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1. 发明申请

WO2004092189A1 DERIVATIVES OF 2-(8,9-DIOXO-2,6-DIAZABICYCLO(5.2.0)NON-1(7)-EN-2-YL)ALKYL PHOSPHONIC ACID AND THEIR USE AS N-METHYL-D-ASPARTATE (NMDA) RECETOR ANTAGONISTS 审中-公开
标题翻译： 2-（8,9-二氧代-2,6-二氮杂双环（5.2.0）NON-1（7）-EN-2-YL）烷基磷酸的衍生物及其作为N-甲基-D-甲磺酸盐（NMDA ）RECETOR ANTAGONISTS
公开(公告)号：WO2004092189A1
公开(公告)日：2004-10-28
申请号：PCT/US2004/010596
申请日：2004-04-07
申请人： WYETH , BAUDY, Reinhardt, Bernhard , BUTERA, John, Anthony
发明人： BAUDY, Reinhardt, Bernhard , BUTERA, John, Anthony
IPC分类号： C07F9/645
CPC分类号： C07F9/645
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided where at least one of R 2 or R 3 is not hydrogen. The compounds of the present invention are N-methyl-D-aspartate (NMDA) receptor antagonists and are useful in treating a variety of conditions present in a mammal that benefit from inhibiting the NMDA receptor.
摘要翻译：提供式（I）化合物或其药学上可接受的盐，其中R 2或R 3中的至少一个不是氢。本发明的化合物是N-甲基-D-天冬氨酸（NMDA）受体拮抗剂，可用于治疗受益于抑制NMDA受体的哺乳动物中存在的各种病症。

2. 发明申请

WO2009012375A3 SQUARATE KINASE INHIBITORS 审中-公开
公开(公告)号：WO2009012375A3
公开(公告)日：2009-01-22
申请号：PCT/US2008/070312
申请日：2008-07-17
申请人： WYETH , LOVERING, Frank Eldridge , KIRINCICH, Steven John , WANG, Weiheng , TELLIEZ, Jean-baptiste , RESNICK, Lynn , SABALSKI, Joan E. , BANKER, Annette L. , BUTERA, John , MCFADYEN, Iain
发明人： LOVERING, Frank Eldridge , KIRINCICH, Steven John , WANG, Weiheng , TELLIEZ, Jean-baptiste , RESNICK, Lynn , SABALSKI, Joan E. , BANKER, Annette L. , BUTERA, John , MCFADYEN, Iain
IPC分类号： C07D401/12 , C07D405/12 , C07D207/44 , A61K31/4409 , A61P11/00 , A61P17/00 , A61P19/00
摘要： The present application provides compounds of Formula (I): and pharmaceutically acceptable salts thereof and pharmaceutical compositions thereof, wherein Het, R 4 , R 9 , and R 10 are defined herein. Compounds of formula (I) are useful as inhibitors of MAP kinase activated protein kinase 2 (MK2).

3. 发明申请

WO2009012375A2 SQUARATE KINASE INHIBITORS 审中-公开
标题翻译：大型激酶抑制剂
公开(公告)号：WO2009012375A2
公开(公告)日：2009-01-22
申请号：PCT/US2008070312
申请日：2008-07-17
申请人： WYETH CORP , LOVERING FRANK ELDRIDGE , KIRINCICH STEVEN JOHN , WANG WEIHENG , TELLIEZ JEAN-BAPTISTE , RESNICK LYNN , SABALSKI JOAN E , BANKER ANNETTE L , BUTERA JOHN , MCFADYEN IAIN
发明人： LOVERING FRANK ELDRIDGE , KIRINCICH STEVEN JOHN , WANG WEIHENG , TELLIEZ JEAN-BAPTISTE , RESNICK LYNN , SABALSKI JOAN E , BANKER ANNETTE L , BUTERA JOHN , MCFADYEN IAIN
CPC分类号： C07D207/456 , C07D211/58 , C07D213/74 , C07D231/38 , C07D239/42 , C07D261/14 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The present application provides compounds of Formula (I): and pharmaceutically acceptable salts thereof and pharmaceutical compositions thereof, wherein Het, R4, R9, and R1 0 are defined herein. Compounds of formula (I) are useful as inhibitors of MAP kinase activated protein kinase 2 (MK2).
摘要翻译：本申请提供式（I）化合物及其药学上可接受的盐及其药物组合物，其中Het，R 4，R 9和R 10在本文中定义。式（I）化合物可用作MAP激酶活化蛋白激酶2（MK2）的抑制剂。

