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1. 发明申请

WO1997020822A1 QUINAZOLIN-2,4-DIAZIRINES AS NPY RECEPTOR ANTAGONIST 审中-公开
标题翻译：喹唑啉-2,4-二氮杂作为NPY受体拮抗剂
公开(公告)号：WO1997020822A1
公开(公告)日：1997-06-12
申请号：PCT/EP1996005066
申请日：1996-11-18
申请人： NOVARTIS AG , RÜEGER, Heinrich , SCHMIDLIN, Tibur , RIGOLLIER, Pascal , YAMAGUCHI, Yasuchika , TINTELNOT-BLOMLEY, Marina , SCHILLING, Walter , CRISCIONE, Leoluca
发明人： NOVARTIS AG
IPC分类号： C07D239/95
CPC分类号： C07D239/95
摘要： The invention relates to a method of treatment of disorders and diseases associated with NPY receptor subtype Y5 comprising administering to a warm-blooded animal, including man, in need of such treatment a therapeutically effective amount of a compound of formula (I), in which the variables are as defined and relates to new compounds of formula (I) or a salt thereof, to pharmaceutical compositions, and to the manufacture of new compounds of formula (I) and salts thereof.
摘要翻译：本发明涉及一种治疗与NPY受体亚型Y5有关的疾病和疾病的方法，其包括向需要这种治疗的温血动物（包括人）施用治疗有效量的式（I）化合物，其中变量如所定义，并涉及新的式（I）化合物或其盐，药物组合物，以及制备新的式（I）化合物及其盐。

2. 发明申请

WO1995011895A1 N-BENZOYL-4-OXY/THIO-2-SUBSTITUTED PIPERIDINES AS SUBSTANCE-P RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为物质受体拮抗剂的N-苯甲酰基-4-氧代/噻二唑替代的哌啶
公开(公告)号：WO1995011895A1
公开(公告)日：1995-05-04
申请号：PCT/EP1994003394
申请日：1994-10-14
申请人： CIBA-GEIGY AG , OFNER, Silvio , ROGGO, Silvio , SCHILLING, Walter , VEENSTRA, Siem, J.
发明人： CIBA-GEIGY AG
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D211/46 , C07D211/54
摘要： 1,2,4-Trisubstituted piperidine compounds of fomula (I), wherein R1 is an unsubstituted or substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical, or is the acyl radical of an alpha -amino acid that is unsubstituted or N-substituted by lower alkanoyl or by carbamoyl-lower alkanoyl; R2 is cycloalkyl or an unsubstituted or substituted aryl or heteroaryl radical; R3 is an unsubstituted or substituted, optionally hydrogenated aryl or heteroaryl radical or, when n is 1, X2 is imino that is unsubstituted or substituted by lower alkyl or by cycloalkyl and X3 is lower alkylene, R3 is lower alkyl or free or esterified or amidated carboxy, R4 is hydrogen or alkyl; X1 is methylene, ethylene, a direct bond, a free or ketalised carbonyl group or a free or etherified hydroxymethylene group; X2 is lower alkylene, imino that is unsubstituted or substituted by lower alkyl or by cycloalkyl, or a direct bond; X3 is lower alkylene or a direct bond; X4 is oxo or thioxo; and n is 1 or, when X2 is lower alkylene and X3 is a direct bond, n is 0; and the salts thereof, have compound-P-antagonistic properties and can be used as active ingredients of medicaments.
摘要翻译：式（I）的1,2,4-三取代哌啶化合物，其中R 1是未取代或取代的芳烷基，芳氧基烷基，杂芳烷基，芳酰基，杂芳酰基，环烷基羰基，芳烷酰基，杂芳基烷酰基，芳烷氧基羰基或芳基氨基甲酰基，或是未被取代或被低级烷酰基或氨基甲酰基 - 低级烷酰基取代的α-氨基酸; R2是环烷基或未取代或取代的芳基或杂芳基; R3是未取代或取代的，任选氢化的芳基或杂芳基，或当n为1时，X 2为未被取代或被低级烷基或环烷基取代的亚氨基，X3为低级亚烷基，R3为低级烷基或游离或酯化或酰胺化羧基，R 4是氢或烷基; X1是亚甲基，亚乙基，直接键，游离的或缩酮化的羰基或游离的或醚化的羟基亚甲基; X2是低级亚烷基，未被取代或被低级烷基或环烷基取代的亚氨基或直接键; X3是低级亚烷基或直接键; X4是氧代或硫代; n为1或X2为低级亚烷基且X3为直接键时，n为0; 及其盐具有化合物P-拮抗性质，可用作药物的有效成分。

