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1. 发明授权

US6040316A 3-alkyl-3-phenyl-piperidines 失效
标题翻译： 3-烷基-3-苯基 - 哌啶
公开(公告)号：US6040316A
公开(公告)日：2000-03-21
申请号：US983584
申请日：1998-01-22
申请人： Michael Huai Gu Chen , Fu-Zon Chung , Helen Tsenwhei Lee
发明人： Michael Huai Gu Chen , Fu-Zon Chung , Helen Tsenwhei Lee
IPC分类号： C07D211/22 , C07D211/26 , C07D211/48 , C07D211/52 , C07D309/12 , C07D401/14 , C07D405/06 , A61K31/445 , C07D401/06
CPC分类号： C07D401/14 , C07D211/22 , C07D211/26 , C07D211/48 , C07D211/52 , C07D309/12 , C07D405/06
摘要： The small nonpeptides of the instant invention are tachykinin antagonists of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein: R.sub.1 is straight or branched alkyl of from 5 to 15 carbon atoms, aryl, or heteroaryl;R.sub.2 is hydrogen, hydroxy, amino, or thiol;R.sub.3 is aryl, arylsulfonylmethyl, or saturated or unsaturated heterocycle;R.sub.4 is from 1 to 4 groups each independently selected from halogen, alkyl, hydroxy, and alkoxy;n is an integer of from 2 to 6; and the carbon atom of (CH.sub.2).sub.n group can be replaced by oxygen, nitrogen, or sulphur. The compounds are highly selective and functional NK.sub.3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.
摘要翻译： PCT No.PCT / US97 / 15443 Sec。 371日期：1998年1月22日 102（e）日期1998年1月22日PCT 1997年9月2日PCT公布。第WO98 / 11090号公报 1998年3月19日本发明的小非肽是下式的速激肽拮抗剂或其药学上可接受的盐，其中：R 1为5至15个碳原子的直链或支链烷基，芳基或杂芳基; R2是氢，羟基，氨基或硫醇; R3是芳基，芳基磺酰基甲基或饱和或不饱和杂环; R 4为1至4个基团，各自独立地选自卤素，烷基，羟基和烷氧基; n为2-6的整数; （CH 2）n基团的碳原子可以被氧，氮或硫代替。这些化合物是高选择性和功能性的NK3拮抗剂，预期可用于治疗疼痛，抑郁症，焦虑症，恐慌症，精神分裂症，神经痛，成瘾症，炎性疾病，胃肠道疾病，血管疾病和神经病理学障碍。

2. 发明授权

US06017918A Phenyl glycine compounds and methods of treating atherosclerosis and restenosis 失效
标题翻译：苯基甘氨酸化合物和治疗动脉粥样硬化和再狭窄的方法
公开(公告)号：US06017918A
公开(公告)日：2000-01-25
申请号：US360556
申请日：1999-07-26
申请人： Helen Tsenwhei Lee , Mark Alan Massa , William Chester Patt , Bruce David Roth
发明人： Helen Tsenwhei Lee , Mark Alan Massa , William Chester Patt , Bruce David Roth
IPC分类号： C07C229/36 , C07D213/74 , C07D295/145 , C07D307/52 , C07D317/64 , C07D317/66 , C07D333/20 , A61K31/215 , A61K31/535 , C07D295/15
CPC分类号： C07D213/74 , C07C229/36 , C07D295/145 , C07D307/52 , C07D317/64 , C07D317/66 , C07D333/20 , C07C2101/02 , C07C2101/14
摘要： The present invention provides compounds having the Formula I ##STR1## The present invention also provides methods of treating atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.
摘要翻译：本发明提供具有式I的化合物本发明还提供使用式I化合物治疗动脉粥样硬化，冠心病和再狭窄的方法，以及包含式I化合物的药物组合物。

