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61. 发明授权

US5137920A Method of treating fungal infections 失效
标题翻译：治疗真菌感染的方法
公开(公告)号：US5137920A
公开(公告)日：1992-08-11
申请号：US533605
申请日：1990-06-05
申请人： Philippe Guerry , Synese Jolidon , Rene Zurfluh
发明人： Philippe Guerry , Synese Jolidon , Rene Zurfluh
IPC分类号： A61K31/135 , A61K31/275 , A61K31/40 , A61P31/04 , C07C215/28 , C07C217/48 , C07C225/16 , C07C253/30 , C07C255/58 , C07D295/10 , C07D295/108
CPC分类号： C07D295/108 , C07C215/28 , C07C217/48 , C07C225/16 , C07C255/58
摘要： Compunds having the formula ##STR1## wherein each of R.sup.1 and R.sup.2 individually is hydrogen, lower alkyl, or lower alkenyl, R.sup.3 is hydrogen, halogen or lower alkyl, Q is alkylene with 2 to 11 carbon atoms and at least 2 carbon atoms between the two free valencies or alkenylene with 4 to 11 carbon atoms and at least 4 carbon atoms between the two free valencies and each of Y and Y' individually is a direct bond, the group R.sup.1 R.sup.2 --N--Q--CH.sub.2 -- is attached to the 3- or 4-position of ring A and the symbol R represents that the ring to which it is attached is unsubstituted or is substituted with at least one of halogen, trifluoromethyl, cyano, nitro, lower alkyl or lower alkoxy, and their pharmaceutically acceptable acid addition salts have valuable pharmacological properties. In particular, they have a pronounced antifungal activity and can be used as medicaments, especially for the control or prevention of topical or systemic infections which are caused by pathogenic fungi.
摘要翻译：具有式“IMAGE”I的组合物，其中R 1和R 2各自独立地为氢，低级烷基或低级烯基，R 3为氢，卤素或低级烷基，Q为具有2至11个碳原子的亚烷基和至少2个碳原子两个自由价之间具有4至11个碳原子和至少4个碳原子的两个自由价或亚烯基，Y和Y'各自独立地为直接键，R1R2-NQ-CH2-基团连接到3- 或环A的4位，符号R表示其所连接的环是未取代的或被至少一个卤素，三氟甲基，氰基，硝基，低级烷基或低级烷氧基取代的化合物及其药学上可接受的酸加成盐具有宝贵的药理性质。特别地，它们具有显着的抗真菌活性，并且可以用作药物，特别是用于控制或预防由病原真菌引起的局部或全身感染。

