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91. 发明申请

WO1993009087A1 ETHYNYL ALANINE AMINO DIOL COMPOUNDS FOR TREATMENT OF HYPERTENSION 审中-公开
标题翻译：用于治疗高血压的乙酰胺亚氨基二醇化合物
公开(公告)号：WO1993009087A1
公开(公告)日：1993-05-13
申请号：PCT/US1992008842
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： A61K31/18 , A61K31/165 , C07C237/22 , C07C271/20 , C07C311/13 , C07C2601/02 , C07C2601/14
摘要： Compounds characterized generally as ethynyl alanine amino 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-trifluoroethyl, 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 R5 is propargyl or a propargyl-containing moiety; wherein R7 is cyclohexylmethyl; wherein each of R4 and R6 is independently selected from hydrido and methyl; wherein R8 is selected from ethyl, n-propyl, isobutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclohexylmethyl, cyclohexylethyl, allyl, vinyl and fluorovinyl; 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.

92. 发明申请

WO1993008164A1 SUBSTITUTED HETEROCYCLIC DERIVATIVES USEFUL AS PLATELET AGGREGATION INHIBITORS 审中-公开
标题翻译：取代的杂环衍生物可用作平板聚集抑制剂
公开(公告)号：WO1993008164A1
公开(公告)日：1993-04-29
申请号：PCT/US1992008511
申请日：1992-10-06
申请人： MONSANTO COMPANY , G.D. SEARLE & CO.
发明人： MONSANTO COMPANY , G.D. SEARLE & CO. , BOVY, Philippe, Roger , RICO, Joseph, Gerace , ROGERS, Thomas, Edward , TJOENG, Foe, Siong , ZABLOCKI, Jeffery, Alan
IPC分类号： C07D213/55
CPC分类号： C07D239/26 , C07D213/55 , C07D307/54 , C07D317/60 , C07D317/62 , C07D317/66 , C07D333/24
摘要： Novel substituted heterocyclic derivatives having general formula (I), are provided, in which e.g. R2 is selected from monocyclic, bicyclic or tricyclic heterocyclyl radicals in which 1 to about 3 heteroatoms are independently selected from oxygen, nitrogen and sulfur, which are optionally substituted with hydroxyl, lower alkoxy, lower alkyl, halogen, nitro, carboxyl, sulfonyl, trifluoromethyl, amino, acyloxy, phenyl and naphthyl which are optionally substituted with halogen, nitro, lower alkoxy, and lower alkyl; the invention also pertains to pharmaceutical compositions comprising such derivatives.

93. 发明申请

WO1993007867A1 SUBSTITUTED 'beta'-AMINO ACID DERIVATIVES USEFUL AS PLATELET AGGREGATION INHIBITORS 审中-公开
标题翻译：取代（BETA） - 氨基酸衍生物作为片剂聚集抑制剂有用
公开(公告)号：WO1993007867A1
公开(公告)日：1993-04-29
申请号：PCT/US1992008512
申请日：1992-10-06
申请人： MONSANTO COMPANY , G.D. SEARLE & CO.
发明人： MONSANTO COMPANY , G.D. SEARLE & CO. , BOVY, Philippe, Roger , RICO, Joseph, Gerace , ROGERS, Thomas, Edward , TJOENG, Foe, Siong , ZABLOCKI, Jeffery, Alan
IPC分类号： A61K31/21
CPC分类号： C07C257/18 , C07C259/06 , C07C311/46 , C07C317/50 , C07C2601/02 , C07F7/081
摘要： Novel substituted beta amino acid derivatives having the general formula: are provided, in which eg. R is selected from the group consisting of hydrogen, lower alkyl radicals, lower alkenyl radicals, lower alkynyl radicals, alicyclic hydrocarbon radicals, aromatic hydrocarbon radicals, wherein said radicals are optionally substituted with hydroixy, lower alkoxy, lower alkyl, halogen, nitro, cyano, azido, ureido, ureylene, carboxyl or carbonyl derivatives, trifluoromethyl, acyloxy, alkylthio, arylthio, alkylsulfenyl, arylsulfenyl, alkylsulfonyl, arylsulfonyl, amino, alkylamino, trialkylsilyl, aminosulfonyl, dialkylamino, alkanoylamino, aroylamino, phenyl, naphtyl, lower alkynyl which are optionally substituted with one or more of the following: halogen, nitro, lower alkoxy, lower alkyl, trialkylsilyl, azide and phenyl; the invention also pertains to pharmaceutical composition comprising such derivatives.

