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41. 发明授权

US4714708A Derivatives of cis, endo-2-azabicyclo[5.3.0]decane-3-carboxylic acid, and their use for treating hypertension 失效
标题翻译：顺式，内-2-氮杂双环[5.3.0]癸烷-3-羧酸的衍生物及其用于治疗高血压的用途
公开(公告)号：US4714708A
公开(公告)日：1987-12-22
申请号：US561230
申请日：1983-12-14
申请人： Hansjorg Urbach , Rainer Henning , Volker Teetz , Reinhard Becker
发明人： Hansjorg Urbach , Rainer Henning , Volker Teetz , Reinhard Becker
IPC分类号： A61K31/40 , A61K31/403 , A61K38/00 , A61P9/12 , A61P43/00 , C07D209/52 , C07K1/113 , C07K5/02 , C07K14/81 , C07D209/02
CPC分类号： C07K5/0222 , C07D209/52 , A61K38/00
摘要： The invention relates to derivatives of cis,endo-2-azabicyclo[5.3.0]decane-3-carboxylic acid of the formula I ##STR1## in which R denotes hydrogen, alkyl, alkenyl or aralkyl, R.sup.1 denotes hydrogen, allyl, vinyl or a side chain of an optionally protected naturally occurring .alpha.-aminoacid, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen, or Y and Z together denote oxygen, X denotes alkyl, alkenyl, cycloalkyl, aryl which can be substituted once, twice or three times by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, and their physiologically acceptable salts, a process for their preparation, agents containing them and their use.
摘要翻译：本发明涉及式I（I）的顺式，内-2-氮杂双环[5.3.0]癸烷-3-羧酸衍生物，其中R表示氢，烷基，烯基或芳烷基，R1表示氢，烯丙基，乙烯基或任选保护的天然α-氨基酸的侧链，R2表示氢，烷基，烯基或芳烷基，Y表示氢或羟基，Z表示氢，或Y和Z一起表示氧，X表示烷基，烯基烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基或亚甲基二氧基取代一次，两次或三次的芳基，或表示吲哚-3-基，及其生理上可接受的盐，他们的准备，包含他们的代理和他们的使用。

42. 发明授权

US4668797A Bicyclic aminoacids as intermediates and processes for their preparation 失效
标题翻译：双环氨基酸作为中间体及其制备方法
公开(公告)号：US4668797A
公开(公告)日：1987-05-26
申请号：US780937
申请日：1985-09-27
申请人： Hansj/o/ rg Urbach , Rainer Henning , Volker Teetz , Hans Wissman , Reinhard Becker
发明人： Hansj/o/ rg Urbach , Rainer Henning , Volker Teetz , Hans Wissman , Reinhard Becker
IPC分类号： A61K31/403 , A61K31/404 , A61K31/405 , A61K38/00 , A61K38/55 , A61P9/12 , C07D209/42 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81 , C07D209/26 , C07D209/18
CPC分类号： C07K5/0222 , C07D209/42 , A61K38/00
摘要： The invention relates to compounds of the formula I ##STR1## in which n denotes 0 or 1,R denotes hydrogen, alkyl or aralky, R.sup.1 denotes hydrogen or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, which each can be substituted by alkyl, alkoxy or halogen, arylalkyl or aroylalkyl, both of which can be substituted in the aryl radical as defined in the aforegoing, a monocyclic or bicyclic sulfur or oxygen and/or nitrogen heterocyclic radical, or a side chain of a naturally occurring aminoacid, R.sup.2 denotes hydrogen, alkyl, alkenyl or arylalkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes alkyl, alkenyl, cycloalkyl, aryl, which is monosubstituted, disubstituted or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy or 3-indolyl,and their physiologically acceptable salts, processes for their preparation, agents containing these and their use as medicaments and also bicyclic amino acids as their intermediates and processes for their preparation.
摘要翻译：本发明涉及式I的化合物，其中n表示0或1，R表示氢，烷基或芳烷基，R 1表示氢或烷基，其可任选被氨基，酰氨基或苯甲酰基氨基取代，，环烷基，环烯基，环烷基烷基，芳基或部分氢化的芳基，其各自可以被烷基，烷氧基或卤素，芳基烷基或芳酰基烷基取代，二者可以在如上所定义的芳基中被取代，单环或双环硫或氧和/或氮杂环基或天然存在的氨基酸的侧链，R 2表示氢，烷基，烯基或芳烷基，Y表示氢或羟基，Z表示氢或Y，Z一起表示氧，X表示烷基，烯基，环烷基，芳基，其被烷基，烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基或亚甲二氧基或3-吲哚基单取代或三取代，并且它们的生理接受其制备方法，含有这些物质的药剂及其作为药物的用途以及双环氨基酸作为其中间体及其制备方法。

