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1. 发明授权

US07414048B2 4,5-dihydro-isoxazole derivatives and their pharmaceutical use 失效
公开(公告)号：US07414048B2
公开(公告)日：2008-08-19
申请号：US10403543
申请日：2003-03-31
申请人： Eddy Jean Edgard Freyne , José Ignacio Andrés-Gil , Frederik Dirk Deroose , Davy Petrus Franciscus Maria Petit , Maria Encarnacion Matesanz-Ballesteros , Rosa Maria Alvarez Escobar
发明人： Eddy Jean Edgard Freyne , José Ignacio Andrés-Gil , Frederik Dirk Deroose , Davy Petrus Franciscus Maria Petit , Maria Encarnacion Matesanz-Ballesteros , Rosa Maria Alvarez Escobar
IPC分类号： C07D413/14 , A61K31/501 , A61K31/496
CPC分类号： C07D413/04 , C07D261/04 , C07D413/14
摘要： The present invention is concerned with the compounds of formula wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; -A1=A2-A3=A4- is a pyridinylidene, pyridazinylidene, pyrimidinylidene, pyrazinylidene or phenylidene; B represents an amide, ketone or oxadiazole; D represents Ar or Het; Q represents a covalent direct bond or a ketone, —N—, —O—, —CR5R6—, amide, ethenyl, imine, sulfonyl, sulfinyl, 3-oxobutenyl, pyrazole, isoxazole or thiazole; L represents Ar or Het; R1 represents hydrogen, halo, hydroxy, C(2-6)alkenyl, C(2-6)alkynyl, C(3-6)cycloalkyl, C(3-6)cycloalkenyl, cyano, guanidine, nitro, NR17R18, an optionally substituted C(1-6)alkyl or C(1-6)alkyloxy; R2 and R3 each independently represent hydrogen, halo, C(1-6)alkyloxy or an optionally substituted C(1-6)alkyl; R5 and R6 each independently represent hydrogen, hydroxy, halo, an optionally substituted C(1-6)alkyl, C(2-6)alkenyl, C(2-6)alkynyl, C(3-6)cycloalkyl, C(3-6)cycloalkenyl, C(1-6)alkyloxy, cyano, (C═O)R25, (C—O)OR16, (SO2)R16, aminocarbonyloxy, aminoC(1-6)alkyl, NR17R18, N3, Ar or Het; or R5 and R6 together with the carbon atom to which they are attached, form an Ar or Het; Ar represents an optionally substituted C(6-14)aryl; Het represents an optionally substituted C(1-14)heterocycle; or a N-oxide, pharmaceutically acceptable addition salt, quaternary amine or stereochemically isomeric form thereof; the processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

