢原子，低级烷基，三氟甲基 基团，卤素原子，氰基或硝基，R 4表示氢原子，低级烷氧基或被低级烷氧基或氨基甲酰基取代的低级烷基，C *是不对称碳原子 ，或其盐。 该化合物可用于治疗循环系统疾病。
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公开(公告)号：US5130314A
公开(公告)日：1992-07-14
申请号：US770287
申请日：1991-09-27
申请人： Kikuo Yasuda , Kenyu Shibata , Nobuyoshi Minami , Toshimi Seki , Masafumi Shiraiwa , Tomio Nakao , Katsuhiko Miyasaka , Tsutomu Ishimori , Kotaro Gotanda , Takako Sasaki
发明人： Kikuo Yasuda , Kenyu Shibata , Nobuyoshi Minami , Toshimi Seki , Masafumi Shiraiwa , Tomio Nakao , Katsuhiko Miyasaka , Tsutomu Ishimori , Kotaro Gotanda , Takako Sasaki
IPC分类号： C07D237/04 , C07D401/12 , C07D403/12
CPC分类号： C07D401/12 , C07D237/04 , C07D403/12
摘要： A pyridazinone compound represented by the general formula ##STR1## wherein Ar is ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 may be identical or different, and each represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, a halogen atom, a cyano group or a nitro group, and R.sup.4 represents a hydrogen atom, a lower alkoxy group, or a lower alkyl group substituted by a lower alkoxy group or a carbamoyl group, and C* is an assymmetric carbon atom,or a salt thereof. This compound is useful for the treatment of diseases of the circulatory system.
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公开(公告)号：US06667325B1
公开(公告)日：2003-12-23
申请号：US09980579
申请日：2001-12-03
申请人： Nobuyoshi Minami , Michitaka Sato , Koichi Hasumi , Norio Yamamoto , Katsuyuki Keino , Teruaki Matsui , Arihiro Kanada , Shuji Ohta , Takahisa Saito , Shuichiro Sato , Akira Asagarasu , Satoshi Doi , Motohiro Kobayashi , Jun Sato , Hajime Asano
发明人： Nobuyoshi Minami , Michitaka Sato , Koichi Hasumi , Norio Yamamoto , Katsuyuki Keino , Teruaki Matsui , Arihiro Kanada , Shuji Ohta , Takahisa Saito , Shuichiro Sato , Akira Asagarasu , Satoshi Doi , Motohiro Kobayashi , Jun Sato , Hajime Asano
IPC分类号： C07D40104
CPC分类号： C07D231/12 , A61K31/4439 , A61K31/4709 , A61K31/4725 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/14 , C07D405/14 , Y02A50/411
摘要： Substituted pyrazole compounds represented by formula (I), or salts thereof are disclosed, wherein R1 is —CH(OH)—CH(R4)—(A)n—Y, —CH2—CH(R4)—(A)n—Y, —CO—B1—A—Y or the like (wherein A is a lower alkylene; Y is an aryl group which may be substituted, for example, by halogen, or the like; R4 is a hydrogen atom or a lower alkyl group; B1 is —CH(R4)— or —N(R4)—; and n is 0 or 1); R2 is a hydrogen atom, a lower alkyl group which may be substituted by hydroxyl or the like, or an aralkyl group; R3 is a phenyl group which may be substituted by halogen or the like, or a pyridyl group; and Q is a pyridyl or quinolyl group. These substituted pyrazole compounds or their salts have an excellent p38MAP kinase inhibiting effect and are hence useful in the prevention or treatment of tumor necrosis factor &agr;-related diseases, interleukin 1-related diseases, interleukin 6-related diseases or cyclooxygenase II-related diseases.
