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31. 发明授权

US06211223B1 Indole derivatives useful in therapy 失效
标题翻译：吲哚衍生物用于治疗
公开(公告)号：US06211223B1
公开(公告)日：2001-04-03
申请号：US09551779
申请日：2000-04-18
申请人： Stephen Challenger , Kevin Neil Dack , Andrew Michael Derrick , Roger Peter Dickinson , David Ellis , Yousef Hajikarimian , Kim James , David James Rawson
发明人： Stephen Challenger , Kevin Neil Dack , Andrew Michael Derrick , Roger Peter Dickinson , David Ellis , Yousef Hajikarimian , Kim James , David James Rawson
IPC分类号： A61K31404
CPC分类号： C07D405/06
摘要： The invention provides S-(+)-3-{1-(1,3-benzodioxol-5-yl)-2-[(2-methoxy-4-methylphenyl)sulfonylamino]-2-oxoethyl}-1-methyl-1H-indole-6-carboxylic acid, which is substantially free from its (R)-(−)-enantiomer, and pharmaceutically acceptable derivatives thereof. The compounds are useful in the treatment of inter alia acute renal failure, restenosis and pulmonary hypertension.
摘要翻译：本发明提供了S - （+） - 3- {1-（1,3-苯并间二氧杂环戊烯-5-基）-2 - [（2-甲氧基-4-甲基苯基）磺酰基氨基] -2-氧代乙基} -1-甲基基本上不含其（R） - （ - ） - 对映异构体的-1H-吲哚-6-羧酸及其药学上可接受的衍生物。该化合物可用于治疗尤其是急性肾衰竭，再狭窄和肺动脉高压

32. 发明授权

US6136843A Indole derivatives useful as endothelin receptor antagonists 失效
标题翻译：用作内皮素受体拮抗剂的吲哚衍生物
公开(公告)号：US6136843A
公开(公告)日：2000-10-24
申请号：US414361
申请日：1999-10-07
申请人： David James Rawson , Kevin Neil Dack , Roger Peter Dickinson , Kim James
发明人： David James Rawson , Kevin Neil Dack , Roger Peter Dickinson , Kim James
IPC分类号： A61K31/40 , A61K31/405 , A61K31/41 , A61K31/4178 , A61K31/4196 , A61K31/4245 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5377 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/02 , A61P13/08 , A61P13/12 , A61P15/00 , A61P43/00 , C07D209/18 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14
CPC分类号： C07D405/06 , C07D209/18 , C07D405/14 , C07D409/14 , C07D413/14
摘要： ##STR1## Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R
1 and R
2 are optional substituents and independently represent C
1-6 alkyl, C
2-6 alkenyl optionally substituted by CO
2 H or CO
2 (C
1-6 alkyl, C
2-6 alkynyl, halogen, C
1-3 perfluoroalkyl, (CH
2 )
m Ar
1 , (CH
2 )
m Het
1 , (CH
2 )
m CONR
7 R
8 , (CH
2 )
m CO
2 R
8 , O(CH
2 )
q CO
2 R
8 , (CH
2 )
m COR
8 , (CH
2 )
m OR
8 , O(CH
2 )
p OR
8 , (CH
2 )
m NR
7 R
8 , CO
2 (CH
2 )
q NR
7 R
8 , (CH
2 )
m CN, S(O)
n R
8 , SO
2 NR
7 R
8 , CONH(CH
2 )
m Ar
1 or CONH(CH
2 )
m Het
1 ; R
3 represents H, C
1-6 alkyl, (CH
2 )
p CONR
9 R
10 , SO
2 R
10 , SO
2 NR
9 R
10 , (CH
2 )
m COR
10 , C
2-6 alkenyl, C
2-6 alkynyl, (CH
2 )
m CONR
9 R
10 , (CH
2 )
m CO
2 R
10 , (CH
2 )
p CN, (CH
2 )
p R
10 or (CH
2 )
p OR
10 ; R
4 represents H or C
1-6 alkyl; R
5 represents H or OH; R
6 represents phenyl optionally fused to a heterocylic ring, the group as a whole being optionally substituted; R
7-10 are fully defined herein and may independently represent Ar
2 or Het
2 ; Z represents CO
2 H, CONH(tetrazol-5-yl), CONHSO
2 O(C
1-4 alkyl), CO
2 Ar
3 , CO
2 (C
1-6 alkyl), tetrazol-5-yl, CONHSO
2 Ar
3 , CONHSO
2 (CH
2 )
q Ar
3 or CONHSO
2 (C
1-6 alkyl); Ar
1-3 independently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het
1 and Het
2 independently represent a non-aromatic heterocycle which is optionally substituted; are useful in the treatment of restenosis, renal failure and pulmonary hypertension.
摘要翻译：式（I）化合物及其药学上可接受的衍生物，其中R 1和R 2是任选的取代基并且独立地表示C 1-6烷基，任选被CO 2 H或CO 2取代的C 2-6烯基（C 1-6烷基，C 2-6炔基，卤素，（CH 2）m CO 2 R 8，O（CH 2）q CO 2 R 8，（CH 2）m COOR 8，（CH 2）mOR 8，O（CH 2）pOR 8，（CH 2）m CO 2 R 8，）mNR7R8，CO2（CH2）qNR7R8，（CH2）mCN，S（O）nR8，SO2NR7R8，CONH（CH2）mAr1或CONH（CH2）mHet1; R3表示H，C1-6烷基，（CH2）pCONR9R10，SO2R10， SO2NR9R10，（CH2）mCOR10，C2-6烯基，C2-6炔基，（CH2）m CONR9R10，（CH2）mCO2R10，（CH2）pCN，（CH2）pR10或（CH2）pOR10; R4表示H或C1-6 烷基; R 5表示H或OH; R 6表示任选地与杂环的稠合的苯基，该基团整体上可以被取代; R 7-10在本文中是完全定义的，可独立地表示Ar 2或Het 2; Z代表CO 2 H，CONH（四唑 - （C 1-4烷基），CO 2 Ar 3，CO 2（C 1-6烷基），四唑-5-基，CONHSO 2 Ar 3，CONHSO 2（CH 2）q A r3或CONHSO2（C1-6烷基）; Ar1-3独立地表示苯基，萘基或芳族杂环，这些基团任选地稠合并任选被取代; Het1和Het2独立地表示任选被取代的非芳族杂环; 可用于治疗再狭窄，肾衰竭和肺动脉高压。

