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11. 发明申请

WO2009097405A3 COMPOUNDS AND METHODS FOR PREPARING DIAZASPIRO DERIVATIVES 审中-公开
标题翻译：制备二氮杂衍生物的化合物和方法
公开(公告)号：WO2009097405A3
公开(公告)日：2009-10-15
申请号：PCT/US2009032400
申请日：2009-01-29
申请人： NEUROGEN CORP , XU YUELIAN , XIE LINGHONG , HAN BINGSONG , MAYNARD GEORGE D , CHENARD BERTRAND L , STAAB ANDREW J
发明人： XU YUELIAN , XIE LINGHONG , HAN BINGSONG , MAYNARD GEORGE D , CHENARD BERTRAND L , STAAB ANDREW J
IPC分类号： C07D487/04 , C07D487/02
CPC分类号： C07D471/10 , C07D471/20
摘要： Compounds and methods are provided for the synthesis of diazaspiro derivatives of the Formula: wherein R is as described herein. Such compounds are useful, for example, as intermediates in the synthesis of biologically active compounds.
摘要翻译：提供了用于合成下式的二氮杂螺衍生物的化合物和方法：其中R如本文所述。这样的化合物例如可用作合成生物活性化合物的中间体。

12. 发明申请

WO2007133820A2 DIARYL TRIAZOLONES AS CB1 ANTAGONISTS 审中-公开
标题翻译： DIARYL TRIAZOLONES作为CB1拮抗剂
公开(公告)号：WO2007133820A2
公开(公告)日：2007-11-22
申请号：PCT/US2007060599
申请日：2007-01-17
申请人： NEUROGEN CORP , HUTCHISON ALAN J , MAO JIANMIN , MAYNARD GEORGE D , PRINGLE WALLACE C , ZHAO HE , WUSTROW DAVID J
发明人： HUTCHISON ALAN J , MAO JIANMIN , MAYNARD GEORGE D , PRINGLE WALLACE C , ZHAO HE , WUSTROW DAVID J
IPC分类号： A61F9/00
CPC分类号： C07D401/14 , C07D249/12 , C07D401/04 , C07D403/04 , C07D413/14
摘要： Diaryl triazolones of Formula I are provided, in which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using diaryl traizolones of Formula I to treat such disorders are provided, as are methods for using such compounds as ligands for receptor localization studies and various in vitro assays.
摘要翻译：提供式I的二芳基三唑酮，其中变量如本文所述。这些化合物可用于体内或体外调节CB1活性，并且特别可用于治疗对人，家养伴侣动物和家畜中的CB1调节有反应的病症，包括食欲障碍，肥胖症和成瘾性疾病。还提供了使用式I的二芳基特里诺酮来治疗这些疾病的药物组合物和方法，以及使用这些化合物作为受体定位研究的配体和各种体外测定的方法。

13. 发明专利

JP2012180365A 1-aryl-4-substituted isoquinolines 审中-公开
标题翻译： 1-ARYL-4取代的异喹啉
公开(公告)号：JP2012180365A
公开(公告)日：2012-09-20
申请号：JP2012112249
申请日：2012-05-16
申请人： Neurogen Corp , ニューロジェン・コーポレーション
发明人： LEE KYUNGAE , YUAN JUN , MAYNARD GEORGE D , HUTCHISON ALAN , MITCHELL SCOTT
IPC分类号： C07D217/14 , A61K31/47 , A61K31/472 , A61K31/4725 , A61K31/5377 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P29/00 , C07D217/02 , C07D217/16 , C07D217/22 , C07D401/04 , C07D401/14 , C07D405/12 , C07D413/14
CPC分类号： C07D405/12 , A61K31/47 , C07D217/14 , C07D217/16 , C07D217/22 , C07D401/04 , C07D401/06 , C07D401/14 , C07D413/14
摘要： PROBLEM TO BE SOLVED: To provide compounds which modulate signal transduction associated with C5a-receptor interactions, can inhibit the pathogenic events, including chemotaxis, associated with anaphylatoxin activity contributing to the increase of such inflammatory and autoimmune conditions.SOLUTION: This invention relates to 1-aryl-4-substituted isoquinoline analogues expressed by the following formula (I) (wherein Ris hydrogen, alkyl, alkenyl or the like; Ris -NRR, -CRRNRRor the like; Ris halogen, hydroxy, amino, cyano, optionally substituted alkyl or the like; and Ar is phenyl, naphthyl, indolyl or the like).
摘要翻译：要解决的问题：为了提供调节与C5a受体相互作用相关的信号转导的化合物，可以抑制与过敏性过氧化物活性相关的致病性事件，包括趋化性，这有助于增加这种炎症和自身免疫病症。解决方案：本发明涉及由下式（I）表示的1-芳基-4-取代的异喹啉类似物（其中R 1 是氢，烷基，烯基或类似; R 2 是-NR 4 R 5 SB POS =“POST”> A R B NR 4 R 5 羟基，氨基，氰基，任意取代的烷基等; Ar为苯基，萘基，吲哚基等），其中R 1，R 2，R 3，。版权所有（C）2012，JPO＆INPIT