4. 发明申请

WO2005030199A1 4-(1-BENZOFURAN-3-YL-METHYLIDENEAMINOXY.PROPOXY))-BENZOIC ACID DERIVATIVES AND RELATED COMPOUNDS AS PAI-1 INHIBITORS FOR THE TREATMENT OF IMPAIRMENT OF THE FIBRINOLYTIC SYSTEM AND OF THROMBOSIS 审中-公开
标题翻译： 4-（1-苯并呋喃-3-基-L-甲氧基苯氧基氧基）） - 苯甲酸衍生物及相关化合物作为PAI-1抑制剂治疗纤维蛋白溶解系统和血栓形成的影响
公开(公告)号：WO2005030199A1
公开(公告)日：2005-04-07
申请号：PCT/US2004/031361
申请日：2004-09-24
申请人： WYETH , HAVRAN, Lisa, Marie , BUTERA, John, Anthony , ELOKDAH, Hassan, Mahmoud , JENKINS, Douglas, John , GUNDERSEN, Eric, Gould
发明人： HAVRAN, Lisa, Marie , BUTERA, John, Anthony , ELOKDAH, Hassan, Mahmoud , JENKINS, Douglas, John , GUNDERSEN, Eric, Gould
IPC分类号： A61K31/343
CPC分类号： C07D307/81
摘要： The present invention relates to benzofuryl-oximes of formula (I) or a pharmaceutically acceptable salt or ester form thereof wherein R 1 is a direct bond to A, C 1 -C 4 alkylene, or -O-C 1 -C 4 alkylene; R 2 and R 3 are, independently hydrogen, halogen, C 1 -C 4 alkyl, C 1 -C 3 perfluoroalkyl, -O-C 1 -C 3 perfluoroalkyl, C 1 -C 3 alkoxy, -OH, -NH 2 , -NO 2 , -O(CH 2 ) p -aryl, -O(CH 2 ) P -heteroaryl, aryl, heteroaryl, -NH(CH 2 ) P -aryl, -NH(CH 2 ) P -heteroaryl, -NH(CO)-aryl, NH(CO)-heteroaryl, -O(CO)-aryl, O(CO)-heteroaryl, -NH(CO)-CH=CH-aryl, or -NH(CO)-CH=CH-heteroaryl; p is an integer from 0-6; R 4 is hydrogen, C 1 -C 8 alkyl, or C 3 -C 6 cycloalkyl; A is -COOH or an acid mimic; X is C 1 -C 8 alkylène, C 3 -C 6 cycloalkylene, -(CH 2 ) m O-, or -(CH 2 ) m NH-; m is an integer from 1-6; and R 5 is hydrogen, C 1 -C 8 alkyl, C 3 -C 6 alkyl, C 3 -C 6 cycloalkyl, -CH 2 -C 3 -C 6 cycloalkyl, heteroaryl, -CH 2 -heteroaryl, aryl or benzyl; R 6 and R 7 are independently, hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 perfluoroalkyl, -O-C 1 -C 6 perfluoroalkyl, C 1 -C 6 alkoxy, _OH, -NH 2 , -NO 2 , -O(CH 2 ) n -aryl, -O(CH 2 ) n -heteroaryl, aryl, or heteroaryl; and n is an integer from 0-6, wherein the alkyl, cycloalkyl, aryl and heteroaryl groups are each optionally substituted by one or more substituents. The present compounds are PAI-1 inhibitors for the treatment e.g of impairment of the fibrinolytic system, thrombosis or cardiovascular diseases.
摘要翻译：本发明涉及式（I）的苯并呋喃基 - 肟或其药学上可接受的盐或酯形式，其中R1是与A，C1-C4亚烷基或-O-C1-C4亚烷基的直接键合; R2和R3独立地是氢，卤素，C1-C4烷基，C1-C3全氟烷基，-O-C1-C3全氟烷基，C1-C3烷氧基，-OH，-NH2，-NO2，-O（CH2），-O（CH 2）p - 杂芳基，芳基，杂芳基，-NH（CH 2）P - 芳基，-NH（CH 2）P - 杂芳基，-NH（CO） - 芳基，NH（CO） CO） - 芳基，O（CO） - 杂芳基，-NH（CO）-CH = CH-芳基或-NH（CO）-CH = CH-杂芳基; p是0-6的整数; R4是氢，C1-C8烷基或C3-C6环烷基; A是-COOH或酸模拟物; X是C1-C8烷基，C3-C6亚环烷基， - （CH2）mO-或 - （CH2）mNH-; m是1-6的整数; R 5是氢，C 1 -C 8烷基，C 3 -C 6烷基，C 3 -C 6环烷基，-CH 2 -C 3 -C 6环烷基，杂芳基，-CH 2 - 杂芳基，芳基或苄基; R6和R7独立地为氢，卤素，C1-C6烷基，C1-C6全氟烷基，-O-C1-C6全氟烷基，C1-C6烷氧基，_OH，-NH2，-NO2，-O（CH2）n - 芳基， - 杂芳基， - （CH 2）n - 杂芳基，芳基或杂芳基; 且n为0-6的整数，其中烷基，环烷基，芳基和杂芳基各自任选被一个或多个取代基取代。本发明化合物是用于治疗例如纤维蛋白溶解系统，血栓形成或心血管疾病的损伤的PAI-1抑制剂。

