公开(公告)号：US5641810A

公开(公告)日：1997-06-24

申请号：US373264

申请日：1995-01-25

申请人： Johannes Pill ,  Liesel Doerge ,  Karlheinz Stegmeier

发明人： Johannes Pill ,  Liesel Doerge ,  Karlheinz Stegmeier

IPC分类号： C07D295/10 ,  A61K31/20 ,  A61K31/40 ,  A61K31/445 ,  A61K31/451 ,  A61K31/495 ,  A61P7/02 ,  C07C55/32 ,  C07D211/08

CPC分类号： A61K31/20

摘要： Compounds of .alpha.,.omega.-dicarboxylic acids of the formula I ##STR1## in which X and Y, which can be the same or different, signify hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, hydroxyl, cyano, carboxyl, C.sub.1 -C.sub.6 -alkoxycarbonyl or carbamoyl, R.sub.1 and R.sub.2, which can be the same or different, hydrogen or C.sub.1 -C.sub.6 -alkyl and Q a linear saturated or unsaturated alkylene chain with 2-14 C-atoms in which one or more C-atoms can be replaced by cyclohexyl rings, phenyl or heterocycles, as well as of their in vivo-hydrolysable carboxylic acid derivatives for the preparation of medicaments with fibrinogen-lowering action.

摘要翻译： PCT No.PCT / EP93 / 01894 Sec。 371 1995年1月25日第 102（e）日期1995年1月25日PCT提交1993年7月17日PCT公布。 出版物WO94 / 02128 日期1994年2月3日，式I的α，ω-二羧酸化合物其中X和Y可以相同或不同，表示氢，卤素，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 6 - 烷氧基，羟基，氰基，羧基，C 1 -C 6 - 烷氧基羰基或氨基甲酰基，R 1和R 2可以相同或不同，为氢或C 1 -C 6烷基，Q为直链饱和或不饱和亚烷基链， 其中一个或多个C原子可以被环己基环，苯基或杂环取代的C原子，以及其体内可水解的羧酸衍生物用于制备具有纤维蛋白原降低作用的药物。

公开(公告)号：US4981873A

公开(公告)日：1991-01-01

申请号：US370455

申请日：1989-06-23

申请人： Ernst-Christian Witte ,  Karlheinz Stegmeier ,  Liesel Doerge ,  Robert A. Slater

发明人： Ernst-Christian Witte ,  Karlheinz Stegmeier ,  Liesel Doerge ,  Robert A. Slater

IPC分类号： A61K31/18 ,  A61K31/19 ,  A61K31/22 ,  A61K31/41 ,  A61K31/655 ,  A61P1/04 ,  A61P7/02 ,  A61P9/00 ,  A61P11/00 ,  A61P43/00 ,  C07C311/04 ,  C07C311/05 ,  C07C311/14 ,  C07C311/17 ,  C07C311/18 ,  C07C311/29 ,  C07C311/40 ,  C07C317/14 ,  C07C317/28 ,  C07C317/44 ,  C07C323/49 ,  C07C323/52 ,  C07C323/60 ,  C07C323/67 ,  C07D257/04

CPC分类号： C07C317/14 ,  C07C323/52

摘要： The present invention concerns compounds of the formula: ##STR1## where R.sub.1 is an alkyl or alkenyl radical containing up to 6 carbon atoms, a cycloalkyl radical containing 3 to 7 carbon atoms, an aralkyl, aralkenyl or aryl radical in which the aryl radical or moiety can be substituted one or more times by halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 -alkylamino, C.sub.2 -C.sub.12 -dialkylamino, C.sub.1 -C.sub.6 -acylamino, C.sub.1 -C.sub.16 -acyl, C.sub.1 -C.sub.6 -alkylsulphenyl, -sulphinyl or -sulphonyl or by azido, R.sub.2 is hydrogen atom or a C.sub.1 -C.sub.6 -alkyl, aralkyl, aralkenyl or acyl radical, A and B are saturated or unsaturated alkylene chains containing up to 10 carbon atoms which can be substituted one or more times by C.sub.1 -C.sub.3 -alkyl radicals, the sum of carbon atoms in chains A and B being at least 4 and at most 11, Q is an oxygen or sulphur atom, a sulphonyl or sulphinyl group or an amino group --N(R.sub.2)--, R.sub.2 having the same meaning as above, and Y is a free carboxylic acid group or a carboxylic acid ester, carboxylic acid amide, hydroxymethyl or tetrazolyl radical; the pharmacologically acceptable salts thereof and the optically active and E-Z isomers thereof, as well as mixtures thereof.These compounds are useful as they have an antagonistic action towards thromboxane A.sub.2 as well as against prostaglandin endoperoxide. They inhibit the aggregation of blood platelets and prevent the constriction of the smooth musculature as well as bronchoconstriction.

