公开(公告)号：US06821963B2

公开(公告)日：2004-11-23

申请号：US10163890

申请日：2002-06-04

Applicant: Stephen Douglas Barrett ,  Alexander James Bridges ,  Annette Marian Doherty ,  David Thomas Dudley ,  Alan Robert Saltiel ,  Haile Tecle

Inventor： Stephen Douglas Barrett ,  Alexander James Bridges ,  Annette Marian Doherty ,  David Thomas Dudley ,  Alan Robert Saltiel ,  Haile Tecle

IPC: A61K31397

CPC classification number: C07D295/088 ,  C07C259/10 ,  C07D211/22 ,  C07D213/30 ,  C07D307/42 ,  C07D309/06 ,  C07D333/16

Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.

Abstract translation: 其中R 1，R 2，R 3，R 4，R 5和R 6是氢或取代基如烷基，且其中R 7是氢或有机基团的式（I）的苯基氨基苯并肟酸衍生物是MEK的有效抑制剂 ，有效治疗癌症和其他增殖性疾病如牛皮癣和再狭窄。

公开(公告)号：US06750217B2

公开(公告)日：2004-06-15

申请号：US10198561

申请日：2002-07-18

Applicant: Stephen Douglas Barrett ,  Haile Tecle ,  Richard John Booth

Inventor： Stephen Douglas Barrett ,  Haile Tecle ,  Richard John Booth

IPC: A61K31535

CPC classification number: C07C311/39 ,  C07C2601/02

Abstract: Benzenesulfonamides of formula (I), in which W is OR1, NR2OR1, NRARB, NR2NRARB, or NR2(CH2)2-4NRARB and the other variables as defined in the claims, are inhibitors of MEK and are effective in the treatment of proliferative diseases, cancer, stroke, heart failure, xenograft rejection, arthritis, cystic fibrosis, hepatomegaly, cardiomegaly, Alzheimer's disease, complications of diabetes, septic shock, and viral infection.

Abstract translation: 其中W是OR1，NR2OR1，NRARB，NR2NRARB或NR2（CH2）2-4NRARB的式（I）的苯磺酰胺和权利要求中定义的其它变量是MEK的抑制剂，并且在治疗增殖性疾病中是有效的 ，癌症，中风，心力衰竭，异种移植排斥，关节炎，囊性纤维化，肝肿大，心脏肥大，阿尔茨海默病，糖尿病并发症，败血性休克和病毒感染。

公开(公告)号：US06492363B2

公开(公告)日：2002-12-10

申请号：US09931596

申请日：2001-08-16

Applicant: Stephen Douglas Barrett ,  Alexander James Bridges ,  Donna Reynolds Cody ,  Annette Marian Doherty ,  David Thomas Dudley ,  Alan Robert Saltiel ,  Mel Conrad Schroeder ,  Haile Tecle

Inventor： Stephen Douglas Barrett ,  Alexander James Bridges ,  Donna Reynolds Cody ,  Annette Marian Doherty ,  David Thomas Dudley ,  Alan Robert Saltiel ,  Mel Conrad Schroeder ,  Haile Tecle

IPC: A61K31535

CPC classification number: C07D213/40 ,  C07C215/68 ,  C07C229/58 ,  C07C237/08 ,  C07C237/16 ,  C07C237/20 ,  C07C237/30 ,  C07C237/32 ,  C07C237/36 ,  C07C237/38 ,  C07C239/22 ,  C07C243/38 ,  C07C311/44 ,  C07C2601/02 ,  C07C2601/14 ,  C07D257/04 ,  C07D257/06 ,  C07D295/13 ,  C07D295/155 ,  C07D295/32 ,  C07D333/20

Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, and Z is COOR7, tetrazolyl, CONR6R7, or CH2OR7, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as inflammation, psoriasis and restenosis, as well as stroke, heart failure, and immunodeficiency disorders.

