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91. 发明专利

JPS5773142A Extraction for selectively removing cobalt (ii) from aqueous solution 失效
标题翻译：从水溶液中选择性地去除钴（II）的萃取物
公开(公告)号：JPS5773142A
公开(公告)日：1982-05-07
申请号：JP13266081
申请日：1981-08-26
申请人： Canada Cyanamid
发明人： UIRIAMU ANDORUU RITSUKERUTON , ARAN JIEIMUZU ROBAATOSON , DEBITSUDO RICHIYAADO BAARII
IPC分类号： C22B23/00 , C01G51/00 , C07F9/30 , C22B3/00 , C22B3/38
CPC分类号： C22B3/0077 , C01G51/003 , C07F9/301 , C07F9/303 , C22B3/0066 , Y02P10/234

92. 发明申请

WO2006000043A1 NEUROLOGICALLY-ACTIVE COMPOUNDS 审中-公开
标题翻译：神经生物活性化合物
公开(公告)号：WO2006000043A1
公开(公告)日：2006-01-05
申请号：PCT/AU2005/000928
申请日：2005-06-24
申请人： THE UNIVERSITY OF SYDNEY , CHEBIB, Mary , KUMAR, Rohan John , JOHNSTON, Graham , HANRAHAN, Jane
发明人： CHEBIB, Mary , KUMAR, Rohan John , JOHNSTON, Graham , HANRAHAN, Jane
IPC分类号： C07C13/12
CPC分类号： C07F9/303
摘要： The invention provides a compound of the formula (I): wherein R is methyl, ethyl, propyl, isopropyl, butyl, pentyl, neo-pentyl or cyclohexyl, or a salt or solvate thereof. These compounds are selective GABA C receptor antagonists. The invention also provides pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof. The invention also provides methods of enhancing the cognitive activity of an animal and methods of stimulating memory capacity in an animal, comprising the step of administering to the animal an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof.
摘要翻译：本发明提供了式（I）化合物：其中R是甲基，乙基，丙基，异丙基，丁基，戊基，新戊基或环己基，或其盐或溶剂合物。这些化合物是选择性GABA C受体拮抗剂。本发明还提供包含式（I）化合物或其药学上可接受的盐或溶剂化物的药物组合物。本发明还提供增强动物的认知活动的方法和刺激动物记忆能力的方法，包括向动物施用有效量的式（I）化合物或其药学上可接受的盐或溶剂化物的步骤。

93. 发明申请

WO0222627A3 LIGANDS FOR METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：代谢谷氨酸受体的配体
公开(公告)号：WO0222627A3
公开(公告)日：2002-07-04
申请号：PCT/US0128923
申请日：2001-09-14
申请人： GEORGETWON UNIVERSITY
发明人： KOZIKOWSKI ALAN P , WROBLEWSKI JARDA T , NAN FAJUN
IPC分类号： A61P25/00 , C07C59/347 , C07C69/716 , C07C271/22 , C07C275/16 , C07C275/26 , C07C323/59 , C07C335/08 , C07D257/04 , C07F9/30 , A61K31/095 , A61K31/17 , A61K31/194 , A61K31/41 , A61K31/662
CPC分类号： C07D257/04 , C07C59/347 , C07C69/716 , C07C271/22 , C07C275/16 , C07C275/26 , C07C323/59 , C07C335/08 , C07F9/301 , C07F9/303
摘要： The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity o a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.
摘要翻译：本发明涉及其化合物是代谢型谷氨酸受体或NAALADase酶或两者的配体，例如激动剂或拮抗剂的新化合物及其制剂。本发明还涉及使用本发明的化合物或制剂调节代谢型谷氨酸受体或NAALADase酶或两者的活性的方法，例如在有需要的受试者中。本发明还涉及使用化合物或至少部分由内源性代谢型谷氨酸受体或NAALADase酶或两者的活性异常而治疗患有慢性或急性疾病，疾病或病症的受试者的方法，本发明的制剂。