3. 发明申请

WO1997020823A2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：受体拮抗剂
公开(公告)号：WO1997020823A2
公开(公告)日：1997-06-12
申请号：PCT/EP1996005067
申请日：1996-11-18
申请人： NOVARTIS AG , RÜEGER, Heinrich , SCHMIDLIN, Tibur , RIGOLLIER, Pascal , YAMAGUCHI, Yasuchika , TINTELNOT-BLOMLEY, Marina , SCHILLING, Walter , CRISCIONE, Leoluca , MAH, Robert
发明人： NOVARTIS AG
IPC分类号： C07D239/95
CPC分类号： C07D239/95
摘要： The invention relates to a compound of formula (I) in which the variables are as defined and/or a salt or a tautomer thereof; and relates to a method of treatment of disorders or diseases associated with NPY receptor subtype Y5, to pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof and to the manufacture of the compounds of formula (I) or a salt thereof.
摘要翻译：本发明涉及其中变量如所定义的式（I）化合物和/或其盐或其互变异构体; 涉及一种治疗与NPY受体亚型Y5相关的疾病或疾病的方法，涉及包含式（I）化合物或其药学上可接受的盐的药物组合物和制备式（I）化合物或其盐它们。

4. 发明申请

WO9720823A3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：受体拮抗剂
公开(公告)号：WO9720823A3
公开(公告)日：1997-07-17
申请号：PCT/EP9605067
申请日：1996-11-18
申请人： CIBA GEIGY AG , RUEEGER HEINRICH , SCHMIDLIN TIBUR , RIGOLLIER PASCAL , YAMAGUCHI YASUCHIKA , TINTELNOT BLOMLEY MARINA , SCHILLING WALTER , CRISCIONE LEOLUCA , MAH ROBERT
发明人： RUEEGER HEINRICH , SCHMIDLIN TIBUR , RIGOLLIER PASCAL , YAMAGUCHI YASUCHIKA , TINTELNOT-BLOMLEY MARINA , SCHILLING WALTER , CRISCIONE LEOLUCA , MAH ROBERT
IPC分类号： C07D239/95 , A61K31/505
CPC分类号： C07D239/95
摘要： The invention relates to a compound of formula (I) in which the variables are as defined and or a salt or a tautomer thereof; and relates to a method of treatment of disorders or diseases associated with NPY receptor subtype Y5, to pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof and to the manufacture of the compounds of formula (I) or a salt thereof.

5. 发明申请

WO1997020820A1 HETEROARYL COMPOUNDS 审中-公开
标题翻译：杂环化合物
公开(公告)号：WO1997020820A1
公开(公告)日：1997-06-12
申请号：PCT/EP1996005055
申请日：1996-11-18
申请人： NOVARTIS AG , RÜEGER, Heinrich , SCHMIDLIN, Tibur , RIGOLLIER, Pascal , YAMAGUCHI, Yasuchika , TINTELNOT-BLOMLEY, Marina , SCHILLING, Walter , CRISCIONE, Leoluca
发明人： NOVARTIS AG
IPC分类号： C07D239/95
CPC分类号： C07D239/95
摘要： The invention relates to a method of treatment of disorders and diseases associated with NPY receptor subtype Y5 comprising administering to a warm-blooded animal, including man, in need of such treatment a therapeutically effective amount of a compound of formula (I) in which the variables are as defined and relates to new compounds of formula (I) or a salt thereof, to pharmaceutical compositions, and to the manufacture of new compounds of formula (I) and salts thereof.
摘要翻译：本发明涉及一种治疗与NPY受体亚型Y5有关的病症和疾病的方法，包括向需要这种治疗的温血动物（包括人）施用治疗有效量的式（I）化合物，其中变量如所定义，并涉及新的式（I）化合物或其盐，药物组合物，以及制备式（I）的新化合物及其盐。