Abstract translation: 式R 1，R 2，R 3，R 4，R 5和R 6的苯基氨基苯甲酸，苯甲酰胺和苄醇衍生物是氢或取代基如烷基，其中R 7是氢或有机基团，Z是COOR 7，四唑基 ，CONR6R7或CH2OR7是MEK的有效抑制剂，因此在治疗癌症和其它增殖性疾病如炎症，牛皮癣和再狭窄以及中风，心力衰竭和免疫缺陷障碍中是有效的。

公开(公告)号：US06469004B1

公开(公告)日：2002-10-22

申请号：US09889059

申请日：2001-07-11

Applicant: Stephen Barrett ,  Haile Tecle ,  Alexander J. Bridges

Inventor： Stephen Barrett ,  Haile Tecle ,  Alexander J. Bridges

IPC: C07D23506

CPC classification number: C07D235/06 ,  C07D235/12 ,  C07D235/14 ,  C07D241/42 ,  C07D249/18 ,  C07D263/56 ,  C07D271/12 ,  C07D277/62 ,  C07D285/14

Abstract: The invention provides compounds having formula (I), wherein W is OH, or derivatives of the carboxylic acid, and Q is a heterocyclo-condensed ortho-phenylene residue. These compounds are useful as MEK inhibitors, particularly in the treatment of proliferative diseases such as cancer.

Abstract translation: 本发明提供了具有式（I）的化合物，其中W是OH或羧酸的衍生物，Q是杂环稠合的邻 - 苯基残基。 这些化合物可用作MEK抑制剂，特别是用于治疗增殖性疾病例如癌症。

公开(公告)号：US5482938A

公开(公告)日：1996-01-09

申请号：US189620

申请日：1994-02-01

Applicant: David J. Lauffer ,  Walter H. Moos ,  Michael R. Pavia ,  Haile Tecle ,  Anthony J. Thomas

Inventor： David J. Lauffer ,  Walter H. Moos ,  Michael R. Pavia ,  Haile Tecle ,  Anthony J. Thomas

IPC: A61K31/395 ,  A61K31/397 ,  A61K31/40 ,  A61K31/407 ,  A61K31/435 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/46 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/28 ,  A61P43/00 ,  C07D205/06 ,  C07D207/22 ,  C07D211/72 ,  C07D223/06 ,  C07D225/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D451/02 ,  C07D451/04 ,  C07D451/06 ,  C07D451/10 ,  C07D453/02 ,  C07D471/08 ,  C07D487/08 ,  A61K31/535 ,  C07D413/00

CPC classification number: C07D487/08 ,  C07D211/72 ,  C07D451/04 ,  C07D453/02

Abstract: Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds are disclosed which are azabicyclo[2.2.2]oximes, azabicyclo[2.2.2]-amines, azabicyclo[3.2.1]oximes and amine containing heterocyclic oximes wherein the heterocyclic ring contains from 3 to 7 carbon atoms.

Abstract translation: 公开了含有有机氮的环状肟和胺取代的化合物，其是氮杂双环[2.2.2]肟，氮杂双环[2.2.2] - 胺，氮杂双环[3.2.1]肟和含胺杂环肟，其中杂环包含3 至7个碳原子。

公开(公告)号：US4996201A

公开(公告)日：1991-02-26

申请号：US388777

申请日：1989-08-02

Applicant: Stephen C. Bergmeier ,  Jeffrey A. Kester ,  Walter H. Moos ,  Haile Tecle ,  Anthony J. Thomas

Inventor： Stephen C. Bergmeier ,  Jeffrey A. Kester ,  Walter H. Moos ,  Haile Tecle ,  Anthony J. Thomas

IPC: A61K31/27 ,  A61K31/40 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61P25/02 ,  A61P25/28 ,  C07C271/20 ,  C07C271/24 ,  C07C271/28 ,  C07C333/04 ,  C07D205/04 ,  C07D211/14 ,  C07D211/22 ,  C07D295/12 ,  C07D295/125

CPC classification number: C07D295/125 ,  C07C271/20 ,  C07D205/04

Abstract: 4-(N-Substituted amino)-2-butynyl-1-carbamates and thiocarbamates and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.

