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1. 发明申请

US20050282886A1 Lactam tachykinin receptor antagonists 失效
标题翻译：内酰胺速激肽受体拮抗剂
公开(公告)号：US20050282886A1
公开(公告)日：2005-12-22
申请号：US11135240
申请日：2005-05-23
申请人： Paul Finke , Laura Meurer , Sander Mills
发明人： Paul Finke , Laura Meurer , Sander Mills
IPC分类号： A61K31/4015 , C07D207/12 , C07D207/26 , C07D207/27 , C07D207/273
CPC分类号： C07D207/27 , C07D207/273
摘要： The present invention is directed to certain lactam compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
摘要翻译：本发明涉及可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的某些内酰胺化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂和使用化合物及其制剂治疗某些疾病，包括呕吐，尿失禁，抑郁和焦虑。

2. 发明申请

US20050182103A1 Substituted 2,3-diphenyl pyridines 失效
标题翻译：取代的2,3-二苯基吡啶
公开(公告)号：US20050182103A1
公开(公告)日：2005-08-18
申请号：US10508043
申请日：2003-03-24
申请人： Paul Finke , Laura Meurer , John Debenham , Richard Toupence , Thomas Walsh
发明人： Paul Finke , Laura Meurer , John Debenham , Richard Toupence , Thomas Walsh
IPC分类号： C07D213/64 , A61K31/44 , A61K31/4418 , A61K31/4439 , A61K31/4545 , A61K31/455 , A61K31/496 , A61K31/5377 , A61K45/00 , A61K47/02 , A61K47/10 , A61K47/26 , A61K47/34 , A61P1/04 , A61P1/10 , A61P1/16 , A61P3/04 , A61P9/00 , A61P11/06 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P29/00 , A61P43/00 , C07D213/56 , C07D213/65 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/85 , C07D213/86 , C07D213/87 , C07D401/12 , C07D41/02
CPC分类号： C07D213/79 , C04B35/632 , C07D213/65 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/85 , C07D213/86 , C07D213/87 , C07D401/12
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管事故和头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

3. 发明授权

US5750549A Cycloalkyl tachykinin receptor antagonists 失效
标题翻译：环烷基速激肽受体拮抗剂
公开(公告)号：US5750549A
公开(公告)日：1998-05-12
申请号：US730277
申请日：1996-10-15
申请人： Charles G. Caldwell , Ping Chen , Philippe L. Durette , Paul Finke , Jeffrey Hale , Edward Holson , Ihor Kopka , Malcolm MacCoss , Laura Meurer , Sander G. Mills , Albert Robichaud
发明人： Charles G. Caldwell , Ping Chen , Philippe L. Durette , Paul Finke , Jeffrey Hale , Edward Holson , Ihor Kopka , Malcolm MacCoss , Laura Meurer , Sander G. Mills , Albert Robichaud
IPC分类号： C07C69/757 , C07C217/52 , C07C237/06 , C07C255/59 , C07D207/08 , C07D207/16 , C07D207/26 , C07D213/30 , C07D213/38 , C07D213/61 , C07D215/18 , C07D215/20 , C07D233/70 , C07D239/26 , C07D249/08 , C07D249/12 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/28 , C07D277/64 , C07D307/12 , C07D307/82 , C07D333/20 , C07D333/32 , C07D333/64 , C07D401/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D513/04 , C07D521/00 , A61K31/41
CPC分类号： C07D207/26 , C07C217/52 , C07C237/06 , C07C255/59 , C07C69/757 , C07D207/08 , C07D207/16 , C07D213/30 , C07D213/38 , C07D213/61 , C07D215/18 , C07D215/20 , C07D231/12 , C07D233/56 , C07D233/70 , C07D239/26 , C07D249/08 , C07D249/12 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/28 , C07D277/64 , C07D307/12 , C07D307/82 , C07D333/20 , C07D333/32 , C07D333/64 , C07D401/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D513/04 , C07C2101/08 , C07C2101/14
摘要： The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, A, Q, W, X, Y, Z and n are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
摘要翻译：本发明涉及由结构式I表示的某些新化合物：其中R3，R6，R7，R8，R11，R12，R13，A，Q，W，X，Y，Z和n如本文所定义。本发明还涉及包含这些新化合物作为活性成分的药物制剂，以及新型化合物及其制剂在治疗某些疾病中的用途。本发明化合物是速激肽受体拮抗剂，可用于治疗炎性疾病，疼痛或偏头痛，哮喘和呕吐。

4. 发明申请

US20060089356A1 Substituted imidazoles as cannabinoid receptor modulators 失效
公开(公告)号：US20060089356A1
公开(公告)日：2006-04-27
申请号：US11265850
申请日：2005-11-03
申请人： Paul Finke , Sander Mills , Christopher Plummer , Shrenik Shah , Quang Truong
发明人： Paul Finke , Sander Mills , Christopher Plummer , Shrenik Shah , Quang Truong
IPC分类号： A61K31/5377 , A61K31/454 , A61K31/4172 , A61K31/4178 , C07D413/02 , C07D403/02
CPC分类号： C07D405/12 , C07D233/90
摘要： The use of compounds of the present invention as antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor particularly in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB1) receptor. The invention is concerned with the use of these novel compounds to selectively antagonize the Cannabinoid-1 (CB1) receptor. As such, compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith. Novel compounds of structural formula (I) are also claimed.

