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81. 发明专利

PT100347A New cycloalkyl and aza:cycloalkyl-pyrrolo-pyrimidine derivs. - are GABAa brain receptor agonists used for treating and diagnosing anxiety, sleep disorders etc. 未知
公开(公告)号：PT100347A
公开(公告)日：1993-11-30
申请号：PT10034792
申请日：1992-04-03
申请人： NEUROGEN CORP
发明人： THURKAUF ANDREW , HUTCHISON ALAN , SINGH VINOD
IPC分类号： C07D471/00 , C07D487/00
摘要： Cycloalkyl- and azacycloalkyl-pyrrolopyrimidine derivs. of formula (I), and their salts, are new. R1, R2= H or 1-6C alkyl; X= H or OH; W= phenyl, thienyl or pyridyl (all opt. substd. by 1 or 2 of halogen, OH, 1-6C alkyl, amino, mono- and di- (1-6Calkyl)amino, or 1-6C alkoxy); Y= N3, CO, CR6OR5, CR6COR5, CR6COOR5, CR60C0R5, CR5R6, CR6CONR7R8, CR6(CH2)MNR7R8, CR6NR9COOR10, CR6C(OH)R11R11, or a gp. (a); m, n= 0-2; R3= H, 1-6C alkyl, phenyl, pyridyl, phenyl 1-6C alkyl, 1-6C aminoalkyl, mono- or di-(1-6C alkyl)1-6C aminoalkyl, or 1-indamyl, 4-(thio)chromanyl or 1-(1,2,3,4-tetrahydronaphthyl) (all three opt. monosubstd. by halogen, 1-6C alkyl, or 1-6C alkoxy), COR4 or SO2R4. R4= 1-6C alkyl, phenyl, phenyl 1-6C alkyl or phenyl 1-6C alkoxy; R5, R8= H, 1-6C alkyl, phenyl, pyridyl or phenyl 1-6C alkyl; R6, R7= H or 1-6C alkyl; or NR7R8= morpholyl, piperidyl, pyrrolidyl or N-alkylpiperazinyl; R11, R12= 1-6C alkyl, phenyl or phenyl 1-6C alkyl; T= CH2 or O; Z= T, NR14 or CHCONR14; and R9, R10, R13, R14 = as R5.

82. 发明专利

EG24590A Benzimidazole and pyridylimidazole derivative as ligands gabaa receptors 未知
公开(公告)号：EG24590A
公开(公告)日：2009-12-07
申请号：EG20011360
申请日：2001-12-22
申请人： NEUROGEN CORP , PFIZER
发明人： LI GUIYING , PETERSON JOHN M , ALBAUGH PAMELA , CURRIE KEVIN S , CAI GUOLIN , GUSTAVSON LINDA M , LEE KYUNGAE , HUTCHISON ALAN , SINGH VINOD , MAYNARD GEORGE , YUAN JUN , HONG XIE LING , GHOSH MANUKA , LIU NIAN , LUKE GEORGE P , MITCHELL SCOTT , ALLEN MARTIN P , LIRAS SPIROS
IPC分类号： A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/4188 , 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 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/02 , C07D471/04 , C07D471/18 , 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.

83. 发明专利

AT387447T 未知
公开(公告)号：AT387447T
公开(公告)日：2008-03-15
申请号：AT97915905
申请日：1997-03-12
申请人： NEUROGEN CORP
发明人： CHEN PAUL , HUTCHISON ALAN , CAI GUOLIN
IPC分类号： C07D487/04 , A61K31/505 , A61K31/519 , A61P25/22 , C07D401/14 , C07D403/14
摘要： Disclosed are compounds of compounds of the formula: or the pharmaceutically acceptable nontoxic salts thereof wherein: X is oxygen, H2 or sulfur Y is hydrogen, or optionally substituted alkyl, alkenyl, (substituted)arylalkyl, aryl or heteroaryl, or a carbonyl group substituted with alkyl, cycloalkyl, aryl, or amino groups; W is alkyl, arylalkyl or heteroarylalkyl, where each aryl group is optionally substituted with up to two groups; or W is aryl, thienyl, pyridyl or heteroaryl, each of which is optionally substituted; and Z1, Z2, Z3, and Z4 independently represent nitrogen or C-R1 where R1 is hydrogen, halogen, hydroxy, amino, or phenyl or pyridyl optionally mono- or independently disubstituted with halogen, hydroxy, lower alkyl, or lower alkoxy, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.

