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1. 发明授权

US4402957A Heterocyclic derivatives of [4-(piperazin-1-ylphenyloxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazole s and 1H-1,2,4-triazoles 失效
标题翻译： [4-（哌嗪-1-基苯氧基甲基）-1,3-二氧戊环-2-基甲基] -1H-咪唑和1H-1,2,4-三唑的杂环衍生物
公开(公告)号：US4402957A
公开(公告)日：1983-09-06
申请号：US261420
申请日：1981-05-07
申请人： Jan Heeres , Robert Hendrickx
发明人： Jan Heeres , Robert Hendrickx
IPC分类号： C07D213/74 , C07D215/38 , C07D233/84 , C07D249/14 , C07D277/18 , C07D277/42 , C07D295/28 , C07D473/06 , C07D419/14 , A61K31/52
CPC分类号： C07D213/74 , C07D215/38 , C07D233/84 , C07D249/14 , C07D277/18 , C07D277/42 , C07D295/28 , C07D473/06
摘要： Novel heterocyclic derivatives of [4-(piperazin-1-yl-phenoxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazoles and 1H-1,2,4-triazoles, useful as antifungal and antibacterial agents.
摘要翻译：可用作抗真菌和抗菌剂的[4-（哌嗪-1-基 - 苯氧基甲基）-1,3-二氧戊环-2-基甲基] -1H-咪唑和1H-1,2,4-三唑的新型杂环衍生物。

2. 发明申请

US20070203189A1 2-Amino-4,5-Trisubstituted Thiazolyl Derivatives 有权
标题翻译： 2-氨基-4,5-三取代噻唑衍生物
公开(公告)号：US20070203189A1
公开(公告)日：2007-08-30
申请号：US11742741
申请日：2007-05-01
申请人： Christopher Love , Guy Van Lommen , Julien Georges Doyon , Jean-Pierre Bongartz , Marcel Van der Aa , Robert Hendrickx , Peter Jacobus Antonius Buijnsters , Ludwig Cooymans , Nele Vandermaesen , Erwin Coesemans , Gustaaf Boeckx
发明人： Christopher Love , Guy Van Lommen , Julien Georges Doyon , Jean-Pierre Bongartz , Marcel Van der Aa , Robert Hendrickx , Peter Jacobus Antonius Buijnsters , Ludwig Cooymans , Nele Vandermaesen , Erwin Coesemans , Gustaaf Boeckx
IPC分类号： A61K31/454 , A61K31/427 , A61K31/426 , C07D417/02
CPC分类号： C07D417/04 , C07D277/42 , C07D471/04
摘要： This invention concerns the use of a compound of formula (I′) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(═O)2—; mono- or di(C1-6alkyl)aminoS(═O)2; —C(═N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula L is optionally substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of inflammatory and/or auto-immune diseases mediated through TNF-α and/or IL-12.
摘要翻译：本发明涉及式（I'）化合物的N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构体形式的用途，其中Z为卤素; C 1-6烷基; C 1-6烷基羰基; C 1-6烷氧基羰基; 氨基羰基; 用羟基，羧基，氰基，氨基，被哌啶取代的氨基，被C 1-4烷基取代的哌啶基取代的氨基，单或二（ C 1-6烷基）氨基，氨基羰基，一或二（C 1-6烷基）氨基羰基，C 1-6烷氧基羰基， C 1-6烷基氧基，哌啶基，哌嗪基，吗啉基，硫代吗啉基; 多卤代1-4烷基; 氰基; 氨基; 单或二（C 1-6烷基）氨基羰基; C 1-6烷氧基羰基; C 1-6烷基羰基氧基; 氨基-S（-O）2 - ; 单或二（C 1-6烷基）氨基S（-O）2; -C（-N-R x X）NR z R z Z; Q是任选取代的C 3-6环烷基，苯基，吡啶基，嘧啶基，吡嗪基，哒嗪基，苯并噻唑基，苯并恶唑基，苯并咪唑基，吲唑基或咪唑并吡啶基，或Q是式L的基团是任选取代的苯基或任选取代的单环5或6元部分饱和或芳族杂环或双环部分饱和或芳族杂环; 芳基是任选取代的苯基; 用于制备用于预防或治疗通过TNF-α和/或IL-12介导的炎症和/或自身免疫疾病的药物。