摘要翻译： 本发明涉及下式的化合物：其中R1是含有至多6个碳原子的烷基或烯基，含有3-7个碳原子的环烷基，芳烷基，芳烯基或芳基，其中芳基或 C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，羟基，三氟甲基，氰基，硝基，氨基，C 1 -C 6 - 烷基氨基，C 2 -C 12 - 二烷基氨基，C 1 -C 6酰基氨基 ，C 1 -C 16 - 酰基，C 1 -C 6 - 烷基亚磺酰基， - 亚磺酰基或 - 磺酰基或叠氮基，R 2是氢原子或C 1 -C 6烷基，芳烷基，芳烯基或酰基，A和B是饱和或不饱和亚烷基链 含有多至10个可被C 1 -C 3 - 烷基取代一次或多次的碳原子，链A和B中的碳原子总数至少为4且至多为11，Q是氧或硫原子， 磺酰基或亚磺酰基或氨基-N（R2） - ，R2具有与上述相同的含义，Y是游离羧酸基或羧基 C酸酯，羧酸酰胺，羟甲基或四唑基; 其药理学上可接受的盐及其光学活性和E-Z异构体，以及它们的混合物。 这些化合物是有用的，因为它们对血栓素A2以及前列腺素过氧化物具有拮抗作用。 它们抑制血小板聚集，防止平滑肌肉收缩以及支气管收缩。

公开(公告)号：US5140038A

公开(公告)日：1992-08-18

申请号：US401254

申请日：1989-08-31

申请人： Ernst-Christian Witte ,  Karlheinz Stegmeier ,  Liesel Doerge

发明人： Ernst-Christian Witte ,  Karlheinz Stegmeier ,  Liesel Doerge

IPC分类号： A61K31/18 ,  A61K31/195 ,  A61K31/22 ,  A61K31/41 ,  A61P1/04 ,  A61P3/00 ,  A61P7/02 ,  A61P9/00 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/28 ,  C07C311/19 ,  C07C323/65 ,  C07D257/04 ,  C07D257/06

CPC分类号： C07D257/04 ,  C07C311/19 ,  C07D257/06 ,  C07C2101/14

摘要： The present invention provides sulphonamides of the general formula: ##STR1## wherein R.sup.1 and R.sup.2, which can be the same or different, are hydrogen or halogen atoms or C.sub.1 -C.sub.6 -alkyl, trifluoro-methyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, N-alkylaminocarbonyl or N,N-dialkylaminocarbonyl radicals or, when R.sup.1 and R.sup.2 are alkyl radicals ortho to one another, R.sup.1 and R.sup.2, together with the carbon atoms to which they are attached, form a saturated or unsaturated C.sub.5 -C.sub.7 -alkylene ring, R.sup.3 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical, a phenylalkyl or phenylalkenyl radical, the phenyl moiety of which can be substituted by halogen, alkyl or trifluoromethyl, C is a --(CH.sub.2).sub.m -- radical, in which m is 0, 1, 2 or 3, or a branched C.sub.2 -C.sub.5 alkylene radical, whereby a methylene radical --CH.sub.2 -- of the group C can be replaced by an oxygen or sulphur atom or by a hydroxymethylene radical --CHOH-- or carbonyl group --CO--, B is a 1,2-, 1,3-, 1,4-cyclohexylidene or 1,2- or 1,3-cyclopentylidene radical.

