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81. 发明专利

ECSP003641A PIRROLCARBOZAMIDAS FUSIONADAS; UNA NUEVA CLASE DE LIGANDOS DE RECEPTORES CEREBRALES DE GABA 未知
公开(公告)号：ECSP003641A
公开(公告)日：2002-03-25
申请号：ECSP003641
申请日：2000-08-31
申请人： NEUROGEN CORP
发明人： ALBAUGH PAMELA A , HUTCHISON ALAN , SHAW KENNETH
IPC分类号： A61K20060101 , C07D20060101 , C07D207/00
摘要： Se trata de compuestos de pirrolcarboxamida sustituidos. Estos compuestos son agonistas, antagonistas o agonistas inversos altamente selectivos de los recptores cerebrales GABAa o prodrogas de los agonistas, antagonistas o agonistas inversos de los receptores cerebrales GABA. Por lo tanto, son útiles en el diagnóstico y tratamiento de ansiedad,m depresión, demencia causada por la enfermedad de Alzheimer, transtonos del sueño y convulsivos, sobredosis, con benzodiazepinas y para mejorar la memoria. También existen compuestos farmacéuticos, incluidos compuestos farmacéuticos envasados. Los compuestos del invento también son titiles como pruebas para la localización de receptores GABA en muestra de tejidos.

82. 发明专利

NO20020948L 未知
公开(公告)号：NO20020948L
公开(公告)日：2002-02-28
申请号：NO20020948
申请日：2002-02-27
申请人： NEUROGEN CORP
发明人： ALBAUGH PAMELA , SHAW KENNETH , HUTCHISON ALAN
IPC分类号： G01N33/566 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/407 , A61K31/4178 , A61K31/4196 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/496 , A61K31/501 , A61K31/5377 , A61K31/538 , A61K51/04 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D209/42 , C07D209/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08
摘要： Substituted pyrrolecarboxamide compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABA A brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABA A brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Alzheimer's dementia, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABA A receptors in tissue samples.

83. 发明专利

CA2415606A1 CAPSAICIN RECEPTOR LIGANDS 未知
公开(公告)号：CA2415606A1
公开(公告)日：2002-01-31
申请号：CA2415606
申请日：2001-07-20
申请人： NEUROGEN CORP
发明人： BAKTHAVATCHALAM RAJAGOPAL , HODGETTS KEVIN J , KRAUSE JAMES E , DESIMONE ROBERT W , HUTCHISON ALAN , WHITE GEOFFREY G
IPC分类号： A61K31/496 , A61K31/497 , A61P11/08 , A61P13/02 , A61P17/02 , A61P19/02 , A61P25/02 , A61P25/04 , A61P25/06 , A61P27/02 , A61P29/00 , A61P43/00 , C07D213/74 , C07D213/75 , C07D217/22 , C07D241/20 , C07D295/194 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/12 , C07D405/14 , C07D407/14 , C07D417/12 , C07D417/14 , C07D295/192 , C07D295/21 , C07D295/215 , A61K31/44 , A61K31/4402 , A61K31/444 , A61K31/4725 , A61K31/495
摘要： Disclosed are diaryl piperazines and related compounds. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acu te pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided . Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor bindin g and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.

