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1. 发明申请

WO2018035259A1 METHODS AND PROCESSES FOR THE PREPARATION OF KDM1A INHIBITORS 审中-公开
标题翻译：制备KDM1A抑制剂的方法和过程
公开(公告)号：WO2018035259A1
公开(公告)日：2018-02-22
申请号：PCT/US2017/047208
申请日：2017-08-16
申请人： IMAGO BIOSCIENCES, INC. , TAPPER, Amy, E. , CELATKA, Cassandra , ROMERO, Arthur, Glenn , MCCALL, John, M. , CHANCELLOR, Toni , CHEN, Jian-Xie , CHEN, Xuemei , ZHAO, He , BIOLATTO, Betina , BROT, Elisabeth, C.A. , LI, Zhihua , LIAO, Xiaoming
发明人： TAPPER, Amy, E. , CELATKA, Cassandra , ROMERO, Arthur, Glenn , MCCALL, John, M. , CHANCELLOR, Toni , CHEN, Jian-Xie , CHEN, Xuemei , ZHAO, He , BIOLATTO, Betina , BROT, Elisabeth, C.A. , LI, Zhihua , LIAO, Xiaoming
IPC分类号： C07C211/35 , C07C237/22 , A61P35/02
摘要： Provided in this disclosure are methods for the synthesis of substituted 2-arylcyclopropylamines and 2-heteroarylcyclopropylamines and related compounds. Also provided are methods for reduction of thioesters to aldehydes, and methods for reductive animation of cyclopropylamines.
摘要翻译：在本公开中提供了合成取代的2-芳基环丙胺和2-杂芳基环丙胺及相关化合物的方法。还提供了用于将硫酯还原为醛的方法以及用于还原动画环丙胺的方法。

2. 发明申请

WO2003006466A1 HEXAHYDROAZEPINO (4, 5-G) INDOLES AND INDOLINES AS 5-HT RECEPTOR LIGANDS 审中-公开
标题翻译：作为5-HT受体配体的HEXAHYDROAZEPINO（4,5-G）吲哚和吲哚
公开(公告)号：WO2003006466A1
公开(公告)日：2003-01-23
申请号：PCT/US2002/019804
申请日：2002-07-10
申请人： PHARMACIA & UPJOHN COMPANY , FU, Jian-Min , MORRIS, Jeanette, Kay , ROMERO, Arthur, Glenn
发明人： FU, Jian-Min , MORRIS, Jeanette, Kay , ROMERO, Arthur, Glenn
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides compounds of Formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and --- have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are useful as 5-HT ligands.
摘要翻译：本发明提供式（I）的化合物：其中R 1，R 2，R 3，R 4，R 5，R 6和 - 具有任何值在本说明书中定义，以及包含该化合物的药物组合物。本发明还提供治疗方法以及可用于制备式（I）化合物的方法和中间体。该化合物可用作5-HT配体。

3. 发明申请

WO1992000282A1 SUBSTITUTED 1-(ALKOXYPHENYL)PIPERAZINES WITH CNS AND ANTIHYPERTENSIVE ACTIVITY 审中-公开
标题翻译：取代的1-（烷氧基苯基）哌嗪与CNS和抗真菌活性
公开(公告)号：WO1992000282A1
公开(公告)日：1992-01-09
申请号：PCT/US1991003943
申请日：1991-06-10
申请人： THE UPJOHN COMPANY , PIERCEY, Montford, F. , DARLINGTON, William, Harold , ROMERO, Arthur, Glenn
发明人： THE UPJOHN COMPANY
IPC分类号： C07D233/58
CPC分类号： C07D233/36
摘要： Substituted 1-(alkoxyphenyl)piperazines of formula (I) are disclosed as partial dopamine agonists useful in the treatment of dopaminergic dysregulation. The compounds 1-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-3-phenyl-2-imidazolidinone and 1-(3-chlorophenyl)-3-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-2-im idazolidinone, are preferred in the treatment of Parkinsonism, schizophrenia, and drug addiction.
摘要翻译：公开了式（I）的取代的1-（烷氧基苯基）哌嗪作为可用于治疗多巴胺能失调的部分多巴胺激动剂。化合物1- [4- [4-（2-甲氧基苯基）-1-哌嗪基]丁基] -3-苯基-2-咪唑啉酮和1-（3-氯苯基）-3- [4- [4-（2- 甲氧基苯基）-1-哌嗪基]丁基] -2-咪唑烷酮在治疗帕金森综合征，精神分裂症和药物成瘾中是优选的。

