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51. 发明申请

WO2002094799A2 MELANIN CONCENTRATING HORMONE RECEPTOR LIGANDS: SUBSTITUTED 1-BENZYL-4-ARYL PIPERAZINE ANALOGUES 审中-公开
标题翻译：梅拉宁浓缩激素受体配体：取代的1-苄氧基-4-芳基哌嗪类似物
公开(公告)号：WO2002094799A2
公开(公告)日：2002-11-28
申请号：PCT/US2002/015979
申请日：2002-05-21
申请人： NEUROGEN CORPORATION , HUTCHISON, Alan , PETERSON, John , DOLLER, Dario , GUSTAVSON, Linda, E. , CALDWELL, Timothy , YOON, Taeyoung , PRINGLE, Wallace , BAKTHAVATCHALAM, Rajagopal , SHEN, Yiping , STEENSTRA, Cheryl , YIN, Helen , DE SIMONE, Robert , HE, Xiao-shu
发明人： HUTCHISON, Alan , PETERSON, John , DOLLER, Dario , GUSTAVSON, Linda, E. , CALDWELL, Timothy , YOON, Taeyoung , PRINGLE, Wallace , BAKTHAVATCHALAM, Rajagopal , SHEN, Yiping , STEENSTRA, Cheryl , YIN, Helen , DE SIMONE, Robert , HE, Xiao-shu
IPC分类号： C07D295/00
CPC分类号： C07D513/04 , C07D209/86 , C07D211/52 , C07D213/64 , C07D213/74 , C07D215/12 , C07D215/20 , C07D243/08 , C07D295/096 , C07D295/108 , C07D311/18 , C07D317/58 , C07D401/12 , C07D471/04 , C07D487/04 , C07D487/08
摘要： Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptir activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
摘要翻译：提供能够调节MCH受体活性的黑色素浓缩激素受体配体（特别是1-苄基-4-芳基哌嗪，1-苄基-4-芳基哌啶和相关化合物）。这样的配体可用于在体内或体外调节MCH与MCH受体的结合，并且特别可用于治疗人，驯养的伴侣动物和家畜中的各种代谢，喂养和性障碍。提供了用于治疗这种病症的药物组合物和方法，以及使用这些配体检测MCH受体的方法（例如，受体定位研究）。

52. 发明申请

WO1998045295A1 CERTAIN PYRROLOPYRIDINE DERIVATIVES; NOVEL CRF1 SPECIFIC LIGANDS 审中-公开
标题翻译：某些吡咯啉衍生物; 新型CRF1特殊配置
公开(公告)号：WO1998045295A1
公开(公告)日：1998-10-15
申请号：PCT/US1997005979
申请日：1997-04-10
申请人： NEUROGEN CORPORATION , HORVATH, Raymond, F. , HUTCHINSON, Alan
发明人： NEUROGEN CORPORATION
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D471/14
摘要： Disclosed are compounds of formula (I) wherein Ar is optionally substituted aryl or heteroaryl; R1 is hydrogen or alkyl; R7 is hydrogen or alkyl; R2 is hydrogen, halogen, alkyl or alkoxy; or R1 and R2 taken together with the ring to which they are attached for a 5-9 membered saturated or aromatic ring optionally having a hetero atom selected from oxygen, sulfur or nitrogen; R3 and R4 are independently hydrogen, alkyl, cycloalkyl, aryl or heteroaryl groups; or R3 and R4 together with the nitrogen atom to which they are attached form a 5-8 membered ring; and R5 is hydrogen, halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, or straight or branched chain lower alkoxy or thioalkoxy having 1-6 carbon atoms, which compounds are highly selective partial agonists or antagonists at human Corticotropin-Releasing Factor 1 (CRF1) receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.
摘要翻译：公开了式（I）的化合物，其中Ar是任选取代的芳基或杂芳基; R1是氢或烷基; R7是氢或烷基; R2是氢，卤素，烷基或烷氧基; 或R 1和R 2与它们所连接的环一起连接5-9元饱和或芳环，任选具有选自氧，硫或氮的杂原子; R3和R4独立地是氢，烷基，环烷基，芳基或杂芳基; 或R 3和R 4与它们所连接的氮原子一起形成5-8元环; R5为氢，卤素，具有1-6个碳原子的直链或支链低级烷基，或具有1-6个碳原子的直链或支链低级烷氧基或硫代烷氧基，该化合物是人促皮素激素释放的高度选择性部分激动剂或拮抗剂因子1（CRF1）受体，可用于治疗压力相关疾病如创伤后应激障碍（PTSD）以及抑郁，头痛和焦虑症的诊断和治疗。

