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1. 发明授权

US4425360A Pharmacologically active novel O-substituted pyruvic acid oximes 失效
标题翻译：药理活性新型O-取代丙酮酸肟
公开(公告)号：US4425360A
公开(公告)日：1984-01-10
申请号：US300076
申请日：1981-09-08
申请人： Hans P. Wolff , Ruth Heerdt , Manfred Hubner, deceased , Hans Kuhnle , Felix H. Schmidt
发明人： Hans P. Wolff , Ruth Heerdt , Manfred Hubner, deceased , Hans Kuhnle , Felix H. Schmidt
IPC分类号： A61K31/15 , A61K31/19 , A61K31/195 , A61P3/06 , A61P3/08 , A61P3/10 , C07C249/08 , C07C251/32 , C07C251/36 , C07C251/50 , C07C251/52 , C07C251/54 , C07C251/60 , C07C253/30 , C07C255/50 , C07D295/185 , C07C131/00
CPC分类号： C07D295/185 , Y10S514/866
摘要： The present invention provides pyruvic acid oximes of the general formula: ##STR1## wherein R is a hydrogen atom, a C.sub.3 -C.sub.8 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, cinnamyloxy, phenylamino, phenyl-N-alkylamino or phenylthio radical or an aryl or aryloxy radical, the aryl moiety of which can be substituted one or more times by C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halogen, hydroxyl, trifluoromethyl, amino, acetylamino, nitrile, nitro or methylenedioxy, A is a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon chain containing up to 10 carbon atoms, which can be substituted one or more times by halogen or hydroxyl, and R.sub.1 is a C.sub.1 -C.sub.8 alkyl radical, which can be substituted one or more times by halogen, hydroxyl, nitrile, phenyl or carboxyl, or is a nitrile or formyl group, with the proviso that when R--A-- is a methyl or ethyl radical, R.sub.1 is not a methyl radical or a nitrile group and when R--A-- is a benzyl radical, R.sub.1 is not a methyl or benzyl radical; and the physiologically acceptable salts, carboxylic acid esters and amides thereof. The invention also provides processes for the preparation of these compounds pharmaceutical compositions containing them, and their use in combating hypoglycaemia.
摘要翻译：本发明提供以下通式的丙酮酸肟：其中R为氢原子，C 3 -C 8环烷基，C 1 -C 6烷氧基，肉桂氧基，苯基氨基，苯基-N-烷基氨基或苯硫基或芳基或芳氧基，其芳基部分可以被C 1 -C 6烷基，C 1 -C 6烷氧基，卤素，羟基，三氟甲基，氨基，乙酰氨基，腈，硝基或亚甲二氧基取代一次或多次，A是直链或含有至多10个碳原子的支链，饱和或不饱和脂族烃链，其可以被卤素或羟基取代一次或多次，并且R 1是可被卤素取代一次或多次的C 1 -C 8烷基，羟基，腈，苯基或羧基，或者是腈或甲酰基，条件是当RA-是甲基或乙基时，R 1不是甲基或腈基，当RA-是苄基时，R 1 不是甲基或苄基; 和其生理上可接受的盐，羧酸酯和酰胺。本发明还提供了制备这些化合物的方法，含有它们的药物组合物及其在抗低血糖中的应用。

