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51. 发明申请

WO1993010087A1 DERIVATIVES OF CYCLIC PHENOLIC THIOETHERS AS INHIBITORS OR STIMULATORS OF SUPEROXIDE GENERATION 审中-公开
标题翻译：作为抑制剂或超氧化物生成刺激剂的循环酚类衍生物的衍生物
公开(公告)号：WO1993010087A1
公开(公告)日：1993-05-27
申请号：PCT/US1992009560
申请日：1992-11-17
申请人： G.D. SEARLE & CO. , MUELLER, Richard, August , PARTIS, Richard, Allen
发明人： G.D. SEARLE & CO.
IPC分类号： C07C323/52
CPC分类号： C07D213/40 , C07C323/17 , C07C323/20 , C07C323/22 , C07C323/52 , C07C323/60 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D307/18 , C07D307/20 , C07D493/04
摘要： The present invention relates to compounds of formula (I) and the pharmaceutically acceptable salts thereof wherein R , R and R are the same or different and independently represent alkyl, alkoxy, hydroxy, phenyl, halogen, trifluoromethyl, cyano, or hydrogen; q is 0 or 1; R represents hydrogen, alkyl, alkoxy, or hydroxy; X represents O, S or (CH2)m wherein m is an integer from 0 to 4; A represents O or S(O)n wherein n is 0, 1, or 2; Alk is straight or branched chain alkyl having 1 to 6 carbon atoms; p is 0 or 1; and R represents: (a) alkyl; (b) OH; (c) OR wherein R is alkyl of 1 to 6 carbon atoms; (d) NR R wherein R is hydrogen or alkyl, and R is hydrogen, alkyl, alkoxyalkyl, heterocyclealkyl, substituted heterocyclealkyl, cycloalkyl, substituted cycloalkyl, phenyl, substituted phenyl, phenylalkyl, substituted phenylalkyl, or Alk-NR R wherein Alk is alkyl of 1 to 10 carbon atoms and R and R each independently are hydrogen or alkyl; or NR R together form a heterocyclic ring which may optionally be substituted; or (e) (CH2)tCOOR wherein t is an integer from 1 to 4 and r is hydrogen or alkyl of 1 to 4 carbon atoms. The compounds are inhibitors or stimulators of superoxide generation.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，其中R 1，R 2和R 10相同或不同并且独立地表示烷基，烷氧基，羟基，苯基，卤素，三氟甲基，氰基或氢; q为0或1; R 3表示氢，烷基，烷氧基或羟基; X表示O，S或（CH 2）m，其中m为0至4的整数; A表示O或S（O）n，其中n为0,1或2; Alk 1是具有1至6个碳原子的直链或支链烷基; p为0或1; 并且R表示：（a）烷基; （b）OH; （c）OR 4其中R 4为1至6个碳原子的烷基; （d）NR 5 R 6其中R 5是氢或烷基，R 6是氢，烷基，烷氧基烷基，杂环烷基，取代的杂环烷基，环烷基，取代的环烷基，苯基，取代的苯基，苯基烷基，取代的苯基烷基或Alk-NR 8 R 9其中Alk是1-10个碳原子的烷基，R 8和R 9各自独立地是氢或烷基; 或NR 5 R 6一起形成可任选被取代的杂环; 或（e）（CH 2）t COOR 7，其中t是1至4的整数，r 7是氢或1至4个碳原子的烷基。这些化合物是超氧化物产生的抑制剂或刺激剂。

52. 发明申请

WO1993010077A1 N,N-DI-ALKYL(PHENOXY)BENZAMIDE DERIVATIVES 审中-公开
标题翻译： N，N-DI-ALKYL（PHENOXY）BENZAMIDE DERIVATIVES
公开(公告)号：WO1993010077A1
公开(公告)日：1993-05-27
申请号：PCT/US1992009014
申请日：1992-10-29
申请人： G.D. SEARLE & CO. , NOSAL, Roger, Anthony , STEALEY, Michael, Allan , WEIER, Richard, Mathias
发明人： G.D. SEARLE & CO.
IPC分类号： C07C233/64
CPC分类号： C07C235/54 , C07C233/65 , C07C235/42 , C07C235/84 , C07C237/38 , C07C2601/08 , C07C2601/14 , C07D317/60 , C07D317/64 , Y10S514/826 , Y10S514/886
摘要： The present invention relates to compounds of formula (I), and the pharmaceutically acceptable salts thereof, wherein Z can be (a) wherein R3 is alkyl having 1 to 6 carbon atoms and, when n is greater than 1, each R3 can be the same or different; and n is an integer from 1 to 3; or (b); R?1 and R2¿ can each independently be hydrogen, straight or branched chain alkyl, or cycloalkyl having 3 to 8 carbon atoms which can optionally be substituted at one or more positions by alkyl of 1 to 6 carbon atoms; X is oxygen, sulfur, NR4, wherein R4 is hydrogen or alkyl having 1 to 4 carbon atoms, C=O, CHOH, or CH¿2?; Y is hydrogen, alkoxy, halogen, alkyl, or hydroxy; and m is an integer from 0 to 3. The compounds are antagonists of platelet-activating factor (PAF).