33. 发明授权

US5922747A Indole derivatives as steroid 5.alpha.-reductase inhibitors 失效
标题翻译：吲哚衍生物作为类固醇5α-还原酶抑制剂
公开(公告)号：US5922747A
公开(公告)日：1999-07-13
申请号：US982735
申请日：1997-12-02
申请人： Julian Blagg , Graham Nigel Maw , David James Rawson
发明人： Julian Blagg , Graham Nigel Maw , David James Rawson
IPC分类号： A61K31/405 , A61K31/41 , A61P5/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P35/00 , A61P43/00 , C07D405/06 , C07D405/14 , A61K31/40
CPC分类号： C07D405/06
摘要： A method of treatment of a human to inhibit a steroid 5.alpha.-reductase, particularly a testosterone 5.alpha.-reductase, which comprises treating said human with an effective amount of a compound of the formula (I) ##STR1## or a pharmaceutically acceptable base salt thereof, wherein R is --CO.sub.2 H or tetrazol-5-yl;R.sup.1 is C.sub.3 -C.sub.8 alkyl optionally substituted by fluoro; andR.sup.2 is C.sub.2 -C.sub.4 alkylor with a pharmaceutically acceptable base salt or composition thereof. Conditions which are treatable by such inhibition include acne vulgaris, alopecia, seborrhoea, female hirsutism, benign prostatic hypertropy, male pattern baldness and human prostate adenocarcinomas.
摘要翻译：一种治疗人类以抑制类固醇5α-还原酶，特别是睾丸激素5α-还原酶的方法，其包括用有效量的式（I）化合物或其药学上可接受的碱盐处理所述人，其中R是-CO 2 H或四唑-5-基; R1是任选被氟取代的C3-C8烷基; 并且R 2是C 2 -C 4烷基或其药学上可接受的碱盐或组合物。通过这种抑制可治疗的病症包括寻常痤疮，脱发，皮脂溢，女性多毛症，良性前列腺肥大，男性型秃发和人类前列腺腺癌。