94. 发明申请

WO1992018092A2 1-ARYLHETEROARYLALKYL SUBSTITUTED-1H-1,2,4-TRIAZOLE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS 审中-公开
标题翻译：用于治疗循环障碍的1-ARYLHETEROARYLALKYL取代的1 H-1,2,4-三唑类化合物
公开(公告)号：WO1992018092A2
公开(公告)日：1992-10-29
申请号：PCT/US1992002801
申请日：1992-04-10
申请人： G.D. SEARLE & CO. , REITZ, David, B.
发明人： G.D. SEARLE & CO.
IPC分类号： A61K0
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/10 , C07D401/14
摘要： A class of 1-arylheteroarylalkyl substituted-1H-1,2,4-triazole compounds is described for use in treatment of circulatory disorders such as hypertension. Compounds of particular interest are angiotensin II antagonists of the formula (I) wherein A is selected from (1, 2, 3, 4, 5 and 6), wherein m is one; wherein R1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, 2-ethylbutyl, 1,1-difluorobutyl, N-methylamido, N-methyl-N-tertbutylamido, 2-methylphenyl, 2-isopropylphenyl, 2-methoxyphenyl, 2-chlorophenyl, 2,6-difluorophenyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R2 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, ethylbutyl, n-pentyl, 1-oxo-2-phenylethyl, 1-oxo-2-cyclohexylethyl, 1,1-difluoro-2-phenylethyl, 1,1-difluoro-2-cyclohexylethyl, 2-cyclohexylethyl, 1,1-difluoro-3-cyclohexylpropyl, 1,1-dimethoxybutyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, phenyl, benzyl, 2-phenylethyl, 1,1-difluoro-3-phenylpropyl, cyclohexylmethyl, cyclohexanoyl, N-methylamido, N-methyl-N-tertbutylamido, 2-methylphenyl, 2-isopropylphenyl, 2-methoxyphenyl, 2-chlorophenyl, 2,6-difluorophenyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-butynyl, 2-butynyl, 3-butynyl, propylthio and buthylthio; wherein R5 is an acidic group selected from CO¿2?H and tetrazole radicals; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.

95. 发明申请

WO1992011255A1 N-SUBSTITUTED N-('alpha'-TRIAZOLYL-TOLUYL)PYRROLE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS 审中-公开
标题翻译： N-取代的N-（α-三唑基 - 叔丁基）吡咯烷化合物，用于治疗循环障碍
公开(公告)号：WO1992011255A1
公开(公告)日：1992-07-09
申请号：PCT/US1991008726
申请日：1991-11-26
申请人： G.D. SEARLE & CO. , BOVY, Philippe, R. , REITZ, David, B. , MANNING, Robert, E.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D403/14
CPC分类号： C07D403/10 , C07D403/14
摘要： A class of N-substituted N-(α-triazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of formula (I), wherein m is one; wherein R1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R?3, R4, R5, R6, R7, R8, R9 and R10¿ is independently selected from hybrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R?5 and R8¿ must be selected from COOH, SH, PO¿3?H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, a), b) and c) wherein each of R?42 and R43¿ is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