5. 发明申请

WO2019246300A1 BENZODIAZEPINE DERIVATIVES, COMPOSITIONS, AND METHODS FOR TREATING COGNITIVE IMPAIRMENT 审中-公开
公开(公告)号：WO2019246300A1
公开(公告)日：2019-12-26
申请号：PCT/US2019/038038
申请日：2019-06-19
申请人： AGENEBIO, INC. , MEKONNEN, Belew , BUTERA, John, A. , HUANG, Jianxing , PATEL, Hemantbhai , JIANG, Qin , HERR, Robert, Jason , MAYHEW, Nicholas, James , FREEMAN, Emily, Elizabeth
发明人： MEKONNEN, Belew , BUTERA, John, A. , HUANG, Jianxing , PATEL, Hemantbhai , JIANG, Qin , HERR, Robert, Jason , MAYHEW, Nicholas, James , FREEMAN, Emily, Elizabeth
IPC分类号： C07D487/14 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/28 , A61P35/00 , A61K31/551 , A61K31/5517
摘要： This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with CNS disorders. It also relates to the use of an α5-containing GABA A receptor agonist ( e.g ., an α5-containing GABA A receptor positive allosteric modulator) in treating cognitive impairment associated with CNS disorders in a subject in need or at risk thereof, including age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI, Age-Associated Memory Impairment, Age Related Cognitive Decline, dementia, Alzheimer's Disease(AD), prodromal AD, PTSD, schizophrenia, bipolar disorder, ALS, cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease, autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction. It also relates to the use of an α5-containing GABA A receptor agonist (e.g., an α5-containing GABA A receptor positive allosteric modulator) in treating brain cancers (including brain tumors, e.g., medulloblastomas), and cognitive impairment associated therewith.

6. 发明申请

WO2007078990A2 MODIFIED LYSINE-MIMETIC COMPOUNDS 审中-公开
标题翻译：改性赖氨酸 - 化合物
公开(公告)号：WO2007078990A2
公开(公告)日：2007-07-12
申请号：PCT/US2006048790
申请日：2006-12-21
申请人： ZEALAND PHARMA AS , WYETH CORP , LARSEN BJARNE DUE , PETERSEN JORGEN SOBERG , HAUGAN KETIL JORGEN , BUTERA JOHN A , HENNAN JAMES K , KERNS EDWARD H , PIATNITSKI EVGUENI LVOVICH
发明人： LARSEN BJARNE DUE , PETERSEN JORGEN SOBERG , HAUGAN KETIL JORGEN , BUTERA JOHN A , HENNAN JAMES K , KERNS EDWARD H , PIATNITSKI EVGUENI LVOVICH
IPC分类号： C07C233/81 , A61K31/4015 , A61K31/4166 , A61P9/00 , C07D207/16 , C07D207/50 , C07D233/02
CPC分类号： C07D207/16 , C07C233/31 , C07C233/61 , C07C233/83 , C07C237/20 , C07C237/24 , C07C237/30 , C07D233/02 , C07D403/04 , C07D403/06 , C07D405/04 , C07D407/12 , C07D413/04 , C07K5/06026
摘要： Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.
摘要翻译：公开了具有有用的药理学活性如抗心律不齐活性和所需生物利用度性质的赖氨酸模拟物质。