摘要翻译： 本发明提供通式如下的磺酰胺：其中R 1和R 2可以相同或不同，为氢或卤素原子或C 1 -C 6烷基，三氟甲基，氰基，羧基，烷氧基羰基 ，氨基羰基，N-烷基氨基羰基或N，N-二烷基氨基羰基，或者当R 1和R 2是彼此相邻的烷基时，R 1和R 2与它们连接的碳原子一起形成饱和或不饱和的C5-C7 - 亚烷基环，R3是氢原子，含有至多6个碳原子的烷基，酰基，苯基烷基或苯基烯基，其苯基部分可以被卤素，烷基或三氟甲基取代，C是 - （ CH 2）m - 基，其中m为0,1,2或3，或支链C 2 -C 5亚烷基，其中基团C的亚甲基-CH 2可以被氧或硫原子或羟基亚甲基 基团-CHOH-或羰基-CO-，B是1,2-，1,3-，1,4-亚环己基或1,2-或 1,3-亚环戊基。

公开(公告)号：US4931462A

公开(公告)日：1990-06-05

申请号：US287888

申请日：1988-12-21

申请人： Walter-Gunar Friebe ,  Erhard Reinholz ,  Liesel Doerge ,  Karlheinz Stegmeier

发明人： Walter-Gunar Friebe ,  Erhard Reinholz ,  Liesel Doerge ,  Karlheinz Stegmeier

IPC分类号： A61K31/34 ,  A61K31/343 ,  A61P7/02 ,  A61P9/00 ,  A61P11/08 ,  A61P11/14 ,  C07D209/42 ,  C07D307/85 ,  C07D333/70

CPC分类号： C07D307/85 ,  C07D209/42 ,  C07D333/70

摘要： New Sulphonamides of the formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are hydrogen or halogen atoms, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulphinyl, C.sub.1 -C.sub.6 -alkylsulphonyl or trifluoromethyl radicals or hydroxyl or cyano groups, R.sub.3 and R.sub.8, which can be the same or different, are hydrogen atoms, C.sub.1 -C.sub.6 -alkyl, benzyl or C.sub.1 -C.sub.6 -alkanoyl radicals, R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms or C.sub.1 -C.sub.6 -alkyl radicals, R.sub.6 and R.sub.7 are both hydrogen atoms or together form a valency bind, X is an oxygen or sulphur atom or an .dbd.NOH or .dbd.NR.sub.8 group and n is a whole number of from 1 to 4; and the physiologically acceptable salts thereof with inorganic and organic bases. These compounds are useful for example in the treatment of asthma or cardiovascular disease, thrombosis prevention and treatment, and to combat broncoconstriction.

摘要翻译： 新的具有下式的磺酰胺：其中R 1和R 2可以相同或不同，为氢或卤原子，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷硫基，C 1 C 1-6 - 烷基亚磺酰基，C 1 -C 6 - 烷基磺酰基或三氟甲基或羟基或氰基，可以相同或不同的R 3和R 8为氢原子，C 1 -C 6 - 烷基，苄基或C 1 -C 6 - 烷酰基， R4和R5可以相同或不同，是氢原子或C1-C6-烷基，R6和R7都是氢原子或一起形成价键，X是氧或硫原子或= NOH或= NR8组，n为1〜4的整数; 以及其与无机和有机碱的生理上可接受的盐。 这些化合物可用于例如治疗哮喘或心血管疾病，预防和预防血栓以及治疗支气管收缩。

公开(公告)号：US5446065A

公开(公告)日：1995-08-29

申请号：US75489

申请日：1993-06-21

申请人： Ernst-Christian Witte ,  Hansjorg Beckh ,  Karlheinz Stegmeier ,  Liesel Doerge

发明人： Ernst-Christian Witte ,  Hansjorg Beckh ,  Karlheinz Stegmeier ,  Liesel Doerge

