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1.发明专利
公开(公告)号：JPS59110696A
公开(公告)日：1984-06-26
申请号：JP22163382
申请日：1982-12-16
IPC分类号： C07D501/20 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/22
摘要： NEW MATERIAL:A compound(salt) shown by the formula I [R
1 is H, or OH; R
2 is lower alkoxycarbonyloxy(lower)alkyl, or 1-propionyloxyethyl].
EXAMPLE: 7-[2-(2-Aminothiazol-4-yl)acetamido]-3-cephem-4-carboxylic acid 1-ethoxycarbonyloxyethyl ester.
USE: An oral antibacterial agent for a wide range of bacteria including Gram- positive and Gram-negative bacteria.
PROCESS: A 7-substituted-3-cephem-4-carboxylic acid (reactive derivative) shown by the formula I or its salt is reacted with a compound(reactive derivative) shown by the formula R
2 -OH usually in the presence of a base.
COPYRIGHT: (C)1984,JPO&Japio摘要翻译： 新材料：由式I [R 1]表示的化合物（盐）是H或OH; R 2是低级烷氧羰基氧基（低级）烷基或1-丙酰氧基乙基]。 实例：7- [2-（2-氨基噻唑-4-基）乙酰氨基] -3-头孢烯-4-羧酸1-乙氧基羰氧基乙酯。 用途：用于广泛细菌的口服抗菌剂，包括革兰氏阳性菌和革兰氏阴性菌。 方法：将式I所示的7-取代-3-头孢烯-4-羧酸（反应性衍生物）或其盐与通式R 2 -OH所示的化合物（反应性衍生物）反应，通常在存在 的基地。
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2.发明专利Novel cephen compound, or its salt, its preparation, and preventive it as active ingredient 失效新型化合物或其盐，其制备和预防作为活性成分
公开(公告)号：JPS5777689A
公开(公告)日：1982-05-15
申请号：JP13943081
申请日：1981-09-03
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D257/04 , C07D417/12 , C07D501/20 , C07D501/22 , C07D501/34 , C07D501/36 , C07D501/46
CPC分类号： C07D257/04 , C07D417/12 , Y02P20/55
摘要： NEW MATERIAL:A cephem compound shown by the formulaI(R
1 is optionally protected amino; R
2 is 4W8 membered saturated single ring containing one S; R
3 is optionally protected carboxy; R
4 is H, lower alkyl, etc.) and its pharmaceutically acceptable acid addition salt.
EXAMPLE: 7-[2-(2-Aminothiozole-4-yl)-2-(3-thiethanyloxyimino)acetamide]-3-methyl- 3-cephem-4-carboxlic acid.
USE: An antibacterial agent. Having high antibacterial activity against many bacteria including Gram-positive and Gram-negative bacteria.
PROCESS: For example, a compond shown by the formula II is reacted with a compound shown by the formula I, to give a compound shown by the formulaI. The copound shown by the formula III, for example, can be obtained by reacting a comound shown by the fomula IV with a compound shown by the formula V.
COPYRIGHT: (C)1982,JPO&Japio摘要翻译： 新材料：由式I表示的头孢烯化合物（R 1）是任选保护的氨基; R 2是含有一个S的4-8元饱和单环; R 3任选被保护的羧基; R 4是 H，低级烷基等）及其药学上可接受的酸加成盐。 实施例7-〔2-（2-氨基噻唑-4-基）-2-（3-硫代氧基亚氨基）乙酰胺〕-3-甲基-3-头孢烯-4-羧酸。 用途：抗菌剂。 对许多细菌具有高抗菌活性，包括革兰氏阳性菌和革兰氏阴性菌。 方法：例如，式II所示的化合物与式所示的化合物反应，得到式I所示的化合物。 例如式III所示的结构可以通过将由式IV表示的化合物与式V所示的化合物反应来获得。
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公开(公告)号：JPS59186983A
公开(公告)日：1984-10-23
申请号：JP3507284
申请日：1984-02-24
发明人： TAKATANI TAKAO , TAKASUGI HISASHI
IPC分类号： A61K31/435 , A61K31/495 , A61K31/505 , A61P1/04 , A61P9/04 , C07D263/58 , C07D265/36 , C07D277/68 , C07D279/10 , C07D471/04 , C07D487/04
CPC分类号： C07D263/58 , C07D265/36 , C07D277/68 , C07D279/10 , C07D471/04 , C07D487/04
摘要： NEW MATERIAL:The imidazo-heterocyclic compound of formula I [R
1 is H, lower alkyl or halogen; R
2 is R
1 , or aminomethyl or piperazin-1-ylmethyl each of which may be substituted with lower alkyl; R
3 is benzothiazolinyl, benzoxazolinyl, etc.; Y is N cr CR
4 (R
4 is H, OH, lower alkyl, etc.)] and its salt.
