公开(公告)号：US20080139546A1

公开(公告)日：2008-06-12

申请号：US11904773

申请日：2007-09-28

Applicant: Minsheng Zhang ,  Charles J. Stanton ,  Boyd Lynn Harrison ,  Terrance H. Andree

Inventor： Minsheng Zhang ,  Charles J. Stanton ,  Boyd Lynn Harrison ,  Terrance H. Andree

IPC: A61K31/4741 ,  C07D413/14 ,  C07D405/14 ,  A61P25/00 ,  A61P25/30 ,  C12N5/06 ,  C12N5/08 ,  A61P25/18 ,  A61P25/28 ,  C07D405/12 ,  A61K31/538

CPC classification number: C07D491/056

Abstract: The present invention relates to a compound of the formula: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, useful as modulators of 5-HT1A receptor activity and/or serotonin reuptake. These compounds are useful in treating nervous system disorders, such as anxiety-related disorders, cognition-related disorders, depression, schizophrenia, or sexual dysfunction and related illnesses.

Abstract translation: 本发明涉及可用作5-HT 1A受体活性和/或5-羟色胺再摄取调节剂的下式化合物或其对映异构体，非对映异构体，互变异构体或其药学上可接受的盐或溶剂合物。 这些化合物可用于治疗神经系统疾病，例如焦虑相关障碍，认知相关障碍，抑郁症，精神分裂症或性功能障碍及相关疾病。

公开(公告)号：US06391901B1

公开(公告)日：2002-05-21

申请号：US09423148

申请日：2000-01-21

Applicant: Nickolay Y Chirgadze ,  Michael L Denney ,  Matthew J Fisher ,  Robert J Foglesong ,  Richard W Harper ,  Mary G Johnson ,  Ho-Shen Lin ,  Michael P Lynch ,  Jefferson R McCowan ,  Shawn C Miller ,  Alan D Palkowitz ,  Michael E Richett ,  Daniel J Sall ,  Gerald F Smith ,  Kumiko Takeuchi ,  Minsheng Zhang

Inventor： Nickolay Y Chirgadze ,  Michael L Denney ,  Matthew J Fisher ,  Robert J Foglesong ,  Richard W Harper ,  Mary G Johnson ,  Ho-Shen Lin ,  Michael P Lynch ,  Jefferson R McCowan ,  Shawn C Miller ,  Alan D Palkowitz ,  Michael E Richett ,  Daniel J Sall ,  Gerald F Smith ,  Kumiko Takeuchi ,  Minsheng Zhang

IPC: A61K314025

CPC classification number: C07D333/58 ,  A61K31/4025 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  C07D333/56 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of defined compounds of formula I as thrombin inhibitors.

Abstract translation: 本申请涉及本文定义的式I（及其药学上可接受的盐）的新型化合物，其制备方法和中间体，包含式I的新化合物的药物制剂，以及定义的式I化合物作为凝血酶抑制剂的用途 。

公开(公告)号：US06284756B1

公开(公告)日：2001-09-04

申请号：US09423166

申请日：2000-01-21

Applicant: Nickolay Y Chirgadze ,  Richard W Harper ,  Todd J Kohn ,  Ho-Shen Lin ,  Jefferson R McCowan ,  Alan D Palkowitz ,  Daniel J Sall ,  Gerald F Smith ,  Kumiko Takeuchi ,  Michael R Wiley ,  Minsheng Zhang

Inventor： Nickolay Y Chirgadze ,  Richard W Harper ,  Todd J Kohn ,  Ho-Shen Lin ,  Jefferson R McCowan ,  Alan D Palkowitz ,  Daniel J Sall ,  Gerald F Smith ,  Kumiko Takeuchi ,  Michael R Wiley ,  Minsheng Zhang

IPC: A61K314025

CPC classification number: C07D333/58 ,  C07D333/56 ,  C07D409/10 ,  C07D409/12

Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.