IPC分类号： C07C311/13 ,  C07C311/17 ,  C07C311/18 ,  C07C311/21 ,  C07C311/29 ,  C07C323/67 ,  C07D295/185 ,  A61K31/18

CPC分类号： C07D295/185 ,  C07C311/17 ,  C07C311/18 ,  C07C2101/14

摘要： Compounds of the formula I ##STR1## in which R.sub.1 signifies an aryl, aralkyl or an aralkenyl group, the aryl radical of which can, in each case, be substituted one or more times by halogen, cyano, alkyl, trifluoromethyl, alkoxy, alkylthio, trifluoromethoxy, hydroxyl or carboxyl, m a whole number from 1 to 3, n a whole number from 1 to 5, R.sub.2 hydrogen, an alkyl, aralkyl or acyl group, Q a bond or an oxygen atom, R.sub.3 hydrogen or a lower alkyl radical which is possibly terminally substituted by carboxyl or by a hydroxyl group and R.sub.4 hydrogen, a lower alkyl group with 1-4 C-atoms, which is possibly terminally substituted by carboxyl or hydroxyl, a possibly substituted phenyl, heteroaryl, cycloalkyl or acyl group or a group ##STR2## in which R.sub.5 represents a straight-chained or branched alkyl chain with 1-4 C-atoms which is possibly terminally substituted by carboxyl, alkoxycarbonyl, aminocarbonyl, hydroxyl, mercapto, alkylthio or imidazolyl and Y a carboxyl, an alkoxycarbonyl, aminocarbonyl or cyano, formyl, hydroxymethyl, aminomethyl or ortho ester group, whereby R.sub.3 and R.sub.4 can also be component of a 5- or 6-membered saturated or unsaturated possibly substituted heterocycle with 1-4 heteroatoms which can be annellated with further ring compounds via one or more bonds, as well as their salts, esters and amides, processes for their preparation and medicaments with thromboxane-antagonistic action which contain these compounds.

摘要翻译： PCT No.PCT / EP91 / 02456 Sec。 371日期：1993年6月21日 102（e）日期1993年6月21日PCT 1991年12月19日PCT公布。 出版物WO92 / 日期：1992年7月9日。式Ⅰ化合物（Ⅰ）其中R1表示芳基，芳烷基或芳烯基，其芳基可以在每种情况下被卤素取代一次或多次 氰基，烷基，三氟甲基，烷氧基，烷硫基，三氟甲氧基，羟基或羧基，整数为1至3，na整数1至5，R 2氢，烷基，芳烷基或酰基，Q a键或氧 原子，R3氢或可能被羧基或羟基末端取代的低级烷基，R4为氢原子，可被羧基或羟基末端取代的具有1-4个C原子的低级烷基，可能被取代 苯基，杂芳基，环烷基或酰基或基团，其中R 5表示具有1-4个C原子的直链或支链烷基链，其可以被羧基末端取代，烷氧基羰基，氨基羰基，羟基，巯基，烷硫基 或咪唑基，Y是羧基，烷氧基羰基 1，氨基羰基或氰基，甲酰基，羟甲基，氨基甲基或原酸酯基，其中R3和R4也可以是具有1-4个杂原子的5或6元饱和或不饱和可能取代的杂环的组分，其可以与另外的环 通过一个或多个键的化合物，以及它们的盐，酯和酰胺，其制备方法和含有这些化合物的血栓烷拮抗作用的药物。

公开(公告)号：US5407951A

公开(公告)日：1995-04-18

申请号：US906339

申请日：1992-06-30

申请人： Ernst-Christian Witte ,  Karlheinz Stegmeier ,  Liesel Doerge

发明人： Ernst-Christian Witte ,  Karlheinz Stegmeier ,  Liesel Doerge

IPC分类号： A61K31/18 ,  A61K31/195 ,  A61K31/22 ,  A61K31/41 ,  A61P1/04 ,  A61P3/00 ,  A61P7/02 ,  A61P9/00 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/28 ,  C07C311/19 ,  C07C323/65 ,  C07D257/04 ,  C07D257/06 ,  C07C311/16 ,  C07C311/17