53. 发明申请

WO1993009086A1 PROPARGYL GLYCINE AMINO PROPARGYL DIOL COMPOUNDS FOR TREATMENT OF HYPERTENSION 审中-公开
标题翻译：用于治疗高血压的丙二醇氨基酚丙二醇化合物
公开(公告)号：WO1993009086A1
公开(公告)日：1993-05-13
申请号：PCT/US1992008840
申请日：1992-10-22
申请人： G.D. SEARLE & CO. , HANSON, Gunnar, J. , BARAN, John, S.
发明人： G.D. SEARLE & CO.
IPC分类号： C07C237/22
CPC分类号： C07C237/22 , C07C271/20 , C07C2601/14 , C07D277/30
摘要： Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of formula (I) wherein A is selected from CO and SO2 wherein X is selected from oxygen atom and methylene; wherein each of R1 and R9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b,b,b-trifluororethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R1 and R9 are attached may be combined with oxygen to form an N-oxide; wherein R2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R5 and R8 is independently propargyl or a propargyl-contaning moiety; wherein R7 is cyclohexylmethyl; wherein each of R4 and R6 is independently selected from hydrido and methyl; wherein each of R11 and R12 is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.

54. 发明申请

WO1992022279A2 N-[ARYLETHYL]-N-ALKYL-2-(1-PYRROLIDINYL)ETHYLAMINE DERIVATIVES FOR CNS DISORDERS 审中-公开
标题翻译：用于CNS疾病的N-（ARYLETHYL）-N-烷基-2-（1-吡咯烷基）乙酰胺衍生物
公开(公告)号：WO1992022279A2
公开(公告)日：1992-12-23
申请号：PCT/US1992004436
申请日：1992-06-03
申请人： G.D. SEARLE & CO. , DE COSTA, Brian, R. , RADESCA, Lilian , BOWEN, Wayne , LONG, Joseph , WALKER, J., Michael , RICE, Kenner, C. , GRAY, Nancy, M. , CONTRERAS, Patricia, C.
发明人： G.D. SEARLE & CO.
IPC分类号： A61K0
CPC分类号： C07D295/13
摘要： Certain N-[arylethyl]-N-alkyl-2-(1-pyrrolidinyl)-ethylamine compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders, convulsions and parkinsonism. Compounds of particular interest are of formula (I) wherein R1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms and loweralkenylloweralkyl; wherein each of R?2 and R3¿ is independently selected from hydrido and loweralkyl; wherein each of R4 through R9 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein m is a number selected from one through three; wherein n is a number selected from four through seven; wherein p is a number selected from zero through four; wherein A is selected from phenyl, naphthyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.

55. 发明申请

WO1992020705A1 PEPTIDE MIMETIC COMPOUNDS USEFUL AS PLATELET AGGREGATION INHIBITORS 审中-公开
标题翻译：肽类化合物可用作片剂聚集抑制剂
公开(公告)号：WO1992020705A1
公开(公告)日：1992-11-26
申请号：PCT/US1992003573
申请日：1992-05-06
申请人： G.D. SEARLE & CO. , THE MONSANTO COMPANY , GARLAND, Robert, Bruce , MIYANO, Masateru , ZABLOCKI, Jeffery, Alan , BOVY, Philippe, Roger , MCMACKINS, Dudley, Elgin , RICO, Joseph, Gerace , TJOENG, Foe, Siong , TOTH, Mihaly, Vadkerti
发明人： G.D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： C07K05/02
CPC分类号： C07D333/60 , C07C257/18 , C07D213/55 , C07D317/60
摘要： This invention relates to a compound having formula (I) or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidines derivatives.

56. 发明申请

WO1992019591A1 PROCESS FOR PREPARATION OF ALPHA-ALKOXY ACETIC ACIDS AND THEIR SALTS 审中-公开
标题翻译：制备ALPHA-ALKOXY ACEIC酸及其盐的方法
公开(公告)号：WO1992019591A1
公开(公告)日：1992-11-12
申请号：PCT/US1992003108
申请日：1992-04-22
申请人： G.D. SEARLE & CO. , MUELLER, Richard, August , PARTIS, Richard, Allen
发明人： G.D. SEARLE & CO.
IPC分类号： C07C323/20
CPC分类号： C07C51/367 , C07C319/20 , C07C323/20
摘要： A process for producing α-alkoxy acetic acids and salts thereof which comprises reacting an alcohol of formula (II), wherein R?1, R2 and R3¿ can be hydrogen, alkyl, alkoxy, halo, phenyl, substituted phenyl, or hydroxy; A can be S, O or -CH¿2?-; and Alk is straight or branched chain alkylene, with a base in an aprotic solvent, then reacting the resulting alkoxide with a monohaloacetic acid ester to give an alkoxyacetate followed by reaction of the alkoxyacetate with a hydrogen halide, organic acid or Lewis acid in nitromethane to give the corresponding α-alkoxyacetic acid which then may be recovered or may optionally be converted to the corresponding salt by contacting the α-alkoxy acetic acid with a base.