34. 发明授权

US5912357A Indole derivatives as 5-.alpha.-reductase-1-inhibitors 失效
标题翻译：吲哚衍生物作为5-α-还原酶-1抑制剂
公开(公告)号：US5912357A
公开(公告)日：1999-06-15
申请号：US592315
申请日：1996-02-15
申请人： Julian Blagg , Graham Nigel Maw , David James Rawson
发明人： Julian Blagg , Graham Nigel Maw , David James Rawson
IPC分类号： A61K31/40 , A61K31/405 , A61K31/41 , A61P17/00 , A61P35/00 , A61P43/00 , C07C43/307 , C07C43/313 , C07C45/45 , C07C49/76 , C07C49/784 , C07C49/813 , C07C321/20 , C07C323/07 , C07C325/02 , C07D405/06 , C07D405/14
CPC分类号： C07D405/06 , C07C43/307 , C07C43/313 , C07C45/45 , C07C49/76 , C07C49/784 , C07C49/813 , C07D405/14
摘要： A compound of formula (I): ##STR1## and the pharmaceutically acceptable base salts thereof, wherein: R is CO.sub.2 R.sup.12 where R.sup.12 is H or a biolabile ester-forming group, or R is tetrazol-5-yl, and either (a) R.sup.1 is ##STR2## and R.sup.2 is F, Cl, Br, I, CH.sub.3 or CF.sub.3, or (b) R.sup.1 is C.sub.3 -C.sub.6 alkyl and R.sup.2 is C.sub.2 -C.sub.4 alkyl, useful as steroid 5-.alpha.-reductase inhibitors.
摘要翻译： PCT No.PCT / EP94 / 02563。 371日期：1996年2月15日 102（e）日期1996年2月15日PCT 1994年8月2日PCT公布。出版物WO95 / 05375 PCT 日期：1995年2月23日一种式（I）化合物及其药学上可接受的碱盐，其中：R为CO 2 R 12，其中R 12为H或不生物不稳定酯形成基团，或R为四唑-5-基， a）R1是和R2是F，Cl，Br，I，CH3或CF3，或（b）R1是C3-C6烷基，R2是C2-C4烷基，可用作类固醇5-α-还原酶抑制剂。

35. 发明授权

US07649004B2 Pyridine derivatives 失效
标题翻译：吡啶衍生物
公开(公告)号：US07649004B2
公开(公告)日：2010-01-19
申请号：US11572533
申请日：2005-07-12
申请人： Charlotte Alice Louise Lane , Graham Nigel Maw , David James Rawson , Lisa Rosemary Thompson
发明人： Charlotte Alice Louise Lane , Graham Nigel Maw , David James Rawson , Lisa Rosemary Thompson
IPC分类号： A61K31/5377 , A61K31/44 , C07D401/12 , C07D413/12
CPC分类号： C07D213/81 , C07D401/12
摘要： The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐和溶剂合物，其制备方法，用于制备的中间体和含有这些化合物的组合物以及这些化合物用于治疗疼痛的用途。

36. 发明授权

US07612226B2 Amino acid derivatives 失效
标题翻译：氨基酸衍生物
公开(公告)号：US07612226B2
公开(公告)日：2009-11-03
申请号：US11414422
申请日：2006-04-28
申请人： Shelley Rene Graham , Simon John Mantell , David James Rawson , Jacob Bradely Schwarz
发明人： Shelley Rene Graham , Simon John Mantell , David James Rawson , Jacob Bradely Schwarz
IPC分类号： C07C261/00
CPC分类号： A61K31/325 , A61K31/401 , A61K31/405 , A61K31/4172 , C07C229/08 , C07C229/28 , C07C2601/04 , C07C2601/08
摘要： The present invention relates to a method of treating pain using a compound of formula wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to certain novel derivatives of formula (I).
摘要翻译：本发明涉及使用下式化合物治疗疼痛的方法：其中R1，R2，R3和R4如本文所定义。本发明还涉及式（I）的某些新型衍生物。