94. 发明申请

WO01014390A3 METABOTROPIC GLUTAMATE RECEPTOR LIGAND DERIVATIVES AS NAALADase INHIBITORS 审中-公开
标题翻译：代谢谷氨酸受体配体衍生物作为NAALADase抑制剂
公开(公告)号：WO01014390A3
公开(公告)日：2001-09-27
申请号：PCT/US2000/022412
申请日：2000-08-16
IPC分类号： C07C229/14 , C07C229/16 , C07C229/46 , C07C259/08 , C07F9/30 , C07F9/38 , C07F9/572 , C07F9/6561 , C07F9/44 , C07C229/50 , C07F9/40
CPC分类号： C07F9/5727 , C07C229/14 , C07C229/16 , C07C229/46 , C07C259/08 , C07C2601/02 , C07F9/303 , C07F9/383 , C07F9/5722 , C07F9/6561
摘要： The present invention relates to metabotropic glutamate receptor ligand derivatives and methods of using the same to inhibit NAALADase enzyme activity, to effect neuronal activities, to inhibit angiogenesis, and to treat glutamate abnormalities, compulsive disorders, pain, diabetic neuropathy, and prostate diseases, as well as pharmaceutical compositions comprising the same.
摘要翻译：本发明涉及代谢型谷氨酸受体配体衍生物及其使用方法，以抑制NAALADase酶活性，影响神经元活性，抑制血管发生，以及治疗谷氨酸异常，强迫症，疼痛，糖尿病性神经病和前列腺疾病，如以及包含其的药物组合物。

95. 发明申请

WO1996004233A1 ARYLOXY AND ARYLTHIOPROPANOLAMINE DERIVATIVES USEFUL AS BETA 3-ADRENORECEPTOR AGONISTS AND ANTAGONISTS OF THE BETA 1 AND BETA 2-ADRENORECEPTORS AND PHARMACEUTICAL COMPOSITION THEREOF 审中-公开
标题翻译：有利于ARALOXY和ARYLROPOPOLOLOLINE衍生物作为β-3受体激动剂和β1和β-2-肾上腺素受体拮抗剂及其药物组合物
公开(公告)号：WO1996004233A1
公开(公告)日：1996-02-15
申请号：PCT/EP1995003037
申请日：1995-07-27
申请人： SMITHKLINE BEECHAM PLC , BEELEY, Lee, James , THOMPSON, Mervyn , DEAN, David, Kenneth , KOTECHA, Nikesh, Rasiklal , BERGE, John, Michael , WARD, Robert, William
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07C217/60
CPC分类号： C07F9/3211 , C07C217/34 , C07C2601/14 , C07D317/46 , C07F9/301 , C07F9/303 , C07F9/3223 , C07F9/4006
摘要： A compound formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein R represents an aryl group optionally substituted with one, two or three substituents selected from the list consisting of: hydroxy, hydroxymethyl, nitro, amino, alkylamino, dialkylamino, alkylsulphonamido, arylsulphonamido, formamido, halogen, alkoxy and allyl; X represents O or S; R and R each independently represents hydrogen or an alkyl group; R represents OCH2CO2H, or an ester or amide thereof, or R represents a moiety of formula (b), wherein R represents hydrogen, alkyl, hydroxyalkyl, arylalkyl, aryloxyalkyl, aralkyloxyalkyl or cycloalkyl and R represents hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, aryloxyalkyloxy, arylalkoxyalkyloxy or cycloalkyloxy or R represents hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, aryloxyalkyl, arylalkyloxyalkyl or R together with OR represents O(CH2)nO, wherein n is 2, 3 or 4; and R represents hydrogen, halogen, alkyl or alkoxy or R together with R represents a moiety of formula (c) or an ester or amide thereof; providing that 4-[2-[2-hydroxy-3-(4-hydroxyphenoxy)propylamino]propyl]phenoxyacetic acid and salts and esters thereof and the compounds of examples 1 to 36 disclosed in EP0328251 are excluded from the scope of formula (I); a pharmaceutical composition containing such a compound, a process of preparing such a compound and the use of such a compound in medicine.
摘要翻译：式（I）化合物或其药学上可接受的盐或其药学上可接受的溶剂合物，其中R 0表示任选被1,2或3个选自羟基，羟甲基，硝基的取代基取代的芳基，氨基，烷基氨基，二烷基氨基，烷基磺酰氨基，芳基磺酰氨基，甲酰氨基，卤素，烷氧基和烯丙基; X表示O或S; R 1和R 1a各自独立地表示氢或烷基; R 2表示OCH 2 CO 2 H或其酯或酰胺，或R 2表示式（b）的部分，其中R 4表示氢，烷基，羟烷基，芳烷基，芳氧基烷基，芳烷氧基烷基或环烷基， R 5代表羟基，烷氧基，芳基烷氧基，羟基烷氧基，烷氧基烷氧基，芳氧基烷氧基，芳基烷氧基氧基或环烷氧基或R 5表示氢，烷基，取代烷基，环烷基，芳基，芳基烷基，芳氧基烷基，芳基烷氧基烷基或R 5与OR 4 >表示O（CH 2）n O，其中n为2,3或4; 和R 3代表氢，卤素，烷基或烷氧基或R 3与R 2一起代表式（c）的部分或其酯或酰胺; 提供4- [2- [2-羟基-3-（4-羟基苯氧基）丙基氨基]丙基]苯氧基乙酸及其盐和酯以及EP0328251中公开的实施例1至36的化合物不包括在式（I ）; 含有这种化合物的药物组合物，制备这种化合物的方法以及这种化合物在医药中的用途。