3. 发明授权

US06780883B2 Amide inhibitors of microsomal triglyceride transfer protein 失效
标题翻译：微粒体甘油三酯转移蛋白的酰胺抑制剂
公开(公告)号：US06780883B2
公开(公告)日：2004-08-24
申请号：US10021633
申请日：2001-12-12
申请人： Richard John Booth , Helen Tsenwhei Lee , Jason Keith Pontrello , Randy Ranjee Ramharack , Bruce David Roth
发明人： Richard John Booth , Helen Tsenwhei Lee , Jason Keith Pontrello , Randy Ranjee Ramharack , Bruce David Roth
IPC分类号： A61K3144
CPC分类号： C07D213/40 , C07D213/75 , C07D215/38 , C07D333/38 , C07D405/12 , C07D409/12
摘要： The present invention provides compounds having the Formula I The present invention also provides pharmaceutical compositions comprising a compound of Formula I and methods of treatment of atherosclerosis, obesity, restenosis, coronary heart disease, hyperlipoproteinemia, hypercholesterolemia, and hypertriglyceridemia.
摘要翻译：本发明提供了具有式I的化合物本发明还提供包含式I化合物和治疗动脉粥样硬化，肥胖症，再狭窄，冠心病，高脂蛋白血症，高胆固醇血症和高甘油三酯血症的药物组合物。

4. 发明授权

US06506751B1 Thiazolidinone compounds useful as chemokine inhibitors 有权
标题翻译：可用作趋化因子抑制剂的噻唑烷酮化合物
公开(公告)号：US06506751B1
公开(公告)日：2003-01-14
申请号：US09705219
申请日：2000-11-02
申请人： Stephanie Elizabeth Ault Justus , Helen Tsenwhei Lee , Jason Keith Pontrello , Bruce David Roth , Karen Elaine Sexton , Michael William Wilson
发明人： Stephanie Elizabeth Ault Justus , Helen Tsenwhei Lee , Jason Keith Pontrello , Bruce David Roth , Karen Elaine Sexton , Michael William Wilson
IPC分类号： C07D41306
CPC分类号： C07D417/04 , C07D277/34 , C07D417/06
摘要： Disclosed are compounds of the Formula I wherein: Z is C or nothing, provided that when Z is nothing, R3 and R4 are nothing; A is S, S═O or O═S═O; R1 and R2 are independently hydrogen, lower alkyl, halogen, hydroxy or lower alkoxy, (un)substituted aryl, (un)substituted arylalkyl, (un)substituted heteroaryl or(un)substituted heteroarylakyl; R3 and R4 independently represent hydrogen, lower alkyl, cycloalkyl, aminoalkyl, mono- or dialkylaminoalkyl, (un)substituted aryl or (un)substituted heteroaryl; R5 represents a (un)substituted carbocyclic group containing from 3-7 members, up to two of which members are optionally hetero atoms; or R5 is (CR6R7)—(CH2)n—XR8R9; X is S or N; R6, R7, R8, R9, and n are as defined in the specification. The compounds are useful in the treatment and prevention of the AIDS virus. Intermediates useful in the preparation of the final products, pharmaceutical compositions containing the final products are also taught.
摘要翻译：公开了式I的化合物，其中Z为C或无，条件是当Z不为任何时，R 3和R 4不为任何; A为S，S = O或O = S = O; R 1和R 2独立地为氢，低级烷基，卤素，羟基或低级烷氧基，（未）取代的芳基，（未）取代的芳基烷基，（未）取代的杂芳基或（未）取代的杂芳基; R3和R4独立地表示氢，低级烷基，环烷基，氨基烷基，，（un）取代的芳基或（未）取代的杂芳基; R 5表示含有3-7个成员的（未）取代的碳环基，其中至多两个为任意的杂原子; 或R 5是（CR 6 R 7） - （CH 2）n -XR 8 R 9; X是S或N; R 6，R 7，R 8，R 9和n如说明书中所定义。该化合物可用于治疗和预防艾滋病毒。还教导了用于制备最终产品的中间体，含有最终产品的药物组合物。