2. 发明授权

US5145611A Carboxylic acid derivatives, and pharmaceutical compositions containing them 失效
标题翻译：羧酸衍生物和含有它们的药物组合物
公开(公告)号：US5145611A
公开(公告)日：1992-09-08
申请号：US143456
申请日：1988-01-12
申请人： Hans P. Wolff , Ernst-Christian Witte , Hans-Frieder Kuehnle
发明人： Hans P. Wolff , Ernst-Christian Witte , Hans-Frieder Kuehnle
IPC分类号： C07C69/708 , A61K20060101 , A61K31/095 , A61K31/16 , A61K31/185 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/255 , A61P3/00 , A61P3/08 , A61P3/10 , C07C20060101 , C07C51/00 , C07C51/06 , C07C51/09 , C07C51/367 , C07C53/126 , C07C59/00 , C07C59/125 , C07C59/13 , C07C59/58 , C07C59/64 , C07C59/68 , C07C59/70 , C07C67/00 , C07C69/712 , C07C69/734 , C07C69/736 , C07C229/22 , C07C233/00 , C07C233/01 , C07C309/00 , C07C313/00 , C07C315/02 , C07C317/00 , C07C317/02 , C07C317/04 , C07C317/06 , C07C317/14 , C07C317/16 , C07C317/44 , C07C317/46 , C07C317/48 , C07C319/14 , C07C321/00 , C07C321/02 , C07C323/02 , C07C323/09 , C07C323/12 , C07C323/15 , C07C323/16 , C07C323/19 , C07C323/25 , C07C323/30 , C07C323/52 , C07C323/54 , C07C323/56 , C07C323/65
CPC分类号： C07C317/00 , Y10S514/866
摘要： Carboxylic acid derivatives of the formula ##STR1## R.sub.1 is alkoxy, alkylthio, alkylsulphinyl, alkulsulphonyl, alkylamino, cycloalkyl, or cycloalkoxy or optionally substituted aryl, aryloxy, arylthio, arylsulphinyl, arylsulphonyl or arylamino. R.sub.2 is optionally substituted aryl or, when B is alkylene also a hydrogen atom. A is a straight-chained or branched, saturated or unsaturated alkylene containing 3 to 10 carbon atoms which is optionally interrupted by a heteratom attached to a saturated carbon and has a chain length of at least 3 atoms. Y is S(O).sub.n group or oxygen, n being 0, 1 or 2. B is a valency bond or a straight-chained or branched, saturated or unsaturated alkylene containing 1 to 18 carbon atoms. Physiologically acceptable salts, esters and amides thereof are also included. The compounds are useful in the treatment of metabolic diseases.
摘要翻译：式R1的羧酸衍生物是烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基，环烷基或环烷氧基或任选取代的芳基，芳氧基，芳硫基，芳基亚磺酰基，芳基磺酰基或芳基氨基。 R2是任选取代的芳基，或当B是亚烷基也是氢原子时。 A是含有3至10个碳原子的直链或支链，饱和或不饱和的亚烷基，其任选被连接到饱和碳上的杂原子中断并具有至少3个原子的链长度。 Y是S（O）n基或氧，n是0,1或2.B是价键或含有1至18个碳原子的直链或支链，饱和或不饱和的亚烷基。还包括其生理上可接受的盐，酯和酰胺。该化合物可用于治疗代谢性疾病。

3. 发明授权

US4151303A Phenoxyalkylcarboxylic acid compounds and serum-lipid and triglyceride depressing therapeutic compositions 失效
标题翻译：苯氧基烷基羧酸化合物和血清 - 脂质和甘油三酯抑制治疗组合物
公开(公告)号：US4151303A
公开(公告)日：1979-04-24
申请号：US719878
申请日：1976-09-01
申请人： Ernst-Christian Witte , Hans P. Wolff , Kurt Stach, deceased , Wolfgang Schaumann , Karlheinz Stegmeier
发明人： Ernst-Christian Witte , Hans P. Wolff , Kurt Stach, deceased , Wolfgang Schaumann , Karlheinz Stegmeier
IPC分类号： A61K31/22 , A61K31/19 , A61P3/06 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/12 , C07C233/19 , C07C233/22 , C07C235/20 , C07C101/42 , A01N9/20
CPC分类号： C07C233/12
摘要： Novel phenoxyalkylcarboxylic acid compounds of the formula ##STR1## wherein A is aryl, aryloxy, substituted aryl or substituted aryloxy, wherein the substituents are selected from lower alkyl, lower alkoxy, halogen and haloalkyl;B is a straight-chained or branched, saturated or unsaturated hydrocarbyl containing up to 5 carbon atoms;N is 1, 2 or 3 andR.sub.1, r.sub.2 and R.sub.3, which may be the same or different, are hydrogen or lower alkyl;And the pharmacologically compatible salts thereof; have been found to be outstandingly effective in depressing serum-lipid and triglycerides in the serum of mammals.
摘要翻译：式（I）的新型苯氧基烷基羧酸化合物，其中A是芳基，芳氧基，取代的芳基或取代的芳氧基，其中取代基选自低级烷基，低级烷氧基，卤素和卤代烷基; B是含有至多5个碳原子的直链或支链饱和或不饱和烃基; N IS 1，2 OR 3，R 1，R 2和R 3可以相同或不同，为氢或低级烷基; 及其药理学兼容性; 已被认为是非常有效地抑制血清中的血清和血清中的血清脂蛋白。