CPC分类号： C07D257/04 ,  C07C311/19 ,  C07D257/06 ,  C07C2101/14

摘要： The present invention provides sulphonamides of the general formula: ##STR1## wherein R.sup.1 and R.sup.2, which can be the same or different, are hydrogen or halogen atoms or C.sub.1 -C.sub.6 -alkyl, trifluoro-methyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, N-alkylaminocarbonyl or N,N-dialkylaminocarbonyl radicals or, when R.sup.1 and R.sup.2 are alkyl radicals ortho to one another, R.sup.1 and R.sup.2 together with the carbon atoms to which they are attached, form a saturated or unsaturated C.sub.5-C.sub.7 -alkylene ring, R.sup.3 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical, a phenylalkyl or phenylalkenyl radical, the phenyl moiety of which can be substituted by halogen, alkyl or trifluoromethyl, C is a --(CH.sub.2).sub.m --radical, in which m is 0, 1, 2 or 3, or a branched C.sub.2 -C.sub.5 -alkylene radical, whereby a methylene radical --CH.sub.2 --of the group C can be replaced by an oxygen or sulphur atom or by a hydroxymethylene radical --CHOH--or carbonyl group --CO--, B is a 1,2-, 1,3-, 1,4-cyclohexylidene or 1,2- or 1,3-cyclopentylidene radical.

摘要翻译： 本发明提供通式如下的磺酰胺：其中R 1和R 2可以相同或不同，为氢或卤素原子或C 1 -C 6烷基，三氟甲基，氰基，羧基，烷氧基羰基 ，氨基羰基，N-烷基氨基羰基或N，N-二烷基氨基羰基，或者当R 1和R 2是彼此邻位的烷基时，R 1和R 2与它们所连接的碳原子一起形成饱和或不饱和的C 5 -C 7 - 亚烷基环，R 3是氢原子，含有至多6个碳原子的烷基，酰基，苯基烷基或苯基烯基，其苯基部分可以被卤素，烷基或三氟甲基取代，C是 - （CH 2 ）m-基，其中m为0,1,2或3，或支链C 2 -C 5 - 亚烷基，其中基团C的亚甲基-CH 2可以被氧或硫原子替代，或由 羟基亚甲基-CHOH-或羰基-CO-，B是1,2-，1,3-，1,4-亚环己基或1,2-或1， 3-环戊基。

公开(公告)号：US4948809A

公开(公告)日：1990-08-14

申请号：US281955

申请日：1988-12-05

申请人： Ernst-Christian Witte ,  Hans-Peter Wolff ,  Karlheinz Stegmeier ,  Johannes Pill

发明人： Ernst-Christian Witte ,  Hans-Peter Wolff ,  Karlheinz Stegmeier ,  Johannes Pill

IPC分类号： A61K31/655 ,  A61K31/18 ,  A61K31/185 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K31/275 ,  A61P1/04 ,  A61P7/02 ,  A61P9/00 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P43/00 ,  C07C67/00 ,  C07C301/00 ,  C07C303/38 ,  C07C303/40 ,  C07C311/00 ,  C07C311/15 ,  C07C311/16 ,  C07C311/17 ,  C07C311/29 ,  C07C311/39 ,  C07D307/33

CPC分类号： C07D307/33 ,  C07C309/00

摘要： The present invention provides sulphonylphenylalkylamines of the general formula: ##STR1## wherein R.sub.1 is an alkyl radical containing up to 6 carbon atoms, a cycloalkyl radical containing 3-7 carbon atoms or an aralkyl, aralkenyl or aryl radical, the aryl moiety, in each case, being optionally substituted one or more times by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino, C.sub.1 -C.sub.6 acylamino, C.sub.1 -C.sub.16 acyl or azide, R.sub.2 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical or an aralkyl or aralkenyl radical, the aryl moiety, in each case, optionally being substituted one or more times by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.1 -C.sub.12 dialkylamino, C.sub.1 -C.sub.6 acylamino, C.sub.1 -C.sub.16 acyl or azide, B is an unbranched or branched alkylene chain with a maximum of 4 carbon atoms and A an alkyl or alkenyl radical containing up to 6 carbon atoms, a C.sub.1 -C.sub.6 formylalkyl radical, a C.sub.1 -C.sub.6 hydroxy-alkyl group or a radical --D--R.sub.3, in which D is a ##STR2## and R.sub.3 is a hydrogen atom, a C.sub.1 -C.sub.5 alkyl, a C.sub.1 -C.sub.5 hydroxyalkyl or a C.sub.1 -C.sub.5 alkylcarboxylic acid radical, as well as the pharmacologically acceptable salts thereof, the esters and amides thereof and the lactones of those compounds which contain a hydroxyl and a carboxyl group, with the exception of the compound benzene-sulphonic acid-(4-acetylphenethylamide).The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.