37. 发明授权

US06756373B1 Pharmaceutically active compounds 失效
标题翻译：药物活性化合物
公开(公告)号：US06756373B1
公开(公告)日：2004-06-29
申请号：US09684228
申请日：2000-10-06
申请人： Charlotte Moira Norfor Allerton , Christopher Gordon Barber , Graham Nigel Maw , David James Rawson
发明人： Charlotte Moira Norfor Allerton , Christopher Gordon Barber , Graham Nigel Maw , David James Rawson
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： There is provided a compound of formula I: wherein X represents O or NR5 R4 represents H, halo, cyano, nitro, halo(loweralkyl), OR6, OC(O)R7, C(O)R8, C(O)OR9, C(O)NR10R11, NR12R13, NR16Y(O)R17, N[Y(O)R17]2, SOR18, SO2R19, C(O)AZ, lower alkyl, lower alkenyl, lower alkynyl, Het, alkylHet, aryl, alkylaryl (which latter seven groups are all optionally substituted with one or more substituents selected from halo, cyano, nitro, lower alkyl, halo(loweralkyl), OR6, OC(O)R7, C(O)R8, C(O)OR9, C(O)NR10R11, NR12R13 and SO2NR14R15) which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g., cGMP PDE5) is desired.
摘要翻译：提供式I化合物：其中X代表O或NR 5 R 4表示H，卤素，氰基，硝基，卤素（低级烷基），OR 6，OC（O）R 7，C （O）R 8，C（O）OR 9，C（O）NR 10 R 11，NR 12 R 13，NR 16 Y（O）R 17 >，N [Y（O）R 17] 2，SOR 18，SO 2 R 19，C（O）AZ，低级烷基，低级烯基，低级炔基，Het，烷基Het，芳基，烷基芳基七个基团都可以被一个或多个选自卤素，氰基，硝基，低级烷基，卤代（低级烷基），OR 6，OC（O）R 7，C（O）R 8， C（O）OR 9，C（O）NR 10 R 11，NR 12 R 13和SO 2 NR 14 R 15），其可用于治疗和预防性治疗需要抑制环鸟嘌呤3'，5'-单磷酸磷酸二酯酶（例如cGMP PDE5）的医学病症。

38. 发明授权

US6017945A Indole derivatives useful as endothelin receptor antagonists 失效
标题翻译：用作内皮素受体拮抗剂的吲哚衍生物
公开(公告)号：US6017945A
公开(公告)日：2000-01-25
申请号：US147096
申请日：1998-10-05
申请人： David James Rawson , Kevin Neil Dack , Roger Peter Dickinson , Kim James
发明人： David James Rawson , Kevin Neil Dack , Roger Peter Dickinson , Kim James
IPC分类号： A61K31/40 , A61K31/405 , A61K31/41 , A61K31/4178 , A61K31/4196 , A61K31/4245 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5377 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/02 , A61P13/08 , A61P13/12 , A61P15/00 , A61P43/00 , C07D209/18 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D405/02
CPC分类号： C07D405/06 , C07D209/18 , C07D405/14 , C07D409/14 , C07D413/14
摘要： Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R.sup.1 and R.sup.2 are optional substituents and independently represent C.sub.1-6 alkyl, C.sub.2-6 alkenyl [optionally substituted by CO.sub.2 H or CO.sub.2 (C.sub.1-6 alkyl)], C.sub.2-6 alkynyl, halogen, C.sub.1-3 perfluoroalkyl, (CH.sub.2).sub.m Ar.sup.1, (CH.sub.2).sub.m Het.sup.1, (CH.sub.2).sub.m CONR.sup.7 R.sup.8, (CH.sub.2).sub.m CO.sub.2 R.sup.8, O(CH.sub.2).sub.q CO.sub.2 R.sup.8, (CH.sub.2).sub.m COR.sup.8, (CH.sub.2).sub.m OR.sup.8, O(CH.sub.2).sub.p OR.sup.8, (CH.sub.2).sub.m NR.sup.7 R.sup.8, CO.sub.2 (CH.sub.2).sub.q NR.sup.7 R.sup.8, (CH.sub.2).sub.m CN, S(O).sub.n R.sup.8, SO.sub.2 NR.sup.7 R.sup.8, CONH(CH.sub.2).sub.m Ar.sup.1 or CONH(CH.sub.2).sub.m Het.sup.1 ; R.sup.3 represents H, C.sub.1-6, alkyl, (CH.sub.2).sub.p NR.sup.9 R.sup.10, SO.sub.2 R.sup.10, SO.sub.2 NR.sup.9 R.sup.10, (CH.sub.2).sub.m COR.sup.10, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, (CH.sub.2).sub.m CONR.sup.9 R.sup.10, (CH.sub.2).sub.m CO.sub.2 R.sup.10, (CH.sub.2).sub.p CN, (CH.sub.2).sub.p R.sup.10 or (CH.sub.2).sub.p OR.sup.10 ; R.sup.4 represents H or C.sub.1-6 alkyl; R.sup.5 represents H or OH; R.sup.6 represents phenyl optionally fused to a heterocyclic ring, the group as a whole being optionally substituted; R.sup.7-10 are fully defined herein and may independently represent Ar.sup.2 or Het.sup.2 ; Z represents CO.sub.2 H, CONH(tetrazol-5-yl), CONHSO.sub.2 O(C.sub.1-4 alkyl), CO.sub.2 Ar.sup.3, CO.sub.2 (C.sub.1-6 alkyl), tetrazol-5-yl, CONHSO.sub.2 Ar.sup.3, CONHSO.sub.2 (CH.sub.2).sub.q Ar.sup.3 or CONHSO.sub.2 (C.sub.1-6 alkyl); Ar.sup.1-3 independently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het.sup.1 and Het.sup.2 independently represent a non-aromatic heterocycle which is optionally substituted; are useful in the treatment of restenosis, renal failure and pulmonary hypertension.
摘要翻译： PCT No.PCT / EP97 / 01882 Sec。 371日期：1998年10月5日 102（e）日期1998年10月5日PCT 1997年4月11日PCT PCT。公开号WO97 / 43260 PCT 日期1997年11月20日式（I）化合物及其药学上可接受的衍生物，其中R 1和R 2是任选的取代基并且独立地表示C 1-6烷基，C 2-6烯基[任选被CO 2 H或CO 2（C 1-6烷基），（CH 2）m CONR 7 R 8，（CH 2）m CO 2 R 8，O（CH 2）q CO 2 R 8，（CH 2）m COOR 8，（CH 2）m OR 8， O（CH2）pOR8，（CH2）mNR7R8，CO2（CH2）qNR7R8，（CH2）mCN，S（O）nR8，SO2NR7R8，CONH（CH2）mAr1或CONH（CH2）mHet1; R3代表H，C1-6，烷基，（CH2）pNR9R10，SO2R10，SO2NR9R10，（CH2）mCOR10，C2-6烯基，C2-6炔基，（CH2）mCONR9R10，（CH2）mCO2R10，（CH2） CH2）pR10或（CH2）pOR10; R 4表示H或C 1-6烷基; R5表示H或OH; R6表示任选地与杂环稠合的苯基，该基团作为整体任选被取代; 本文完全定义R7-10，并且可以独立地表示Ar2或Het2; Z表示CO 2 H，CONH（四唑-5-基），CONHSO 2 O（C 1-4烷基），CO 2 Ar 3，CO 2（C 1-6烷基），四唑-5-基，CONHSO 2 Ar 3，CONHSO 2（CH 2）qAr 3或CONHSO 2 ）; Ar1-3独立地表示苯基，萘基或芳族杂环，这些基团任选地稠合并任选被取代; Het1和Het2独立地表示任选被取代的非芳族杂环; 可用于治疗再狭窄，肾衰竭和肺动脉高压。

