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1. 发明申请

WO1995029910A1 IMIDAZOLIDINEDIONE DERIVATIVE 审中-公开
标题翻译：咪唑啉酮衍生物
公开(公告)号：WO1995029910A1
公开(公告)日：1995-11-09
申请号：PCT/JP1995000817
申请日：1995-04-26
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , NODA, Ichio , IWATA, Masahiro , MORITA, Takuma , KOSHIYA, Kazuo , SAKAMOTO, Syuichi , KIMURA, Takenori , MURAKAMI, Takeshi
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D403/10
CPC分类号： C07D409/06 , C07D233/76 , C07D233/78 , C07D233/96
摘要： An imidazolidinedione derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, each having an anti-PCP(phencyclidine) effect and being useful as a psychotropic drug, etc. In said formula, n represents an integer of 2 to 9; A represents lower alkylene; ring B represents thiophene or benzene; R and R represent each independently hydrogen, or (un)substituted lower alkyl or aralkyl; R represents hydrogen or hydroxy; R represents hydrogen, lower alkyl, hydroxy, lower alkoxy or lower alkoxy-lower alkoxy; and symbol ----- represents a single or double bond.
摘要翻译：由通式（I）表示的咪唑烷二酮衍生物或其药学上可接受的盐各自具有抗PCP（phenycclidine）作用，可用作精神药物等。在所述式中，n表示2至9的整数; A代表低级亚烷基; 环B表示噻吩或苯; R 1和R 2各自独立地表示氢，或（un）取代的低级烷基或芳烷基; R 3表示氢或羟基; R 4表示氢，低级烷基，羟基，低级烷氧基或低级烷氧基 - 低级烷氧基; 符号 ----- 表示单键或双键。

2. 发明申请

WO1994025450A1 SERINE DERIVATIVE 审中-公开
标题翻译：丝氨酸衍生物
公开(公告)号：WO1994025450A1
公开(公告)日：1994-11-10
申请号：PCT/JP1994000697
申请日：1994-04-26
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , NODA, Ichio , IWATA, Masahiro , SAKAMOTO, Shuichi , KOSHIYA, Kazuo , MORITA, Takuma , KOHARA, Atsuyuki
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D307/52
CPC分类号： C07D409/06 , C07D307/52 , C07D307/54 , C07D333/20 , C07D333/24 , Y02P20/55
摘要： A serine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, having an anti-PCP(phencyclidine) activity and being useful as a psychotropic, wherein X represents sulfur or oxygen; Y represents nitrogen or CH; R and R represent each independently hydrogen, lower alkyl or an amino-protecting group, or R and R may be combined together to form 4- to 9-membered nitrogenous cycloalkyl; R represents hydrogen, carboxy, protected carboxy, aralkyl, or lower alkyl which may be hydroxylated; R represents hydrogen or hydroxy; R represents hydrogen or lower alkyl; A represents lower alkylene; B represents (1) an (un)saturated 4- to 10-membered nitrogenous cycloalkyl group which may be substituted by lower alkyl or aralkyl, or (2) a bicyclic nitrogenous hydrocarbon ring group comprising a 4- to 8-membered nitrogenous cycloalkyl group and a benzene ring fused together; and . &cir& _. &cir& _. &cir& _ represents a single or a double bond.
摘要翻译：由通式（I）表示的丝氨酸衍生物或其药学上可接受的盐，具有抗PCP（苯环利定）活性，可用作精神药物，其中X表示硫或氧; Y表示氮或CH; R 1和R 2各自独立地表示氢，低级烷基或氨基保护基，或者R 1和R 2可以组合在一起形成4-至9-元含氮环烷基; R 3表示氢，羧基，保护的羧基，芳烷基或可被羟基化的低级烷基; R 4表示氢或羟基; R 5表示氢或低级烷基; A表示低级亚烷基; B表示（1）可被低级烷基或芳烷基取代的（未）饱和的4-至10-元含氮环烷基，或（2）包含4-至8-元含氮环烷基的双环含氮环烃基和苯环稠合在一起; 和。＆cir＆_。＆cir＆_。＆cir＆_代表单一或双重债券。