6. 发明申请

WO1997020821A1 HETEROARYL DERIVATIVES 审中-公开
标题翻译： HETEROARYL衍生物
公开(公告)号：WO1997020821A1
公开(公告)日：1997-06-12
申请号：PCT/EP1996005056
申请日：1996-11-18
申请人： NOVARTIS AG , RÜEGER, Heinrich , SCHMIDLIN, Tibur , RIGOLLIER, Pascal , YAMAGUCHI, Yasuchika , TINTELNOT-BLOMLEY, Marina , SCHILLING, Walter , CRISCIONE, Leoluca , STUTZ, Stefan
发明人： NOVARTIS AG
IPC分类号： C07D239/95
CPC分类号： C07D231/12 , C07D233/56 , C07D239/95 , C07D249/08
摘要： The invention relates to a method of treatment of disorders and diseases associated with NPY receptor subtype Y5 comprising administering to a warm-blooded animal, including man, in need of such treatment a therapeutically effective amount of a compound of formula (I), the variables are as defined and relates to new compounds of formula (I) or a salt thereof, to pharmaceutical compositions, and to the manufacture of new compounds of formula (I) and salts thereof.
摘要翻译：本发明涉及一种治疗与NPY受体亚型Y5相关的病症和疾病的方法，包括向需要这种治疗的温血动物（包括人）施用治疗有效量的式（I）化合物，变量定义并涉及新的式（I）化合物或其盐，药物组合物，以及制备新的式（I）化合物及其盐。

7. 发明申请

WO1996026183A1 1-ARYL-2-ACYLAMINO-ETHANE COMPOUNDS AND THEIR USE AS NEUROKININ ESPECIALLY NEUROKININ 1 ANTAGONISTS 审中-公开
标题翻译： 1-ARYL-2-ACYLAMINO-ETHANE化合物及其作为神经元素特异性神经营养因子1拮抗剂
公开(公告)号：WO1996026183A1
公开(公告)日：1996-08-29
申请号：PCT/EP1996000555
申请日：1996-02-09
申请人： CIBA-GEIGY AG , GERSPACHER, Marc , VON SPRECHER, Andreas , ROGGO, Silvio , MAH, Robert , OFNER, Silvio , VEENSTRA, Siem, Jacob , BETSCHART, Claudia , AUBERSON, Yves , SCHILLING, Walter
发明人： CIBA-GEIGY AG
IPC分类号： C07C237/22
CPC分类号： C07D213/40 , C07C237/22 , C07C255/29 , C07C311/51 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D209/08 , C07D209/12 , C07D209/20 , C07D211/22 , C07D211/44 , C07D211/48 , C07D211/58 , C07D213/70 , C07D215/46 , C07D223/12 , C07D231/12 , C07D231/38 , C07D233/56 , C07D235/16 , C07D235/28 , C07D239/42 , C07D241/20 , C07D249/08 , C07D295/13 , C07D295/135 , C07D295/185 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/10
摘要： 1-Aryl-2-acylamino-ethane compounds of formula (I), wherein R1 is aryl or heteroaryl; R2 is hydrogen, lower alkyl or aryl-lower alkyl; R3 is hydrogen, lower alkyl, aryl or heteroaryl; R4 is aryl or heteroaryl; X is C1-C7alkylene, C2-C7 alkenyline or C4-C7 alkanedienylene, and Am is an unsubstituted or mono- or di-substituted amino group, a disubstituted amino group being understood as including also an amino group in which the amino nitrogen is bonded into a ring, or a salt thereof, have valuable pharmaceutical properties and are especially effective as NK1 antagonists. They are prepared in a manner known per se.
摘要翻译：式（I）的1-芳基-2-酰基氨基 - 乙烷化合物，其中R 1是芳基或杂芳基; R2是氢，低级烷基或芳基 - 低级烷基; R3是氢，低级烷基，芳基或杂芳基; R4是芳基或杂芳基; X是C 1 -C 7亚烷基，C 2 -C 7链烯基或C 4 -C 7链烷二烯基，并且Am是未取代或单取代或二取代的氨基，二取代的氨基也被理解为也包括其中氨基氮键合的氨基成环或其盐具有有价值的药物性质，并且作为NK1拮抗剂是特别有效的。它们是以本身已知的方式准备的。

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