2. 发明授权

US06583141B1 4,5-dihydro-isoxazole derivatives and their pharmaceutical use 失效
标题翻译： 4,5-二氢异恶唑衍生物及其药物用途
公开(公告)号：US06583141B1
公开(公告)日：2003-06-24
申请号：US09807149
申请日：2001-04-06
申请人： Eddy Jean Edgard Freyne , José Ignacio Andrés-Gil , Frederik Dirk Deroose , Davy Petrus Franciscus Maria Petit , Maria Encarnacion Matesanz-Ballesteros , Rosa Maria Alvarez Escobar
发明人： Eddy Jean Edgard Freyne , José Ignacio Andrés-Gil , Frederik Dirk Deroose , Davy Petrus Franciscus Maria Petit , Maria Encarnacion Matesanz-Ballesteros , Rosa Maria Alvarez Escobar
IPC分类号： C07D41304
CPC分类号： C07D413/04 , C07D261/04 , C07D413/14
摘要： The present invention is concerned with the compounds of formula wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; —A1═A2—A3═A4— is a pyridinylidene, pyridazinylidene, pyrimidinylidene, pyrazinylidene or phenylidene; B represents an amide, ketone or oxadiazole; D represents Ar or Het; Q represents a covalent direct bond or a ketone, —N—, —O—, —CR5R6—, amide ethenyl, imine, sulfonyl, sulfinyl, 3-oxobutenyl, pyrazole, isoxazole or thiazole; L represents Ar or Het; R1 represents hydrogen, halo, hydroxy, C(2-6)alkenyl, C(2-6)alkynyl, C(3-6)cycloalkyl, C(3-6)cycloalkenyl, cyano, guanidine, nitro, NR17R18, an optionally substituted C(1-6)alkyl or C(1-6)alkyloxy; R2 and R3 each independently represent hydrogen, halo, C(1-6)alkyloxy or an optionally substituted C(1-6)alkyl; R5 and R6 each independently represent hydrogen, hydroxy, halo, an optionally substituted C(1-6)alkyl, C(2-6)alkenyl, C(2-6)alkynyl, C(3-6)cycloalkyl, C(3-6)cycloalkenyl, C(1-6)alkyloxy, cyano, (C═O)R25, (C═O)OR16, (SO2)R16, aminocarbonyloxy, aminoC(1-6)alkyl, NR17R18, N3, Ar or Het; or R5 and R6 together with the carbon atom to which they are attached, form an Ar or Het; Ar represents an optionally substituted C(6-14)aryl; Het represents an optionally substituted C(1-14)heterocycle; or a N-oxide, pharmaceutically acceptable addition salt, quaternary amine or stereochemically isomeric form thereof; the processes for their preparation and compositions comprising them. It further relates to their use as a medicine.
摘要翻译：本发明涉及糠醛的化合物m，n和p各自独立地为0或1，q为0,1,2,3,4或5; -A1 = A2-A3 = A4-是亚吡啶基，哒嗪亚基，亚嘧啶亚基，亚吡嗪基或亚苯基; B代表酰胺，酮或恶二唑; D表示Ar或Het; Q表示共价直接键或酮，-N-，-O-，-CR5R6-，酰胺乙烯基，亚胺，磺酰基，亚磺酰基，3-氧代丁烯基，吡唑，异恶唑或噻唑; L表示Ar或Het; R1表示氢，卤素，羟基，C（2-6）烯基，C（2-6）炔基，C（3-6）环烷基，C（3-6）环烯基，氰基，胍，硝基，NR17R18，取代的C（1-6）烷基或C（1-6）烷氧基; R2和R3各自独立地表示氢，卤素，C（1-6）烷氧基或任选取代的C 1-6烷基; R 5和R 6各自独立地表示氢，羟基，卤素，任选取代的C 1-6烷基，C（2-6）烯基，C（2-6）炔基，C（3-6）环烷基，C（3） -6）环烯基，C（1-6）烷氧基，氰基，（C = O）R25，（C = O）OR16，（SO2）R16，氨基羰基氧基，氨基C（1-6）烷基，NR17R18，N3，Ar或 Het; 或R 5和R 6与它们所连接的碳原子一起形成Ar或Het; Ar表示任选取代的C（6-14）芳基; Het表示任选取代的C（1-14）杂环; 或N-氧化物，药学上可接受的加成盐，季胺或其立体化学异构体形式; 其制备方法和包含它们的组合物。它还涉及它们作为药物的用途。

3. 发明授权

US07081453B2 Compounds for treating impaired fundic relaxation 有权
公开(公告)号：US07081453B2
公开(公告)日：2006-07-25
申请号：US10311612
申请日：2001-06-13
申请人： Kristof Van Emelen , Marcel Frans Leopold De Bruyn , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Maria Encarnacion Matesanz-Ballesteros , José Manuel Bartolomé-Nebreda
发明人： Kristof Van Emelen , Marcel Frans Leopold De Bruyn , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Maria Encarnacion Matesanz-Ballesteros , José Manuel Bartolomé-Nebreda
IPC分类号： A61K31/397
CPC分类号： C07D411/04 , C07D491/04
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharma-ceutically acceptable acid addition salt thereof, wherein —a1═a2—a3═a4— is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH═; —Z1—Z2— is a bivalent radical; —A— is a bivalent radical of formula —N(R6)—Alk2— or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula (d-1), (d-2), (d-3), (d-4), (d-5) wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to disturbed fundic accomodation