5. 发明授权

US08466165B2 4-phenylamino-quinazolin-6-yl-amides 有权
标题翻译： 4-苯基氨基 - 喹唑啉-6-基 - 酰胺
公开(公告)号：US08466165B2
公开(公告)日：2013-06-18
申请号：US12754556
申请日：2010-04-05
申请人： Stephen Alan Fakhoury , Helen Tsenwhei Lee , Jessica Elizabeth Reed , Kevin Matthew Schlosser , Karen Elaine Sexton , Haile Tecle , Roy Thomas Winters
发明人： Stephen Alan Fakhoury , Helen Tsenwhei Lee , Jessica Elizabeth Reed , Kevin Matthew Schlosser , Karen Elaine Sexton , Haile Tecle , Roy Thomas Winters
IPC分类号： A61K31/517 , A01N43/90 , C07D239/72
CPC分类号： C07D239/94 , C07D401/12 , C07D403/12
摘要： This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) —(CH2)n-morpholino, —(CH2)n-piperidine, —(CH2)n-piperazine, —(CH2)n-piperazine-N(C1-C3 alkyl), —(CH2)n-pyrrolidine, or —(CH2)n-imidazole; n is 1 to 4; R4 is —(CH2)m-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C1-C3 alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N(C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.
摘要翻译：本发明提供下式的喹唑啉化合物：其中：R1是卤素; R2是H或卤素; R3是a）任选被卤素取代的C 1 -C 3烷基; 或（b） - （CH 2）n - 吗啉代， - （CH 2）n - 哌啶， - （CH 2）n - 哌嗪， - （CH 2）n - 哌嗪-N（C 1 -C 3烷基）， - （CH 2），或 - （CH 2）n - 咪唑; n为1〜4; R4是 - （CH2）m-Het; Het是吗啉，哌啶，哌嗪，哌嗪-N（C 1 -C 3烷基），咪唑，吡咯烷，氮杂环庚烷，3,4-二氢-2H-吡啶或3,6-二氢-2H-吡啶，各自任选被烷基，卤素，OH，NH 2，NH（C 1 -C 3烷基）或N（C 1 -C 3烷基）2; m为1-3; X为O，S或NH; 或其药学上可接受的盐，以及制备它们的方法和中间体化合物，有用的药物组合物和使用该化合物治疗增殖性疾病的方法。

6. 发明授权

US06458815B2 Sulfonamide compounds and methods of treating atherosclerosis and restenosis 失效
标题翻译：磺酰胺化合物和治疗动脉粥样硬化和再狭窄的方法
公开(公告)号：US06458815B2
公开(公告)日：2002-10-01
申请号：US09835239
申请日：2001-04-13
申请人： Helen Tsenwhei Lee , Randy Ranjee Ramharack , Bruce David Roth , Karen Elaine Sexton
发明人： Helen Tsenwhei Lee , Randy Ranjee Ramharack , Bruce David Roth , Karen Elaine Sexton
IPC分类号： A61K314436
CPC分类号： C07D213/76 , C07C311/13 , C07C2601/14 , C07D409/12 , C07D409/14
摘要： The present invention provides compounds having the Formula I The present invention also provides methods of treating or preventing atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.
摘要翻译：本发明提供具有式I的化合物本发明还提供使用式I化合物治疗或预防动脉粥样硬化，冠心病和再狭窄的方法，以及包含式I化合物的药物组合物。