84. 发明专利

CZ288027B6 Pyrrolecarboxamides 未知
公开(公告)号：CZ288027B6
公开(公告)日：2001-04-11
申请号：CZ112996
申请日：1994-10-26
申请人： NEUROGEN CORP
发明人： HUTCHISON ALAN , ALBAUGH PAMELA
IPC分类号： C07D401/12 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/4375 , A61K31/4439 , A61K31/4709 , A61K31/55 , A61P25/00 , A61P25/08 , A61P25/20 , A61P39/02 , A61P43/00 , C07D209/08 , C07D209/42 , C07D209/52 , C07D307/84 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D471/04 , C07D471/12 , A61K31/44
摘要： In the present invention there are disclosed pyrrolecarboxamides of the general formula I, in which T represents a halogen, hydrogen, OH, NHi2 or alkyl containing 1 to 6 carbon atoms; X represents hydrogen, OH or alkyl having 1 to 6 carbon atoms; W represents an optionally substituted phenyl, 2- or 3-thienyl, 2-, 3- or 4-pyridyl or 6-quinolyl; and the ring designated by the letter c represents the group of the general formula i or ii, wherein Y represents C-Ri4; Z represents C(Ri8)(Ri9); n is 2 or 3; Ri3 represents hydrogen H, phenyl, 2-, 3- or 4-pyridyl, alkyl containing 1 to 6 carbon atoms, phenylalkyl or 2-, 3- or 4-pyridylalkyl having each 1 to 6 carbon atoms in the alkyl moiety; Ri4 represents a halogen or CFi3, -ORi10, -CORi10, -COi2Ri10, -OCORi10, or -Ri10, wherein Ri10, represents hydrogen, phenyl, 2-, 3- or 4-pyridyl, alkyl having 1 to 6 carbon atoms or phenylalkyl or 2-, 3- or 4-pyridylalkyl having each 1 to 6 carbon atoms in the alkyl moiety, or -CONRi11Ri12 or -(CHi2)imNRi11Ri12, wherein m is 0, 1 or 2; Ri11 represents hydrogen or alkyl with 1 to 6 C; and Ri12 represents hydrogen, phenyl, 2-, 3- or 4-pyridyl, alkyl with 1 to 6 C or phenylalkyl or 2-, 3- or 4-pyridylalkyl having each 1 to 6 carbon atoms in the alkyl moiety, or NRi11Ri12 forms morpholinyl, piperidyl, pyrrolidinyl and N-alkylpiperazinyl; Ri5 and Ri6 represent each hydrogen, a halogen, alkyl with 1 to 6 carbon atoms or alkoxy containing 1 to 6 carbon atoms; Ri8 represents hydrogen or alkyl having 1 to 6 carbon atoms; and Ri9 represents -CORi13, -COi2Ri13 or Ri13, wherein Ri13 represents hydrogen, phenyl, 2-, 3- or 4-pyridyl, alkyl containing 1 to 6 carbon atoms or phenylalkyl or 2-, 3- or 4-pyridylalkyl having each 1 to 6 carbon atoms in the alkyl moiety, or -CONRi14Ri15 or -(CHi2)ikNRi14Ri15, wherein k is 0, 1 or 2, Ri14 represents hydrogen or alkyl containing 1 to 6 carbon atoms; and Ri15 represents hydrogen, phenyl, 2-, 3- or 4-pyridyl, alkyl containing 1 to 6 carbon atoms or phenylalkyl or 2-, 3- or 4-pyridylalkyl having each 1 to 6 carbon atoms in the alkyl moiety, or NRi14Ri15 forms morpholinyl, piperidyl, pyrrolidinyl and N-alkylpiperazinyl; and pharmaceutically acceptable non-toxic salts thereof. The above-defined compounds can be used for treating anxiety, somnipathy, paroxysms and overdose with benzodiazepine medicaments.

85. 发明专利

AU729634B2 Certain fused pyrrolecarboxanilides: A new class of GABA brain receptor ligands 未知
公开(公告)号：AU729634B2
公开(公告)日：2001-02-08
申请号：AU2379999
申请日：1999-04-16
申请人： NEUROGEN CORP
发明人： ALBAUGH PAMELA , HUTCHISON ALAN
IPC分类号： C07D209/42 , C07D405/12 , C07D413/04 , C07D471/04

86. 发明专利

AU4038600A 4-substituted quinoline derivatives as nk-3 and/or gaba(a) receptor ligands 未知
公开(公告)号：AU4038600A
公开(公告)日：2000-10-16
申请号：AU4038600
申请日：2000-03-28
申请人： NEUROGEN CORP
发明人： YUAN JUN , MAYNARD GEORGE D , HUTCHISON ALAN , RACHWAL STANISLAW
IPC分类号： G01N33/50 , A61K31/4709 , A61K31/5377 , A61P9/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D401/04 , C07D401/14 , C07D413/04 , C07D487/04 , G01N33/15 , G01N33/566 , G01N33/94 , A61K31/47