57. 发明申请

WO1992004020A1 METHOD OF INHIBITING SUPEROXIDE GENERATION 审中-公开
标题翻译：抑制超氧化物生成的方法
公开(公告)号：WO1992004020A1
公开(公告)日：1992-03-19
申请号：PCT/US1991006101
申请日：1991-08-30
申请人： G.D. SEARLE & CO. , MUELLER, Richard, August , NAKAO, Akira , PARTIS, Richard, Allen
发明人： G.D. SEARLE & CO.
IPC分类号： A61K31/19
CPC分类号： A61K31/19 , C07C315/02 , C07C319/02 , C07C323/52 , C07C331/10 , C07C317/22 , C07C323/20
摘要： The present invention relates to a method of inhibiting superoxide generation which comprises administering to a mammal in need of such treatment an amount of a compound of formula (I), wherein R?1 and R2¿ are the same or different and independently represent tert-alkyl or phenyl; Alk1 represents straight or branched chain alkylene of 1 to 10 carbon atoms, X represents sulfur or oxygen, Alk2 represents straight or branched chain alkylene of 1 to 4 carbon atoms; and m is 0, 1 or 2; or a pharmaceutically acceptable salt or stereoisomer or geometric isomer thereof, which is effective to inhibit superoxide generation.

58. 发明申请

WO1991018888A1 N-SUBSTITUTED-1,2,4-TRIAZOLONE COMPOUNDS FOR TREATMENT OF CARDIOVASCULAR DISORDERS 审中-公开
标题翻译：用于治疗心血管疾病的N-取代的1,2,4-三唑酮化合物
公开(公告)号：WO1991018888A1
公开(公告)日：1991-12-12
申请号：PCT/US1991003449
申请日：1991-05-23
申请人： G.D. SEARLE & CO. , MANNING, Robert, E. , REITZ, David, B. , HUANG, Horng-Chih
发明人： G.D. SEARLE & CO.
IPC分类号： C07D249/12
CPC分类号： C07D403/10 , C07D249/12
摘要： A class of N-substituted-1,2,4-triazolone compounds is described for use in treatment of cardiovascular disorders. Compounds of particular interest are angiotensin II antagonists of formula (I), wherein R is selected from 2-oxo-2-(tricyclo[3.3.1.1. ]dec-2-yl)ethyl, 3-phenylpropyl, 2-oxo-2-phenylethyl, 2-hyroxy-2-phenylethyl, 1,1-dimethylethyloxycarbonylmethyl, hexyl, ethoxycarbonylmethyl, carboxymethyl, 1-naphthalenylmethyl, 2-cyclohexylethyl, pentyl, ethoxycarbonylmethoxyethyl substituted with phenyl, carboxymethoxyethyl substituted with phenyl, 3,5,5-trimethylhexyl, (2-phenylmethoxy)-1-(phenylmethyl)-E-ethenyl, 1-benzoyl-2-phenylethyl, 1-oxobutyl, 2-(2,5-dimethyoxyphenyl)-2-oxoethyl, 2-phenyl-2-(phenylmethoxyethyl, 2-(2,5-dimethioxy-phenyl)-2-hydroxyethyl, 2-naphthalenylmethyl, methoxycarbonyl-butyl, ethoxycarbonylethyl substituted with benzoyl, 1-benzyoyl-1-methylethyl, 1-pentanoic acid, cyclopropylmethyl, 3-phenyl-2E-propenyl and 3-acetonitrile; wherein R is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl, neopentyl, 1-cyanobutyl, propylthio and butylthio; wherein each of R through R is hydrido with the proviso that at least one of R and R must be selected from COOH, SH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, (a), (b) and (c), wherein each of R and R is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
摘要翻译：描述了一类用于治疗心血管疾病的N-取代的1,2,4-三唑酮化合物。特别感兴趣的化合物是式（I）的血管紧张素II拮抗剂，其中R 1选自2-氧代-2-（三环[3.3.1.1.33.2]癸-2-基）乙基，3-苯基丙基，2-氧代-2-苯基乙基，2-羟基-2-苯基乙基，1,1-二甲基乙氧基羰基甲基，己基，乙氧基羰基甲基，羧甲基，1-萘基甲基，2-环己基乙基，戊基，被苯基取代的乙氧基羰基甲氧基乙基，被苯基取代的羧基甲氧基乙基，，5,5-三甲基己基，（2-苯基甲氧基）-1-（苯基甲基）-E-乙烯基，1-苯甲酰基-2-苯基乙基，1-氧代丁基，2-（2,5-二甲氧基苯基）-2-氧代乙基，2 - 苯基-2-（苯基甲氧基乙基，2-（2,5-二甲氧基 - 苯基）-2-羟乙基，2-萘基甲基，甲氧基羰基 - 丁基，苯甲酰基取代的乙氧基羰基乙基，1-苯甲酰基-1-甲基乙基，1-戊酸，环丙基甲基，3-苯基-2-丙烯基和3-乙腈;其中R 2选自乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，4-甲基丁基，叔丁基，戊基，新戊基，1-氰基乙硫基，丁硫基; 其中R 3至R 11各自为氢，条件是R 5和R 9中的至少一个必须选自COOH，SH，PO 3 H 2，SO 3 H，CONHNH 2，CONHNHSO 2 CF 3，OH，（ a），（b）和（c），其中R 42和R 43各自独立地选自氯，氰基，硝基，三氟甲基，甲氧基羰基和三氟甲基磺酰基。这些化合物特别可用于治疗或控制高血压和充血性心力衰竭。