7. 发明授权

US5786335A Sulfhydryl containing peptides for treating vascular disease 失效
标题翻译：含巯基的肽用于治疗血管疾病
公开(公告)号：US5786335A
公开(公告)日：1998-07-28
申请号：US744698
申请日：1996-10-31
申请人： Wayne Livingston Cody , Helen Tsenwhei Lee , Randy Ranjee Ramharack , Bruce David Roth , Tomi Sawyer , Drago Robert Sliskovic
发明人： Wayne Livingston Cody , Helen Tsenwhei Lee , Randy Ranjee Ramharack , Bruce David Roth , Tomi Sawyer , Drago Robert Sliskovic
IPC分类号： A61K38/00 , C07K5/06 , C07K5/083 , C07K5/103 , C07K7/06 , C07K5/00 , C07K7/00 , C07K16/00
CPC分类号： C07K7/06 , C07K5/06026 , C07K5/081 , C07K5/1008 , C07K5/1013 , A61K38/00
摘要： Sulfhydryl containing peptides having the formula X--A.sub.1 --A.sub.2 --A.sub.3 --A.sub.4 --A.sub.5 --Y inhibit the formation of Lp(a) and thus are useful for treating vascular diseases such as coronary heart disease, myocardial infarction, ischemic stroke, cervical atherosclerosis, cerebral infarction, and restenosis.
摘要翻译：具有式X-A1-A2-A3-A4-A5-Y的含巯基的肽抑制Lp（a）的形成，因此可用于治疗血管疾病如冠心病，心肌梗塞，缺血性中风，颈动脉粥样硬化，脑梗死和再狭窄。

8. 发明授权

US07772243B2 4-phenylamino-quinazolin-6-yl-amides 有权
标题翻译： 4-苯基氨基 - 喹唑啉-6-基 - 酰胺
公开(公告)号：US07772243B2
公开(公告)日：2010-08-10
申请号：US11122345
申请日：2005-05-05
申请人： Stephen Alan Fakhoury , Helen Tsenwhei Lee , Jessica Elizabeth Reed , Kevin Matthew Schlosser , Karen Elaine Sexton , Haile Tecle , Roy Thomas Winters
发明人： Stephen Alan Fakhoury , Helen Tsenwhei Lee , Jessica Elizabeth Reed , Kevin Matthew Schlosser , Karen Elaine Sexton , Haile Tecle , Roy Thomas Winters
IPC分类号： A61K31/517 , C07D239/94 , C07D413/12
CPC分类号： C07D239/94 , C07D401/12 , C07D403/12
摘要： This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) —(CH2)n-morpholino, —(CH2)n-piperidine, —(CH2)n-piperazine, —(CH2)n—-piperazine-N(C1-C3 alkyl), —(CH2)n-pyrrolidine, or —(CH2)n-imidazole; n is 1 to 4; R4 is —(CH2)m-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C1-C3 alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N (C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.
摘要翻译：本发明提供下式的喹唑啉化合物：其中：R1是卤素; R2是H或卤素; R3是a）任选被卤素取代的C 1 -C 3烷基; 或（b） - （CH 2）n - 吗啉代， - （CH 2）n - 哌啶， - （CH 2）n - 哌嗪， - （CH 2）n - 哌嗪-N（C 1 -C 3烷基）吡咯烷或 - （CH 2）n - 咪唑; n为1〜4; R4是 - （CH2）m-Het; Het是吗啉，哌啶，哌嗪，哌嗪-N（C 1 -C 3烷基），咪唑，吡咯烷，氮杂环庚烷，3,4-二氢-2H-吡啶或3,6-二氢-2H-吡啶，各自任选被烷基，卤素，OH，NH 2，NH（C 1 -C 3烷基）或N（C 1 -C 3烷基）2; m为1-3; X为O，S或NH; 或其药学上可接受的盐，以及制备它们的方法和中间体化合物，有用的药物组合物和使用该化合物治疗增殖性疾病的方法。