EXAMPLE: 5-[3-( 4-Methylpiperazin-1-ylmethyl )imidazo[1,2-a]pyridin-2-yl]-3-methyl- 2-benzothiazolinone.
USE: Cardiotonic agent and antiulcer agent.
PREPARATION: The compound of formula I a can be prepared by reacting the compound of formula II or its salt with the compound of formula III in a solvent such as water, methanol, THF, etc. in the presence of an alkali metal hydride, alkali metal carbonate, etc.
COPYRIGHT: (C)1984,JPO&Japio摘要翻译： 新物质：式I的咪唑并杂环化合物[R 1]为H，低级烷基或卤素; R 2是R 1，或者可以被低级烷基取代的氨基甲基或哌嗪-1-基甲基; R 3是苯并噻唑啉基，苯并恶唑啉基等; Y是N cr CR 4（R 4是H，OH，低级烷基等）]及其盐。 实例：5- [3-（4-甲基哌嗪-1-基甲基）咪唑并[1,2-a]吡啶-2-基] -3-甲基-2-苯并噻唑啉酮。 用途：强心剂和抗溃疡剂。 制备：式Ⅰa化合物可以通过使式II化合物或其盐与式III化合物在溶剂如水，甲醇，THF等中在碱金属氢化物，碱 金属碳酸盐等
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公开(公告)号：JPS59122494A
公开(公告)日：1984-07-14
申请号：JP23850783
申请日：1983-12-16
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/20 , C07D501/34 , C07D501/36 , C07D501/56 , C07D519/06
CPC分类号： C07D501/20
摘要： NEW MATERIAL:A compound of formula I [R
1 is carboxy-(lower)-alkyl; R
2 is protected or unprotected carboxyl; R
3 is acyloxy-(lower)-alkyl, unsubstituted or substituted heterocyclic thio-(lower)-alkyl] and its salt.
EXAMPLE: 7-[2-Carbomethoxyimino-2-( 1,2,4-thiadiazol-3-yl )acetamide]-3-(tetrazolo [1.5-b]pyridazin-6-yl)thiomethyl-3-cephem-4-carboxylic acid (syn-isomer).
USE: Preventing and treating agent for microbism.
PREPARATION: The reaction between a compound of formula II, its reactive derivative or salt and a compound of formula III, its reactive derivative or salt gives the objective compound.
COPYRIGHT: (C)1984,JPO&Japio摘要翻译： 新物质：式I化合物[R 1]为羧基 - （低级） - 烷基; R 2是被保护或未被保护的羧基; R 3是酰氧基 - （低级） - 烷基，未取代或取代的杂环硫代（低级） - 烷基]及其盐。 实施例7- [2-甲酯基亚氨基-2-（1,2,4-噻二唑-3-基）乙酰胺] -3-（四唑并[1,5-b]哒嗪-6-基）硫代甲基-3-头孢-4-基 羧酸（顺式异构体）。 用途：防治微生物剂。 制备：式II化合物，其反应性衍生物或盐与式III化合物，其反应性衍生物或盐之间的反应产生目标化合物。
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5.发明专利Syn-isomer of 3,7-disubstituted-3-cephem-4-carboxylic acid compound, its salt and their preparation 失效3,7-取代-3-羧基-4-羧酸化合物的SYN-ISOMER，其盐及其制备
公开(公告)号：JPS5962597A
公开(公告)日：1984-04-10
申请号：JP12867683
申请日：1983-07-13
IPC分类号： A01N37/50 , A01N43/78 , A61K31/545 , A61K31/546 , A61P31/04 , C07C251/48 , C07C251/60 , C07D277/20 , C07D277/38 , C07D277/40 , C07D277/46 , C07D333/16 , C07D501/06 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/32 , C07D501/34 , C07D501/36
CPC分类号： C07D277/20 , C07D277/46 , C07D333/16
摘要： NEW MATERIAL:The compound (salt) of formula I {R
1 is group of formula III R
5 is H, halogen, OH, etc.; R
6 is OH, alkoxy, etc.), formula III (R
7 is amino, OH, etc.), or formula IV (R
8 is alkyl; R
9 is imino or oxo); R
2 is (substituted) aliphatic hydrocarbon group; R
3 is carboxyl; R
4 is acyloxymethyl [excluding (substituted) carbamoyloxymethyl], hydroxymethyl, etc., or R
3 and R
4 together form -COOCH
2 -}.