摘要翻译： 本发明提供通式如下的磺酰基苯基烷基胺：其中R 1是含有至多6个碳原子的烷基，含有3-7个碳原子的环烷基或芳烷基，芳烯基或芳基，芳基部分 任选被卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，三氟甲基，氰基，硝基，氨基，C 1 -C 6烷基氨基，C 2 -C 12二烷基氨基，C 1 -C 6酰基氨基， C1-C16酰基或叠氮化物，R2是氢原子，含有至多6个碳原子的烷基，酰基或芳烷基或芳烯基，芳基部分，在每种情况下，任选被卤素取代一次或多次 ，C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，三氟甲基，氰基，硝基，氨基，C 1 -C 6烷基氨基，C 1 -C 12二烷基氨基，C 1 -C 6酰氨基，C 1 -C 16酰基或叠氮基，B是无支链或支链亚烷基 具有最多4个碳原子的链，A是含有至多6个碳的烷基或烯基 原子，C 1 -C 6甲酰基烷基，C 1 -C 6羟基烷基或基团-D-R 3，其中D是R 3，R 3是氢原子，C 1 -C 5烷基，C 1 -C 5 羟基烷基或C1-C5烷基羧酸基团，以及其药理学上可接受的盐，其中含有羟基和羧基的那些化合物的酯和酰胺和内酯，除了化合物苯磺酸 - （4-乙酰苯乙胺）。 本发明还提供了制备这些化合物的方法和含有它们的药物组合物。

公开(公告)号：US4711896A

公开(公告)日：1987-12-08

申请号：US840563

申请日：1986-02-21

申请人： Jacob Bar-Tana ,  Ernst-Christian Witte ,  Bernd Hagenbruch ,  Johannes Pill ,  Karlheinz Stegmeier

发明人： Jacob Bar-Tana ,  Ernst-Christian Witte ,  Bernd Hagenbruch ,  Johannes Pill ,  Karlheinz Stegmeier

IPC分类号： C07C55/02 ,  A61K31/19 ,  A61P3/06 ,  A61P3/08 ,  C07C51/00 ,  C07C55/28 ,  C07C55/32 ,  C07C57/13 ,  C07C57/30 ,  C07C57/34 ,  C07C57/38 ,  C07C57/42 ,  C07C57/52 ,  C07C59/245 ,  C07C59/305 ,  C07C59/84 ,  C07C67/00 ,  C07C121/48 ,  C07C121/50

CPC分类号： C07C57/42 ,  C07C55/28 ,  C07C55/32 ,  C07C57/13 ,  C07C57/34 ,  C07C57/38 ,  C07C59/245 ,  C07C59/305 ,  C07C59/84

摘要： ##STR1## α, ω-dicarboxylic acids having the general formula (I') in which: R
1 and R
2 , which may be different or the same, represent a lower alkyl group which can be substituted by hydroxy, lower alkoxy, halogen or phenyl, the phenyl being capable of substitution one or several times by hydroxy, lower alkoxy, lower alkyl or halogen; a lower alkenyl or alkinyl group; a C
3 -C
7 -cyclo-alkyl group or a phenyl group possibly substituted by hydroxy, halogen, lower alkyl or lower alkoxy, and X and Y, which may be different or the same, represent hydrogen, lower alkyl, lower alkoxy, hydroxy, cyano, halogen, carboxyl, lower alkoxycarbonyl or carbamoyl, and Q represents non-ramified, saturated or unsaturated alkyl chain with 8-14 C atoms, which can be substituted, interrupted by hetero-atoms, and form part of a cyclic system, as well as their carboxylic acid derivatives in vivo, provided that when Q represents an unramified, saturated alkyl chain with 8-14 C atoms, and R
1 and R
2 represent methyl and Y represents hydrogen, X may not represent hydrogen, ethoxy-carbonyl, bromine, cyano or methyl, and if R
1 and R
2 represent methyl and X and Y hydrogen, then Q may not represent any formula (II) group. Process for their preparation and medicines containing these compounds, which have an anti-diabetic action and lower the level of lipids.