43. 发明授权

US4624962A Substituted derivatives of 2-azabicyclo-[3.3.0]octanes 失效
标题翻译：取代的2-氮杂双环[3.3.0]辛烷的衍生物
公开(公告)号：US4624962A
公开(公告)日：1986-11-25
申请号：US697340
申请日：1985-02-01
申请人： Rainer Henning , Hansjorg Urbach , Rolf Geiger , Volker Teetz , Bernward Scholkens
发明人： Rainer Henning , Hansjorg Urbach , Rolf Geiger , Volker Teetz , Bernward Scholkens
IPC分类号： C07C275/16 , C07C67/00 , C07C239/00 , C07C275/24 , C07C279/14 , C07C301/00 , C07C303/40 , C07C311/30 , C07C313/00 , C07C315/04 , C07C317/50 , C07C323/44 , C07C323/57 , C07C323/59 , C07D207/16 , C07D207/22 , C07D209/20 , C07D209/42 , C07D209/52 , C07D211/60 , C07D213/55 , C07D217/12 , C07D217/26 , C07D223/06 , C07D231/12 , C07D233/54 , C07D277/06 , C07D333/24 , C07D333/60 , C07D401/12 , C07D403/12 , C07D409/12 , C07D471/04 , C07D495/04 , A61K31/40
CPC分类号： C07D231/12 , C07C275/24 , C07C323/44 , C07D207/16 , C07D207/22 , C07D209/20 , C07D209/42 , C07D209/52 , C07D211/60 , C07D213/55 , C07D217/26 , C07D223/06 , C07D233/64 , C07D277/06 , C07D333/24 , C07D333/60 , C07D401/12 , C07D403/12 , C07D409/12 , C07D471/04 , C07D495/04 , C07C2101/04 , C07C2101/08
摘要： Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.sup.6 denotes hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, optionally monosubstituted or disubstituted phenyl or naphthyl, their salts, a process for their preparation and their use as medicaments.
摘要翻译：式I的化合物其中n表示0-3，R1和R1'相同或不同，表示氢，烷基或链烯基，苯基或苄基，各自根据需要取代; R2表示氢，烷基或烯基; R3表示氢，烷基，羟基烷基，烷氧基烷基或氨基烷基，烷酰基氨基烷基，胍基烷基，咪唑基烷基，吲哚基烷基，巯基烷基或烷硫基烷基，苯基烷基，羟基苯基烷基，苯氧基烷基或苯硫基烷基，或R2和R3与携带它们的C和N原子一起表示饱和或不饱和的4至8元单环或8至10元双环的单环或杂环，任选被羟基，具有1至3个C原子的烷氧基或烷基单取代或二取代，R4表示氢，烷基，烯基，链烯基，炔基，链烯基或烷撑基，环烷基，苯基，苄基，苯乙基或苯基丙基，它们各自可以任选被单取代或二取代; R5表示氢或烷基，羟基或烷氧基，R6表示氢，任选取代的烷基，环烷基，烯基，任选单取代或二取代的苯基或萘基，它们的盐，其制备方法及其作为药物的用途。