96. 发明申请

WO1996000732A1 PHOSPHINIC ACID DERIVATIVES 审中-公开
标题翻译：磷酸衍生物
公开(公告)号：WO1996000732A1
公开(公告)日：1996-01-11
申请号：PCT/US1995007128
申请日：1995-06-19
申请人： SCHERING CORPORATION
发明人： SCHERING CORPORATION , MCKITTRICK, Brian, A. , CZARNIECKI, Michael, F. , CHACKALAMANNIL, Samuel , CHUNG, Shin , DEFREES, Shawn , STAMFORD, Andrew, W.
IPC分类号： C07F09/30
CPC分类号： C07F9/65583 , C07F9/303 , C07F9/5728
摘要： Phosphinic acid derivatives of structural formula (I) or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene; R1, R2, R3 and R4 are H, alkyl, alkenyl, alkenylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, carboxyalkyl, thioalkyl, alkoxythioalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl-substituted alkyl or heterocycloalkyl; or R1 and R2 form a cycloalkyl ring of 3-8 members and R3 and R4 are as defined; or R3 and R4 form a cycloalkyl ring of 3-7 members and R1 and R2 are as defined; or R1 and R2 together, and R3 and R4 together, each form a cycloalkyl ring; R5 is -OR9 or -NHR9, wherein R9 is hydrogen or alkyl; n is 0 or 1; A1 is p-aminobenzoyl or p-aminobenzenesulfonyl, or A1 and R5 together form a radical of an alpha -aminoacyl derivative; and R6 is phenylmethoxycarbonyl, arylcarbonyl, heteroarylcarbonyl or -A2-R7, wherein A2 is a divalent alpha -iminoacyl radical, and R7 is a substituent on the alpha -imino atom selected from H, R8OCO-, R8SO2- and R8NHCO-, wherein R8 is aryl, arylmethyl or (C1-C8)alkyl; are disclosed for use as endothelin converting enzyme inhibitors; also disclosed are a genus of novel compounds wherein R and R form a cycloalkyl ring, and pharmaceutical compositions comprising said novel compounds.
摘要翻译：结构式（I）的亚磷酸衍生物或其药学上可接受的盐，其中R是H，烷基或烷酰氧基亚甲基; R 1，R 2，R 3和R 4是H，烷基，烯基，烯基烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，羟基烷基，羧基烷基，硫代烷基，烷氧基硫代烷基，氨基烷基，烷基氨基烷基，环烷基取代的烷基或杂环烷基。或R 1和R 2形成3-8成员的环烷基环，并且R 3和R 4如所定义; 或R 3和R 4形成3-7成员的环烷基环，并且R 1和R 2如所定义; 或R 1和R 2一起，并且R 3和R 4一起形成环烷基环; R5是-OR9或-NHR9，其中R9是氢或烷基; n为0或1; A1是对氨基苯甲酰基或对氨基苯磺酰基，或者A1和R5一起形成α-氨基酰基衍生物的基团; R6为苯基甲氧基羰基，芳基羰基，杂芳基羰基或-A2-R7，其中A2为二价α-亚氨酰基，R7为选自H，R8OCO-，R8SO2-和R8NHCO-的α-亚氨基原子上的取代基，其中R8 是芳基，芳甲基或（C1-C8）烷基; 被公开用作内皮素转化酶抑制剂; 还公开了其中R 3和R 4形成环烷基环的新化合物的属，以及包含所述新化合物的药物组合物。