Abstract translation: 本申请涉及本文定义的式I（及其药学上可接受的盐）的新型化合物，其制备方法和中间体，包含式I的新型化合物的药物制剂以及式I化合物作为凝血酶抑制剂的用途 。

公开(公告)号：US06265416B1

公开(公告)日：2001-07-24

申请号：US09429424

申请日：1999-10-28

Applicant: Jolie Anne Bastian ,  Matthew Joseph Fisher ,  Richard Waltz Harper ,  Ho-Shen Lin ,  Jefferson Ray McCowan ,  Daniel Jon Sall ,  Gerald Floyd Smith ,  Kumiko Takeuchi ,  Michael Robert Wiley ,  Minsheng Zhang

Inventor： Jolie Anne Bastian ,  Matthew Joseph Fisher ,  Richard Waltz Harper ,  Ho-Shen Lin ,  Jefferson Ray McCowan ,  Daniel Jon Sall ,  Gerald Floyd Smith ,  Kumiko Takeuchi ,  Michael Robert Wiley ,  Minsheng Zhang

IPC: A61K31535

CPC classification number: C07D471/04

Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.

公开(公告)号：US6025382A

公开(公告)日：2000-02-15

申请号：US846647

申请日：1997-04-30

Applicant: Jolie Anne Bastian ,  Nickolay Yuri Chirgadze ,  Michael Lyle Denney ,  Matthew Joseph Fisher ,  Robert James Foglesong ,  Richard Waltz Harper ,  Mary George Johnson ,  Valentine Joseph Klimkowski ,  Todd Jonathan Kohn ,  Ho-Shen Lin ,  Michael Patrick Lynch ,  Jefferson Ray McCowan ,  Alan David Palkowitz ,  Michael Enrico Richett ,  Daniel Jon Sall ,  Gerald Floyd Smith ,  Kumiko Takeuchi ,  Jennifer Marie Tinsley ,  Minsheng Zhang

Inventor： Jolie Anne Bastian ,  Nickolay Yuri Chirgadze ,  Michael Lyle Denney ,  Matthew Joseph Fisher ,  Robert James Foglesong ,  Richard Waltz Harper ,  Mary George Johnson ,  Valentine Joseph Klimkowski ,  Todd Jonathan Kohn ,  Ho-Shen Lin ,  Michael Patrick Lynch ,  Jefferson Ray McCowan ,  Alan David Palkowitz ,  Michael Enrico Richett ,  Daniel Jon Sall ,  Gerald Floyd Smith ,  Kumiko Takeuchi ,  Jennifer Marie Tinsley ,  Minsheng Zhang

IPC: C07D295/08 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/4453 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/55 ,  A61P7/02 ,  C07D333/56 ,  C07D333/58 ,  C07D333/62 ,  C07D333/64 ,  C07D333/66 ,  C07D409/04 ,  C07D409/06 ,  C07D409/10 ,  C07D409/12 ,  C07D413/06 ,  C07D521/00 ,  A61K31/40 ,  A61K31/38 ,  C07D409/14

CPC classification number: C07D333/62 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/55 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D333/56 ,  C07D333/58 ,  C07D333/64 ,  C07D333/66 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06

Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.

Abstract translation: 本申请涉及作为本文定义的式I二胺的凝血酶抑制剂，凝血抑制剂和血栓栓塞障碍剂的用途。 它还提供式I的新型化合物，其制备方法和中间体，以及包含式I化合物的药物制剂。

公开(公告)号：US09090568B2

公开(公告)日：2015-07-28

申请号：US14004633

申请日：2012-03-12

Applicant: Dong Liu ,  Minsheng Zhang ,  Kan He ,  Lianshan Zhang

Inventor： Dong Liu ,  Minsheng Zhang ,  Kan He ,  Lianshan Zhang

IPC: C07D239/96 ,  C07D239/80 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D239/96 ,  C07D239/80 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts or prodrugs thereof, which inhibit the poly(ADP-ribose) polymerases (PARP) and therefore are useful for treating diseases, disorders, and conditions related to PARP. The present invention also discloses pharmaceutical compositions comprising a compound of formula (I), and methods of using such compounds to inhibit PARP enzymes, and to treat diseases, disorders, and conditions related to PARP.