44. 发明授权

US4620012A Spirocyclic aminoacid derivatives, processes for their preparation, agents containing them and their use and new spirocyclic aminoacids as intermediates and processes for their preparation 失效
标题翻译：螺环氨基酸衍生物，其制备方法，含有它们的药剂及其用途和新的螺环氨基酸作为中间体及其制备方法
公开(公告)号：US4620012A
公开(公告)日：1986-10-28
申请号：US569758
申请日：1984-01-10
申请人： Rainer Henning , Hansjorg Urbach , Volker Teetz , Reinhard Becker
发明人： Rainer Henning , Hansjorg Urbach , Volker Teetz , Reinhard Becker
IPC分类号： A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07D209/96 , C07D317/28 , C07D317/30 , C07D317/32 , C07D317/72 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/078 , C07K14/81 , C07C103/52 , A61K37/02
CPC分类号： C07K5/0222 , C07D209/96 , C07D317/28 , C07D317/30 , A61K38/00
摘要： The invention relates to new spirocyclic aminoacid derivatives of the formula I ##STR1## in which m denotes 1 or 2, n denotes 0 or 1, R denotes hydrogen, alkyl or aralkyl, R.sup.1 denotes hydrogen or alkyl which can be optionally substituted by amino, acylamino or benzoylamino, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, each of which can be substituted by alkyl, alkoxy or halogen, arylalkyl or aroylalkyl, both of which can be substituted as defined above in the aryl radical, an S- or O- and/or N-heterocyclic radical or a side chain of an .alpha.-aminoacid, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen, or Y and Z together denote oxygen and X denotes alkyl, alkenyl, cycloalkyl, aryl, which can be monosubstituted, disubstituted or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino and/or methylenedioxy, or 3-indolyl, processes for their preparation, agents containing them and their use and new spirocyclic aminoacids as intermediates and a process for their preparation.
摘要翻译：本发明涉及式I（I）的新的螺环氨基酸衍生物，其中m表示1或2，n表示0或1，R表示氢，烷基或芳烷基，R1表示氢或可任意取代的烷基芳基或部分氢化的芳基，其中每一个可以被烷基，烷氧基或卤素取代，芳基烷基或芳酰基烷基，它们都可以如上所述被取代，在芳基基团，S-或O-和/或N-杂环基团或α-氨基酸的侧链，R2表示氢，烷基，烯基或芳烷基，Y表示氢或羟基，Z表示氢，或Y和Z在一起表示氧，X表示烷基，烯基，环烷基，芳基，其可以被烷基，烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基和/或亚甲二氧基或3-吲哚基单取代或三取代，准备工作包含它们及其用途和新的螺环氨基酸作为中间体及其制备方法。

45. 发明授权

US4515960A Spiro-2-aza-alkane-3-carbonitriles, their preparation and their use 失效
标题翻译：螺-2-氮杂 - 烷烃-3-碳腈，它们的制备及其用途
公开(公告)号：US4515960A
公开(公告)日：1985-05-07
申请号：US494983
申请日：1983-05-16
申请人： Volker Teetz
发明人： Volker Teetz
IPC分类号： C07D209/54 , C07D215/48 , C07D221/04 , C07D221/20 , C07D223/14 , C07D223/32 , C07D225/04 , C07D225/06 , C07K5/06
CPC分类号： C07D209/54
摘要： The invention provides compounds of the formula I ##STR1## in which m is 1 to 3 and n is 1 to 4, a process for their preparation, and their use as intermediates for the manufacture of valuable medicaments, and starting products for the preparation of compounds of the formula I.
摘要翻译：本发明提供了式I（I）化合物，其中m为1至3，n为1至4，其制备方法及其作为制备有价值药物的中间体的用途，以及用于制备式Ⅰ化合物。