5. 发明申请

US20050070609A1 Cyclopentyl modulators of chemokine receptor activity 失效
标题翻译：趋化因子受体活性的环戊基调节剂
公开(公告)号：US20050070609A1
公开(公告)日：2005-03-31
申请号：US10901414
申请日：2004-07-28
申请人： Paul Finke , Jennifer Loebach , Kerry Parker , Christopher Plummer , Sander Mills
发明人： Paul Finke , Jennifer Loebach , Kerry Parker , Christopher Plummer , Sander Mills
IPC分类号： A61K31/19 , C07D471/10 , C07D471/20 , C07D491/10 , C07D491/20 , C07D498/10
CPC分类号： C07D471/10 , C07D471/20 , C07D491/10 , C07D491/20 , C07D498/10
摘要： Cyclopentyl compounds of Formula (I) are modulators of chemokine receptor activity: wherein D, G, R2, R3 and R8 in Formula (I) are defined herein. The compounds, and pharmaceutically acceptable salts and individual diastereomers thereof, are useful in the treatment and prevention of HIV infection, in delaying the onset of AIDS, and in the treatment of AIDS. The compounds are also useful for treating other diseases and conditions mediated by chemokine receptors.
摘要翻译：式（I）的环戊基化合物是趋化因子受体活性的调节剂：其中式（I）中的D，G，R 2，R 3和R 8在本文中定义。化合物及其药学上可接受的盐和单独的非对映异构体可用于治疗和预防艾滋病毒感染，延缓艾滋病的发病和艾滋病的治疗。该化合物也可用于治疗趋化因子受体介导的其它疾病和病症。

6. 发明授权

US5952321A Substituted azetidinones as anti-inflammatory and antidegenerative agents 失效
标题翻译：取代的氮杂环丁酮作为抗炎和抗再生剂
公开(公告)号：US5952321A
公开(公告)日：1999-09-14
申请号：US764775
申请日：1996-12-12
申请人： James Doherty , Conrad Dorn , Philippe Durette , Paul Finke , Malcolm Maccoss , Sander Mills , Shrenik Shah , Soumya Sahoo , William Hagmann , Scott Polo
发明人： James Doherty , Conrad Dorn , Philippe Durette , Paul Finke , Malcolm Maccoss , Sander Mills , Shrenik Shah , Soumya Sahoo , William Hagmann , Scott Polo
IPC分类号： A61K31/395 , A61K31/397 , A61K31/40 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54 , A61P29/00 , C07D205/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
CPC分类号： C07D401/12 , C07D205/08 , C07D403/12 , C07D405/12
摘要： New substituted azetidinones of the general Formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described, wherein n is
摘要翻译：描述了已经被发现是有效的弹性蛋白酶抑制剂和由此有用的抗炎和抗代谢剂的通式（I）的新的取代的氮杂环丁酮，其中n为0

7. 发明授权

US5877191A Phenyl spiroethercycloalkyl tachykinin receptor antagonists 失效
标题翻译：苯基螺醚醚环烷基速激肽受体拮抗剂
公开(公告)号：US5877191A
公开(公告)日：1999-03-02
申请号：US955898
申请日：1997-10-22
申请人： Charles G. Caldwell , Yuan-Ching Chiang , Conrad Dorn , Paul Finke , Jeffrey Hale , Malcolm Maccoss , Sander Mills , Albert Robichaud
发明人： Charles G. Caldwell , Yuan-Ching Chiang , Conrad Dorn , Paul Finke , Jeffrey Hale , Malcolm Maccoss , Sander Mills , Albert Robichaud
IPC分类号： C07D307/94 , C07D405/10 , C07D405/12 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12 , A61K31/36 , C07D285/04 , C07D311/96
CPC分类号： C07D307/94 , C07D405/10 , C07D405/12 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12
摘要： The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
摘要翻译：本发明涉及由结构式I表示的某些新化合物：其中R3，R6，R7，R8，R11，R12，R13，m，n和虚线在本文中定义。本发明还涉及包含这些新化合物作为活性成分的药物制剂，以及新型化合物及其制剂在治疗某些疾病中的用途。本发明化合物是速激肽受体拮抗剂，可用于治疗炎性疾病，疼痛或偏头痛，哮喘和呕吐。