3. 发明申请

US20050209253A1 Pyrrolopyrimidine and pyrrolopyridine derivatives substituted with cyclic amino group 审中-公开
标题翻译：吡咯并嘧啶和环状氨基取代的吡咯并吡啶衍生物
公开(公告)号：US20050209253A1
公开(公告)日：2005-09-22
申请号：US10504981
申请日：2003-12-24
申请人： Atsuro Nakazato , Taketoshi Okubo , Dai Nozawa , Mikato Yamaguchi , Tomoko Tamita , Ludo Kennis , Marcel De Bruyn , Jean-Pierre Bongartz , Frans Van Den Keybus , Yves Van Roosbroeck , Marcel Luyckx , Robert Hendrickx
发明人： Atsuro Nakazato , Taketoshi Okubo , Dai Nozawa , Mikato Yamaguchi , Tomoko Tamita , Ludo Kennis , Marcel De Bruyn , Jean-Pierre Bongartz , Frans Van Den Keybus , Yves Van Roosbroeck , Marcel Luyckx , Robert Hendrickx
IPC分类号： A61K31/436 , A61K31/437 , A61K31/519 , A61K31/661 , A61P1/00 , A61P1/04 , A61P9/10 , A61P9/12 , A61P17/00 , A61P17/14 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/36 , A61P29/00 , A61P37/00 , A61P43/00 , C07D471/04 , C07D471/08 , C07D487/04 , C07D491/08 , C07D519/00 , C07F9/59 , C07F9/6561 , C07D471/02 , A61K31/4745
CPC分类号： C07D471/04 , C07D487/04 , C07F9/6561
摘要： An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. [Solution] A pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.
摘要翻译：本发明的目的是提供一种抗CRF受体的拮抗剂，其作为治疗或预防药物是有效的，其涉及CRF被认为涉及的疾病，例如抑郁症，焦虑症，阿尔茨海默氏病，帕金森病，亨廷顿氏舞蹈病，进食疾病，高血压，胃疾病，药物依赖，癫痫，脑梗死，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，脱发，肠易激综合征，睡眠障碍，癫痫，皮肤病，精神分裂症等。溶液]由下式[I]表示的环状氨基取代的吡咯并嘧啶或吡咯并吡啶衍生物对CRF受体具有高亲和力，对于被认为涉及CRF的疾病有效。

4. 发明授权

US4456605A Heterocyclic derivatives of [4-(piperazin-1-yl-phenyloxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazol es and 1H-1,2,4-triazoles 失效
标题翻译： [4-（哌嗪-1-基 - 苯氧基甲基）-1,3-二氧戊环-2-基甲基] -1H-咪唑和1H-1,2,4-三唑的杂环衍生物
公开(公告)号：US4456605A
公开(公告)日：1984-06-26
申请号：US509562
申请日：1983-06-30
申请人： Jan Heeres , Robert Hendrickx
发明人： Jan Heeres , Robert Hendrickx
IPC分类号： C07D213/74 , C07D215/38 , C07D233/84 , C07D249/14 , C07D277/18 , C07D277/42 , C07D295/28 , C07D473/06 , C07D419/14 , A61K31/52
CPC分类号： C07D213/74 , C07D215/38 , C07D233/84 , C07D249/14 , C07D277/18 , C07D277/42 , C07D295/28 , C07D473/06
摘要： Novel heterocyclic derivatives of [4-(piperazin-1-yl-phenoxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazoles and 1H-1,2,4-triazoles, useful as antifungal and antibacterial agents.
摘要翻译：可用作抗真菌和抗菌剂的[4-（哌嗪-1-基 - 苯氧基甲基）-1,3-二氧戊环-2-基甲基] -1H-咪唑和1H-1,2,4-三唑的新型杂环衍生物。

5. 发明授权

US4287195A Heterocyclic derivatives of [4-(piperazin-1-yl-phenyloxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazol es and 1H-1,2,4-triazoles 失效
标题翻译： [4-（哌嗪-1-基 - 苯氧基甲基）-1,3-二氧戊环-2-基甲基] -1H-咪唑和1H-1,2,4-三唑的杂环衍生物
公开(公告)号：US4287195A
公开(公告)日：1981-09-01
申请号：US27178
申请日：1979-04-04
申请人： Jan Heeres , Robert Hendrickx
发明人： Jan Heeres , Robert Hendrickx
IPC分类号： C07D213/74 , C07D215/38 , C07D233/84 , C07D249/14 , C07D277/18 , C07D277/42 , C07D295/28 , C07D473/06 , C07D521/00 , C07D419/14 , A61K31/495
CPC分类号： C07D213/74 , C07D215/38 , C07D231/12 , C07D233/56 , C07D233/84 , C07D249/08 , C07D249/14 , C07D277/18 , C07D277/42 , C07D295/28 , C07D473/06
摘要： Novel heterocyclic derivatives of [4-(piperazin-1-yl-phenloxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazoles and 1H-1,2,4-triazoles, useful as antifungal and antibacterial agents.
摘要翻译：可用作抗真菌和抗菌剂的[4-（哌嗪-1-基 - 苯氧基甲基）-1,3-二氧戊环-2-基甲基] -1H-咪唑和1H-1,2,4-三唑的新型杂环衍生物。

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