53. 发明申请

WO1998029413A1 3-ARYL SUBSTITUTED PYRAZOLO[4,3-d]PYRIMIDINE DERIVATIVES; CORTICOTROPIN-RELEASING FACTOR RECEPTOR (CRF1) SPECIFIC LIGANDS 审中-公开
标题翻译： 3-ARYL取代的吡唑并[4,3-d]吡啶衍生物; CORTICOTROPIN释放因子受体（CRF1）特异性配体
公开(公告)号：WO1998029413A1
公开(公告)日：1998-07-09
申请号：PCT/US1997024172
申请日：1997-12-23
申请人： NEUROGEN CORPORATION , YUAN, Jun
发明人： NEUROGEN CORPORATION
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： This invention encompasses compounds of formula (I), wherein Ar represents a mono-, di- or trisubstituted aryl group where at least one position on Ar ortho to the point of attachment to the pyrazole ring is substituted; and R1 represents lower alkyl; R2 is hydrogen or lower alkyl; and R3 and R4 independently represent organic and inorganic substituents, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.
摘要翻译：本发明包括式（I）的化合物，其中Ar表示一个，二或三取代的芳基，其中与吡唑环的连接点上Ar邻位的至少一个位置被取代; 并且R 1表示低级烷基; R2是氢或低级烷基; R3和R4独立地表示有机和无机取代基，该化合物是人CRF1受体的高选择性部分激动剂或拮抗剂，可用于诊断和治疗应激相关疾病如创伤后应激障碍（PTSD）以及抑郁症，头痛和焦虑。

54. 发明申请

WO1998003492A1 CERTAIN SUBSTITUTED BENZYLAMINE DERIVATIVES; A NEW CLASS OF NEUROPEPTIDE Y1 SPECIFIC LIGANDS 审中-公开
标题翻译：某些取代的苯甲酰胺衍生物; 新一代神经元Y1特定配偶
公开(公告)号：WO1998003492A1
公开(公告)日：1998-01-29
申请号：PCT/US1997012614
申请日：1997-07-18
申请人： NEUROGEN CORPORATION
发明人： NEUROGEN CORPORATION , BLUM, Charles, A. , HUTCHISON, Alan , PETERSON, John, M.
IPC分类号： C07D295/18
CPC分类号： C07D213/75 , C07C2601/14 , C07D215/38 , C07D233/38 , C07D295/135 , C07D295/155
摘要： This invention encompasses compounds of formula (I) and the pharmaceutically acceptable salts thereof wherein X1, X2, X3 represent organic or inorganic substituents, n is 1, 2, or 3, m is 2, 3, or 4, R1-R4 are hydrogen or organic substituents, and B is nitrogen, carbon, sulfur or oxygen, useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to mammalian Neuropeptide Y1 receptors.
摘要翻译：本发明包括式（I）化合物及其可药用盐，其中X 1，X 2，X 3表示有机或无机取代基，n为1,2或3，m为2,3或4，R 1 -R 4为氢或有机取代基，B是氮，碳，硫或氧，可用于诊断和治疗哺乳障碍如肥胖症和贪食症以及心血管疾病如原发性高血压和充血性心力衰竭，因为这些化合物与哺乳动物神经肽的结合 Y1受体。