摘要翻译： 公开了由式（I）表示的取代的吡唑化合物或其盐，其中R 1是-CH（OH）-CH（R 4） - （A）n Y，-CH 2 -CH（R 4） ） - （A）nY，-CO-B 1 -AY等（其中A是低级亚烷基; Y是可以被卤素取代的芳基等; R 4 >是氢原子或低级烷基; B 1是-CH（R 4） - 或-N（R 4） - ，n是0或1）; R 2是氢原子，可以被羟基等取代的低级烷基或芳烷基; R 3是可被卤素等取代的苯基或吡啶基; Q为吡啶基或喹啉基。 这些取代的吡唑化合物或其盐具有优异的p38MAP激酶抑制作用，因此可用于预防或治疗肿瘤坏死因子α相关疾病，白细胞介素1相关疾病，白介素6相关疾病或环加氧酶II相关疾病。
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公开(公告)号：US06511997B1
公开(公告)日：2003-01-28
申请号：US09869051
申请日：2001-06-22
申请人： Nobuyoshi Minami , Michitaka Sato , Koichi Hasumi , Norio Yamamoto , Katsuyuki Keino , Teruaki Matsui , Arihiro Kanada , Shuji Ohta , Takahisa Saito , Shuichiro Sato , Akira Asagarasu , Satoshi Doi , Motohiro Kobayashi , Jun Sato , Hajime Asano
发明人： Nobuyoshi Minami , Michitaka Sato , Koichi Hasumi , Norio Yamamoto , Katsuyuki Keino , Teruaki Matsui , Arihiro Kanada , Shuji Ohta , Takahisa Saito , Shuichiro Sato , Akira Asagarasu , Satoshi Doi , Motohiro Kobayashi , Jun Sato , Hajime Asano
IPC分类号： A61K314409
CPC分类号： C07D401/04 , C07D405/14
摘要： Aminopyrazole derivatives represented by formula (I), or salts thereof, wherein X1 and X2 are each a hydrogen atom or a halogen atom, or X1 and X2 may be united together to form a lower alkylenedioxy group, Q is a pyridyl group or a quinolyl group, R1 is a hydrogen atom, a substituted or unsubstituted lower alkyl or aryl group, R2 is a hydrogen atom, a lower alkyl group, or an aralkyl group, and R3 represents a hydrogen atom, an organic sulfonyl group, or —C(═Y)—R4 in which R4 is a hydrogen atom or an organic residue and Y is an oxygen or sulfur atom, provided that, when R3 is a hydrogen atom, R1 is a group other than a hydrogen atom and R2 is a hydrogen atom. These amimopyrazole derivatives or their salts have excellent p38MAP kinase inhibiting activities and are hence useful in the prevention or treatment of diseases associated with tumor necrosis sis factor &agr;, interleukin 1, interleukin 6 or cyclooxygenase II.
摘要翻译： 式（I）表示的氨基吡唑衍生物或其盐，其中X 1和X 2各自为氢原子或卤素原子，或者X 1和X 2可以一起结合形成低级亚烷基二氧基，Q是吡啶基或喹啉基 基团，R 1是氢原子，取代或未取代的低级烷基或芳基，R 2是氢原子，低级烷基或芳烷基，R 3表示氢原子，有机磺酰基或-C（ = Y）-R4，其中R4为氢原子或有机残基，Y为氧或硫原子，条件是当R3为氢原子时，R1为氢原子以外的基团，R2为氢原子 。 这些酰胺吡唑衍生物或其盐具有优异的p38MAP激酶抑制活性，因此可用于预防或治疗与肿瘤坏死因子α，白细胞介素1，白介素6或环加氧酶II相关的疾病。
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公开(公告)号：US07087624B2
公开(公告)日：2006-08-08
申请号：US10693461
申请日：2003-10-27
申请人： Nobuyoshi Minami , Michitaka Sato , Koichi Hasumi , Norio Yamamoto , Katsuyuki Keino , Teruaki Matsui , Arihiro Kanada , Shuji Ohta , Takahisa Saito , Shuichiro Sato , Akira Asagarasu , Satoshi Doi , Motohiro Kobayashi , Jun Sato , Hajime Asano
发明人： Nobuyoshi Minami , Michitaka Sato , Koichi Hasumi , Norio Yamamoto , Katsuyuki Keino , Teruaki Matsui , Arihiro Kanada , Shuji Ohta , Takahisa Saito , Shuichiro Sato , Akira Asagarasu , Satoshi Doi , Motohiro Kobayashi , Jun Sato , Hajime Asano