3. 发明申请

WO1998000420A1 NOVEL THIOPHENE DERIVATIVES AND DRUG COMPOSITIONS CONTAINING THE SAME 审中-公开
标题翻译：新型噻吩衍生物和含有它们的药物组合物
公开(公告)号：WO1998000420A1
公开(公告)日：1998-01-08
申请号：PCT/JP1997002255
申请日：1997-06-30
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , KIMURA, Takenori , MURAKAMI, Takeshi , OHMORI, Junya , MORITA, Takuma , TSUKAMOTO, Shin-ichi
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D333/24
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D333/24 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： Thiophene derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds act as an anti-PCP agonist, thus being useful as psychotropic or antischizophrenic agents and so on. In said formula R1 is -A1-X1-R3; R2 is -A2-X2-R4 or nil; B is a four- to ten-membered nitrogenous cycloalkyl or a five- or six-membered nitrogenous unsaturated heterocycle; Ar is aryl or heteroaryl; A1, A2 and A3 are each independently a bond or lower alkylene; X1 and X2 are each independently a bond, -O-, -S- or the like; and R3 and R4 are each independently hydrogen, cyclic imido, lower alkyl, cycloalkyl, aryl or aralkyl, with the provisos that when Ar is a thiazole ring, at least either of A1 and A2 is lower alkylene and that when Ar is a benzene ring, compounds wherein one of R1 and R2 is methyl or halogeno and the other thereof is hydrogen are excepted.
摘要翻译：通式（I）的噻吩衍生物及其药学上可接受的盐。这些化合物作为抗PCP激动剂，因此可用作精神药物或抗精神分裂药剂等。在所述式中，R1是-A1-X1-R3; R2是-A2-X2-R4或nil; B是4至10元含氮环烷基或5或6元含氮不饱和杂环; Ar是芳基或杂芳基; A1，A2和A3各自独立地为键或低级亚烷基; X 1和X 2各自独立地为键，-O-，-S-等; 并且R 3和R 4各自独立地为氢，环状亚氨基，低级烷基，环烷基，芳基或芳烷基，条件是当Ar为噻唑环时，A1和A2中的至少一个为低级亚烷基，当Ar为苯环时，其中R1和R2之一是甲基或卤代，另一个是氢的化合物除外。

4. 发明申请

WO1993020053A1 PYRIDYLSERINE DERIVATIVE 审中-公开
标题翻译：吡啶衍生物
公开(公告)号：WO1993020053A1
公开(公告)日：1993-10-14
申请号：PCT/JP1993000356
申请日：1993-03-25
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , SAKAMOTO, Shuichi , NODA, Ichio , KONDOH, Yutaka , KOSHIYA, Kazuo , HIDAKA, Kazuyuki
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D213/55
CPC分类号： C07D249/08 , C07D213/55 , C07D231/12 , C07D233/56 , C07D401/06 , C07D401/12 , Y02P20/55
摘要： A pyridylserine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, wherein R represents hydrogen or an amino-protecting group, R represents hydrogen or a carboxyl-protecting group, A represents a single bond or lower alkylene, B represents -NR R , or mercapto which may be substituted by lower alkyl or cycloalkyl, R and R may be the same or different from each other and each represents hydrogen; a lower alkyl group which may be substituted by amino, lower alkylamino or carbocyclic aryl; an acyl group which may be substituted by amino; an aminocarbonyl group which may be substituted by lower alkyl or cycloalkyl; lower alkoxycarbonyl; cycloalkylcarbonyl; a nitrogenous heterocyclic group; or alternatively, R and R may be combined together to represent a nitrogenous heterocyclic group, a fused nitrogenous heterocyclic group or a cross-linked nitrogenous heterocyclic group. It has an anti-PCP effect and is useful as a psychotropic.
摘要翻译：由通式（I）表示的吡啶基丝氨酸衍生物或其药学上可接受的盐，其中R 1表示氢或氨基保护基，R 2表示氢或羧基保护基，A表示单键或低级亚烷基，B表示-NR 3 R 4或可被低级烷基或环烷基取代的巯基，R 3和R 4可以彼此相同或不同，各自表示氢; 可被氨基，低级烷基氨基或碳环芳基取代的低级烷基; 可被氨基取代的酰基; 可被低级烷基或环烷基取代的氨基羰基; 低级烷氧基羰基; 环烷基; 含氮杂环基; 或者R 3和R 4可以组合在一起以表示含氮杂环基，稠合杂环基或交联的含氮杂环基。它具有抗PCP作用，可作为精神药物使用。