62. 发明授权

US5106878A Use of substituted aminoalkoxybenzene derivatives in the control or prevention of fungal infections 失效
标题翻译：在控制或预防真菌感染中使用取代的氨基甲苯苯衍生物
公开(公告)号：US5106878A
公开(公告)日：1992-04-21
申请号：US556241
申请日：1990-07-20
申请人： Philippe Guerry , Synese Jolidon , Rene Zurfluh
发明人： Philippe Guerry , Synese Jolidon , Rene Zurfluh
IPC分类号： A61K31/13 , A61K31/135 , A61K31/395 , A61P31/04 , C07C43/205 , C07C49/84 , C07C213/02 , C07C213/08 , C07C217/18 , C07C217/20 , C07C217/22 , C07C217/46 , C07D205/04 , C07D207/08 , C07D295/08 , C07D295/092
CPC分类号： C07D295/088 , C07C217/18 , C07C217/20 , C07C217/22 , C07C217/46 , C07D205/04
摘要： The compound of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 individually is hydrogen, lower alkyl or lower alkenyl or together signify straight-chain alkylene with 2 or 4 carbon atoms, R.sup.3 is hydrogen, halogen or lower alkyl, Q is alkylene with 4 to 11 carbon atoms and at least 4 carbon atoms between the two free valencies or alkenylene with 4 to 11 carbon atoms and at least 4 carbon atoms between the two free valencies and each of Y and Y' individually is a direct bond or the group --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--, the group R.sup.1 R.sup.2 N--Q--O-- is attached to the 3- or 4-position of ring A and the symbol R designates that the ring to which it is attached is unsubstituted or is substituted with at least one substituent selected from the group consisting of halogen, trifluoromethyl, cyano, nitro, lower alkyl and lower alkoxy, and their pharmaceutically acceptable acid addition salts can be used for the control or prevention of fungal infections, especially of topical or systemic infections which are caused by pathogenic fungi, and for the manufacture of antifungally-active medicaments. The compounds of formula I have not only a pronounced antifungal activity, but they also exhibit synergistic effects in combination with other known antifungally-active substances which inhibit sterol biosynthesis such as ketoconazole and terbinafine.
摘要翻译：式Ⅰ化合物，其中R 1和R 2各自独立地为氢，低级烷基或低级烯基或一起表示具有2或4个碳原子的直链亚烷基，R 3为氢，卤素或低级烷基，Q为亚烷基在两个自由价之间具有4至11个碳原子和至少4个碳原子，在两个自由价之间具有4至11个碳原子和至少4个碳原子的亚烯基，Y和Y'各自独立地是直接键合或基团-CH 2 - ， - CH 2 CH 2 - ， - CH = CH-或-C 3BOND C-，基团R 1 R 2 N-QO-连接到环A的3-或4-位，符号R表示环其连接是未取代的或被至少一个选自卤素，三氟甲基，氰基，硝基，低级烷基和低级烷氧基的取代基取代，并且其药学上可接受的酸加成盐可用于控制或预防真菌感染，特别是局部或全身感染由致病真菌引起的离子和用于制造抗真菌药物的离子。式I化合物不仅具有显着的抗真菌活性，而且还与抑制甾醇生物合成的其它已知的抗真菌活性物质如酮康唑和特比萘芬组合显示协同效应。

63. 发明授权

US4946847A Quinoline derivatives 失效
公开(公告)号：US4946847A
公开(公告)日：1990-08-07
申请号：US274162
申请日：1988-11-21
申请人： Synese Jolidon , Rita Locher , Ivan Kompis , Ekkehard Weiss , Pierre-Charles Wyss
发明人： Synese Jolidon , Rita Locher , Ivan Kompis , Ekkehard Weiss , Pierre-Charles Wyss
IPC分类号： A61K31/495 , A61K31/535 , C07D401/04 , C07D401/06 , C07D401/12 , C07D471/14 , C07D498/14 , C07D513/14
CPC分类号： C07D401/04 , C07D401/12
摘要： Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as hereinafter described, and salts thereof, prepared starting from corresponding tricyclic compounds, are described. The compounds I and some of the said tricyclic compounds have antibacterial activity, and are therefore useful as antibacterial agents.

64. 发明授权

US4558158A Process for the production of 4-(trialkylammonium)-acetoacetarylides 失效
标题翻译：制备4-（三烷基铵） - 乙酰乙酰胺的方法
公开(公告)号：US4558158A
公开(公告)日：1985-12-10
申请号：US501898
申请日：1983-06-07
申请人： Leander Tenud , Synese Jolidon
发明人： Leander Tenud , Synese Jolidon
IPC分类号： C07C231/00 , C07C67/00 , C07C231/12 , C07C237/04 , C09B44/02 , C07C91/42
CPC分类号： C09B44/02
摘要： Process for the production of 4-(trialkylammonium)-acetoacetarylides having the formula: ##STR1## wherein R is H, a lower alkyl, --OCH.sub.3, --OC.sub.2 H.sub.5, --Cl, --Br, --NO.sub.2, --NHCOCH.sub.3 or an anilated heterocyclic ring; n is 1 to 3; R.sup.1, R.sup.2 and R.sup.3 each is an alkyl having 1 to 18 C atoms; and X is Cl or Br. Such arylide is prepared by reacting a corresponding trialkylamine with a corresponding 4-haloacetoacetarylide at a low temperature in the presence of an organic solvent.
摘要翻译：制备具有下式的4-（三烷基铵） - 乙酰乙酰基化合物的方法：其中R是H，低级烷基，-OCH 3，-OC 2 H 5，-Cl，-Br，-NO 2，-NHCOCH 3或被杂环的杂环 ; n为1〜3; R1，R2和R3各自为具有1至18个C原子的烷基; X为Cl或Br。在有机溶剂存在下，通过使相应的三烷基胺与相应的4-卤代乙酰基乙酰胺在低温下反应来制备。