46. 发明授权

US4515803A Substituted derivatives of octahydroindole-2-carboxylic acids 失效
标题翻译：取代的八氢吲哚-2-羧酸的衍生物
公开(公告)号：US4515803A
公开(公告)日：1985-05-07
申请号：US413663
申请日：1982-09-01
申请人： Rainer Henning , Hansjorg Urbach , Rolf Geiger , Volker Teetz , Bernward Scholkens
发明人： Rainer Henning , Hansjorg Urbach , Rolf Geiger , Volker Teetz , Bernward Scholkens
IPC分类号： C07C275/16 , C07C67/00 , C07C239/00 , C07C275/24 , C07C279/14 , C07C301/00 , C07C303/40 , C07C311/30 , C07C313/00 , C07C315/04 , C07C317/50 , C07C323/44 , C07C323/57 , C07C323/59 , C07D207/16 , C07D207/22 , C07D209/20 , C07D209/42 , C07D209/52 , C07D211/60 , C07D213/55 , C07D217/12 , C07D217/26 , C07D223/06 , C07D231/12 , C07D233/54 , C07D277/06 , C07D333/24 , C07D333/60 , C07D401/12 , C07D403/12 , C07D409/12 , C07D471/04 , C07D495/04 , C07D209/12
CPC分类号： C07D231/12 , C07C275/24 , C07C323/44 , C07D207/16 , C07D207/22 , C07D209/20 , C07D209/42 , C07D209/52 , C07D211/60 , C07D213/55 , C07D217/26 , C07D223/06 , C07D233/64 , C07D277/06 , C07D333/24 , C07D333/60 , C07D401/12 , C07D403/12 , C07D409/12 , C07D471/04 , C07D495/04 , C07C2101/04 , C07C2101/08
摘要： Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxyphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.sup.6 denotes hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, optionally monosubstituted or disubstituted phenyl or naphthyl,their salts, a process for their preparation and their use as medicaments.
摘要翻译：式I的化合物其中n表示0-3，R1和R1'相同或不同，表示氢，烷基或链烯基，苯基或苄基，各自根据需要取代; R2表示氢，烷基或烯基; R3表示氢，烷基，羟基烷基，烷氧基烷基或氨基烷基，烷酰基氨基烷基，胍基烷基，咪唑基烷基，吲哚基烷基，巯基烷基或烷硫基烷基，苯基烷基，羟基苯基烷基，苯氧基烷基或苯硫基烷基，或R2和R3与携带它们的C和N原子一起表示饱和或不饱和的4至8元单环或8至10元双环的单环或杂环，任选被羟基，具有1至3个C原子的烷氧基或烷基单取代或二取代，R4表示氢，烷基，烯基，链烯基，炔基，链烯基或烷撑基，环烷基，苯基，苄基，苯乙基或苯基丙基，它们各自可以任选被单取代或二取代; R5表示氢或烷基，羟基或烷氧基，R6表示氢，任选取代的烷基，环烷基，烯基，任选单取代或二取代的苯基或萘基，它们的盐，其制备方法及其作为药物的用途。

47. 发明授权

US4459225A Peptide amides and process for their manufacture 失效
标题翻译：肽酰胺及其制造方法
公开(公告)号：US4459225A
公开(公告)日：1984-07-10
申请号：US359242
申请日：1982-03-18
申请人： Volker Teetz , Rolf Geiger , Hans G. Alpermann , Martin Bickel
发明人： Volker Teetz , Rolf Geiger , Hans G. Alpermann , Martin Bickel
IPC分类号： C07K5/08 , A61K38/00 , A61P25/04 , C07K5/087 , C07K5/10 , C07K5/107 , C07K7/06 , C07K14/70 , C07C103/52
CPC分类号： C07K5/0812 , C07K14/702 , C07K5/1016
摘要： New peptide amides of the formula IH--Tyr--D--Lys(For)--Gly--X (I)whereinFor is formyl,X is alkylamino, dehydro-Phe or Phe-alkylamido having up to 6 carbon atoms in the alkyl moiety, which moiety may be substituted by hydroxy and/or phenyl, Phe-cycloalkylamide or Phe-cycloalkylene amide having up to 8 carbon atoms in the cycloalkyl or cyclalkylene moiety, 1 to 2 CH.sub.2 groups being optionally replaced by --NH--, --O--, --S-- or --CO--, Phe-alkylene-cycloalkylamide having from 5 to 6 ring carbon atoms, which amide may be substituted by carbonamido,N-alkylcarbonamido or alkyl and 1 carbon atom whereof may be replaced by nitrogen, Phe-endo- or exo-norbornylamide or Phe-thiazolamide or Phe-thiazolidine-carboxylic acid amide, which may be substituted by 1 to 4 methyl groups each,and process for their manufacture are disclosed. These peptide amides are distinguished by an analgetic activity and suppress the motility of the ileum of the guinea pig.
摘要翻译：式I H-Tyr-D-Lys（For）-Gly-X（I）的新肽酰胺其中For为甲酰基，X为烷基部分中具有至多6个碳原子的烷基氨基，脱氢-Phe或Phe-烷基酰氨基，该部分可以被羟基和/或苯基取代，在环烷基或环亚烷基部分具有至多8个碳原子的Phe-环烷基酰胺或Phe-亚环烷基酰胺，1至2个CH 2基团任选地被-NH-，-O- ，具有5至6个环碳原子的-S-或-CO-，Phe-亚烷基 - 环烷基酰胺，该酰胺可以被碳酰氨基取代，N-烷基碳酰氨基或其烷基和碳原子可以被氮取代，Phe-内 - 或外 - 降冰片烷酰胺或Phe-噻唑胺或Phe-噻唑烷 - 羧酸酰胺，其可以各自被1至4个甲基取代，以及其制造方法。这些肽酰胺通过止痛活性来区分，并抑制豚鼠回肠的动力。