55. 发明申请

WO1998002433A1 CERTAIN FUSED PYRROLECARBOXAMIDES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS 审中-公开
标题翻译：某些熔融的吡咯烷新类型的GABA脑受体配体
公开(公告)号：WO1998002433A1
公开(公告)日：1998-01-22
申请号：PCT/US1997007830
申请日：1997-05-09
申请人： NEUROGEN CORPORATION , ALBAUGH, Pamela , LIU, Gang , HUTCHISON, Alan
发明人： NEUROGEN CORPORATION
IPC分类号： C07D401/12
CPC分类号： C07D209/08 , A61K31/404 , C07D209/42 , C07D209/52 , C07D307/84 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D417/12 , C07D471/04
摘要： The present invention encompasses structures of formula (I) or the pharmaceutically acceptable non-toxic salts thereof wherein (a) represents (i) or (ii) or (iii) or (iv) wherein W represents substituted or unsubstituted heteroaryl; X is hydrogen, hydroxy or lower alkyl; T is hydrogen, halogen, hydroxy, nitro, amino or alkyl; R3 is hydrogen or an organic group; R4 is hydrogen or substituted or unsubstituted organic substituent; R5 and R6 represent organic, and inorganic substituents; and n is 1, 2, 3, or 4, which 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.
摘要翻译：本发明包括式（I）的结构或其药学上可接受的无毒盐，其中（a）表示（i）或（ii）或（iii）或（iv）其中W表示取代或未取代的杂芳基; X为氢，羟基或低级烷基; T是氢，卤素，羟基，硝基，氨基或烷基; R3是氢或有机基团; R4是氢或取代或未取代的有机取代基; R5和R6代表有机和无机取代基; 和n为1,2,3或4，这些化合物是用于GABAa脑受体的高选择性激动剂，拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。这些化合物可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物过量并用于记忆增强。

56. 发明申请

WO1997038989A1 N-AMINOALKYL-2-ANTHRAQUINONECARBOXAMIDES; NEW DOPAMINE RECEPTOR SUBTYPE SPECIFIC LIGANDS 审中-公开
标题翻译：的N-氨基烷基-2- ANTHRAQUINONECARBOXAMIDES; 新型多巴胺受体亚型特异性配体
公开(公告)号：WO1997038989A1
公开(公告)日：1997-10-23
申请号：PCT/US1997006162
申请日：1997-04-16
申请人： NEUROGEN CORPORATION , CHEN, Xi , WASLEY, Jan, W., F.
发明人： NEUROGEN CORPORATION
IPC分类号： C07D295/12
CPC分类号： C07D295/13 , C07D211/70 , C07D215/40
摘要： Disclosed are compounds of formula (I) or the pharmaceutically acceptable acid addition salts thereof wherein: R1, R2, R3, R4, R5, R6, and R7 are the same or different and represent hydrogen, halogen, alkyl, alkoxy, hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy; -O2CR', -NHCOR', -COR', -SOmR', where R' is C1-C6alkyl and wherein m is 0, 1 or 2; or R1, R2, R3, R4, R5, R6, and R7 independently represent -CONR'R'', or -NR'R'' where R' and R'' independently represent hydrogen or C1-C6alkyl; R8 is hydrogen or lower alkyl; X represents an optionally substituted alkylene group; and Y represents a mono-, di- or trisubstituted cyclic amino group, which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.
摘要翻译：公开了式（I）化合物或其药学上可接受的酸加成盐，其中：R1，R2，R3，R4，R5，R6和R7相同或不同，代表氢，卤素，烷基，烷氧基，羟基，氰基，硝基，三氟甲基，三氟甲氧基; -O2CR'， - NHCOR'， - CON'，-SOmR'，其中R'是C1-C6烷基，其中m是0,1或2; 或R 1，R 2，R 3，R 4，R 5，R 6和R 7独立地表示-CONR'R“或-NR'R”，其中R'和R“独立地表示氢或C 1 -C 6烷基; R8是氢或低级烷基; X表示任选取代的亚烷基; 并且Y代表单取代或二取代或三取代的环状氨基，该化合物可用于治疗情感障碍如精神分裂症，抑郁症，阿尔茨海默氏病，运动障碍如帕金森综合征和肌张力障碍，以及其他对多巴胺能阻滞作用的疾病例如药物滥用和强迫症。此外，本发明的化合物可用于治疗与使用常规精神抑制剂相关的锥体束外副作用。

57. 发明申请

WO1997034870A1 CERTAIN FUSED PYRROLECARBOXAMIDES AS GABA BRAIN RECEPTOR LIGANDS 审中-公开
标题翻译：某些熔化的吡咯类抗生素作为GABA脑受体配体
公开(公告)号：WO1997034870A1
公开(公告)日：1997-09-25
申请号：PCT/US1997004623
申请日：1997-03-20
申请人： NEUROGEN CORPORATION , ALBAUGH, Pamela , LIU, Gang , HUTCHISON, Alan
发明人： NEUROGEN CORPORATION
IPC分类号： C07D209/42
CPC分类号： C07D401/12 , C07D209/42 , C07D409/12 , 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.
摘要翻译：被称为式（I）化合物或其药学上可接受的无毒盐，其中W表示取代或未取代的苯基; T是氢，卤素，羟基，氨基或烷基; X是氢，羟基或低级烷基; m为0,1或2; n为0,1或2; 并且R 3和R 4表示取代或未取代的有机残基。这些化合物是GABAa脑受体的高选择性激动剂，拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。这些化合物可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物过量并用于记忆增强。