4. 发明授权

US4833161A Carboxylic acid derivatives and pharmaceutical compositions and uses 失效
标题翻译：羧酸衍生物和药物组合物及用途
公开(公告)号：US4833161A
公开(公告)日：1989-05-23
申请号：US141312
申请日：1988-01-06
申请人： Hans P. Wolff , Hans-Frieder Kuhnle
发明人： Hans P. Wolff , Hans-Frieder Kuhnle
IPC分类号： A61K31/19 , A61K31/195 , A61K31/33 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P3/00 , A61P3/08 , A61P3/10 , C07C59/64 , C07C67/00 , C07C229/22 , C07C313/00 , C07C315/00 , C07C315/02 , C07C315/04 , C07C317/46 , C07C317/48 , C07C319/14 , C07C319/20 , C07C323/52 , C07C323/54 , C07C323/56 , C07C323/65 , C07D213/55 , C07D233/64 , C07D263/32 , C07D307/54 , C07D333/24 , C07D333/32 , C07D333/34 , C07D521/00
CPC分类号： C07D333/24
摘要： The present invention provides carboxylic acid derivatives of the general formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are optionally substituted aryl radicals or optionally substituted heterocyclic radicals, A is a straight-chained or branched, saturated or unsaturated alkylene chain containing up to 10 carbon atoms which can contain an oxygen, sulphur or nitrogen atom and is optionally substituted by a hydroxyl group, Y is an S(O).sub.n group or an oxygen atom, n is 0, 1 or 2 and B is a valency bond or a saturated or unsaturated alkylene radical containing up to 5 carbon atoms; as well as the physiologically acceptable salts, esters and amides thereof, with the proviso that(a) R.sub.1 and R.sub.2 are not simultaneously aryl radicals and(b) when an unsaturated alkylene chain is present which contains a heteroatom, the heteroatom is not connected to an unsaturated aliphatic carbon atom.The present invention also provides processes for the preparation of these new compounds and pharmaceutical compositions containing them.
摘要翻译：本发明提供以下通式的羧酸衍生物：其中R 1和R 2可以相同或不同，是任选取代的芳基或任选取代的杂环基，A是直链或支链的，含有至多10个碳原子的饱和或不饱和亚烷基链，其可以含有氧，硫或氮原子，并且任选被羟基取代，Y是S（O）n基团或氧原子，n是0,1 或2和B是价键或含有至多5个碳原子的饱和或不饱和亚烷基; 以及其生理上可接受的盐，酯和酰胺，条件是（a）R 1和R 2不同时为芳基，和（b）当存在含有杂原子的不饱和亚烷基链时，杂原子不连接不饱和脂肪族碳原子。本发明还提供了制备这些新化合物和含有它们的药物组合物的方法。

5. 发明授权

US4616086A Piperazine-substituted aryl and aralkyl carboxylic acids useful for treating infirmaties caused by excess lipids or thrombocyte 失效
标题翻译：哌嗪取代的芳基和芳烷基羧酸，可用于治疗由过量脂质或血小板细胞引起的体温
公开(公告)号：US4616086A
公开(公告)日：1986-10-07
申请号：US657032
申请日：1984-10-01
申请人： Ernst-Christian Witte , Hans P. Wolff , Bernd Hagenbruch , Karlheinz Stegmeir , Johannes Pill
发明人： Ernst-Christian Witte , Hans P. Wolff , Bernd Hagenbruch , Karlheinz Stegmeir , Johannes Pill
IPC分类号： C07D295/02 , A61K31/495 , A61P7/00 , C07D295/06 , C07D295/08 , C07D295/096 , C07D295/112 , C07D295/14 , C07D295/15 , C07D295/155 , C07D295/185 , C07D295/192 , C07D295/194 , C07D295/20 , C07D295/205 , C07D295/26 , C07D241/04
CPC分类号： C07D295/185 , C07D295/096 , C07D295/112 , C07D295/15 , C07D295/155 , C07D295/192 , C07D295/194 , C07D295/205 , C07D295/26
摘要： The present invention is concerned with new carboxylic acid derivatives, with processes for the preparation thereof and with pharmaceutical compositions for lipid depression and thrombocyte aggregation, containing them, and to methods for treating infirmaties caused by excess lipids or thrombocyte aggregation.The new carboxylic acid derivatives according to the present invention are compounds of the general formula: ##STR1## wherein A is a valency bond or a lower alkylene chain, B is a valency bond or a saturated or unsaturated lower alkylene chain, R is hydrogen, an alkyl group which can be substituted by hydroxyl, carboxyl, sulphonic acid or optionally substituted phenoxy group, or R is an aralkyl radical, the aryl moiety of which can be substituted and the alkyl moiety of which is optionally unsaturated and can contain up to 4 carbon atoms, or R is a phenacyl radical, the phenyl moiety optionally substituted, or R is an acyl radical derived from aliphatic, araliphatic or aromatic carboxylic or sulphonic acid, or R is an aryl radical optionally substituted with the proviso that when A is a valency bond, R cannot be hydrogen, methyl, ethyl, hydroxyethyl, benzyl or phenyl, and the physiologically acceptable salts, esters and amides thereof.
摘要翻译：本发明涉及新的羧酸衍生物，其制备方法和含有它们的脂质抑制和血小板聚集的药物组合物，以及用于治疗由过量脂质或凝血细胞聚集引起的不孕症的方法。根据本发明的新的羧酸衍生物是下列通式的化合物：其中A是价键或低级亚烷基链，B是价键或饱和或不饱和的低级亚烷基链，R 是氢，可以被羟基，羧基，磺酸或任选取代的苯氧基取代的烷基，或R是芳烷基，其芳基部分可以被取代，并且其烷基部分任选是不饱和的并且可以含有最多4个碳原子，或R是苯甲酰基，苯基部分任选被取代，或R是衍生自脂族，芳脂族或芳族羧酸或磺酸的酰基，或R是任选被取代的芳基，条件是当 A是价键，R不能是氢，甲基，乙基，羟乙基，苄基或苯基，以及它们的生理上可接受的盐，酯和酰胺。