5. 发明申请

WO1992013828A1 NOVEL BENZANILIDE DERIVATIVE OR SALT THEREOF 审中-公开
标题翻译：新的苯甲酰胺衍生物或其盐
公开(公告)号：WO1992013828A1
公开(公告)日：1992-08-20
申请号：PCT/JP1992000121
申请日：1992-02-06
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , MASE, Toshiyasu , IGARASHI, Susumu , NODA, Ichio , KIMURA, Takenori , KOUTOKU, Hiroshi
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07C235/56
CPC分类号： C07C235/64 , C07C235/56
摘要： A benzanilide derivative represented by general formula (I), which has a testosterone 5 alpha reductase inhibitory activity, a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and a process for producing the same.
摘要翻译：由通式（I）表示的具有睾酮5α还原酶抑制活性的苯甲酰苯胺衍生物及其药学上可接受的盐，其药物组合物及其制备方法。

6. 发明申请

WO1998001133A1 BONE RESORPTION INHIBITORS 审中-公开
标题翻译：骨质内分泌抑制剂
公开(公告)号：WO1998001133A1
公开(公告)日：1998-01-15
申请号：PCT/JP1997002357
申请日：1997-07-08
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , AIBE, Kazuhiko , TAKEBAYASHI, Yukihiro , ISHII, Yasutaka , NOSHIRO, Osamu , NODA, Ichio , IGARASHI, Susumu
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/40
CPC分类号： C07K5/06165 , C07D207/16 , Y02P20/55
摘要： Drugs, in particular, bone resorption inhibitors containing as the active ingredient compounds having selective cathepsin K inhibitory effects, among all, proline derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof, wherein each symbol has the meaning as specified below: X: a moiety (except for the C-terminal carbonyl group) of an amino acid residue with its side chain optionally protected; R : an amino-protective group; G: a glycine residue; n: 0 or 1; R : a group inhibiting the activity of the SH group of cysteine protease; and R : hydrogen, hydroxy or phenyl.
摘要翻译：药物，特别是包含具有选择性组织蛋白酶K抑制作用的活性成分化合物的骨吸收抑制剂，其中包括由通式（I）表示的脯氨酸衍生物或其药学上可接受的盐，其中每个符号具有以下指定的含义：X ：氨基酸残基的一部分（C端羰基除外），其侧链任选被保护; R 1：氨基保护基; G：甘氨酸残基; n：0或1; R 3：抑制半胱氨酸蛋白酶SH基的活性的基团; 和R 4：氢，羟基或苯基。

7. 发明申请

WO1995002407A1 NEURON PROTECTIVE AND NOVEL OROTIC ESTER 审中-公开
标题翻译：神经保护和新型OROTIC ESTER
公开(公告)号：WO1995002407A1
公开(公告)日：1995-01-26
申请号：PCT/JP1994001134
申请日：1994-07-12
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , AKIHO, Hiraku , IWAI, Akihiko , TSUKAMOTO, Shin-ichi , KOSHIYA, Kazuo , YAMAGUCHI, Tokio
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/505
CPC分类号： C07D239/557 , A61K31/505
摘要： A neuron protective containing a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof as the active ingredient and capable of treating disorders and diseases accompanying neuron injury and degeneration, wherein R represents hydrogen or C1-C10 linear, branched or cyclic alkyl. The protective can treat effectively various diseases accompanying neuron degeneration, such as cerebral stroke, infarction, thrombosis and hemorrhage, and subarachnoidal hemorrhage.
摘要翻译：一种含有通式（I）表示的化合物或其药学上可接受的盐作为活性成分并能够治疗伴随神经元损伤和变性的病症和疾病的神经元保护剂，其中R表示氢或C1-C10直链，支链或环状烷基。保护性可有效治疗伴随神经元变性的各种疾病，如脑卒中，梗塞，血栓形成和出血，以及蛛网膜下腔出血。