EXAMPLE: 7-[ 2-Methoxylimino-2-( 3-hydroxyphenyl )acetamido ]-3-( 1-methyl-1H- tetrazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid (syn-isomer).
USE: An antibacterial agent.
PROCESS: The compound of formula V or its reactive derivative is made to react with the substituted acetic acid conpound of formula VI or its reactive derivative or their salt.
COPYRIGHT: (C)1984,JPO&Japio摘要翻译： 新物质：式I的化合物（盐）R 1是式III的基团R 5是H，卤素，OH等; R 6是OH，烷氧基等），式III（R 7是氨基，OH等）或式IV（R 8是烷基; R 9是亚氨基或氧代）; R 2是（取代的）脂族烃基; R 3是羧基; R 4是酰氧基甲基[不包括（取代的）氨基甲酰氧基甲基]，羟甲基等，或者R 3和R 4一起形成-COOCH 2 - }。 实施例7-〔2-甲氧基亚氨基-2-（3-羟基苯基）乙酰氨基〕-3-（1-甲基-1H-四唑-5-基）硫甲基-3-头孢烯-4-羧酸（顺式异构体）。 用途：抗菌剂。 方法：使式V化合物或其反应性衍生物与式VI的取代乙酸或其反应性衍生物或其盐反应。
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6.发明专利Novel cephem compound or its salt, their preparation and prophylactic or remedy for microbism containing the same as active ingredient 失效新型化合物或其盐，它们作为活性成分的微生物的制备和预处理或补救
公开(公告)号：JPS5756486A
公开(公告)日：1982-04-05
申请号：JP12584581
申请日：1981-08-10
IPC分类号： C07D501/46 , A61K31/545 , A61K31/546 , A61P31/04
CPC分类号： Y02A50/473
摘要： NEW MATERIAL:A cephem compound of formulaI(R
1 is arbitrarily protected primary amino group; R
2 is lower alkenyl, lower alkynyl, cycloalkyl; R
3 is H, carbamoyl, hydroxy-lower-alkyl) and its medically permissible salt.
EXAMPLE: 7-[2-(2-Propynyloximino)-2-( 2-aminothiazol-4-yl )acetamide]-3-( 1-pyridiniomethyl)-3-cephem-4-carboxylate. (syn isomer).
USE: Antibiotic: it is effective against gram-positive and-negative bacteria.
PREPARATION: For example, the reaction of a compound of formula II with another compound of formula III affords the compound of formulaI. The reaction is effected in water or an organic solvent in the presence of a condensing agent.
COPYRIGHT: (C)1982,JPO&Japio摘要翻译： 新材料：式I的头孢烯化合物（R 1是任意保护的伯氨基; R 2是低级链烯基，低级炔基，环烷基; R 3是H，氨基甲酰基，羟基 - 低级烷基）及其 医学上允许的盐。 实施例7-〔2-（2-丙炔肟基）-2-（2-氨基噻唑-4-基）乙酰胺〕-3-（1-吡啶基甲基）-3-头孢烯-4-羧酸酯。 （顺式异构体）。 用途：抗生素：对革兰氏阳性菌和阴性菌有效。 制备：例如，式II化合物与另一种式III化合物的反应得到式Ⅰ化合物。 该反应在缩合剂存在下在水或有机溶剂中进行。
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公开(公告)号：JPS6156180A
公开(公告)日：1986-03-20
申请号：JP18651485
申请日：1985-08-23
发明人： TAKATANI TAKAO , TAKASUGI HISASHI
IPC分类号： C07D471/04 , A61K31/435 , A61K31/505 , A61P1/04 , A61P7/02 , C07D487/04
摘要： NEW MATERIAL:The compound of formula I [R
1 is H, amino or alkyl; R
2 is H, alkyl, alkoxy, halogen, OH or piperazin-1-yl; R
3 is H or alkyl; R
4 is pyridyl or group of formula II (R
5 is alkoxy, nitro, ureido, etc.; R
6 is H, NO
2 , amino, OH, alkoxy, etc.; R
7 is H or halogen); Y is N or CR
8 (R
8 is H, alkoxy, etc.); Z is N or group of formula III (R
9 is alkyl; J is acid residue)] and its salt.