96. 发明申请

WO1992004324A1 PHENOLIC THIOETHERAMIDES AS 5-LIPOXYGENASE INHIBITORS 审中-公开
标题翻译：作为5-LIPOXYGENASE抑制剂的酚醛树脂
公开(公告)号：WO1992004324A1
公开(公告)日：1992-03-19
申请号：PCT/US1991006235
申请日：1991-09-05
申请人： G.D. SEARLE & CO. , MUELLER, Richard, August , PARTIS, Richard, Allen
发明人： G.D. SEARLE & CO.
IPC分类号： C07D213/40
CPC分类号： C07D213/40 , C07D211/16 , C07D295/185
摘要： The present invention relates to phenolic thioetheramides of formula (I) wherein R and R are tert-alkyl or phenyl, Alk and Alk are alkylene; X is sulfer or oxygen, m is 0, 1, or 2; and R is a) wherein R and R are hydrogen or alkyl and Alk is alkylene; or b) wherein Y is CH, N, O, or S; R is hydrogen, alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl or a heterocyclic amine; and R is hydrogen or alkyl. The compounds inhibit 5-lipoxygenase and are useful in the treatment of inflammation and allergic conditions.
摘要翻译：本发明涉及式（I）的酚硫醚酰胺，其中R 1和R 2是叔烷基或苯基，Alk 1和Alk 2是亚烷基; X是硫或氧，m是0,1或2; 和R为a）其中R 3和R 4为氢或烷基，Alk 3为亚烷基; 或b）其中Y是CH，N，O或S; R 6是氢，烷基，苯基，取代的苯基，苄基，取代的苄基或杂环胺; 和R 7是氢或烷基。该化合物抑制5-脂氧合酶，可用于治疗炎症和过敏症状。

97. 发明申请

WO1992003131A1 USE OF HETEROCYCLIC AMINO-ALCOHOL COMPOUNDS FOR TREATMENT OF CNS DISEASES 审中-公开
标题翻译：用于治疗CNS疾病的杂环氨基醇化合物的应用
公开(公告)号：WO1992003131A1
公开(公告)日：1992-03-05
申请号：PCT/US1991005028
申请日：1991-07-22
申请人： G.D. SEARLE & CO. , ROBA, Joseph, L. , GILLET, Claude, L. , RAFFERTY, Michel, F. , JARROT, Bevyn , BEART, Philip, Mark
发明人： G.D. SEARLE & CO.
IPC分类号： A61K31/38
CPC分类号： A61K31/445 , A61K31/135 , A61K31/34 , A61K31/38 , A61K31/385 , A61K31/39 , A61K31/40 , A61K31/415 , A61K31/495 , A61K31/535 , A61K31/55 , Y02A50/395
摘要： A class of heterocyclic amino-alcohol compounds is described for treatment of CNS-related diseases, namely, for use as a neuroprotective agent, to reduce neurotoxic injury associated with conditions of hypoxia, anoxia or ischemia which typically follows stroke, myocardial infarct, perinatal asphyxia, or hypoglycemic events. Other examples of treatable CNS-related diseases include neurodegenerative diseases such as Parkinson's disease, Huntington's chorea and Alzheimer's disease, and also psychotic disorders such as schizophrenia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as a mediator to alter excitatory actions at the NMDA excitatory amino acid receptor complex. A compound of this class of specific interest is formula (I).
摘要翻译：描述了一类杂环氨基醇化合物用于治疗中枢神经系统相关疾病，即用作神经保护剂，以减少与缺氧，缺氧或局部缺血相关的神经毒性损伤，其通常在卒中，心肌梗死，围产期窒息，或低血糖事件。可治疗CNS相关疾病的其他实例包括神经变性疾病如帕金森病，亨廷顿舞蹈病和阿尔茨海默氏病，以及精神病性精神障碍如精神分裂症。治疗包括单独施用该类化合物或以有效作为介质的量的组合物施用以改变NMDA兴奋性氨基酸受体复合物的兴奋性作用。这类具体感兴趣的化合物是式（I）。

98. 发明申请

WO1992001477A1 POLYMERIC DRUG DELIVERY SYSTEM 审中-公开
标题翻译：聚合物药物递送系统
公开(公告)号：WO1992001477A1
公开(公告)日：1992-02-06
申请号：PCT/US1991005029
申请日：1991-07-22
申请人： G.D. SEARLE & CO. , THE MONSANTO COMPANY , TREMONT, Samuel, J. , COLLINS, Paul, Waddell , PERKINS, Williams, Eldredge , JONES, Peter, Hadley
发明人： G.D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： A61K47/48
CPC分类号： C08G73/0226 , A61K31/557 , A61K47/58 , A61K47/59 , A61K47/61 , C08G73/02 , Y10S514/925 , Y10S525/923
摘要： A drug delivery system adapted to release an effective amount of a drug at pH values of about 1 to 7 without releasing a significant amount of the drug at pH values of about 7 and above, the system comprising a polymeric material and a drug covalently bonded to the polymeric material through a pH sensitive covalent bond capable of being cleaved in the pH range of 1 to about 7.
摘要翻译：一种药物递送系统，适于以约1至7的pH值释放有效量的药物，而不在大约7及更高的pH值下释放大量的药物，所述系统包含聚合物材料和共价键合到聚合物材料通过能够在1至约7的pH范围内被切割的pH敏感的共价键。