6. 发明授权

US4258058A Phenoxyalkylcarboxylic acid compounds and thrombocyte-aggregation inhibition 失效
标题翻译：苯氧基烷基羧酸化合物和血小板聚集抑制作用
公开(公告)号：US4258058A
公开(公告)日：1981-03-24
申请号：US15536
申请日：1979-02-26
申请人： Ernst-Christian Witte , Hans P. Wolff , Max Thiel , Karlheinz Stegmeier , Egon Roesch
发明人： Ernst-Christian Witte , Hans P. Wolff , Max Thiel , Karlheinz Stegmeier , Egon Roesch
IPC分类号： A61K31/19 , A61K31/165 , A61K31/195 , A61K31/22 , A61P3/06 , A61P7/02 , C07C67/00 , C07C301/00 , C07C303/38 , C07C303/40 , C07C311/03 , C07C311/04 , C07C311/06 , C07C311/14 , C07C311/16 , C07C311/17 , C07C311/29 , C07D209/48 , C07C143/78 , A61K31/24
CPC分类号： C07D209/48
摘要： Phenoxyalkylcarboxylic acid compounds of the formula ##STR1## wherein R is hydrogen or lower alkylR.sub.1 is alkyl or aryl, aralkyl or aralkenyl radical, the aryl moiety of which can be substituted one or more times by halogen, hydroxyl, trifluoromethyl or lower alkyl, alkoxy or acylR.sub.2 and R.sub.3 are individually selected from hydrogen or lower alkyl, andn is 0, 1, 2 or 3and the physiologically acceptable salts, esters and amides thereof; are outstandingly effective in inhibiting thrombocyte aggregation.
摘要翻译：其中R为氢或低级烷基R 1的苯氧基烷基羧酸化合物为烷基或芳基，芳烷基或芳烯基，其芳基部分可被卤素，羟基，三氟甲基或低级烷基烷氧基取代一次或多次或酰基R2和R3分别选自氢或低级烷基，n为0,1,2或3及其生理上可接受的盐，酯和酰胺; 在抑制血小板聚集方面效果显着。

7. 发明授权

US4153728A Phenoxyalkylcarboxylic acid compounds and therapeutic compositions 失效
标题翻译：苯氧基烷基羧酸化合物和治疗组合物
公开(公告)号：US4153728A
公开(公告)日：1979-05-08
申请号：US733542
申请日：1976-10-18
申请人： Hans P. Wolff , Ernst-Christian Witte , Max Thiel , Harald Stork , Egon Roesch
发明人： Hans P. Wolff , Ernst-Christian Witte , Max Thiel , Harald Stork , Egon Roesch
IPC分类号： A61K31/215 , A61K20060101 , A61K31/16 , A61K31/19 , A61K31/22 , A61P3/06 , A61P7/02 , C07C20060101 , C07C51/00 , C07C59/68 , C07C67/00 , C07C69/734 , C07C69/76 , C07C231/00 , C07C231/02 , C07C231/12 , C07C235/34 , C07C235/48 , C07C101/42 , A01N9/20
CPC分类号： C07C2101/14 , Y10S514/824
摘要： Novel phenoxyalkylcarboxylic acid compounds of the formula ##STR1## wherein B is a valency bond or a straight-chained or branched, saturated or unsaturated hydrocarbon radical containing up to 3 carbon atoms;N is 1 or 2 andR.sub.1, r.sub.2 and R.sub.3 are hydrogen or lower alkyl; and the pharmacologically compatible salts thereof; have been found to be outstandingly effective in lowering the serum lipid level and the cholesterol level in mammals without inducing undesired side effects and to possess excellent thrombocyte-aggregation inhibiting activity.
摘要翻译：式（I）的新型苯氧基烷基羧酸化合物，其中B是含有至多3个碳原子的价键或直链或支链，饱和或不饱和的烃基; N 1 OR 2，R 1，R 2和R 3为氢或低级烷基; 和其药理学上相容的盐; 已被发现在降低哺乳动物血清脂质水平和胆固醇水平而没有诱导不期望的副作用并且具有优异的血小板聚集抑制活性方面是非常有效的。