EXAMPLE: 3,7-Dimethyl-2-(4-methoxy-3-nitrophenyl)imidazo[1,2-a]-pyridine.
USE: It has antitumor activity and antithrombotic activity, and is useful for the remedy of ulcer, thrombosis, etc.
PREPARATION: The compound of formula I wherein Z is N or its salt can be prepared e.g. by reacting the compound of formula IV (X is eliminable group) or its salt with the compound of formula V or its salt.
COPYRIGHT: (C)1986,JPO&Japio摘要翻译： 新材料：式I化合物[R 1]为H，氨基或烷基; R 2是H，烷基，烷氧基，卤素，OH或哌嗪-1-基; R 3是H或烷基; R 4是吡啶基或式II的基团（R 5是烷氧基，硝基，脲基等; R 6是H，NO 2，氨基，OH，烷氧基等; R 7是H 或卤素）; Y是N或CR 8（R 8是H，烷氧基等）; Z是N或式III的基团（R 9是烷基; J是酸残基）]及其盐。 实施例：3,7-二甲基-2-（4-甲氧基-3-硝基苯基）咪唑并[1,2-a] - 吡啶。 用途：具有抗肿瘤活性和抗血栓活性，可用于治疗溃疡，血栓形成等。制剂：其中Z为N或其盐的式I化合物可以制备如下： 通过使式IV化合物（X是可消除基团）或其盐与式V化合物或其盐反应。
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8.发明专利Pyrimidine derivative, its preparation, and pharmaceutical composition containing same 失效吡嗪衍生物，其制剂和含有其的药物组合物
公开(公告)号：JPS6140272A
公开(公告)日：1986-02-26
申请号：JP16078485
申请日：1985-07-19
IPC分类号： C07D213/50 , A61K31/505 , A61P9/00 , A61P25/28 , C07C205/56 , C07D213/55 , C07D239/20 , C07D239/26 , C07D239/28 , C07D239/30 , C07D239/34 , C07D239/42 , C07D333/00 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D491/04 , C07D491/048 , C07D491/052
CPC分类号： C07D239/26 , C07C205/45 , C07C205/56 , C07D239/20 , C07D239/30 , C07D239/42 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D491/04
摘要： NEW MATERIAL:The compound of formula I [Ar is NO
2 , NH
2 , halogen, N-containing heterocyclic group, aryl substituted with group of formula II(R
4 WR
6 are H, NO
2 , alkyl, etc.; X is O or S; l is 0W6), etc., or heterocyclic group having one N and/or one S atoms; R
1 is carboxy, alkanoyl, CN, amino, carboxyamino, etc.; R
2 is H, aryl, or (substituted) alkyl; R
1 and R
2 may together with adjacent C form lactone ring; R
3 is alkyl, (halogen-substituted) aryl, etc.] and its salt.
EXAMPLE: 6-Methyl-5-( 4-methylpiperazin-1-ylcarbonyl )-4-(3-nitrophenyl)-2-phenylpyrimidine.
USE: Useful for the remedy of cerebrovascular diseases (e.g. cerebral hemorrhage, transient ischemic attack, etc.).
PREPARATION: The compound of formula I or its salt can be prepared e.g. by oxidizing the compound of formula III or its salt with an oxidizing agent such as manganese dioxide, nickel peroxide, etc.