4. 发明申请

WO2018035249A1 COMPOSITIONS AND METHODS FOR PRODUCING STEREOISOMERICALLY PURE AMINOCYCLOPROPANES 审中-公开
标题翻译：用于制备立体异构纯氨基环丙烷的组合物和方法
公开(公告)号：WO2018035249A1
公开(公告)日：2018-02-22
申请号：PCT/US2017/047192
申请日：2017-08-16
申请人： IMAGO BIOSCIENCES, INC. , TAPPER, Amy, E. , CELATKA, Cassandra , ROMERO, Arthur, Glenn , MCCALL, John, M. , CHANCELLOR, Toni , ZHAO, He , BIOLATTO, Betina , CHEN, Jian-xie , BROT, Elisabeth, C.A. , MICHELS, Peter, C. , CHARI, Venkat, K. , COTTERILL, Ian, C.
发明人： TAPPER, Amy, E. , CELATKA, Cassandra , ROMERO, Arthur, Glenn , MCCALL, John, M. , CHANCELLOR, Toni , ZHAO, He , BIOLATTO, Betina , CHEN, Jian-xie , BROT, Elisabeth, C.A. , MICHELS, Peter, C. , CHARI, Venkat, K. , COTTERILL, Ian, C.
IPC分类号： C12P17/00 , C12N9/02 , C12N9/04 , C12N9/06 , C12P13/04
摘要： The present disclosure relates to compositions and methods for producing stereoisomerically pure aminocyclopropanes.
摘要翻译：本公开涉及用于生产立体异构纯的氨基环丙烷的组合物和方法。

5. 发明申请

WO2002098849A2 HYDROXY ALKYL AMINES 审中-公开
标题翻译：羟基烷基氨基酸
公开(公告)号：WO2002098849A2
公开(公告)日：2002-12-12
申请号：PCT/US2002/017698
申请日：2002-05-31
申请人： ELAN PHARMACEUTICALS, INC. , PHARMACIA & UPJOHN COMPANY , FRESKOS, John , AQUINO, Jose , BROWN, David, L. , FANG, Larry , FOBIAN, Yvette, M. , GAILUNAS, Andrea , GUINN, Ashley , VARGHESE, John , ROMERO, Arthur, Glenn , TUCKER, John , TUNG, Jay , WALKER, Donald
发明人： FRESKOS, John , AQUINO, Jose , BROWN, David, L. , FANG, Larry , FOBIAN, Yvette, M. , GAILUNAS, Andrea , GUINN, Ashley , VARGHESE, John , ROMERO, Arthur, Glenn , TUCKER, John , TUNG, Jay , WALKER, Donald
IPC分类号： C07C317/26
CPC分类号： C07D207/26 , C07C317/46 , C07C317/48 , C07C317/50 , C07C323/60 , C07C327/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/12 , C07D207/28 , C07D209/08 , C07D211/46 , C07D211/96 , C07D213/30 , C07D213/81 , C07D213/82 , C07D231/12 , C07D231/14 , C07D233/56 , C07D233/64 , C07D233/74 , C07D233/90 , C07D237/04 , C07D241/24 , C07D249/08 , C07D261/18 , C07D277/36 , C07D277/56 , C07D295/185 , C07D307/20 , C07D309/12 , C07D317/30 , C07D319/06 , C07D333/32 , C07D333/34 , C07D333/48
摘要： Disclosed are compounds of formula X, where R n , R 20 , R 1 , R 2 , R 3 , and R c are defined herein. These compounds are useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions comprising compounds of formula X and methods of preparing the compounds of formula X are also disclosed.
摘要翻译：公开了式X的化合物，其中R n，R 20，R 1，R 2，R 3和R c如本文所定义。这些化合物可用于治疗阿尔茨海默病和其他类似疾病。还公开了包含式X化合物的药物组合物和制备式X化合物的方法。