58. 发明申请

WO1996039404A1 NOVEL SUBSTITUTED ARYL AND CYCLOALKYL IMIDAZOLONES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS 审中-公开
标题翻译：新型取代的芳基和环烷基咪唑烷酮; 新类型的GABA脑受体配体
公开(公告)号：WO1996039404A1
公开(公告)日：1996-12-12
申请号：PCT/US1996010214
申请日：1996-06-04
申请人： NEUROGEN CORPORATION , DESIMONE, Robert, W. , BLUM, Charles, A.
发明人： NEUROGEN CORPORATION
IPC分类号： C07D413/04
CPC分类号： C07D413/04 , C07D417/04
摘要： Disclosed are compounds of formula (I) wherein: T is NH, O, or S; X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide; the W ring is an optionally substituted aryl or heteroaryl group; and (a) represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring. 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 compouns are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
摘要翻译：公开了式（I）的化合物，其中：T是NH，O或S; X是氢，羟基，低级烷基或任意取代的酰胺; W环是任选取代的芳基或杂芳基; 和（a）表示任选取代的苯并基或任选取代的5,6,7或8元环。这些化合物是GABAa脑受体的高选择性激动剂，拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。这些配方可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物服用过量药物和提高记忆力。

59. 发明申请

WO1996032390A1 PREPARATION OF CHIRAL 5-AMINOCARBONYL-5H-DIBENZO-[a,d]CYCLOHEPTEN-5,10-IMINES BY OPTICAL RESOLUTION 审中-公开
标题翻译：通过光解决方案制备正丙基5-氨基羰基-5H-二苯并[a，d]环己基-5,10-咪唑
公开(公告)号：WO1996032390A1
公开(公告)日：1996-10-17
申请号：PCT/US1996004906
申请日：1996-04-10
申请人： NEUROGEN CORPORATION , THE GOVERNMENT OF THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , JONES, Tappey, H. , RICE, Kenner, C.
发明人： NEUROGEN CORPORATION , THE GOVERNMENT OF THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
IPC分类号： C07D451/02
CPC分类号： C07D451/00
摘要： Disclosed are processes for resolving a racemic mixture of 5-aminocarbonyl-5H-dibenzo[a,d]cyclohepten-5,10-imines into component enantiomers comprising recrystallization of diasteriomeric tartrate salts.
摘要翻译：公开了将5-氨基羰基-5H-二苯并[a，d]环庚烯-5,10-亚胺的外消旋混合物分解成包含非对映体酒石酸盐的重结晶的组分对映异构体的方法。

60. 发明申请

WO1996016058A1 AMINOMETHYL ARYL COMPOUNDS; DOPAMINE RECEPTOR SUBTYPE SELECTIVE LIGANDS 审中-公开
标题翻译：氨基甲醛化合物多巴胺受体亚型选择性配体
公开(公告)号：WO1996016058A1
公开(公告)日：1996-05-30
申请号：PCT/US1995016040
申请日：1995-11-22
申请人： NEUROGEN CORPORATION , YUAN, Jun , THURKAUF, Andrew
发明人： NEUROGEN CORPORATION
IPC分类号： C07D401/06
CPC分类号： C07D239/42 , C07C211/27 , C07D211/14 , C07D211/70 , C07D295/096 , C07D401/06
摘要： Disclosed are compounds of formula (I), where S and V are various organic or inorganic substituents; G and K are the same or different and represent N or CR' where R' is an organic or inorganic substituent; R is hydrogen or an alkyl group; R1, X, Y, Z and T are organic or inorganic substituents; and R2 and R3 represent hydrogen or organic substituents; or NR2R3 together represents a heterocyclic ring system; and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了式（I）的化合物，其中S和V是各种有机或无机取代基; G和K相同或不同，表示N或CR'，其中R'是有机或无机取代基; R是氢或烷基; R1，X，Y，Z和T是有机或无机取代基; R2和R3代表氢或有机取代基; 或NR2R3一起表示杂环体系; 及其药学上可接受的盐; 其是脑多巴胺受体亚型的高度选择性部分激动剂或拮抗剂，因此可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征。

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