65. 发明申请

US20120277243A1 PYRAZOLIDIN-3-ONE DERIVATIVES 有权
标题翻译：吡唑啉-3-酮衍生物
公开(公告)号：US20120277243A1
公开(公告)日：2012-11-01
申请号：US13454167
申请日：2012-04-24
申请人： Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Antonio Ricci , Daniel Rueher , Heinz Stadler , Eric Vieira
发明人： Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Antonio Ricci , Daniel Rueher , Heinz Stadler , Eric Vieira
IPC分类号： A61K31/4439 , A61P25/00 , A61P25/28 , C07D401/04 , A61K31/501 , A61K31/506 , C07D487/04 , C07D401/14 , A61K31/444 , A61P25/18 , C07D403/04
CPC分类号： C07D401/04 , C07D403/04 , C07D487/04
摘要： The present invention relates to ethynyl derivatives of formula I wherein G, X, R1, R2, R3, R3′, R4, and R4′ are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).
摘要翻译：本发明涉及式I的乙炔基衍生物，其中G，X，R 1，R 2，R 3，R 3'，R 4和R 4'如本文所定义，或其药学上可接受的酸加成盐，涉及外消旋混合物或其相应的对映体和/或其光学异构体和/或立体异构体。式I化合物是代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂（PAM）。

66. 发明授权

US07790763B2 Substituted phenyl methanone derivatives 失效
标题翻译：取代苯甲酮衍生物
公开(公告)号：US07790763B2
公开(公告)日：2010-09-07
申请号：US11332999
申请日：2006-01-17
申请人： Synese Jolidon , Robert Narquizian , Roger David Norcross , Emmanuel Pinard
发明人： Synese Jolidon , Robert Narquizian , Roger David Norcross , Emmanuel Pinard
IPC分类号： A61K31/40 , C07D295/27
CPC分类号： C07D207/12 , C07D205/04 , C07D211/46 , C07D401/12
摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, n, and m, are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. These compounds are good inhibitors of the glycine transporter 1 (GlyT-1) and are useful for the treatment of CNS disorders such as schizophrenia, cognitive impairment, and Alzheimer's disease.
摘要翻译：本发明涉及式I化合物，其中R 1，R 2，R 3，n和m如说明书中所定义，及其药学上可接受的酸加成盐。这些化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂，可用于治疗中枢神经系统疾病如精神分裂症，认知障碍和阿尔茨海默病。

67. 发明授权

US07595314B2 Benzoyl-piperazine derivatives 有权
标题翻译：苯甲酰哌嗪衍生物
公开(公告)号：US07595314B2
公开(公告)日：2009-09-29
申请号：US12177386
申请日：2008-07-22
申请人： Daniela Alberati-Giani , Synese Jolidon , Robert Narquizian , Matthias Heinrich Nettekoven , Roger David Norcross , Emmanuel Pinard , Henri Stalder
发明人： Daniela Alberati-Giani , Synese Jolidon , Robert Narquizian , Matthias Heinrich Nettekoven , Roger David Norcross , Emmanuel Pinard , Henri Stalder
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/55 , C07D413/12
CPC分类号： C07D295/192 , A61K31/495 , A61K31/496 , C07D207/08 , C07D207/12 , C07D207/20 , C07D211/42 , C07D231/12 , C07D233/54 , C07D237/20 , C07D249/08 , C07D257/04 , C07D307/14 , C07D309/14
摘要： A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
摘要翻译：式的化合物，其中取代基如治疗精神病，疼痛，记忆和学习中的神经变性功能障碍，精神分裂症，痴呆和其他认知过程受损的其他疾病（如注意力缺陷障碍或阿尔茨海默氏病）的描述中所述。