CPC分类号： C07D231/12 , A61K31/4439 , A61K31/4709 , A61K31/4725 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/14 , C07D405/14 , Y02A50/411
摘要： Substituted pyrazole compounds represented by formula (I), or salts thereof are disclosed, wherein R1 is —CH(OH)—CH(R4)-(A)n-Y, —CH2—CH(R4)-(A)n-Y, —CO-B1-A-Y or the like (wherein A is a lower alkylene; Y is an aryl group which may be substituted, for example, by halogen, or the like; R4 is a hydrogen atom or a lower alkyl group; B1 is —CH(R4)— or —N(R4)—; and n is 0 or 1); R2 is a hydrogen atom, a lower alkyl group which may be substituted by hydroxyl or the like, or an aralkyl group; R3 is a phenyl group which may be substituted by halogen or the like, or a pyridyl group; and Q is a pyridyl or quinolyl group. These substituted pyrazole compounds or their salts have an excellent p38MAP kinase inhibiting effect and are hence useful in the prevention or treatment of tumor necrosis factor α-related diseases, interleukin 1-related diseases, interleukin 6-related diseases or cyclooxygenase II-related diseases
摘要翻译： 公开了由式（I）表示的取代的吡唑化合物或其盐，其中R 1是-CH（OH）-CH（R 4） - （A） -CH（R 4） - （A）n -Y， - CO（CH 2） -B 1 -I 1等（其中A是低级亚烷基; Y是可以被卤素取代的芳基等）; R 4， SUP>是氢原子或低级烷基; B 1是-CH（R 4） - 或-N（R 4） - ;和n为0或1）; R 2是氢原子，可以被羟基等取代的低级烷基或芳烷基; R 3是可以被卤素等取代的苯基或吡啶基; Q为吡啶基或喹啉基。 这些取代的吡唑化合物或其盐具有优异的p38MAP激酶抑制作用，因此可用于预防或治疗肿瘤坏死因子α相关疾病，白细胞介素1相关疾病，白细胞介素6相关疾病或环氧合酶II相关疾病
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公开(公告)号：US20050267041A1
公开(公告)日：2005-12-01
申请号：US11180582
申请日：2005-07-14
CPC分类号： C07K5/101 , A61K38/00 , C07K5/0205
摘要： The invention provides crystals of N2-(N,N-dimethyl-L-valyl)-N-[(1S, 2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[(2-phenylethyl)amino]propyl]-1-pyrrolidinyl]-1-[(S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide or salts thereof which possess potent antitumor activity and methods for their preparation.
摘要翻译： 本发明提供N 2 - （N，N-二甲基-L-缬氨酰基）-N - [（1S，2R）-2-甲氧基-4 - [（2S）-2- [ （1R，2R）-1-甲氧基-2-甲基-3-氧代-3 - [（2-苯基乙基）氨基]丙基] -1-吡咯烷基] -1 - [（S）-1-甲基丙基] 氧代丁基] -N-甲基-L-缬氨酰胺或其盐，其具有有效的抗肿瘤活性及其制备方法。
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公开(公告)号：US07385029B2
公开(公告)日：2008-06-10
申请号：US11180582
申请日：2005-07-14
CPC分类号： C07K5/101 , A61K38/00 , C07K5/0205
摘要： The invention provides crystals of N2-(N,N-dimethyl-L-valyl)-N-[(1S,2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[(2-phenylethyl)amino]propyl]-1-pyrrolidinyl]-1-[(S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide or salts thereof which possess potent antitumor activity and methods for their preparation.
摘要翻译： 本发明提供N 2 - （N，N-二甲基-L-缬氨酰基）-N - [（1S，2R）-2-甲氧基-4 - [（2S）-2- [ （1R，2R）-1-甲氧基-2-甲基-3-氧代-3 - [（2-苯基乙基）氨基]丙基] -1-吡咯烷基] -1 - [（S）-1-甲基丙基] 氧代丁基] -N-甲基-L-缬氨酰胺或其盐，其具有有效的抗肿瘤活性及其制备方法。
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