摘要翻译： PCT No.PCT / EP85 / 00288 Sec。 371日期1986年2月21日 102（e）日期1986年2月21日PCT归档1985年6月15日PCT公布。 公开号WO86 / 00298 日本1月16日，1986年1月16日，具有通式（I'）的α，ω-二羧酸，其中：R1和R2可以不同或相同，表示 可被羟基，低级烷氧基，卤素或苯基取代的低级烷基，苯基能够被羟基，低级烷氧基，低级烷基或卤素取代一次或几次; 低级烯基或炔基; 可以被羟基，卤素，低级烷基或低级烷氧基取代的C 3 -C 7 - 环烷基或苯基，X和Y可以不同或相同，表示氢，低级烷基，低级烷氧基，羟基， 氰基，卤素，羧基，低级烷氧基羰基或氨基甲酰基，Q表示具有8-14个C原子的非分支，饱和或不饱和的烷基链，其可被取代，被杂原子间隔并形成环系的一部分，如 以及它们的体内羧酸衍生物，条件是当Q表示具有8-14个C原子的未饱和的饱和烷基链时，R 1和R 2表示甲基且Y表示氢，X可以不表示氢，乙氧羰基，溴， 氰基或甲基，并且如果R 1和R 2表示甲基且X和Y氢，则Q可以不表示任何式（II）基团。 其制备方法和含有这些化合物的药物，其具有抗糖尿病作用并降低脂质水平。

公开(公告)号：US4609673A

公开(公告)日：1986-09-02

申请号：US682935

申请日：1984-12-18

申请人： Hermann Eggerer ,  Bernd Hagenbruch ,  Tran G. Nguyen ,  Karlheinz Stegmeier ,  Johannes Pill

发明人： Hermann Eggerer ,  Bernd Hagenbruch ,  Tran G. Nguyen ,  Karlheinz Stegmeier ,  Johannes Pill

IPC分类号： A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K31/23 ,  A61P3/06 ,  C07C67/00 ,  C07C301/00 ,  C07C313/00 ,  C07C315/04 ,  C07C317/44 ,  C07C317/46 ,  C07C323/51 ,  C07C149/20 ,  C07C147/05

CPC分类号： A61K31/23

摘要： The present invention provides carboxylic acid derivatives of the general formula: ##STR1## wherein R is a hydrogen atom, alkyl, a metal cation or an ammonium or alkylammonium ion, R.sub.1 is a hydrogen atom, a hydroxyl group or an alkyl, O-alkyl,O-benzyl or O-acyl radical, R.sub.2 is a hydrogen atom or an alkyl, aryl or aralkyl radical, n is 0, 1 or 2 and R.sub.3 is an acyl radical, this radical being(a) a straight-chained or branched, saturated or unsaturated alkanoyl radical containing 2 to 11 carbon atoms; or(b) the radical ##STR2## in which A is a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon radical containing up to 4 carbon atoms, which is optionally substituted by hydroxyl, and B is a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon radical containing up to 8 carbon atoms, which is optionally substituted one or more times by hydroxyl, carboxyl or phenyl, or B is a phenyl or cycloalkyl radical; or(c) the radical ##STR3## in which A and B have the same meanings as in (b) and R.sub.4 is a hydrogen atom or an alkyl or aralkyl radical; as well as the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these compounds, as well as 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是氢原子，烷基，金属阳离子或铵或烷基铵离子，R1是氢原子，羟基或烷基， O-烷基，O-苄基或O-酰基，R2是氢原子或烷基，芳基或芳烷基，n是0,1或2，R3是酰基，该基团是（a） 含有2至11个碳原子的链或支链，饱和或不饱和烷酰基; 或（b）其中A是含有至多4个碳原子的直链或支链，饱和或不饱和的脂族烃基的基团，其任选被羟基取代，B是直链或支链的， 含有至多8个碳原子的饱和或不饱和脂族烃基，其任选被羟基，羧基或苯基取代一次或多次，或B是苯基或环烷基; 或（c）其中A和B具有与（b）中相同含义的基团，R4为氢原子或烷基或芳烷基; 以及其药理学上可接受的盐。 本发明还提供了制备这些化合物的方法，以及含有它们的药物组合物。

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。