6. 发明申请

WO1993008166A1 BENZO-ISOQUINOLINE DERIVATIVES AND ANALOGS AND THEIR USE IN THERAPEUTICS 审中-公开
标题翻译：苯并异喹啉衍生物和类似物及其在治疗中的应用
公开(公告)号：WO1993008166A1
公开(公告)日：1993-04-29
申请号：PCT/US1992007314
申请日：1992-09-03
申请人： THE UPJOHN COMPANY , ROMERO, Arthur, Glenn
发明人： THE UPJOHN COMPANY
IPC分类号： C07D221/10
CPC分类号： C07D221/10 , C07D223/32
摘要： The present invention encompasses: 1) compounds of formula (I), wherein p and s are independent and may be either 1 or 2, wherein R1 is -H, -Halo, -CN, -CO2H, -CO2R1-1, -CONH2, -CONHR1-1, -CON(R1-1)2, -SH, -SR1-1, -SO2R1-1, -SO2NH2, -SO2NHR1-1, -SO2N(R1-1)2, -OR1-1, -OSO2CF3, -OSO2R1-1, -NH2, -NHR1-1, or -N(R1-1)2; wherein R1-1 is -H, -(C1-C8 alkyl), -(C1-C8 alkenyl), -(C3-C10 cycloalkyl), -(C6 aryl), -5 or 6 member heterocyclics, -(C1-C8 alkyl)-(5 or 6 member heterocyclics), wherein R2 is -H, -Halo, -CN, -CF3, -SH, or -SR2-1; wherein R2-1=R1-1, wherein R3 is -H, -(C1-C8 alkyl), -(C1-C8 alkenyl), -(C6 aryl), -(C3-C10 cycloalkyl), -(5 or 6 member heterocyclics), -(C1-C8 alkyl)-5 or 6 member heterocyclics), wherein R3-1=R1-1 or a pharmacologically acceptable salt thereof; 2) a pharmaceutical composition consisting essentially of a pharmaceutically acceptable carrier and an effective amount of a compound of formula (I); 3) a method of treating central nervous system disorders, associated with serotonin and/or dopamine receptor activity comprising: administering an effective amount of a compound of formula (I) to a patient in need thereof. The compounds of this invention possess selective pharmacological properties and are useful in treating central nervous system disorders.
摘要翻译：本发明包括：1）式（I）化合物，其中p和s独立并且可以是1或2，其中R 1是-H，-Halo，-CN，-CO 2 H，-CO 2 R 1，-CONH 2 ，-CONHR1-1，-CON（R1-1）2，-SH，-SR1-1，-SO2R1-1，-SO2NH2，-SO2NHR1-1，-SO2N（R1-1）2，-OR1-1， -OSO2CF3，-OSO2R1-1，-NH2，-NHR1-1或-N（R1-1）2; 其中R1-1是-H， - （C1-C8烷基）， - （C1-C8链烯基）， - （C3-C10环烷基）， - （C6芳基），或5或6元杂环， - （C1-C8 烷基） - （5或6元杂环），其中R2是-H，-Halo，-CN，-CF3，-SH或-SR2-1; （C1-C8链烯基）， - （C6芳基）， - （C3-C10环烷基）， - （5或6）（C1-C8烷基）-5或6元杂环），其中R3-1 = R1-1或其药理学上可接受的盐; 2）基本上由药学上可接受的载体和有效量的式（I）化合物组成的药物组合物; 3）治疗与5-羟色胺和/或多巴胺受体活性相关的中枢神经系统疾病的方法，包括：向有需要的患者施用有效量的式（I）化合物。本发明的化合物具有选择性药理学性质，可用于治疗中枢神经系统疾病。

7. 发明申请

WO1990015047A1 THERAPEUTICALLY USEFUL 2-AMINOTETRALIN DERIVATIVES 审中-公开
标题翻译：可治疗2-AMINOTETRALIN衍生物
公开(公告)号：WO1990015047A1
公开(公告)日：1990-12-13
申请号：PCT/US1990002726
申请日：1990-05-22
申请人： THE UPJOHN COMPANY , LIN, Chiu-Hong , HAADSMA, Susanne, R. , PIERCEY, Montford, F. , ROMERO, Arthur, Glenn , DARLINGTON, William, H.
发明人： THE UPJOHN COMPANY
IPC分类号： C07C237/48
CPC分类号： C07D207/335 , C07C45/46 , C07C45/59 , C07C45/673 , C07C45/68 , C07C211/48 , C07C215/64 , C07C217/74 , C07C223/04 , C07C229/14 , C07C229/50 , C07C233/23 , C07C237/48 , C07C255/58 , C07C271/64 , C07C311/16 , C07C311/37 , C07C327/48 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07D209/60 , C07D275/06 , C07D295/073 , C07D295/096 , C07D295/155 , C07D317/58 , C07C49/697 , C07C49/755 , C07C49/683
摘要： This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of formula (I). These compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.
摘要翻译：本发明是治疗上有用的式（I）的2-氨基四氢萘酮及其药学上可接受的酸加成盐。这些化合物可用于治疗中枢神经系统疾病，高血压，糖尿病，性功能障碍和控制食欲。