8. 发明申请

WO1994029293A1 NOVEL 8-(2-AMINOALKOXY)FLUOROCHROMAN DERIVATIVE 审中-公开
标题翻译：新型8-（2-氨基烷氧基）氟代吡啶衍生物
公开(公告)号：WO1994029293A1
公开(公告)日：1994-12-22
申请号：PCT/JP1994000923
申请日：1994-06-08
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , YASUNAGA, Tomoyuki , KIMURA, Takenori , NAITO, Ryo , KONTANI, Toru , YAMAGUCHI, Tokio , WANIBUCHI, Fumikazu
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D311/22
CPC分类号： C07D407/12 , C07D311/22
摘要： An 8-(2-aminoalkoxy)fluorochroman derivative represented by general formula (I) or a salt thereof, both having a selective affinity for 5-HT1A receptors and being useful for treating psychoneurotic diseases such as anxiety, manic-depressive state and schizophrenia, sex disorder, eating disorder, sleep disorder, and drug dependence: wherein R, R2 and R3 represent each lower alkoxy, etc., or R1 and R2 may be combined together to represent -O-(CH2)m-O- (wherein m is an integer of 1 to 3), etc.; R4 represents hydrogen, lower alkyl or aralkyl; R represent hydroxy, amino or lower alkoxy; R6 represents hydrogen or lower alkyl, provided R5, R6 and the carbon atom to which they are bonded are combined together to represent carbonyl; A represents an ethylene group which may be substituted by lower alkyl; and B represents optionally branched C1-C10 alkylene.
摘要翻译：对通式（I）表示的8-（2-氨基烷氧基）氟苯并喃喃衍生物或其盐对5-HT 1A受体具有选择性亲和力，可用于治疗焦虑，躁狂抑郁状态和精神分裂症等精神病性疾病，性障碍，进食障碍，睡眠障碍和药物依赖性：其中R，R 2和R 3表示各个低级烷氧基等，或者R 1和R 2可以组合在一起代表-O-（CH 2）m O-（其中m是 1〜3的整数）等; R4代表氢，低级烷基或芳烷基; R 5代表羟基，氨基或低级烷氧基; R6表示氢或低级烷基，其中R5，R6和它们所键合的碳原子结合在一起代表羰基; A表示可被低级烷基取代的亚乙基; B表示任选支链的C 1 -C 10亚烷基。

9. 发明申请

WO1993024442A1 MEDICINE CONTAINING BENZOIC ACID DERIVATIVE AND NOVEL BENZOIC ACID DERIVATIVE 审中-公开
标题翻译：含有苯甲酸衍生物和新型苯甲酸衍生物的药物
公开(公告)号：WO1993024442A1
公开(公告)日：1993-12-09
申请号：PCT/JP1993000710
申请日：1993-05-27
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , HARA, Hiromu , IGARASHI, Susumu , KIMURA, Takenori , ISAKA, Masahiko , NAITO, Ryo , NAGAOKA, Hitoshi , KOUTOKU, Hiroshi , TOMIOKA, Ken-ichi , MASE, Toshiyasu
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07C63/331
CPC分类号： C07C217/90 , C07C63/331 , C07C217/58 , C07C217/80 , C07C229/60
摘要： A medicine containing a benzoic acid derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, and any of novel benzoic acid derivatives represented by general formulae (II), (III) and (IV), all included in general formula (I), or a pharmaceutically acceptable salt thereof. These compounds have a testosterone 5 alpha -reductase inhibiting activity and are useful for preventing and/or treating prostatomegaly, prostate cancer and the like.
摘要翻译：含有通式（I）表示的苯甲酸衍生物或其药学上可接受的盐和通式（II），（III）和（IV）表示的任何新型苯甲酸衍生物的药物全部包括在通式 I）或其药学上可接受的盐。这些化合物具有睾丸激素5α-还原酶抑制活性，并且可用于预防和/或治疗前列腺肥大，前列腺癌等。