8. 发明授权

US5747485A Substituted azetidiones as anti-inflammatory and antidegenerative agents 失效
标题翻译：取代的氮杂环丁酮作为抗炎剂和抗再生剂
公开(公告)号：US5747485A
公开(公告)日：1998-05-05
申请号：US848076
申请日：1997-06-05
申请人： James Doherty , Conrad Dorn , Philippe Durette , Paul Finke , Malcolm Maccoss , Sander Mills , Shrenik Shah , Soumya Sahoo , William Hagmann , Jeffrey Hale , Thomas Lanza
发明人： James Doherty , Conrad Dorn , Philippe Durette , Paul Finke , Malcolm Maccoss , Sander Mills , Shrenik Shah , Soumya Sahoo , William Hagmann , Jeffrey Hale , Thomas Lanza
IPC分类号： A61K31/397 , A61K31/496 , A61K31/5377 , A61K31/395
CPC分类号： A61K31/496 , A61K31/397 , A61K31/5377
摘要： Substituted azetidinones are herein disclosed for use in the treatment of various elastase-mediated diseases.
摘要翻译：本文公开了取代的氮杂环丁酮，用于治疗各种弹性蛋白酶介导的疾病。

9. 发明授权

US5719149A Morpholine derivatives and their use as therapeutic agents 失效
标题翻译：吗啉衍生物及其作为治疗剂的用途
公开(公告)号：US5719149A
公开(公告)日：1998-02-17
申请号：US793573
申请日：1997-02-27
申请人： Paul Finke , Timothy Harrison , Richard Thomas Lewis , Angus Murray MacLeod , Andrew Pate Owens
发明人： Paul Finke , Timothy Harrison , Richard Thomas Lewis , Angus Murray MacLeod , Andrew Pate Owens
IPC分类号： A61K31/535 , A61K31/5375 , A61P1/08 , A61P25/04 , A61P29/00 , A61P43/00 , C07D265/32 , C07D413/06
CPC分类号： C07D413/06 , C07D265/32
摘要： The present invention relates to compounds of formula (I) wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are selected from a variety of suitable aromatic substituents; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, or C.sub.2 -alkyl substituted by C.sub.1-4 alkoxy or hydroxy; R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, C.sub.2-4 alkyl substituted by C.sub.1-4 alkoxy or hydroxy, or the group C(.dbd.NR.sup.c)NR.sup.a R.sup.b ; or R.sup.6 and R.sup.7, together with the nitrogen atom to which they are attached, form an optionally substituted saturated heterocyclic ring of 4 to 7 ring atoms which may optionally contain in the ring one oxygen or sulphur atom or a group selected from NR.sup.8, S(O) or S(O).sub.2 ; or R.sup.6 and R.sup.7, together with the nitrogen atom to which they are attached, form a piperidino ring substituted by a spiro-fused indene or indoline group, each of which may be unsubstituted or substituted; R.sup.8 is hydrogen, C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl or C.sub.1-4 alkoxyC.sub.1-4 alkyl; R.sup.9a and R.sup.9b are each independently hydrogen or C.sub.1-4 alkyl, or R.sup.9a and R.sup.9b are joined so, together with the carbon atoms to which they are attached, there is formed a C.sub.5-7 ring; X is selected from --CH.sub.2 CH.sub.2 --, --COCH.sub.2 -- or --CH.sub.2 CO--; and Y is hydrogen, or C.sub.1-4 alkyl optionally substituted by a hydroxyl group; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia. ##STR1##
摘要翻译： PCT No.PCT / GB95 / 02039 Sec。 371日期1997年2月27日 102（e）1997年2月27日PCT PCT 1995年8月30日PCT公布。公开号WO96 / 07649 日期：1996年3月14日本发明涉及式（I）化合物，其中：R 1，R 2，R 3，R 4和R 5选自多种合适的芳族取代基; R 6是氢，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基或被C 1-4烷氧基或羟基取代的C 2-烷基; R 7是氢，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基，被C 1-4烷氧基或羟基取代的C 2-4烷基或基团C（= NR c）NR a R b; 或R6和R7与它们所连接的氮原子一起形成任选取代的4至7个环原子的饱和杂环，其可以任选地在环中含有一个氧或硫原子或选自NR8，S（ O）或S（O）2; 或R6和R7与它们所连接的氮原子一起形成被螺稠合的茚或二氢吲哚基团取代的哌啶子基环，它们各自可以是未取代的或取代的; R 8是氢，C 1-4烷基，羟基C 1-4烷基或C 1-4烷氧基C 1-4烷基; R9a和R9b各自独立地为氢或C1-4烷基，或者R9a和R9b与它们所连接的碳原子一起连接形成C5-7环; X选自-CH 2 CH 2 - ， - COCH 2 - 或-CH 2 CO-; Y为氢或任选被羟基取代的C 1-4烷基; 或其药学上可接受的盐。该化合物特别用于治疗或预防疼痛，炎症，偏头痛，呕吐和带状疱疹后神经痛。（一）

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