97. 发明申请

WO2012034680A2 PHOSPHORHALTIGE MISCHUNGEN, VERFAHREN ZU DEREN HERSTELLUNG UND IHRE VERWENDUNG 审中-公开
标题翻译：磷混合混合物，其生产方法及其用途
公开(公告)号：WO2012034680A2
公开(公告)日：2012-03-22
申请号：PCT/EP2011/004597
申请日：2011-09-13
申请人： CLARIANT INTERNATIONAL LTD , BAUER, Harald , HÖROLD, Sebastian , SICKEN, Martin
发明人： BAUER, Harald , HÖROLD, Sebastian , SICKEN, Martin
IPC分类号： C07F9/30
CPC分类号： C07F9/303 , C07F9/383 , C07F9/48 , C08K5/5313 , C08L25/06 , C08L77/00
摘要： Gegenstand der Erfindung sind phosphorhaltige Mischungen, enthaltend a) 50 - 100 mol-% Verbindungen der Formel (1) worin R 1 und R 2 gleich oder verschieden sind und C 6 -C 9 -Alkyl, b) 0 bis 50 mol-% Verbindungen der Formel (1), worin R 1 H und R 2 C 6 -C 9 - Alkyl, c) 0 bis 50 mol-% Verbindungen der Formel (1), worin R 1 OH und R 2 C 6 -C 9 - Alkyl, d) 0 bis 50 mol-% Verbindungen der Formel (1), worin R 1 OH und R 2 H und e) 0 bis 50 mol-% Verbindungen der Formel (1), worin R 1 H und R 2 H bedeuten, wobei die Summe von a), b), c), d) und e) immer 100 mol-% ergibt.
摘要翻译：本发明涉及含磷混合物，其包含a）50-100mol％式（1）的化合物，其中R 1和R 2彼此独立地为氢，是相同或不同的C 6至C 9亚烷基，b）0至50摩尔％的式（1）化合物，其中R 1， H和R 2 C 6 -C 9 - 烷基，c）0-50摩尔％式（1）化合物，其中R 1 OH和R 2 C 6 -C 9烷基，d）0-50摩尔％％式（1）化合物，其中R 1和OH以及e）0-50mol％式（1）化合物其中R ^{1 H和R 2 H，a），b），c），d）和e）的总和总是100摩尔％。}

98. 发明申请

WO2010108051A3 INHIBITORS OF DIACYLGLYCEROL O-ACYLTRANSFERASE 1(DGAT-1) AND USES THEREOF 审中-公开
标题翻译：二乙酰胆碱酯酶A（DGAT-1）的抑制剂及其用途
公开(公告)号：WO2010108051A3
公开(公告)日：2010-11-11
申请号：PCT/US2010027889
申请日：2010-03-19
申请人： LIGAND PHARMACEUTICALS , REDDY K RAJA , STEBBINS JEFF , BOYER SERGE H , ERION MARK D , HECKER SCOTT J , RAFFAELE NICHOLAS BRIAN , BOOKSER BRETT C , REDDY MALI VENKAT
发明人： REDDY K RAJA , STEBBINS JEFF , BOYER SERGE H , ERION MARK D , HECKER SCOTT J , RAFFAELE NICHOLAS BRIAN , BOOKSER BRETT C , REDDY MALI VENKAT
IPC分类号： C07D473/16 , A61K31/52 , A61K31/662 , A61K31/665 , A61K31/675 , A61P3/04 , A61P3/10 , C07D473/34 , C07D473/40 , C07F9/30 , C07F9/32 , C07F9/653 , C07F9/6561 , C07F9/6574
CPC分类号： A61K31/675 , A61K31/52 , A61K31/542 , A61K31/662 , A61K31/665 , A61K31/683 , A61K31/688 , A61K45/06 , C07D473/16 , C07D473/34 , C07D473/40 , C07F9/303 , C07F9/3229 , C07F9/40 , C07F9/48 , C07F9/65312 , C07F9/6552 , C07F9/6561 , C07F9/65616 , C07F9/65742 , A61K2300/00
摘要： The invention pertains to use of DGAT-I inhibitors to treat and/or prevent overweight, obesity and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease. Compounds and compositions suitable for use in the disclosed methods are also provided.
摘要翻译：本发明涉及使用DGAT-1抑制剂治疗和/或预防超重，肥胖以及与之相关的各种疾病和病症。其他条件也可以被改善或避免，如高餐后甘油三酸酯或饮食相关的高甘油三酯血症，与过量甘油三酯相关的心血管风险，以及超重患者，糖尿病患者或其他葡萄糖代谢紊乱如X综合症患者和胰岛素抵抗/葡萄糖不耐受 /或多囊卵巢疾病。还提供适用于所公开方法的化合物和组合物。

99. 发明申请

WO2004010846A2 DESIGN AND SYNTHESIS OF RENAL DIPEPTIDASE INHIBITORS 审中-公开
标题翻译：肾脏双磷脂酶抑制剂的设计与合成
公开(公告)号：WO2004010846A2
公开(公告)日：2004-02-05
申请号：PCT/US2003/023363
申请日：2003-07-28
申请人： THE JOHNS HOPKINS SCHOOL OF MEDICINE , KHAN, Saeed, R. , VOGELSTEIN, Bert , KINZLER, Kenneth, W. , GURULINGAPPA, Hallur , BUCKHAULTS, Phillip
发明人： KHAN, Saeed, R. , VOGELSTEIN, Bert , KINZLER, Kenneth, W. , GURULINGAPPA, Hallur , BUCKHAULTS, Phillip
IPC分类号： A61B
CPC分类号： C07F9/303 , A61K51/0489 , C07B59/004 , C07B2200/05
摘要： Aminophosphinic acid derivatives were synthesized as potential inhibitors of renal dipeptidase, an enzyme overexpressed in benign and malignant colon tumors. Several compounds showed potent enzyme-inhibitory activity. These compounds can be used therapeutically and diagnostically for treatment and detection of tumors.
摘要翻译：氨基次膦酸衍生物作为肾二肽酶的潜在抑制剂合成，所述肾二肽酶是在良性和恶性结肠肿瘤中过表达的酶。几种化合物显示出有效的酶抑制活性。这些化合物可用于治疗和诊断治疗和检测肿瘤。