87. 发明专利

CA2369553A1 N-BENZIMIDAZOLYLMETHYL AND N-INDOLYLMETHYL-BENZAMIDES AND THEIR USE AS CRF MODULATORS 未知
公开(公告)号：CA2369553A1
公开(公告)日：2000-10-12
申请号：CA2369553
申请日：2000-03-31
申请人： NEUROGEN CORP
发明人： HUTCHISON ALAN , YOON TAEYOUNG , HORVATH RAYMOND F , GE PING
IPC分类号： A61K31/4045 , A61K31/4184 , A61P3/04 , A61P7/12 , A61P25/00 , A61P25/22 , A61P25/24 , C07D209/14 , C07D235/10 , C07D235/14 , G01N33/50
摘要： Disclosed are compounds of formula (I); or the pharmaceutically acceptable n on- toxic salts thereof wherein; A is N or CH; R1 and R2 represents hydrogen or lower alkyl; G, R3, R4, R5, R6, R7 and R8 are variables defined herein. Thes e compounds are modulators of CRF receptors and are therefore useful for treating affective disorders, anxiety, depression, eating disorders, and stress disorders in humans and other animals. Methods of treatment of such disorders as well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods o f using the compounds in receptor localization studies are given.

88. 发明专利

CO4900049A1 CIERTAS PIRROLACARBOXAMIDAS FUSIONADAS; UNA NUEVA CLASE DE LIGANDOS RECEPTORES CEREBRALES DE GABA 未知
公开(公告)号：CO4900049A1
公开(公告)日：2000-03-27
申请号：CO97054328
申请日：1997-09-17
申请人： NEUROGEN CORP
发明人： ALBAUGH PAMELA , GANG LIU , HUTCHISON ALAN
IPC分类号： A61K31/16 , A61K31/40
摘要： Un compuesto de la fórmula:o sales no tóxicas farmacéuticamente aceptables de la misma en donde: W es arilo o heteroarilo, cada uno de los cuales es sustituido opcionalmente con hasta 5 grupos seleccionados independientemente de halógeno, ciano, hidroxi, alquilo o cicloalquilo con 3 a 7 átomos de carbono, amino o mono- o dialquilamino en donde cada alquilo es independientemente un alquilo menor o un cicloalquilo que tiene 3 a 7 átomos de carbono, alcoxi o cicloalquilalcoxi con 3 a 7 átomos de carbono, o NR1 COR2 , COR2 , CONR1 R2 o CO2 R2 donde R1 y R2 son iguales o diferentes y representan hidrógeno o alqui-lo o cicloalquilo con 3 a 6 átomos de carbono; y T es halógeno, hidrógeno, hidroxilo, amino o alcoxi X es hidrógeno, hidroxilo o alquilo; m es 0, 1, ó 2; n es 0, 1, ó 2; y R3 y R4 son iguales o diferentes y son seleccionados de hidrógenos, alquilo, COR5 o CO2 R5 donde R5 es alquilo o cicloalquilo que tiene de 3 a 7 átomos de carbono, CONR6 R7 , donde R6 y R7 son seleccionados independientemente de hidrógeno, alquilo, cicloalquilo que tiene de 3 a 7 átomos de carbono, fenilo, 2-, 3-, o 4-piridilo, o NR6 R7 forman un grupo heterocíclico que es morfolinilo, pi-peridinilo, pirrolidinilo o N-alquilpiperazinilo; o R3 -R4 juntos representan una parte cíclica que tiene de 3 a 7 átomos de carbono. Un compuesto de la fórmula: en donde R3 y R4 son iguales o diferentes y son seleccionados de hidrógeno, alquilo, COR5 o CO2 R5 donde R5 es alquilo o cicloalquilo que tiene de 3 a 7 átomos de carbono, CONR6 R7 , donde R6 y R7 son seleccionados independientemente de hidrógeno, alquilo, cicloalquilo que tiene de 3 a 7 átomos de carbono, fenilo, 2-, 3-, o 4-piridilo, o NR6 R7 , forman un grupo heterocíclico que es morfolinilo, piperidinilo, pirrolidinilo o N-alquilpiperazinilo; o R3 y R4 juntos representan una parte cíclica que tiene de 3 a 7 átomos de carbono; y...