4. 发明授权

US07462717B2 C6-and C9-substituted chromeno[4,3-c]isoxazoline derivatives and their use as anti-depressants 有权
标题翻译： C6-和C9-取代的色烯并[4,3-c]异恶唑啉衍生物及其作为抗抑郁剂的用途
公开(公告)号：US07462717B2
公开(公告)日：2008-12-09
申请号：US10524989
申请日：2003-08-19
申请人： José Ignacio Andrés-Gil , Manuel Jesús Alcázar-Vaca , Maria Encarnacion Matesanz-Ballesteros , Margaretha Henrica Maria Bakker , Antonius Adrianus Hendrikus Petrus Megens
发明人： José Ignacio Andrés-Gil , Manuel Jesús Alcázar-Vaca , Maria Encarnacion Matesanz-Ballesteros , Margaretha Henrica Maria Bakker , Antonius Adrianus Hendrikus Petrus Megens
IPC分类号： A61K31/55 , A61K31/5377 , A61K31/496 , C07D498/04 , C07D413/00
CPC分类号： C07D498/04
摘要： The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on at least one of the C6- and C9-positions of the phenylpart of the tricyclic moiety with a selected radical, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2, R14 and R15 are certain specific substituents, with the proviso that at least one of R14 and R15 is not hydrogen, Pir is preferably an optionally substituted piperidinyl or piperazinyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders. The compounds according to the invention have surprisingly been shown to have a serotonine (5-HT) reuptake inhibitor activity in combination with additional α2-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative. The invention also relates to novel combination of isoxazoline derivatives according to the invention with one or more other compounds selected from the group of antidepressants, anxiolytics, anti-psychotics and anti-Parkinson's disease drugs to improve efficacy and/or onset of action.
摘要翻译：本发明涉及取代的三环异恶唑啉衍生物，更具体地是三环二氢苯并吡喃恶唑啉，二氢喹诺酮异恶唑啉，二氢萘硫基异恶唑啉和二氢苯并噻唑并恶唑啉衍生物，其被三选择基团的苯基部分的C 6 - 和C 9位中的至少一个与选定的基团取代，）其中X = CH 2，N-R 7，S或O，R 1，R 2，R 14和R 15是某些具体取代基，条件是R14和R15中的至少一个不是氢，Pir优选为任选取代的哌啶基或哌嗪基基团和R 3表示任选取代的芳族双环或杂环系统，其包括最多6个原子长的部分或完全氢化的烃链，其中环系统连接到Pir基团，并且其可以含有一个或多个选自以下的杂原子： O，N和S; 其制备方法，包含它们的药物组合物及其作为药物的用途，特别是用于治疗抑郁症，焦虑症，运动障碍，精神病，帕金森病和体重障碍。根据本发明的化合物令人惊奇地显示具有与另外的α2-肾上腺素受体拮抗剂活性组合的5-羟色胺（5-HT）再摄取抑制剂活性，并且在没有镇静作用的情况下表现出强烈的抗抑郁活性。本发明还涉及根据本发明的异恶唑啉衍生物与一种或多种选自抗抑郁药，抗焦虑药，抗精神病药和抗帕金森病药物的其它化合物的新组合，以改善疗效和/或起效。

5. 发明授权

US06403805B1 1,3-dihydro-1-(phenylalkyl)-2H-imidazol-2-one derivatves 有权
标题翻译： 1,3-二氢-1-（苯基烷基）-2H-咪唑-2-酮化合物
公开(公告)号：US06403805B1
公开(公告)日：2002-06-11
申请号：US09362007
申请日：1999-07-27
申请人： Eddy Jean Edgard Freyne , Gaston Stanislas Marcella Diels , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea
发明人： Eddy Jean Edgard Freyne , Gaston Stanislas Marcella Diels , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea
IPC分类号： C07D23332
CPC分类号： C07D401/06 , C07D233/36 , C07D233/38 , C07D233/70
摘要： The present invention describes compounds useful for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases, said compounds having the formula the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof.
摘要翻译：本发明描述了可用于治疗患有与磷酸二酯酶IV（PDE IV）的异常酶促或催化活性相关的疾病状态的温血动物的化合物和/或与生理上有害的细胞因子过量相关的疾病状态，特别是过敏性疾病，特应性和炎症性疾病，所述具有N-氧化物形式的化合物，其药学上可接受的酸或碱加成盐及其立体化学异构形式。