8. 发明授权

US4933367A Carboxylic acid derivatives, processes for the preparation thereof, the use thereof, and pharmaceutical compositions which contain these compounds 失效
标题翻译：羧酸衍生物，其制备方法，用途及含有这些化合物的药物组合物
公开(公告)号：US4933367A
公开(公告)日：1990-06-12
申请号：US27229
申请日：1987-03-12
申请人： Hans P. Wolff , Ernst-Christian Witte , Hans-Frieder Kuhnle
发明人： Hans P. Wolff , Ernst-Christian Witte , Hans-Frieder Kuhnle
IPC分类号： C07C69/736 , A61K31/19 , A61K31/215 , A61K31/255 , A61K31/275 , A61K31/49 , C07C20060101 , C07C51/00 , C07C59/125 , C07C59/215 , C07C59/64 , C07C59/68 , C07C59/76 , C07C59/88 , C07C67/00 , C07C69/65 , C07C69/708 , C07C69/738 , C07C227/00 , C07C227/08 , C07C227/16 , C07C229/22 , C07C229/30 , C07C229/36 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/45 , C07C233/47 , C07C233/51 , C07C233/63 , C07C233/65 , C07C233/81 , C07C235/20 , C07C237/06 , C07C237/22 , C07C253/00 , C07C255/32 , C07C309/29 , C07C309/63 , C07C309/65 , C07C309/77 , C07C311/00 , C07C311/02 , C07C311/03 , C07C311/06 , C07C311/15 , C07C311/19 , C07C313/00 , C07C317/00 , C07C317/04 , C07C317/14 , C07C317/44 , C07C317/46 , C07C323/52 , C07C323/56
CPC分类号： C07C317/00 , A61K31/19 , A61K31/215 , A61K31/255 , A61K31/275 , C07C309/00 , C07C323/00 , C07C59/64 , C07C59/68 , C07C59/88
摘要： This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.
摘要翻译： PCT No.PCT / EP86 / 00406 Sec。 371日期1987年3月12日 102（e）日期1987年3月12日PCT申请1986年7月10日PCT公布。公开号WO87 / 00521 日本1987年1月29日。本发明涉及羧酸衍生物及其用途。该化合物可用于治疗各种疾病如糖尿病，糖尿病前期，脂肪性疾病或动脉粥样硬化。

9. 发明授权

US4387104A N-Substituted pyruvic acid hydrazones, preparation thereof and pharmaceutical compositions containing them 失效
标题翻译： N-取代的丙酮酸腙，其制备物和含有它们的药物组合物
公开(公告)号：US4387104A
公开(公告)日：1983-06-07
申请号：US292869
申请日：1981-08-14
申请人： Ruth Heerdt , Hans P. Wolff , Fritz Kaiser , Wolfgang Schaumann , Hans Kuhnle
发明人： Ruth Heerdt , Hans P. Wolff , Fritz Kaiser , Wolfgang Schaumann , Hans Kuhnle
IPC分类号： A61K31/15 , A61K31/19 , A61K31/195 , A61P3/08 , A61P3/10 , C07C67/00 , C07C241/00 , C07C251/08 , C07C251/76 , C07C317/14 , C07C109/12
CPC分类号： C07C251/72
摘要： A pyruvic acid hydrazone derivative of the formula: ##STR1## wherein R is an aryl radical optionally substituted by lower alkyl or is an aliphatic hydrocarbon radical which can be substituted by a lower alkoxy, a cycloalkyl or an optionally substituted aryl radical,A is an alkylene radical containing 2 to 8 carbon atoms, with at least 2 carbon atoms between B and the nitrogen atom, andB is an oxygen or sulphur atom;or a physiologically acceptable salt, ester or amide thereof which possesses hypoglycaemic activity.
摘要翻译：一种下式的丙酮酸腙衍生物，其中R是任选被低级烷基取代的芳基，或者是可被低级烷氧基，环烷基或任意取代的芳基取代的脂族烃基，A是含有2至8个碳原子的亚烷基，B和氮原子之间至少有2个碳原子，B是氧或硫原子; 或其具有低血糖活性的生理上可接受的盐，酯或酰胺。

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