14. 发明公开

EP1745039A4 3-ARYL-5,6-DISUBSTITUTED PYRIDAZINES 审中-公开
标题翻译： 3-ARYL-5,6-DISUBSTITUTIERTE PYRIDAZINE
公开(公告)号：EP1745039A4
公开(公告)日：2009-07-22
申请号：EP05783074
申请日：2005-05-06
申请人： NEUROGEN CORP
发明人： YOON TAEYOUNG , YUAN JUN , LEE KYUNGAE , MAYNARD GEORGE D , LIU NIAN
IPC分类号： C07D403/04 , A61K31/501 , A61K31/502 , A61K31/5377 , A61K31/55 , C07D403/14 , C07D405/04 , C07D405/14
CPC分类号： C07D237/20 , C07D237/34 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/04
摘要： The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions.

15. 发明公开

EP1745033A4 4,5-DISUBSTITUTED-2-ARYL PYRIMIDINES 审中-公开
标题翻译： 4.5二取代的2-芳基嘧啶类
公开(公告)号：EP1745033A4
公开(公告)日：2009-08-26
申请号：EP05746687
申请日：2005-05-06
申请人： NEUROGEN CORP
发明人： MAYNARD GEORGE D , GHOSH MANUKA , YUAN JUN , CURRIE KEVIN S , MITCHELL SCOTT , GUO QIN , ZHAO HE
IPC分类号： C07D401/04 , A61K31/505 , A61K31/506 , C07D239/26 , C07D239/28 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D417/04 , C07D471/04 , C07D498/04
CPC分类号： A61K31/505 , C07D239/26 , C07D239/28 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D417/04 , C07D471/04 , C07D498/04
摘要： 4,5-disubstituted-2-arylpyrimidines of Formula (I) and Formula (II) are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 4,5-disubstituted-2-arylpyrimidines, which are useful as probes for the localization of C5a receptors.

16. 发明公开

EP1745024A4 1-ARYL-4-SUBSTITUTED ISOQUINOLINES 有权
标题翻译：异喹啉1-芳基-4-取代
公开(公告)号：EP1745024A4
公开(公告)日：2008-01-09
申请号：EP05747952
申请日：2005-05-06
申请人： NEUROGEN CORP
发明人： LEE KYUNGAE , YUAN JUN , MAYNARD GEORGE D , HUTCHISON ALAN , MITCHELL SCOTT
IPC分类号： A61K31/47 , A61P29/00 , C07D217/02 , C07D217/14 , C07D217/16 , C07D217/22 , C07D401/04 , C07D401/14 , C07D405/12 , C07D413/14
CPC分类号： C07D405/12 , A61K31/47 , C07D217/14 , C07D217/16 , C07D217/22 , C07D401/04 , C07D401/06 , C07D401/14 , C07D413/14