99. 发明申请

WO1991017145A1 PROCESS FOR PREPARATION OF 1,5-(ALKYLIMINO)-1,5-DIDEOXY-D-GLUCITOL AND DERIVATIVES THEREOF 审中-公开
标题翻译：制备1,5-（阿霉素）-1,5-二脱氧-D-葡萄糖苷及其衍生物的方法
公开(公告)号：WO1991017145A1
公开(公告)日：1991-11-14
申请号：PCT/US1991002986
申请日：1991-05-01
申请人： G.D. SEARLE & CO. , BEHLING, James, R. , FARID, Payman , KHANNA, Ish , MEDICH, John, R. , PRUNIER, Mike , SCAROS, Mike , WEIER, Richard, M.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D211/46
CPC分类号： C07D493/10 , C07D211/46 , C07D307/20
摘要： Process for the preparation of 1,5-(alkylimino)-1,5-dideoxy-D-glucitol and derivatives thereof. Described is a process for the preparation of 1,5-(n-butylimino)-1,5-dideoxy-D-glucitol and similar compounds and to the use of an adsorption hydrogenation protocol.
摘要翻译：制备1,5-（烷基亚氨基）-1,5-二脱氧-D-葡萄糖醇及其衍生物的方法。描述了制备1,5-（正丁基亚氨基）-1,5-二脱氧-D-葡萄糖醇和类似化合物以及使用吸附氢化方案的方法。

100. 发明申请

WO1991008759A1 ALKYL SUBSTITUTED CYCLIC PENICILLANIC ACID PENTAPAPTIDES 审中-公开
标题翻译： ALKYL取代的环丙苯丙酸
公开(公告)号：WO1991008759A1
公开(公告)日：1991-06-27
申请号：PCT/US1990007444
申请日：1990-12-12
申请人： G.D. SEARLE & CO.
发明人： G.D. SEARLE & CO. , HAMMOND, Donna, L. , HANSEN, Donald, W. , MOSBERG, Henry, I.
IPC分类号： A61K37/02
CPC分类号： C07K14/702 , A61K38/00
摘要： The invention relates to novel compounds of general formula (I) and pharmaceutically acceptable salts thereof, wherein X is H, a halogen, nitro, lower alkyl or lower alkyl substituted by halogen or nitro, aralkyl or alkaryl or substituted aralkyl or alkaryl of from one to ten carbon atoms: R , R , R and R are independently H and furthermore, R , R , R , R , R and R are independently alkyl of from one to ten carbon atoms; R is amino, hydroxy, alkoxy of from one to ten carbon atoms, alkyl amino or dialkylamino of from one to ten carbon atoms; and R is independently H, alkyl of from one to ten carbon atoms, carboxyl, alkoxy carbonyl of from one to ten carbon atoms, amino carbonyl, alkylamino carbonyl and dialkylamino carbonyl of from one to ten carbon atoms, or any of these R constituents being aryl substituted thereon. The compounds and pharmaceutical compositions thereof are useful in the analgesic methods of the invention.
摘要翻译：本发明涉及通式（I）的新化合物及其药学上可接受的盐，其中X为H，卤素，硝基，被卤素或硝基取代的低级烷基或低级烷基，芳烷基或烷芳基或取代的芳烷基或烷芳基至10个碳原子：R 1，R 2，R 3和R 4独立地为H，此外，R 1，R 2，R 3，R 4， R 6和R 7独立地为具有1至10个碳原子的烷基; R 5为氨基，羟基，1至10个碳原子的烷氧基，1至10个碳原子的烷基氨基或二烷基氨基; 和R 8独立地是H，1至10个碳原子的烷基，1至10个碳原子的羧基，烷氧基羰基，1至10个碳原子的氨基羰基，烷基氨基羰基和二烷基氨基羰基，或这些 R 8成分是在其上取代的芳基。本发明的化合物及其药物组合物可用于本发明的止痛方法。

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