84. 发明专利

CA2249562C CERTAIN FUSED PYRROLECARBOXAMIDES AS GABA BRAIN RECEPTOR LIGANDS 未知
公开(公告)号：CA2249562C
公开(公告)日：2006-06-13
申请号：CA2249562
申请日：1997-03-20
申请人： NEUROGEN CORP
发明人： LIU GANG , ALBAUGH PAMELA , HUTCHISON ALAN
IPC分类号： C07D209/42 , C07D209/52 , C07D401/12 , C07D409/12 , C07D417/12 , C07D471/04
摘要： Diclosed are compounds of formula (I), or the pharmaceutically acceptable non-toxic salts thereof, wherein W represents substituted or unsubstituted phenyl; T is hydrogen, halogen, hydroxyl, amino or alkyl; X is hydrogen, hydroxy, or lower alkyl; m is 0, 1, or 2; n is 0, 1, or 2; and R3 and R4 represent substituted or unsubstituted organic residues. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

85. 发明专利

DE69735647D1 未知
公开(公告)号：DE69735647D1
公开(公告)日：2006-05-18
申请号：DE69735647
申请日：1997-01-14
申请人： NEUROGEN CORP
发明人： ALBAUGH PAMELA , LIU GANG , SHAW KENNETH , HUTCHISON ALAN
IPC分类号： C07D209/42 , A61K31/00 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/535 , A61K31/5375 , A61K31/538 , A61P25/00 , A61P25/04 , A61P43/00 , C07D209/52 , C07D401/12 , C07D403/10 , C07D405/12 , C07D413/12
摘要： The present invention encompasses structures of the formula I: or the pharmaceutically acceptable non-toxic salts thereof wherein: G represents where Q is aryl substituents optionally mono or disubstituted with hydroxy or halogen; T is halogen, hydrogen, hydroxyl, amino or alkoxy having 1-6 carbon atoms; W is oxygen, nitrogen, sulfur, or optionally substituted methylene; X is hydrogen, hydroxyl, or alkyl; Z is an organic or inorganic substituent optionally forming a ring with subtituents on Q; independently represent optionally substituted carbon chains; wherein k, m, and n are independently 0, or an integer of from 1-3 R3, R4, R5, and R6 are the same or different and represent organic or inorganic substituents. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

86. 发明专利

DE60114227T2 未知
公开(公告)号：DE60114227T2
公开(公告)日：2006-04-20
申请号：DE60114227
申请日：2001-08-16
申请人： NEUROGEN CORP
发明人： CAI GUOLIN , ALBAUGH PAMELA , YUAN JUN , CURRIE S , HUTCHISON ALAN
IPC分类号： C07D401/06 , A61K31/4365 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/551 , A61P9/00 , A61P9/10 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D215/52 , C07D401/12 , C07D401/14 , C07D409/04 , C07D409/14 , C07D471/04 , C07D495/04 , C07D521/00

87. 发明专利

OA12015A Fused pyrrolecarboxamides: gaba brain receptor ligands. 未知
公开(公告)号：OA12015A
公开(公告)日：2006-04-19
申请号：OA1200200063
申请日：2000-08-30
申请人： NEUROGEN CORP
发明人： ALBAUGH PAMELA , HUTCHISON ALAN , SHAW KENNETH
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.