8. 发明申请

WO2012064744A3 N- SULFONYLATED TETRAHYDROQUINOLINES AND RELATED BICYCLIC COMPOUNDS INHIBITION OF RORY ACTIVITY AND THE TREATMENT OF DISEASES 审中-公开
公开(公告)号：WO2012064744A3
公开(公告)日：2012-05-18
申请号：PCT/US2011/059788
申请日：2011-11-08
申请人： LYCERA CORPORATION , GLICK, Gary, D. , TOOGOOD, Peter, L. , ROMERO, Arthur, Glenn , VANHUIS, Chad, A. , AICHER, Thomas, Daniel , KAUB, Carl , MATTSON, Matthew, N. , THOMAS, William, David , STEIN, Karin, Ann , KROGH-JESPERSEN, Erik , WANG, Zhan
发明人： GLICK, Gary, D. , TOOGOOD, Peter, L. , ROMERO, Arthur, Glenn , VANHUIS, Chad, A. , AICHER, Thomas, Daniel , KAUB, Carl , MATTSON, Matthew, N. , THOMAS, William, David , STEIN, Karin, Ann , KROGH-JESPERSEN, Erik , WANG, Zhan
IPC分类号： C07D215/58 , C07D265/36 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/12 , C07D417/12 , C07D241/50 , C07D209/08 , C07D209/34 , C07D231/56 , C07D403/12 , C07D405/12 , C07D409/12 , A61P37/00
摘要： The invention provides tetrahydroquinoline and related compounds, pharmaceutical compositions, methods of inhibiting RORϒ activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydroquinoline and related compounds are provided.

9. 发明申请

WO2012064744A2 TETRAHYDROQUINOLINE AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF ROR? ACTIVITY AND THE TREATMENT OF DISEASE 审中-公开
标题翻译：四氢喹啉和相关的双相化合物用于抑制ROR？活动和疾病的治疗
公开(公告)号：WO2012064744A2
公开(公告)日：2012-05-18
申请号：PCT/US2011059788
申请日：2011-11-08
申请人： LYCERA CORP , GLICK GARY D , TOOGOOD PETER L , ROMERO ARTHUR GLENN , VANHUIS CHAD A , AICHER THOMAS DANIEL , KAUB CARL , MATTSON MATTHEW N , THOMAS WILLIAM DAVID , STEIN KARIN ANN , KROGH-JESPERSEN ERIK , WANG ZHAN
发明人： GLICK GARY D , TOOGOOD PETER L , ROMERO ARTHUR GLENN , VANHUIS CHAD A , AICHER THOMAS DANIEL , KAUB CARL , MATTSON MATTHEW N , THOMAS WILLIAM DAVID , STEIN KARIN ANN , KROGH-JESPERSEN ERIK , WANG ZHAN
IPC分类号： A61K31/538
CPC分类号： C07D413/06 , C07D209/08 , C07D209/34 , C07D215/58 , C07D231/56 , C07D241/50 , C07D265/36 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The invention provides tetrahydroquinoline and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydroquinoline and related compounds are provided.
摘要翻译：本发明提供四氢喹啉及其相关化合物，药物组合物，抑制ROR的方法？活性，减少受试者中IL-17的量，以及使用这种四氢喹啉和相关化合物治疗免疫疾病和炎性疾病。

10. 发明申请

WO2004031195A1 TRICYCLIC TETRAHYDROQUINOLINE ANTIBACTERIAL AGENTS 审中-公开
标题翻译： TRICYCLIC四氢喹啉抗体药剂
公开(公告)号：WO2004031195A1
公开(公告)日：2004-04-15
申请号：PCT/IB2003/004389
申请日：2003-10-03
申请人： PHARMACIA & UPJOHN COMPANY , BARBACHYN, Michel, Robert , DOBROWOLSKI, Paul, Joseph , HURD, Alexander, Ross , MCNAMARA, Dennis, Joseph , PALMER, John, Raymond , ROMERO, Arthur, Glenn , RUBLE, James, Craig , SHERRY, Debra, Ann , THOMASCO, Lisa, Marie , TOOGOOD, Peter, Laurence
发明人： BARBACHYN, Michel, Robert , DOBROWOLSKI, Paul, Joseph , HURD, Alexander, Ross , MCNAMARA, Dennis, Joseph , PALMER, John, Raymond , ROMERO, Arthur, Glenn , RUBLE, James, Craig , SHERRY, Debra, Ann , THOMASCO, Lisa, Marie , TOOGOOD, Peter, Laurence
IPC分类号： C07D498/20
CPC分类号： C07D471/20 , C07D498/10 , C07D498/20
摘要： The invention includes tetrahydroquinoline and related compounds of formula (I), and pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens.
摘要翻译：本发明包括四氢喹啉和相关的式（I）化合物及其药物组合物，其对广泛的人和兽医病原体表现出有用的抗菌活性。

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