7. 发明申请

WO2005030192A1 4- (1H-INDOL-3-YL-METHYLIDENEAMINOXY-PROPOXY) -BENZIOC ACID DERIVATIVES AND RELATED COMPOUNDS AS PAI-1 INHIBITORS FOR THE TREATMENT OF IMPAIRMENT OF THE FIBRINOLYTIC SYSTEM AND OF THROMBISIS 审中-公开
标题翻译： 4-（1H-吲哚-3-基-L-甲基氨基甲酰氧基 - 丙氧基） - 苯甲酸衍生物及相关化合物作为PAI-1抑制剂治疗纤维蛋白溶解系统和血栓形成的影响
公开(公告)号：WO2005030192A1
公开(公告)日：2005-04-07
申请号：PCT/US2004/031456
申请日：2004-09-24
申请人： WYETH , HAVRAN, Lisa, Marie , BUTERA, John, Anthony , ELOKDAH, Hassan, Mahmoud , JENKINS, Douglas, John , GUNDERSEN, Eric, Gould
发明人： HAVRAN, Lisa, Marie , BUTERA, John, Anthony , ELOKDAH, Hassan, Mahmoud , JENKINS, Douglas, John , GUNDERSEN, Eric, Gould
IPC分类号： A61K31/15
CPC分类号： C07D209/14
摘要： The present invention relates to substituted indole oximes and methods of using them.
摘要翻译：本发明涉及取代的吲哚肟及其使用方法。

8. 发明申请

WO2016205739A1 BENZODIAZEPINE DERIVATIVES, COMPOSITIONS, AND METHODS FOR TREATING COGNITIVE IMPAIRMENT 审中-公开
标题翻译：苯并噻吩衍生物，组合物和治疗认知障碍的方法
公开(公告)号：WO2016205739A1
公开(公告)日：2016-12-22
申请号：PCT/US2016/038224
申请日：2016-06-17
申请人： MEKONNEN, Belew , BUTERA, John, A. , HUANG, Jianxing
发明人： MEKONNEN, Belew , BUTERA, John, A. , HUANG, Jianxing
IPC分类号： C07D487/14 , A61K31/5513 , A61P25/00
CPC分类号： A61K31/551 , A61K31/13 , A61K31/27 , A61K31/445 , A61K31/496 , A61K31/55 , A61K45/06 , C07D487/14 , A61K2300/00
摘要： This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a α5- containing GABA A receptor agonist ( e.g. , a α5-containing GABA A receptor positive allosteric modulator) as described herein in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age- Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer' s Disease(AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson' s disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction.
摘要翻译：本发明涉及苯并二氮杂衍生物，包含治疗有效量的那些苯并二氮杂衍生物的组合物和使用这些衍生物或组合物治疗与中枢神经系统（CNS）病症相关的认知障碍的方法。特别地，本发明涉及在本文所述的含有α5的GABA A受体激动剂（例如，含有α5的GABA A受体阳性变构调节剂）用于治疗有需要的受试者中与中枢神经系统（CNS）紊乱相关的认知障碍或其风险包括但不限于具有年龄相关认知障碍或轻度认知障碍（MCI），遗忘MCI（aMCI），年龄相关记忆障碍（AAMI），年龄相关认知衰退（ARCD）），痴呆，阿尔茨海默病（AD），前驱性AD，创伤后应激障碍（PTSD），精神分裂症，双相情感障碍，肌萎缩性侧索硬化（ALS），癌症治疗相关认知障碍，精神发育迟滞，帕金森病（PD），自闭症谱系障碍，脆性X病症，Rett综合征，强迫行为和物质成瘾。

9. 发明申请

WO2007078990A3 MODIFIED LYSINE-MIMETIC COMPOUNDS 审中-公开
公开(公告)号：WO2007078990A3
公开(公告)日：2007-07-12
申请号：PCT/US2006/048790
申请日：2006-12-21
申请人： ZEALAND PHARMA A/S , WYETH , LARSEN, Bjarne, Due , PETERSEN, Jorgen, Soberg , HAUGAN, Ketil, Jorgen , BUTERA, John, A. , HENNAN, James, K. , KERNS, Edward, H. , PIATNITSKI, Evgueni, Lvovich
发明人： LARSEN, Bjarne, Due , PETERSEN, Jorgen, Soberg , HAUGAN, Ketil, Jorgen , BUTERA, John, A. , HENNAN, James, K. , KERNS, Edward, H. , PIATNITSKI, Evgueni, Lvovich
IPC分类号： C07C233/81 , C07D207/16 , C07D207/50 , C07D233/02 , A61K31/4015 , A61K31/4166 , A61P9/00
摘要： Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.