89. 发明专利

CO4890841A1 CIERTOS DERIVADOS DE BENCILAMINA AMIDO- Y AMINOSUSTITUIDOS : UNA NUEVA CLASE DE LIGANDOS ESPECIFICOS DEL NEUROPEPTIDO Y 1 未知
公开(公告)号：CO4890841A1
公开(公告)日：2000-02-28
申请号：CO97041974
申请日：1997-07-23
申请人： NEUROGEN CORP
发明人： BLUM CHARLES A , DESIMONE ROBERT , HUTCHISON ALAN , PETERSON JOHN M
IPC分类号： C07D295/12 , A61K31/135 , A61K31/165 , A61K31/415 , A61K31/416 , A61K31/42 , A61K31/444 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/502 , A61P3/00 , A61P9/04 , A61P9/12 , A61P43/00 , C07D209/42 , C07D211/76 , C07D213/81 , C07D213/82 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D231/14 , C07D231/56 , C07D237/28 , C07D261/20 , C07D295/02 , C07D295/135 , C07D295/14 , C07D295/155 , C07D333/24 , C07D333/40
摘要： Un compuesto de la fórmula:en la cual uno de X1 X2 y X3 esy el resto de los miembros del grupo X1 , X2 y X3 son hidrógeno; yQ = nitrógeno u oxígeno;D está ausente cuando Q es oxígeno y cuando Q es nitrógeno, D es hidrógeno, alquilo inferior de cadena recta o ramificada con 1 a 6 átomos de carbono, o puede estar unido con G para formar un anillo; E = O o H2 ; o y r son 0 ó 1; G es alquilo inferior de cadena recta o ramificada con 1 a 6 átomos de carbono, arilo, arilo sustituido con halógeno, alquilo inferior de cadena recta o ramificada con 1 a 6 átomos de carbono, heteroarilo seleccionado entre el grupo que consiste en 2-, 3-, o 4-piridilo, 2-pirazilo, 2- ó 3-tienilo, 2-pirazinilo, 2-, 3-, o 4-quinolilo, 1-, 3-, ó 4-isoquinolilo, 2-quinoxalilo, 3-, ó 4-cinolilo, heteroarilo sustituido con halógeno, hidroxi, alquilo inferior de cadena recta o ramificada con 1 a 6 átomos de carbono, alcoxi inferior de cadena recta o ramificada con 1 a 6 átomos de carbono; o está unido a D para formar un anillo; Ar es un grupo arilo preferentemente seleccionado entre el grupo que consiste en fenilo, 2-, 3-, o 4-piridilo, 2- ó 3-tienilo, 4- ó 5-pirimidilo, cada uno de los cuales es optativamente mono- o disustituido con halógeno, hidroxi, o alquilo inferior de cadena recta o ramificada con 1 a 6 átomos de carbono; B es azufre, oxígeno, N(R5 ) o C(R5 )(R6 );n es 1, 2 ó 3; m es 2, 3 ó 4;...

90. 发明专利

DE69603240T2 未知
公开(公告)号：DE69603240T2
公开(公告)日：2000-01-05
申请号：DE69603240
申请日：1996-05-09
申请人： NEUROGEN CORP
发明人： YUAN JUN , HUTCHISON ALAN
IPC分类号： A61K31/435 , A61K31/505 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D471/04 , C07D487/04
摘要： The invention relates to deazapurine compounds of the formulawherein Ar, R1, R2, R3, R4, R5, X are as defined herein; these compounds selectively bind to CRF receptors and are useful in the treatment of stress related disorders.

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