17. 发明专利

ES2384619T3 Isoquinolinas 1-aril-4-sustituidas 未知
公开(公告)号：ES2384619T3
公开(公告)日：2012-07-09
申请号：ES05747952
申请日：2005-05-06
申请人： NEUROGEN CORP , NOVARTIS INT PHARM LTD
发明人： LEE KYUNGAE , YUAN JUN , MAYNARD GEORGE D , HUTCHISON ALAN , MITCHELL SCOTT
IPC分类号： A61K31/47 , A61P29/00 , C07D217/02 , C07D217/14 , C07D217/16 , C07D217/22 , C07D401/04 , C07D401/14 , C07D405/12 , C07D413/14
摘要： Un compuesto según la fórmula I**Fórmula**o una sal farmacéuticamente aceptable de los mismos, en la que:R1 se selecciona de hidrógeno, alquilo de C1-C6, alquenilo de C2-C6, alquinilo de C2-C6, alcoxi de C1-C6, haloalquilode C1-C6, haloalcoxi de C1-C6, (cicloalquil C3-C7)-alquilo de C0-C4;R2 es -(CRARB)OR4;R3 representa entre 0 y 4 sustituyentes, cada uno de los cuales se selecciona independientemente de halógeno,hidroxi, amino, ciano, alquilo opcionalmente sustituido, haloalquilo opcionalmente sustituido, alqueniloopcionalmente sustituido, alquinilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, alcoxiopcionalmente sustituido, haloalcoxi opcionalmente sustituido, hidroxialquilo opcionalmente sustituido,alcoxialquilo opcionalmente sustituido, mono- y di-alquilamino opcionalmente sustituido, aminoalquiloopcionalmente sustituido, -E-(CRCRD)m-Z, y -E-(CRCRD)m-XRA;R4 es:(i) alquilo de C2-C8, alquenilo de C2-C8, alquinilo de C2-C8, (cicloalquil C3-C7)-alquilo de C0-C4, mono- o di-(alquilC1-C4-amino)-alquilo de C2-C4, (heterocicloalquilo de 3 a 7 miembros)-alquilo de C0-C4, aril-alquilo de C0-C4, o(heteroaril)-alquilo de C0-4, cada uno de los cuales está sustituido con 0 a 4 sustituyentes seleccionadosindependientemente de Rx, alcanoilo de C2-C4, mono- y di-(alquil C1-C4)amino(alquilo de C1-C4), mono- y dialquilC1-C4-amino(alcoxi de C1-C4), (heterocicloalquilo de 3 a 7 miembros)alquilo de C0-C4 y XRy; o(ii) se une a R5 para formar, con el nitrógeno al que están unidos R4 y R5, un heterociclo que tiene de 1 a 3 anillos,5 a 7 miembros anulares en cada anillo, en el que el heterociclo está sustituido con 0 a 4 sustituyentesseleccionados independientemente de Rx, oxo y W-Z;R5 es:(i) hidrógeno;(ii) alquilo de C1-C6, alquenilo de C2-C6, alquinilo de C2-C6, (carbociclo C3-C7)-alquilo de C0-C4, cada uno de loscuales está sustituido con 0 a 3 sustituyentes seleccionados independientemente de halógeno, hidroxi, amino,ciano, alquilo de C1-C4, alcoxi de C1-C4, metilamino, dimetilamino, trifluorometilo y trifluorometoxi; o(iii) está unido a R4 para formar, con el nitrógeno al que están unidos R5 y R4, un heterociclo que tiene de 1 a 3anillos, 5 a 7 miembros anulares en cada anillo, en el que el heterociclo está sustituido con 0 a 4 sustituyentesseleccionados independientemente de Rx, oxo y W-Z;Ar es fenilo mono-, di- o tri-sustituido, naftilo opcionalmente sustituido, o heteroarilo opcionalmente sustituido, en elque Ar es heteroarilo opcionalmente sustituido cuando R2 es -NR4R5;RA, RA' y RB, que pueden ser iguales o diferentes, se seleccionan independientemente en cada caso de: (i) hidrógenoe hidroxi, y (ii) grupos alquilo, grupos cicloalquilo, y grupos (cicloalquil)alquilo, cada uno de los cuales estáopcionalmente sustituido con uno o más sustituyente(s) seleccionado(s) independientemente de oxo, hidroxi,halógeno, ciano, amino, alcoxi de C1-6, -NH(alquilo de C1-6), -N(alquilo de C1-6)(alquilo de C1-6), -NHC(>=O)(alquilode C1-6), -N(alquilo de C1-6)C(>=O)(alquilo de C1-6), -NHS(O)n(alquilo de C1-6), -S(O)n(alquilo de C1-6),-S(O)nNH(alquilo de C1-6), -S(O)nN(alquilo de C1-6)(alquilo de C1-6), y Z;Rx se escoge independientemente, en cada caso, de halógeno, hidroxi, amino, ciano, nitro, -COOH, -C(>=O)NH2,alcoxi C1-C6-carbonilo, mono- y di-(alquil C1-6)aminocarbonilo, alquilo de C1-C6, alquenilo de C2-C6, alquinilo deC2-C6, mono- y di-(alquil C1-C6)amino, alcoxi de C1-C6, hidroxialquilo de C1-C2, haloalquilo de C1-C2, haloalcoxide C1-C2, (cicloalquil C3-C7)-alquilo de C0-C4, y -S(On)alquilo de C1-C6;

18. 发明专利

AU2002232768B2 Benzimidazole and pyridylimidazole derivatives as ligands for GABA receptors 未知
公开(公告)号：AU2002232768B2
公开(公告)日：2007-09-06
申请号：AU2002232768
申请日：2001-12-21
申请人： NEUROGEN CORP , PFIZER
发明人： CAI GUOLIN , YUAN JUN , ALLEN MARTIN PATRICK , LIU NIAN , HONG XIE LING , MITCHELL SCOTT , GUSTAVSON LINDA M , PETERSON JOHN M , SINGH VINOD , ALBAUGH PAMELA , LUKE GEORGE P , GHOSH MANUKA , HUTCHISON ALAN , LI GUIYING , CURRIE KEVIN S , LEE KYUNGAE , MAYNARD GEORGE D , LIRAS SPIROS
IPC分类号： C07D401/14 , A61K31/415 , A61K31/4184 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/435 , A61K31/437 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07D233/20 , C07D233/54 , C07D401/04 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10 , C07D491/113
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.