公开(公告)号：US4786648A

公开(公告)日：1988-11-22

申请号：US91893

申请日：1987-09-04

Applicant: Stephen C. Bergmeier ,  David A. Downs ,  Walter H. Moos ,  David W. Moreland ,  Haile Tecle

Inventor： Stephen C. Bergmeier ,  David A. Downs ,  Walter H. Moos ,  David W. Moreland ,  Haile Tecle

IPC: C07D211/70 ,  A61K31/44

CPC classification number: C07D211/70

Abstract: Certain O-substituted-1,2,5,6-tetrahydro-3- or 1,2,3,6-tetrahydro-4-pyridine oximes are useful as agents for treating pain or for treating the symptoms of senile cognitive decline.

Abstract translation: 某些O-取代-1,2,5,6-四氢-3-或1,2,3,6-四氢-4-吡啶肟可用作治疗疼痛或治疗老年认知衰退症状的药剂。

公开(公告)号：US07160915B2

公开(公告)日：2007-01-09

申请号：US10897464

申请日：2004-07-22

Applicant: Stephen Douglas Barrett ,  Cathlin Marie Flamme ,  Michael David Kaufman ,  Jared Bruce John Milbank ,  Haile Tecle ,  Joseph Scott Warmus

Inventor： Stephen Douglas Barrett ,  Cathlin Marie Flamme ,  Michael David Kaufman ,  Jared Bruce John Milbank ,  Haile Tecle ,  Joseph Scott Warmus

IPC: A61K31/4184 ,  C07D235/22 ,  C07D235/06

CPC classification number: C07D235/06 ,  C07D235/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04

Abstract: The present invention relates to N-methyl-substituted benzamidazole derivatives of formula (I): as defined in the specification; pharmaceutical compositions and methods of use thereof.

Abstract translation: 本发明涉及式（I）的N-甲基取代的苯甲胺唑衍生物：如说明书中所定义; 药物组合物及其使用方法。

公开(公告)号：US07078438B2

公开(公告)日：2006-07-18

申请号：US11051142

申请日：2005-02-04

Applicant: Gordon William Rewcastle ,  Julie Ann Spicer ,  Stephen Douglas Barrett ,  Michael David Kaufman ,  Jared Bruce John Milbank ,  Haile Tecle

Inventor： Gordon William Rewcastle ,  Julie Ann Spicer ,  Stephen Douglas Barrett ,  Michael David Kaufman ,  Jared Bruce John Milbank ,  Haile Tecle

IPC: A61K31/165

CPC classification number: C07C317/36 ,  C07C259/10 ,  C07C323/36 ,  Y10S514/825

Abstract: The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.

Abstract translation: 本发明涉及4-取代苯基氨基苯并肟酸衍生物的氧化酯，药物组合物及其使用方法。

公开(公告)号：US07001905B2

公开(公告)日：2006-02-21

申请号：US10221522

申请日：2001-03-12

Applicant: Cathlin Biwersi ,  Haile Tecle ,  Joseph Scott Warmus

Inventor： Cathlin Biwersi ,  Haile Tecle ,  Joseph Scott Warmus

IPC: C07D265/22 ,  C07C237/30 ,  C07C237/32 ,  A61K31/536 ,  A61K31/166

CPC classification number: C07C237/30 ,  C07C237/32 ,  C07C237/34 ,  C07C259/10 ,  C07C2601/02 ,  C07C2601/14 ,  C07D265/22 ,  C07D295/13 ,  C07D295/192 ,  C07D295/26 ,  C07D413/12

Abstract: Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.

Abstract translation: 二芳基胺，例如式（I）或式（II）的5-酰胺取代的二芳基胺，其中A是羟基，C 1-6烷氧基或NR 6或 > 7 ; X是OR 12，NR 13 R 12或NR 14; MEK抑制剂可用于治疗各种增生性疾病状态，例如与MEK的多动症有关的病症以及由MEK级联调节的疾病。