10. 发明申请

WO2005030193A1 4-(PHENYL-ETHYLIDENEAMINOXY-PROPOXY) -PHENYL-ACETIC ACID DERIVATIVES AND RELATED COMPOUNDS AS PAI-1 INHIBITORS FOR THE TREATMENT OF IMPAIRMENT OF THE FIBRINOLYTIC SYSTEM AND OF THROMBOSIS 审中-公开
标题翻译：作为PAI-1抑制剂治疗纤维蛋白溶解系统和血栓形成的相关化合物的4-（苯基 - 乙酰氨基羟胺氧基 - 丙氧基） - 苯乙酸衍生物和相关化合物
公开(公告)号：WO2005030193A1
公开(公告)日：2005-04-07
申请号：PCT/US2004/031460
申请日：2004-09-24
申请人： WYETH , HAVRAN, Lisa, Marie , BUTERA, John, Anthony , ELOKDAH, Hassan, Mahmoud , JENKINS, Douglas, John , GUNDERSEN, Eric, Gould
发明人： HAVRAN, Lisa, Marie , BUTERA, John, Anthony , ELOKDAH, Hassan, Mahmoud , JENKINS, Douglas, John , GUNDERSEN, Eric, Gould
IPC分类号： A61K31/15
CPC分类号： C07D257/04 , A61K31/195 , A61K31/343 , A61K31/40 , A61K31/445 , C07C251/54
摘要： The present invention relates to substituted aryl oximes of formula (I) or a pharmaceutically acceptable salt or ester form thereof wherein R 1 is a direct bond to A, C 1 -C 4 alkylene, or -O-C 1 -C 4 alkylene; R 2 and R 3 are , independently hydrogen, halogen, C 1 -C 4 alkyl, C 1 -C 3 perfluoroalkyl, -O-C 1 -C 3 perfluoroalkyl, C 1 -C 3 alkoxy, -OH, -NH 2 , -NO 2 , -O(CH 2 ) p -aryl, -O(CH 2 ) p -heteroaryl, aryl, heteroaryl, -NH(CH 2 ) p -aryl, -NH(CH 2 ) p -heteroaryl, -NH(CO)-aryl, -NH(CO)-heteroaryl, -O(CO)-aryl, -O(CO)-heteroaryl, -NH(CO)-CH=CH-aryl, or -NH(CO)-CH=CH-heteroaryl; p is an integer from 0-6; R 4 is hydrogen, C 1 -C 8 alkyl, or C 3 -C 6 cycloalkyl; A is COOH or an acid mimic; X is C 1 -C 8 alkylene, C 3 -C 6 cycloalkylene, -(CH 2 ) m O-, or -(CH 2 ) m NH-; m is an integer from 1-6; R 5 and R 6 are, independently, hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 perfluoroalkyl, -O-C 1 -C 6 perfluoroalkyl, C 1 -C 6 alkoxy, -OH, -NH 2 , -NO 2 , -O(CH 2 ) n -aryl, O(CH2)n-heteroaryl, aryl, or heteroaryl; and is an integer from 0-6, wherein C 1 -C 4 alkaline, -O-C 1 -C 4 alkaline, alkyl, aryl and heteroaryl are each optionally substituted by one or more substituents. The present compounds are PAI-1 inhibitors for the treatment e.g of impairment of the fibrinolytic system, thrombosis or cardiovascular diseases.
摘要翻译：本发明涉及式（I）的取代的芳基肟或其药学上可接受的盐或酯形式，其中R 1是与A，C 1 -C 4亚烷基或-O-C 1 -C 4亚烷基的直接键; R2和R3独立地是氢，卤素，C1-C4烷基，C1-C3全氟烷基，-O-C1-C3全氟烷基，C1-C3烷氧基，-OH，-NH2，-NO2，-O（CH2），-O（CH 2）p - 杂芳基，芳基，杂芳基，-NH（CH 2）p - 芳基，-NH（CH 2）p - 杂芳基，-NH（CO） - 芳基，-NH（CO）（CO） - 芳基，-O（CO） - 杂芳基，-NH（CO）-CH = CH-芳基或-NH（CO）-CH = CH-杂芳基; p是0-6的整数; R4是氢，C1-C8烷基或C3-C6环烷基; A是COOH或酸模拟物; X是C1-C8亚烷基，C3-C6亚环烷基， - （CH2）mO-或 - （CH2）mNH-; m是1-6的整数; R5和R6独立地是氢，卤素，C1-C6烷基，C1-C6全氟烷基，-O-C1-C6全氟烷基，C1-C6烷氧基，-OH，-NH2，-NO2，-O（CH2）n- 芳基，O（CH 2）n - 杂芳基，芳基或杂芳基; 并且是0-6的整数，其中C 1 -C 4碱性，-O-C 1 -C 4碱性，烷基，芳基和杂芳基各自任选被一个或多个取代基取代。本发明化合物是用于治疗例如纤维蛋白溶解系统，血栓形成或心血管疾病的损伤的PAI-1抑制剂。

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