100. 发明申请

WO1996004234A1 ARYLOXY ANDARYCTHIO PROPANOLAMINE DERIVATIVES USEFUL AS B3-ADRENORECEPTOR AGONISTS AND ANTAGONS OF THE B1 AND B2 ADRENORECEPTORS AND PHARMACEUTICAL COMPOSITION THEREOF 审中-公开
标题翻译：用于B3和ADBENORECEPTOR激动剂的ARYLOXY ANDARYCTHIO丙酰胺衍生物和B1和B2受体的拮抗剂及其药物组合物
公开(公告)号：WO1996004234A1
公开(公告)日：1996-02-15
申请号：PCT/GB1995001325
申请日：1995-06-07
申请人： SMITHKLINE BEECHAM PLC , BEELEY, Lee, James , THOMPSON, Mervyn , DEAN, David, Kenneth , KOTECHA, Nikesh, Rasiklal , BERGE, John, Michael , WARD, Robert, William
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07C217/60
CPC分类号： C07F9/3211 , C07C217/34 , C07C2601/14 , C07D317/46 , C07F9/301 , C07F9/303 , C07F9/3223 , C07F9/4006
摘要： A compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein, R represents an aryl group optionally substituted with one, two or three substituents selected from the list consisting of: hydroxy, hydroxymethyl, nitro, amino, alkylamino, dialkylamino, alkylsulphonamido, arylsulphonamido, formamido, halogen, alkoxy and allyl; X represents O or S; R and R each independently represents hydrogen or an alkyl group; R represents OCH2CO2H, or an ester or amide thereof, or R represents a moiety of formula (b) wherein R represents hydrogen, alkyl, hydroxyalkyl, arylalkyl, aralkyloxyalkyl or cycloalkyl and R represents hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, arylalkoxyalkyloxy or cycloalkyloxy or R represents hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, arylalkyloxyalkyl or R together with OR represents O(CH2)nO wherein n is 2, 3 or 4; and R represents hydrogen, halogen, alkyl or alkoxy or R together with R represents a moiety of formula (c) or an ester or amide thereof; providing that 4-[2-[2-hydroxy-3-(4-hydroxyphenoxy)propylamino]propyl] phenoxyacetic acid and salts and esters thereof and the examples disclosed in EP0328251 are excluded from the scope of formula (I); a pharmaceutical composition containing such a compound, a process of preparing such a compound and the use of such a compound in medicine.
摘要翻译：式（I）化合物或其药学上可接受的盐或其药学上可接受的溶剂合物，其中R 0表示任选被一个，两个或三个选自以下的取代基取代的芳基：羟基，羟甲基，硝基，氨基，烷基氨基，二烷基氨基，烷基磺酰氨基，芳基磺酰氨基，甲酰氨基，卤素，烷氧基和烯丙基; X表示O或S; R 1和R 1a各自独立地表示氢或烷基; R 2表示OCH 2 CO 2 H或其酯或酰胺，或R 2表示式（b）的部分，其中R 4表示氢，烷基，羟烷基，芳烷基，芳烷氧基烷基或环烷基，R 5表示羟基，烷氧基，芳基烷氧基，羟烷基氧基，烷氧基烷氧基，芳基烷氧基氧基或环烷氧基或R 5表示氢，烷基，取代的烷基，环烷基，芳基，芳基烷基，芳基烷氧基烷基或R 5与OR 4一起代表O（CH 2）n O 其中n为2,3或4; 和R 3代表氢，卤素，烷基或烷氧基或R 3与R 2一起代表式（c）的部分或其酯或酰胺; 提供4- [2- [2-羟基-3-（4-羟基苯氧基）丙基氨基]丙基]苯氧基乙酸及其盐和酯，并且EP0328251中公开的实施例不包括在式（I）的范围内。含有这种化合物的药物组合物，制备这种化合物的方法以及这种化合物在医药中的用途。

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