Abstract translation: 本发明公开了抑制聚（ADP-核糖）聚合酶（PARP）的式（I）化合物或其药学上可接受的盐或前药，因此可用于治疗与PARP相关的疾病，病症和病症。 本发明还公开了包含式（I）化合物的药物组合物，以及使用这些化合物抑制PARP酶以及治疗与PARP有关的疾病，病症和病症的方法。

公开(公告)号：US20100298276A1

公开(公告)日：2010-11-25

申请号：US12469791

申请日：2009-05-21

Applicant: Denis E. Ryono ,  Jon J. Hangeland ,  Todd J. Friends ,  Tamara Dejneka ,  Pratik Devasthale ,  Yolanda V. Caringal ,  Minsheng Zhang ,  Arthur M.P. Doweyko ,  Johan Malm ,  Andrei Sanin

Inventor： Denis E. Ryono ,  Jon J. Hangeland ,  Todd J. Friends ,  Tamara Dejneka ,  Pratik Devasthale ,  Yolanda V. Caringal ,  Minsheng Zhang ,  Arthur M.P. Doweyko ,  Johan Malm ,  Andrei Sanin

IPC: A61K31/662 ,  C07F9/02 ,  A61P3/10

CPC classification number: C07C311/46 ,  A61K31/4439 ,  A61K31/662 ,  A61K45/06 ,  C07C43/29 ,  C07C43/295 ,  C07C59/68 ,  C07C59/72 ,  C07C65/24 ,  C07C65/26 ,  C07C69/16 ,  C07C69/736 ,  C07C69/94 ,  C07C205/38 ,  C07C217/58 ,  C07C233/29 ,  C07C235/34 ,  C07C235/42 ,  C07C235/46 ,  C07C235/52 ,  C07C235/60 ,  C07C235/62 ,  C07C235/64 ,  C07C311/37 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2603/18 ,  C07D213/30 ,  C07D239/26 ,  C07D257/04 ,  C07D263/14 ,  C07D263/32 ,  C07D277/24 ,  C07D285/06 ,  C07D307/42 ,  C07D307/52 ,  C07D307/87 ,  C07D317/58 ,  C07D317/60 ,  C07D333/32 ,  C07F9/306 ,  C07F9/3241 ,  C07F9/4056 ,  A61K2300/00

Abstract: Thyroid receptor ligands are provided which have the general formula I wherein: R1 is R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, provided that at least one of R2 and R3 is other than hydrogen; R4 is R5 and R6 are the same or different and are selected from hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, aralkyl or heteroaralkyl. R7 is aryl, heteroaryl, alkyl, aralkyl, or heteroaralkyl; R8 is aryl, heteroaryl, or cycloalkyl; R9 is R7 or hydrogen; R10 is hydrogen, halogen, cyano or alkyl; R11 and R12 are each independently selected from the group consisting of hydrogen, halogen, alkoxy, hydroxy (—OH) cyano, and alkyl; R13 is carboxylic acid (COOH) or esters thereof, phosphonic and phosphinic acid or esters thereof, sulfonic acid, tetrazole, hydroxamic acid, thiazolidinedione, acylsulfonamide, or other carboxylic acid surrogates known in the art; R14 and R15 may be the same or different and are selected from hydrogen and alkyl, or R14 and R15 may be joined together forming a chain of 2 to 5 methylene groups [—(CH2)m-, m=2, 3, 4 or 5], thus forming 3- to 6-membered cycloalkyl rings; R16 is hydrogen or alkyl of 1 to 4 carbons; R17 and R18 are the same or different and selected from hydrogen, halogen and alkyl; n is 0 or an integer from 1 to 4; X is oxygen (—O—), sulfur (—S—), sulfonyl (—SO2—), sulfenyl (—SO—) selenium (—Se—), carbonyl (—CO—), amino (—NH—) or methylene (—CH2-); wherein the substituents are as described herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

公开(公告)号：US20090227667A1

公开(公告)日：2009-09-10

申请号：US12435442

申请日：2009-05-05

Applicant: Anthony Frank Kreft ,  Lynn Resnick ,  Scott Christian Mayer ,  George Diamantidis ,  Derek Cecil Cole ,  Boyd Lynn Harrison ,  Minsheng Zhang ,  Molly Hoke ,  Tingzhong Wang ,  Rocco John Galante

Inventor： Anthony Frank Kreft ,  Lynn Resnick ,  Scott Christian Mayer ,  George Diamantidis ,  Derek Cecil Cole ,  Boyd Lynn Harrison ,  Minsheng Zhang ,  Molly Hoke ,  Tingzhong Wang ,  Rocco John Galante

IPC: A61K31/381 ,  C07D333/34 ,  C07D333/62

CPC classification number: C07D333/62 ,  C07D231/18 ,  C07D333/34

Abstract: Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.