6. 发明授权

US07465741B2 C-substituted tricyclic isoxazoline derivatives and their use as anti-depressants 有权
标题翻译： C-取代三环异恶唑啉衍生物及其作为抗抑郁剂的用途
公开(公告)号：US07465741B2
公开(公告)日：2008-12-16
申请号：US10524197
申请日：2003-08-12
申请人： José Ignacio Andrés-Gil , José Manuel Bartolomé-Nebreda , Rosa Maria Alvarez-Escobar , Margaretha Henrica Maria Bakker , Antonius Adrianus Hendrikus Petrus Megens
发明人： José Ignacio Andrés-Gil , José Manuel Bartolomé-Nebreda , Rosa Maria Alvarez-Escobar , Margaretha Henrica Maria Bakker , Antonius Adrianus Hendrikus Petrus Megens
IPC分类号： A61K31/44 , C07D401/00 , C07D491/00 , C07D498/00 , C07D515/00 , C07D513/00
CPC分类号： C07D498/04
摘要： The invention concerns substituted tricyclic isoxazoline derivatives according to Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with at least one radical that is attached to the phenyl radical by a carbon-carbon bond as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherin all variables are defined in claim 1. (I) The compounds have surprisingly been shown to have selective serotonine (5-HT) reuptake inhibitor activity in combination with additional α2-adrenocptor antagonist activity and show a strong antidepressant and/or anxiolytic activity and/or antipsychotic and/or a body weight control activity without being sedative. Also, in view of their selective serotonine (5-HT) reuptake inhibitor as well as α2-adrenoceptor antagonist activity, compounds according to the invention are also suitable for treatment and/or prophylaxis in diseases where either one of the activities alone or the combination of said activities may be of therapeutic use.
摘要翻译：本发明涉及取代的式（I）三环异恶唑啉衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式及其N-氧化物形式，更特别地三环二氢苯并吡喃恶唑啉，二氢喹啉基异恶唑啉，二氢萘并恶唑啉和二氢苯并噻喃并恶唑啉衍生物取代在具有至少一个通过碳 - 碳键连接到苯基的基团的三环部分的苯基上，以及它们的制备方法，包含它们的药物组合物及其作为药物的用途，特别是用于治疗抑郁症，焦虑，运动障碍，精神病，帕金森病和包括神经性厌食症和贪食症的体重障碍，所有变量都在权利要求1中定义。（I）化合物令人惊奇地显示具有选择性5-羟色胺（5-HT）再摄取抑制剂活性组合具有额外的α2-肾上腺素能拮抗剂活性，并且显示强的抗抑郁药和/或抗焦虑活性和/或抗精神病和/或体重控制活性而不需要镇静。此外，考虑到它们的选择性5-羟色胺再摄取抑制剂以及α2-肾上腺素能受体拮抗剂活性，根据本发明的化合物也适用于治疗和/或预防疾病，其中单独的一种活性或组合的所述活动可能具有治疗用途。

7. 发明授权

US08592422B2 Bicyclic triazole and pyrazole lactams as allosteric modulators of mGluR5 receptors 失效
标题翻译：双环三唑和吡唑内酰胺作为mGluR5受体的变构调节剂
公开(公告)号：US08592422B2
公开(公告)日：2013-11-26
申请号：US13329025
申请日：2011-12-16
申请人： P. Jeffrey Conn , Craig W. Lindsley , Shaun R. Stauffer , José Manuel Bartolomé-Nebreda , Susana Conde-Ceide , Gregor James MacDonald , Han Min Tong , Carrie K. Jones , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Chrysa Malosh
发明人： P. Jeffrey Conn , Craig W. Lindsley , Shaun R. Stauffer , José Manuel Bartolomé-Nebreda , Susana Conde-Ceide , Gregor James MacDonald , Han Min Tong , Carrie K. Jones , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Chrysa Malosh
IPC分类号： A61K31/4985 , A61P25/00 , C07D487/04
CPC分类号： C07D487/04 , A61K31/40 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/695 , A61K45/06 , C07F7/1804
摘要： In one aspect, the invention relates to bicyclic triazole and pyrazole lactams, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：一方面，本发明涉及双代三唑和吡唑内酰胺，其衍生物和相关化合物，其可用作代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂; 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用所述化合物和组合物治疗与谷氨酸官能障碍相关的神经和精神障碍的方法。该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