59. 发明申请

WO1991017148A1 1H-SUBSTITUTED-1,2,4-TRIAZOLE COMPOUNDS FOR TREATMENT OF CARDIOVASCULAR DISORDERS 审中-公开
标题翻译： 1H-取代的1,2,4-三唑化合物用于治疗心血管疾病
公开(公告)号：WO1991017148A1
公开(公告)日：1991-11-14
申请号：PCT/US1991002926
申请日：1991-05-06
申请人： G.D. SEARLE & CO. , REITZ, David, B.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D249/08
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/10 , C07D403/10
摘要： A class of 1H-substituted-1,2,4-triazole compounds is described for use in treatment of circulatory disorders, especially cardiovascular disorders. Compounds of interest are angiotensin II antagonists of formula (II), wherein R1 is selected from hydroxy, formyl, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, n-hexyl, n-heptyl, n-octyl, n-nonyl, carboxyethyl, phenyl, benzyl, phenethyl, cyclopentyl, cyclohexyl, cyclopentylmethyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, adamantyl, adamantylmethyl, 1-oxoethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl, dimethoxymethyl, diethoxymethyl, 1,1-dimethoxypropyl, 1,1-dimethoxybutyl, 1,1-dimethoxypentyl, hydroxypropyl, halo, monofluoromethyl, difluoromethyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, pentafluoroethyl, heptafluoropropyl, phenylacetyl, phenyldifluoroethyl, aminomethyl, aminoethyl, aminopropyl, acetylaminomethyl, t-butoxycarbonylaminoethyl, glutamic acid methyl ester and glutamic acid ethyl ester; wherein R2 is selected from carboxyethyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl and neopentyl; wherein each of R3 through R11 is hydrido with the proviso that at least one of R?5 and R9¿ must be selected from COOH, SH, PO¿3?H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, (III), (IV) and (V), wherein each of R?40 and R41¿ is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

60. 发明申请

WO1991009051A1 SUBSTITUTED CYCLIC PENICILLANIC ACID TETRAPEPTIDES 审中-公开
标题翻译：取代的环己烷酸酯类
公开(公告)号：WO1991009051A1
公开(公告)日：1991-06-27
申请号：PCT/US1990007443
申请日：1990-12-12
申请人： G.D. SEARLE & CO.
发明人： G.D. SEARLE & CO. , HANSEN, Donald, Willis, Jr. , MOSBERG, Henry, I.
IPC分类号： C07K05/00
CPC分类号： C07K5/1016 , A61K38/00 , C07K14/702
摘要： The present invention provides novel compounds, compositions, methods of their use and methods of their manufacture. The compounds of this invention are cyclic tetrapeptide tyrosyl substituted dipenicillanic acid opioid agonists that are selective for the delta-receptor. The compounds of the invention act as neurotransmitters or neuromodulators in the central nervous system central pain-suppressant system, to induce analgesia. The present invention provides new cyclic peptide derivatives which show improved potency and bioavailability as analgesic agents by central routes of administration.
摘要翻译：本发明提供了新的化合物，组合物，它们的使用方法及其制备方法。本发明化合物是对δ-受体有选择性的环状四肽酪氨酰取代的二十二烷酸阿片样物质激动剂。本发明的化合物作为中枢神经系统中枢性抑制剂系统中的神经递质或神经调节剂，以诱导止痛。本发明提供了新的环肽衍生物，其通过中心给药途径显示出作为止痛剂的效力和生物利用度的改进。

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