Abstract translation: 提供式（I）化合物，其中T是CHO，COR8或C（OH）R 1 R 2; R 1和R 2是氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R3是氢或任选取代的低级烷基; R4是（CF3）n烷基，（CF3）n（取代烷基），（CF3）n烷基苯基，（CF3）n烷基（取代苯基）或（F）n环烷基; n = 1-3; 当Y = C时，R 5为氢，卤素，CF 3，与Y稠合的二烯，或Y = C时与Y稠合的取代二烯; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 且R 8为低级烷基，CF 3或任选取代的苯基。 还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。

公开(公告)号：US07547725B2

公开(公告)日：2009-06-16

申请号：US11818630

申请日：2007-06-15

Applicant: Anthony Frank Kreft ,  Lynn Resnick ,  Scott Christian Mayer ,  George Diamantidis ,  Derek Cecil Cole ,  Boyd Lynn Harrison ,  Minsheng Zhang ,  Molly Hoke ,  Tingzhong Wang ,  Rocco John Galante

Inventor： Anthony Frank Kreft ,  Lynn Resnick ,  Scott Christian Mayer ,  George Diamantidis ,  Derek Cecil Cole ,  Boyd Lynn Harrison ,  Minsheng Zhang ,  Molly Hoke ,  Tingzhong Wang ,  Rocco John Galante

IPC: A61K31/381 ,  C07D333/10 ,  C07D333/34

CPC classification number: C07D333/62 ,  C07D231/18 ,  C07D333/34

Abstract: Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substituted alkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substituted phenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y═C, or substituted diene fused to Y when Y═C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.

Abstract translation: 提供式（I）化合物，其中T是CHO，COR8或C（OH）R 1 R 2; R 1和R 2是氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R3是氢或任选取代的低级烷基; R4是（CF3）n烷基，（CF3）n（取代烷基），（CF3）n烷基苯基，（CF3）n烷基（取代苯基）或（F） n = 1-3; 当Y-C或Y-C与Y稠合时，R 5为氢，卤素，CF 3，二烯稠合至Y; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 且R 8为低级烷基，CF 3或任选取代的苯基。 还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。

公开(公告)号：US07300951B2

公开(公告)日：2007-11-27

申请号：US10810517

申请日：2004-03-26

Applicant: Anthony Frank Kreft ,  Lynn Resnick ,  Scott Christian Mayer ,  George Diamantidis ,  Derek Cecil Cole ,  Boyd Lynn Harrison ,  Minsheng Zhang ,  Molly Hoke ,  Tingzhong Wang ,  Rocco John Galante

Inventor： Anthony Frank Kreft ,  Lynn Resnick ,  Scott Christian Mayer ,  George Diamantidis ,  Derek Cecil Cole ,  Boyd Lynn Harrison ,  Minsheng Zhang ,  Molly Hoke ,  Tingzhong Wang ,  Rocco John Galante

IPC: A61K31/381 ,  C07D333/10 ,  C07D333/34

CPC classification number: C07D333/62 ,  C07D231/18 ,  C07D333/34

Abstract: Compounds of Formula (I), are provided where T is CHO, CON, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y═C, or substituted diene fused to Y when Y═C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.

Abstract translation: 提供式（I）的化合物，其中T是CHO，CON或C（OH）R 1 R 2 R 2; R 1和R 2均为氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R 3是氢或任选取代的低级烷基; R 4是（CF 3）n烷基，（CF 3 N）N（S） （取代的烷基），（CF 3）n烷基苯基，（CF 3）n烷基（取代的苯基）或（C 3 -C 6）烷基 （F）环烷基; n = 1-3; 当Y-C时，R 5是氢，卤素，CF 3 O，与Y稠合的二烯，或Y-C时与Y稠合的取代的二烯; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R 6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 和R 8是低级烷基，CF 3或任选取代的苯基。 还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。