39. 发明授权

US07659305B2 Therapeutic proline derivatives 失效
标题翻译：治疗脯氨酸衍生物
公开(公告)号：US07659305B2
公开(公告)日：2010-02-09
申请号：US10698354
申请日：2003-10-30
申请人： David James Rawson
发明人： David James Rawson
IPC分类号： A61K31/40 , A01N43/36
CPC分类号： C07D401/12 , A61K31/401 , C07D207/16 , C07D405/12
摘要： The compounds of formula (I) or a pharmaceutically acceptable salt, solvate or pro-drug thereof, are proline derivatives useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, fibromyalgia, arthritis, neuropathalogical disorders, sleep disorders, visceral pain disorders and gastrointestinal disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included.
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂化物或前体药物是用于治疗癫痫，眩晕发作，运动功能减退，颅内疾病，神经变性疾病，抑郁症，焦虑症，恐慌症，疼痛，纤维肌痛的脯氨酸衍生物，关节炎，神经病学障碍，睡眠障碍，内脏疼痛障碍和胃肠道疾病。包括用于制备在该方法中有用的最终产物和中间体的方法。还包括含有一种或多种化合物的药物组合物。

40. 发明申请

US20080312235A1 Pyridine Derivatives 失效
标题翻译：吡啶衍生物
公开(公告)号：US20080312235A1
公开(公告)日：2008-12-18
申请号：US11572533
申请日：2005-07-12
申请人： Charlotte Alice Louise Lane , Graham Nigel Maw , David James Rawson , Lisa Rosemary Thompson
发明人： Charlotte Alice Louise Lane , Graham Nigel Maw , David James Rawson , Lisa Rosemary Thompson
IPC分类号： A61K31/5377 , C07D401/12 , A61P25/00
CPC分类号： C07D213/81 , C07D401/12
摘要： The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐和溶剂合物，其制备方法，用于制备的中间体和含有这些化合物的组合物以及这些化合物用于治疗疼痛的用途。

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