88. 发明专利

DE60115092D1 未知
公开(公告)号：DE60115092D1
公开(公告)日：2005-12-22
申请号：DE60115092
申请日：2001-12-11
申请人： NEUROGEN CORP , PFIZER
发明人： BAKTHAVATCHALAM RAJAGOPAL , BLUM A , BRIELMANN L , DARROW WILLIAM , DE LOMBAERT STEPHANE , HUTCHISON ALAN , TRAN JENNIFER , ZHENG XIAOZHANG , ELLIOTT LOUIS , HAMMOND MARLYS
IPC分类号： C07D491/107 , A61K31/438 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K31/506 , A61K31/517 , A61K31/519 , A61K51/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P25/00 , A61P25/18 , A61P25/24 , A61P43/00 , C07D487/04 , C07D487/10 , C07D491/10 , C07D519/00
摘要： Substituted spiro[isobenzofuran-1,4'-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4'-piperidines capable of modulating NPY5 receptor activity are provided. Such compounds may be used to modulate ligand binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders (e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.

89. 发明专利

BR0116385A 未知
公开(公告)号：BR0116385A
公开(公告)日：2005-12-13
申请号：BR0116385
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 , CAI GUOLIN , GUSTAVSON LINDA M , LEE YYUNGAE , HUTCHISON ALAN , SINGH VINOD , MAYNARD GEORGE D , YUAN JUN , XIE LINGHONG , GHOSH MANUKA , LIU NIAN , LUKE GEORGE P , MITCHELL SCOTT , ALLEN MARTIN PATRICK , LIRAS SPIRO
IPC分类号： 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 , C07D401/14 , 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.

90. 发明专利

TNSN97158A1 CERTAINS PYRROLECARBOXANILIDE FONDUS ; UNE NOUVELLE CLASSE DE LIGANDS RECEPTEURS DU CERVEAU (ACIDE GAMMA -AMINOBUTYRIQUE). 未知
公开(公告)号：TNSN97158A1
公开(公告)日：2005-03-15
申请号：TNSN97158
申请日：1997-09-19
申请人： NEUROGEN CORP
发明人： ALBAUGH PAMELA , HUTCHISON ALAN
IPC分类号： C07D209/42 , C07D401/12 , C07D409/12 , C07D471/04
摘要： L'INVENTION ACTUELLE ENGLOBE LES STRUCTURE DE LA FORMUEL I OU LES SELS NON-TOXIQUES ACCEPTABLES PHARMACEUTIQUEMENT EN DECOULANT...... OU W REPRESENTE DU PHENYLE SUBSTITUE OU NON-SUBSTITUE ; X EST DE L'HYDROGENE, HYDROXY OU ALKYLE LEGER ; T EST DE L'HYDROGENE, HALOGENE, HYDROXY, NITRO, AMINO OU ALKYLE ; R3 EST DE L'HYDROGENE OU UN GROUPE ORGANIQUE ; R4 EST DE L'HYDROGENE OU UN SUBSTITUANT ORGANIQUE SUBSTITUE OU NON ; R5 ET R6 REPRESENTENT DES SUBSTITUANTS ORGANIQUES ET INORGANIQUES ; ET n EST 1,2, 3 ET 4 DONT LES COMPOSES SONT DES AGONISTES, ANTAGONISTES OU AGONISTES INVERSES TRES SELECTIFS POUR LES RECEPTEURS DU CERVEAU GABAa OU DES PRODOGUES D'AGONISTES, D'ANTAGONISTES OU D'AGONISTES INVERSES POUR LES RECEPTEURS DU CERVEAU GABAa. CES COMPOSES SONT UTILES POUR LE DIAGNOSTIC ET LE TRAITEMENT DE L'ANXIETE, DES TROUBLES DU SOMMEIL ET EPILEPTIQUE, DES SURDOSES DE DROGUES AU BENZODIAZEPINE ET POUR AMELIORER LA MEMOIRE.

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