10. 发明申请

WO1997019078A1 PYRIDO[2, 3-D] PYRIMIDINE DERIVATIVES AND MEDICINAL COMPOSITIONS THEREOF 审中-公开
标题翻译：吡咯并[2,3-D]吡啶衍生物及其药物组合物
公开(公告)号：WO1997019078A1
公开(公告)日：1997-05-29
申请号：PCT/JP1996003389
申请日：1996-11-20
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , TAKAYAMA, Kazuhisa , HISAMICHI, Hiroyuki , IWATA, Masahiro , KUBOTA, Hideki , AOKI, Motonori
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Compounds represented by general formula (I) or pharmaceutically acceptable salts thereof which have the effect of inhibiting the activity of type IV phosphodiesterases and are usable as drugs, in particular, type IV phosphodiesterase inhibitors or preventives and remedies for diseases in association with the sthenic type IV phosphodiesterase activity, in particular, respiratory diseases such as bronchial asthma. In said formula (I), X represents oxygen or sulfur; R represents lower alkyl, cycloalkyl(lower alkyl) or cycloalkyl; R represents hydrogen, halogeno, lower alkyl, halo(lower alkyl), hydroxy(lower alkyl), mercapto(lower alkyl), (lower alkoxy)(lower alkyl), (lower alkylthio)(lower alkyl), (lower alkanoyloxy)(lower alkyl), (lower alkanoylthio)(lower alkyl), (lower alkanoyl)(lower alkyl), hydroxyimino(lower alkyl), (lower alkoxyimino)(lower alkyl), cycloalkyl, aryl or lower alkanoyl; R represents hydrogen, halogeno or lower alkyl; R represents hydrogen, or lower alkyl; R represents cycloalkyl optionally substituted by the same group as R ; naphthyl optionally substituted by the same group as R ; a 5- or 6-membered monocyclic heterocycle optionally substituted by the same group as R , optionally fused with a benzene ring and having one to four heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur atoms; or a group of formula (a); and R represents halogeno, lower alkyl, halo(lower alkyl), hydroxy, lower alkoxy, cyano or nitro.
摘要翻译：具有抑制IV型磷酸二酯酶活性的通式（I）表示的化合物或其药学上可接受的盐，可用作药物，特别是IV型磷酸二酯酶抑制剂或预防药物以及与该类型相关的疾病的治疗方法 IV磷酸二酯酶活性，特别是呼吸道疾病如支气管哮喘。在所述式（I）中，X表示氧或硫; R 1表示低级烷基，环烷基（低级烷基）或环烷基; R 2表示氢，卤代低级烷基，卤代（低级烷基），羟基（低级烷基），巯基（低级烷基），（低级烷氧基）（低级烷基），（低级烷硫基）（低级烷基），（低级烷酰基）（低级烷基），（低级烷酰基）（低级烷基），羟基亚氨基（低级烷基），（低级烷氧基亚氨基）（低级烷基），环烷基，芳基或低级烷酰基。 R 3表示氢，卤代或低级烷基; R 4表示氢或低级烷基; R 5表示任选被与R 6相同的基团取代的环烷基; 任选被与R 6相同基团取代的萘基; 任选地被与R 6相同的基团取代的5-或6-元单环杂环，任选地与苯环稠合并具有一至四个选自氮，氧和硫原子的杂原子; 或一组式（a）; 和R 6表示卤代，低级烷基，卤代（低级烷基），羟基，低级烷氧基，氰基或硝基。

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