68. 发明申请

US20090203665A1 HETEROCYCLIC-SUBSTITUTED PHENYL METHANONES 有权
标题翻译：杂环取代苯甲酮
公开(公告)号：US20090203665A1
公开(公告)日：2009-08-13
申请号：US12422332
申请日：2009-04-13
申请人： Synese Jolidon , Robert Narquizian , Roger David Norcross , Emmanuel Pinard
发明人： Synese Jolidon , Robert Narquizian , Roger David Norcross , Emmanuel Pinard
IPC分类号： A61K31/4035 , A61K31/5377 , A61K31/437 , C07D471/04 , C07D413/06 , C07D487/04 , C07D209/44
CPC分类号： C07D471/04 , C07D209/08 , C07D209/44 , C07D209/46 , C07D209/88 , C07D231/56 , C07D235/06 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/04 , C07D417/04 , C07D487/04 , C07D491/08
摘要： The present invention relates to compounds of formula I wherein R1, R2, and are defined in the specification and to pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明涉及式I化合物，其中R1，R2和在本说明书中定义及其药学上可接受的酸加成盐。

69. 发明申请

US20090192136A1 BENZOYL-PIPERAZINE DERIVATIVES 有权
标题翻译：苯甲酰哌嗪衍生物
公开(公告)号：US20090192136A1
公开(公告)日：2009-07-30
申请号：US12177386
申请日：2008-07-22
申请人： Daniela Alberati-Giani , Synese Jolidon , Robert Narquizian , Matthias Heinrich Nettekoven , Roger David Norcross , Emmanuel Pinard , Henri Stalder
发明人： Daniela Alberati-Giani , Synese Jolidon , Robert Narquizian , Matthias Heinrich Nettekoven , Roger David Norcross , Emmanuel Pinard , Henri Stalder
IPC分类号： A61K31/496 , C07D413/10 , C07D241/04 , A61K31/55 , A61K31/5377 , A61P25/00 , A61K31/495 , C07D405/12
CPC分类号： C07D295/192 , A61K31/495 , A61K31/496 , C07D207/08 , C07D207/12 , C07D207/20 , C07D211/42 , C07D231/12 , C07D233/54 , C07D237/20 , C07D249/08 , C07D257/04 , C07D307/14 , C07D309/14
摘要： A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
摘要翻译：式的化合物，其中取代基如治疗精神病，疼痛，记忆和学习中的神经变性功能障碍，精神分裂症，痴呆和其他认知过程受损的其他疾病（如注意力缺陷障碍或阿尔茨海默病）的治疗方法所述。

70. 发明授权

US07462617B2 Substituted acylpiperazine derivatives 有权
标题翻译：取代的酰基哌嗪衍生物
公开(公告)号：US07462617B2
公开(公告)日：2008-12-09
申请号：US10933072
申请日：2004-09-01
申请人： Daniela Alberati-Giani , Synese Jolidon , Robert Narquizian , Matthias Heinrich Nettekoven , Roger David Norcross , Emmanuel Pinard , Henri Stalder
发明人： Daniela Alberati-Giani , Synese Jolidon , Robert Narquizian , Matthias Heinrich Nettekoven , Roger David Norcross , Emmanuel Pinard , Henri Stalder
IPC分类号： A61K31/53 , A61K31/496 , C07D295/192 , C07D409/12 , C07D251/22 , C07D251/24 , A61K31/495
CPC分类号： C07D295/16 , A61K31/495 , A61K31/496 , C07D213/56 , C07D213/69 , C07D213/74 , C07D233/64 , C07D239/26 , C07D239/42 , C07D241/12 , C07D251/42 , C07D251/48 , C07D257/04 , C07D263/32 , C07D277/30 , C07D295/185 , C07D309/04 , C07D309/20 , C07D333/24 , C07D409/12
摘要： The invention relates to compounds of formula wherein the substituents are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention further relates to methods for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other d 1iseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
摘要翻译：本发明涉及下式的化合物，其中取代基如说明书中所定义，及其药学上可接受的酸加成盐。本发明还涉及用于治疗精神病，疼痛，记忆和学习中的神经变性功能障碍，精神分裂症，痴呆和其他认知过程受损的其他疾病的方法，例如注意力缺陷障碍或阿尔茨海默病。

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