9. 发明申请

US20100190977A1 4-PHENYLAMINO-QUINAZOLIN-6-YL-AMIDES 有权
标题翻译： 4-苯基氨基 - 喹唑啉-6-基酰胺
公开(公告)号：US20100190977A1
公开(公告)日：2010-07-29
申请号：US12754556
申请日：2010-04-05
申请人： Stephen Alan Fakhoury , Helen Tsenwhei Lee , Jessica Elizabeth Reed , Kevin Matthew Schlosser , Karen Elaine Sexton , Haile Tecle , Roy Thomas Winters
发明人： Stephen Alan Fakhoury , Helen Tsenwhei Lee , Jessica Elizabeth Reed , Kevin Matthew Schlosser , Karen Elaine Sexton , Haile Tecle , Roy Thomas Winters
IPC分类号： C07D403/12 , C07D401/12 , C07D413/14
CPC分类号： C07D239/94 , C07D401/12 , C07D403/12
摘要： This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) —(CH2)n-morpholino, —(CH2)n-piperidine, —(CH2)n-piperazine, —(CH2)n-piperazine-N(C1-C3 alkyl), —(CH2)n-pyrrolidine, or —(CH2)n-imidazole; n is 1 to 4; R4 is —(CH2)m-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C1-C3 alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N(C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.
摘要翻译：本发明提供下式的喹唑啉化合物：其中：R1是卤素; R2是H或卤素; R3是a）任选被卤素取代的C 1 -C 3烷基; 或（b） - （CH 2）n - 吗啉代， - （CH 2）n - 哌啶， - （CH 2）n - 哌嗪， - （CH 2）n - 哌嗪-N（C 1 -C 3烷基）， - （CH 2），或 - （CH 2）n - 咪唑; n为1〜4; R4是 - （CH2）m-Het; Het是吗啉，哌啶，哌嗪，哌嗪-N（C 1 -C 3烷基），咪唑，吡咯烷，氮杂环庚烷，3,4-二氢-2H-吡啶或3,6-二氢-2H-吡啶，各自任选被烷基，卤素，OH，NH 2，NH（C 1 -C 3烷基）或N（C 1 -C 3烷基）2; m为1-3; X为O，S或NH; 或其药学上可接受的盐，以及制备它们的方法和中间体化合物，有用的药物组合物和使用该化合物治疗增殖性疾病的方法。

10. 发明授权

US5929091A Method of lowering plasma levels of lipoprotein(a) 失效
标题翻译：降低脂蛋白血浆水平的方法（a）
公开(公告)号：US5929091A
公开(公告)日：1999-07-27
申请号：US166678
申请日：1998-10-05
申请人： Helen Tsenwhei Lee , Randy Ranjee Ramharack
发明人： Helen Tsenwhei Lee , Randy Ranjee Ramharack
IPC分类号： A61K31/454 , A61K31/445
CPC分类号： A61K31/454
摘要： The present invention comprises a method of lowering plasma levels of Lp(a) in animals by administering an effective Lp(a)-reducing amount of a microsomal triglyceride transfer protein inhibitor of the structural formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is alkyl, alkenyl alkynyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, cycloalkyl, or cycloalkylalkyl, each of which is independently optionally substituted through available carbon atoms with 1, 2, or 3 groups selected from halo, alkyl, alkenyl, alkoxy, aryloxy, aryl, arylalkyl, alkylmercapto, arylmercapto, cycloalkyl, cycloalkylalkyl, heteroaryl, and heteroarylalkyl. By lowering Lp(a) levels, the animals are protected against developing premature atherosclerosis and consequent cardiovascular and cerebrovascular diseases.
摘要翻译：本发明包括通过施用有效的Lp（a）减少量的结构式的微粒体甘油三酯转运蛋白抑制剂或其药学上可接受的盐来降低动物中的血浆Lp（a）水平的方法，其中R1是烷基，烯基炔基，芳基，杂芳基，芳基烷基，杂芳基烷基，环烷基或环烷基烷基，其各自独立地通过可用的碳原子任选被1,2或3个选自卤素，烷基，烯基，烷氧基，芳氧基，芳基，芳基烷基，烷基巯基，芳基巯基，环烷基，环烷基烷基，杂芳基和杂芳基烷基。通过降低Lp（a）水平，动物被保护免于发展过早的动脉粥样硬化和随之而来的心血管和脑血管疾病。

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