19. 发明专利

ES2273008T3 DERIVADOS DE IMIDAZOL CON ANILLOS FUSIONADOS SUSTITUIDOS: LIGANDOS DE RECEPTORES GABA SBA/SB. 未知
公开(公告)号：ES2273008T3
公开(公告)日：2007-05-01
申请号：ES03736638
申请日：2003-05-15
申请人： NEUROGEN CORP
发明人： MAYNARD GEORGE D , YUAN JUN , LUKE GEORGE P , CURRIE KEVIN
IPC分类号： C07D471/04 , A61K31/437 , A61P25/00 , G01N33/566
摘要： Compuesto de fórmula o una sal farmacéuticamente aceptable del mismo, donde: R1 representa arilo o heteroarilo de 5 a 10 miembros, cada uno no sustituido o sustituido con 1 a 4 grupos seleccionados independientemente de R5; R2 representa alquilo C1-C8, alquenilo C2-C8, alquinilo C2-C8, cicloalquilo C3-C10 o (cicloalquil C3-C10) alquilo C1-C8, cada uno no sustituido o sustituido con 1 a 3 sustituyentes seleccionados independientemente de R5; o bien: (a) A es CH2 y B es NR3 o CR3R6; o (b) B es CH2 y A es NR3 o CR3R6; R3 se selecciona de entre: (a) hidrógeno, halógeno, nitro y ciano; y (b) grupos de fórmula: en la que: (i) G es un enlace, alquilo C1-C8, -NH-, -N(RB)-, -(RB)N--O-, -C(=O)-, -C(=O)NH-, -C(=O)NRB-, -S(O)m-, -CH2C(=O)-, -S(O)mNH-, -S(O)mNRB-, -NHC(=O)-, -C(=NRB)-, HC=N-, -NRBC(=O)-, -NHS(O)m- o ¿NRBS(O)-; (ii) RA y RB se seleccionan independientemente de entre alquilo C1-C8, alquenilo C2-C8, alquinilo C2-C8 y carbociclos y heterociclos de 3 a 12 miembros, saturados, parcialmenteinsaturados y aromáticos que tienen 1 anillo o 2 fusionados, anillos colgantes y/o espiro, donde cada anillo está no sustituido o sustituido con 1 a 4 sustituyentes seleccionados independientemente de R5; y(iii) m es 0, 1 ó 2; con la condición de que si A o B son NR3, entonces R3 no es halógeno y G no es ¿NH-, -N(RB)-, -O-, -NHC(=O)-, -NRBC(=O)-, -NHS(O)m o ¿NRBS(O)-; R5 se selecciona independientemente cada vez de entre halógeno, hidroxilo, nitro, ciano, amino, alquilo C1-C8, alcoxi C1-C8, mono- y di-(alquil C1-C8) amino, cicloalquilo C3-C10, (cicloalquil C3-C10) alquilo, (cicloalquil C3-C10) alcoxi, heterocicloalquilo C2-C9, alquenilo C2-C8, alquinilo C2-C8, halo alquilo (C1-C8), halo alcoxi (C1-C8), oxo, amino alquilo (C1-C8) y mono- y di- (alquil C1-C8)amino alquilo C1-C8; y R6 es hidrógeno o alquilo C1-C6.

20. 发明专利

AP1503A Benzimidazole and pyridylimidazole derivatives as ligands for GABA receptors 未知
公开(公告)号：AP1503A
公开(公告)日：2005-12-24
申请号：AP2003002818
申请日：2001-12-21
申请人： NEUROGEN CORP , PFIZER
发明人： LI GUIYING , PETERSON JOHN M , ALBAUGH PAMELA , CURRIE KEVIN S , CAL GUOLIN , GUSTAVSON LINDA M , LEE KYUNGAE , HUTCHISON ALAN , SINGH VINOD , MAYNARD GEORGE D , YUAN JUN , LING HONG XIE , GHOSH MANUKA , LIU NIAN , LUKE GEORGE P , MITCHELL SCOTT , LIRAS SPIROS , ALLEN MARTIN PATRICK
IPC分类号： C07D401/14 , A61K31/00 , A61K31/415 , A61K31/4184 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/435 , A61K31/437 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07D233/20 , C07D233/54 , C07D401/04 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10 , C07D491/113
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of formula (1), the invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (cns) diseases, Novel processes for preparing compounds of formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of formula 1 in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABA receptors in tissue sections.

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