COPYRIGHT: (C)1986,JPO&Japio摘要翻译： 新物质：式I化合物[Ar为NO 2，NH 2，卤素，含N杂环基，被式II取代的芳基（R 4 -R 6）为H，NO 2，烷基等; X为O或S; l为0-6）等，或具有一个N和/或一个S原子的杂环基; R 1是羧基，烷酰基，CN，氨基，羧基氨基等; R 2是H，芳基或（取代的）烷基; R 1和R 2可以与相邻的C形式的内酯环一起; R 3是烷基，（卤素取代的）芳基等]及其盐。 实施例：6-甲基-5-（4-甲基哌嗪-1-基羰基）-4-（3-硝基苯基）-2-苯基嘧啶。 用途：用于治疗脑血管疾病（如脑出血，短暂性脑缺血发作等）。 制备：式I化合物或其盐可以制备如 通过用氧化剂如二氧化锰，过氧化镍等氧化式Ⅲ化合物或其盐
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公开(公告)号：JPS59130292A
公开(公告)日：1984-07-26
申请号：JP23119883
申请日：1983-12-06
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D213/20 , C07D401/06 , C07D501/18 , C07D501/24
CPC分类号： C07D213/20 , C07D401/06
摘要： NEW MATERIAL:A compound shown by the formula I [R
1 is amino, acylamino; R
9 is group shown by the formula II (R
2 is organic group; X is CH, or N; Z is acid residue; Y is CH, or N, and n is 0, or Y is N
+ -R
2 and n is 1), or group shown by the formula -A-N
+ (R
10 )
3 (R
10 is lower alkyl; A is lower alkylene)], or its salt.
EXAMPLE: 7-[ 2-Ethoxyimino-2-( 5-amino-1,2,4-thiadiazol-3-yl )acetamido ]-3-[ 2-( 1- methyl-3-pyridinio)thiovinyl]-3-cephem-4-carboxylate(syn-isomer)(trans-isomer).
USE: An antibacterial agent.
PROCESS: A compound (reactive derivative) shown by the formula III, or salt is acylated to give a compound shown by the formula I wherein the group R
1 is acylamino.
COPYRIGHT: (C)1984,JPO&Japio摘要翻译： 新材料：由式I表示的化合物[R 1]是氨基，酰氨基; R 9是式II所示的基团（R 2是有机基团; X是CH或N; Z是酸残基; Y是CH或N，n是0或Y是N + > -R 2，n为1）或式-AN +（R 10）3（R 10为低级烷基，A为低级亚烷基）]表示的基团或其盐。 实施例7- [2-乙氧基亚氨基-2-（5-氨基-1,2,4-噻二唑-3-基）乙酰氨基] -3- [2-（1-甲基-3-吡啶并）硫代乙烯基] -3- 头孢烯-4-羧酸酯（顺式异构体）（反式异构体）。 用途：抗菌剂。 方法：将由式III表示的化合物（反应性衍生物）或盐进行酰化，得到式I所示的化合物，其中基团R 1为酰氨基。
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10.发明专利Pyrimidine derivative, its preparation, and pharmaceutical composition containing same 失效吡嗪衍生物，其制剂和含有其的药物组合物
公开(公告)号：JPS6187669A
公开(公告)日：1986-05-06
申请号：JP21901085
申请日：1985-10-01
IPC分类号： C07D401/06 , A61K31/505 , A61K31/55 , A61P9/00 , A61P25/28 , C07D20060101 , C07D239/26 , C07D239/28 , C07D243/00 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D487/04
摘要： NEW MATERIAL:The pyrimidine derivative of formula I [Ar is nitro, haloalkyl, alkoxy, or substituted aryl of formula II (R -R are H or halogen; l is 0-6); R is esterified carboxy, alkanoyl, hydroxyalkyl, group of formula III (R and R are H or N-containing heterocyclic group, etc.), or group of formula IV (A is alkylene); R is H, alkyl or group of formula V (B is A); R is alkyl or aryl] and its salt. EXAMPLE:6-Methyl-5-(4-methylpiperazin-1-ylmethyl)-4-(3-nitroph-en-yl)- 2-phenyl pyrimidine. USE:Remedy for cerebrovascular disease such as cerebral apoplexy. PREPARATION:The compound of formula VIII which is one of the compound of formula I can be prepared e.g. by reacting the compound of formula VI or its salt with the compound of formula VII or its salt.
摘要翻译： 新物质：式I的嘧啶衍生物[Ar为硝基，卤代烷基，烷氧基或式II的取代芳基（R 4 -R 6）为H或卤素; l为0-6）; R 1是酯化的羧基，烷酰基，羟基烷基，式III的基团（R 7和R 8是H或含N的杂环基等）或式IV的基团（A是亚烷基）; R 2是H，烷基或式V的基团（B是A）; R 3是烷基或芳基]及其盐。 实施例：6-甲基-5-（4-甲基哌嗪-1-基甲基）-4-（3-硝基 - 烯基）-2-苯基嘧啶。 用途：弥补脑血管疾病如脑中风。 制备：作为式I化合物之一的式VIII化合物可例如制备。 通过式VI化合物或其盐与式VII化合物或其盐反应。
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