8. 发明授权

US08329704B2 Substituted pyrazinone derivatives for use in MCH-1 mediated diseases 有权
标题翻译：用于MCH-1介导的疾病的取代的吡嗪酮衍生物
公开(公告)号：US08329704B2
公开(公告)日：2012-12-11
申请号：US12091365
申请日：2006-12-18
申请人： José Ignacio Andrés-Gil , Manuel Jesús Alcázar-Vaca , Rosa María Álvarez-Escobar , Julen Oyarzabal Santamarina , Frank Matthias Dautzenberg , Jacqueline Macritchie , Donald Simpson , Sonia Martinez Gonzalez
发明人： José Ignacio Andrés-Gil , Manuel Jesús Alcázar-Vaca , Rosa María Álvarez-Escobar , Julen Oyarzabal Santamarina , Frank Matthias Dautzenberg , Jacqueline Macritchie , Donald Simpson , Sonia Martinez Gonzalez
IPC分类号： A61K31/4965 , C07D241/02
CPC分类号： C07D241/20 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D491/10
摘要： The present invention concerns aryl and heteroaryl substituted pyrazinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.
摘要翻译：本发明涉及具有拮抗性黑色素浓缩激素（MCH）活性的芳基和杂芳基取代的吡嗪酮衍生物，特别是根据通式（I）的MCH-1活性，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式或其季铵盐，其中所述变量在权利要求1中定义。它还涉及它们的制备，包含它们的组合物及其作为药物的用途。根据本发明的化合物可用于预防和/或治疗精神病学障碍，包括但不限于焦虑，进食障碍，情绪障碍，例如双相性精神障碍和抑郁症，精神病如精神分裂症和睡眠障碍; 肥胖; 糖尿病; 性障碍和神经障碍。

9. 发明授权

US07423048B2 Compounds for treating fundic disaccomodation 有权
公开(公告)号：US07423048B2
公开(公告)日：2008-09-09
申请号：US11355402
申请日：2006-02-16
申请人： Kristol Van Emelen , Marcel Frans Leopold De Bruyn , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Maria Encamacion Matesanz-Ballesteros , José Manuel Bartolomé-Nebreda
发明人： Kristol Van Emelen , Marcel Frans Leopold De Bruyn , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Maria Encamacion Matesanz-Ballesteros , José Manuel Bartolomé-Nebreda
IPC分类号： C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D403/06 , C07D403/14 , A61K31/436 , A61P1/14
CPC分类号： C07D411/04 , C07D491/04
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -a1═a2-a3═a4- is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH═; -Z1-Z2- is a bivalent radical; -A- is a bivalent radical of formula —N(R6)-Alk2- or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to disturbed fundic accomodation.

10. 发明授权

US08852554B2 Radiolabelled PDE10 ligands 有权
标题翻译：放射性标记的PDE10配体
公开(公告)号：US08852554B2
公开(公告)日：2014-10-07
申请号：US13505157
申请日：2010-10-27
申请人： José Ignacio Andrés-Gil , Meri De Angelis , Guy Maurits R. Bormans , Sofie Jeanne Leopoldine Celen
发明人： José Ignacio Andrés-Gil , Meri De Angelis , Guy Maurits R. Bormans , Sofie Jeanne Leopoldine Celen
IPC分类号： A61K51/04 , C07D401/14
CPC分类号： C07D401/14 , A61K51/0455
摘要： The present invention relates to novel, selective, radiolabelled PDE10 ligands which are useful for imaging and quantifying the PDE10A enzyme in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo.
摘要翻译：本发明涉及用于使用正电子发射断层摄影（PET）在组织中成像和定量PDE10A酶的新型选择性放射性标记的PDE10配体。本发明还涉及包含这些化合物的组合物，制备此类化合物和组合物的方法，以及用于在体外或体内成像组织，细胞或宿主的这些化合物和组合物的用途。

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