48. 发明授权

US4361482A Chromatograph for pressure chromatography 失效
标题翻译：色谱柱进行压力色谱
公开(公告)号：US4361482A
公开(公告)日：1982-11-30
申请号：US309455
申请日：1981-10-07
申请人： Volker Teetz , Rainer Uhmann , Rudolf Knapp
发明人： Volker Teetz , Rainer Uhmann , Rudolf Knapp
IPC分类号： G01J3/46 , B01D15/08 , G01N21/01 , G01N30/36 , G01N30/60
CPC分类号： B01D15/22 , G01N30/6021 , G01N30/36
摘要： In this chromatograph for pressure chromatography, a plunger having a plunger stem is arranged so that it can move within the separation column (3). On the front face of the plunger there is a collecting space (7) for liquid, which is covered by a frit (6) and which has a connecting line (8) to the face of the plunger opposed to the front face. In order to prevent abrasive and chemical attack by the column packing on the plunger, its seal and the cylinder wall of the separation column, the plunger should comprise a lower part (2) having a device (4) to accommodate the plunger stem (5), and an upper part (1), the two parts being arranged so that they can move in relation to one another. The upper part (1) has a centering peg (9) which projects into the lower part (2). A spring (12) on which the upper part (1) is supported, is located concentrically in relation to the peg (9). The upper part (1) has recesses on its circumference to accommodate at least two seals (19 and 21) and a ring channel (16) which is formed by a retaining ring (13) for one seal (19) and is connected to the collecting space (7). The other seal (21) is held in its recess by a ring (23) which is located concentrically around the spring and is supported by the lower part.
摘要翻译：在这种压力色谱色谱仪中，具有柱塞杆的柱塞被布置成使其能够在分离柱（3）内移动。在柱塞的前表面上有用于液体的收集空间（7），其被玻璃料（6）覆盖，并且具有与前表面相对的柱塞的表面的连接线（8）。为了防止柱塞上的柱填料，其密封件和分离柱的气缸壁的研磨和化学侵蚀，柱塞应包括具有装置（4）的下部（2），以容纳柱塞杆（5））和上部（1），两个部分被布置成使得它们可以相对于彼此移动。上部（1）具有突出到下部（2）中的定心栓（9）。支撑上部（1）的弹簧（12）相对于钉（9）同心地定位。上部（1）在其圆周上具有凹部以容纳至少两个密封件（19和21）和环形通道（16），该通道由用于一个密封件（19）的保持环（13）形成，并且连接到收集空间（7）。另一个密封件（21）通过环（23）保持在其凹部中，环（23）同心地位于弹簧周围并由下部支撑。

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