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1. 发明授权

US06306852B1 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：US06306852B1
公开(公告)日：2001-10-23
申请号：US09556651
申请日：2000-04-24
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： A61P910
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 R1 and R2 are optional substituents and independently represent C1-6 alkyl, C2-6 alkenyl, optionally substituted by CO2H or CO2(C1-6 alkyl), C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6 alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCO2R10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 represents H or OH; R6 represents phenyl optionally fused to a herterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 or CONHSO2(C1-4 alkyl); Ar1-3 indenpendently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het1 and Het2 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任选被CO 2 H或CO 2（C 1-6烷基）取代的C 1-6烷基，C 2-6烯基，C 2-6炔基，（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，C 1 -C 3全氟烷基，（CH 2）mr 1，（CH 2）m Het1，（CH 2）m CONR 7 R 8，（CH2）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）pNR9R10，SO2R10，SO2NR9R10，（CH2）mCO2R10，C2-6烯基，C2-6炔基，（CH2）

2. 发明授权

US06384070B2 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：US06384070B2
公开(公告)日：2002-05-07
申请号：US09756835
申请日：2001-01-09
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： A61K314025
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 R1 and R2 are optional substituents and independently represent C1-6 alkyl, C2-6 alkenyl, optionally substituted by CO2H or CO2(C1-6 alkyl), C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6 alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCO2R10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 represents H or OH; R6 represents phenyl optionally fused to a heterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 or CONHSO2(C1-4 alkyl); Ar1-3 independently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het1 and Het2 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任选被CO 2 H或CO 2（C 1-6烷基）取代的C 1-6烷基，C 2-6烯基，C 2-6炔基，（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，C 1 -C 3全氟烷基，（CH 2）mr 1，（CH 2）m Het1，（CH 2）m CONR 7 R 8，（CH2）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）pNR9R10，SO2R10，SO2NR9R10，（CH2）mCO2R10，C2-6烯基，C2-6炔基，（CH2）

3. 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。

4. 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

5. 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。

6. 发明授权

US07612084B2 Amine derivatives for the treatment of asthma and COPD 失效
标题翻译：用于治疗哮喘和COPD的胺衍生物
公开(公告)号：US07612084B2
公开(公告)日：2009-11-03
申请号：US11725335
申请日：2007-03-19
申请人： Kim James , Lyn Howard Jones , David Anthony Price
发明人： Kim James , Lyn Howard Jones , David Anthony Price
IPC分类号： A61K31/44
CPC分类号： C07C311/08 , C07C215/54 , C07C217/48 , C07C217/62 , C07C223/02 , C07C233/43 , C07C255/13 , C07C271/16 , C07C271/66 , C07D215/26 , C07D215/60 , C07F7/1804
摘要： The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
摘要翻译：本发明涉及式（1）化合物以及制备用于制备含这些衍生物的组合物和用途的中间体的方法。根据本发明的化合物可用于许多疾病，病症和病症，特别是炎症，过敏和呼吸道疾病，病症和病症。

7. 发明申请

US20090197912A1 Sulfonamide Derivatives for the Treatment of Diseases 失效
标题翻译：磺酰胺衍生物治疗疾病
公开(公告)号：US20090197912A1
公开(公告)日：2009-08-06
申请号：US12420206
申请日：2009-04-08
申请人： Alan Daniel Brown , Mark Edward Bunnage , Paul Alan Glossop , Kim James , Charlotte Alice Louise Lane , Russel Andrew Lewthwaite , Ian Brian Moses , David Anthony Price , Nicholas Murray Thomson
发明人： Alan Daniel Brown , Mark Edward Bunnage , Paul Alan Glossop , Kim James , Charlotte Alice Louise Lane , Russel Andrew Lewthwaite , Ian Brian Moses , David Anthony Price , Nicholas Murray Thomson
IPC分类号： A61K31/472 , A61K31/18 , A61P11/00
CPC分类号： C07C311/08 , A61K31/18 , A61K31/352 , A61K31/522 , C07C2602/08 , C07D217/06
摘要： The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
摘要翻译：本发明涉及式（1）化合物以及制备用于制备含这些衍生物的组合物和用途的中间体的方法。根据本发明的化合物可用于许多疾病，病症和病症，特别是炎症，过敏和呼吸道疾病，病症和病症。

8. 发明授权

US07547731B2 Formamide derivatives for the treatment of diseases 失效
标题翻译：甲酰胺衍生物用于治疗疾病
公开(公告)号：US07547731B2
公开(公告)日：2009-06-16
申请号：US11773012
申请日：2007-07-03
申请人： Alan Daniel Brown , Mark Edward Bunnage , Charlotte Alice Louise Lane , Russell Andrew Lewthwaite , Paul Alan Glossop , Kim James , David Anthony Price
发明人： Alan Daniel Brown , Mark Edward Bunnage , Charlotte Alice Louise Lane , Russell Andrew Lewthwaite , Paul Alan Glossop , Kim James , David Anthony Price
IPC分类号： A61K31/167 , C07C233/24
CPC分类号： C07C237/20 , C07C237/30 , C07C237/32 , C07C255/60 , C07C311/37 , C07C311/46 , C07C317/32 , C07C323/32 , C07C323/41 , C07C323/42 , C07C2601/14 , C07C2602/08 , C07C2603/74 , C07D209/48 , C07D211/32 , C07D213/38 , C07D213/40 , C07D217/06 , C07D217/16 , C07D221/22 , C07D221/24 , C07D295/192 , C07D335/02
摘要： The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
摘要翻译：本发明涉及式（1）化合物以及制备用于制备含这些衍生物的组合物和用途的中间体的方法。根据本发明的化合物可用于许多疾病，病症和病症，特别是炎症，过敏和呼吸道疾病，病症和病症。

9. 发明授权

US07214694B2 3-ox(adi)azolylpropanohydroxamic acids useful as procollagen C-proteinase inhibitors 失效
标题翻译：可用作原胶原C-蛋白酶抑制剂的3-氧（adi）唑基丙酰异羟肟酸
公开(公告)号：US07214694B2
公开(公告)日：2007-05-08
申请号：US10731707
申请日：2003-12-09
申请人： Usa Datta , Paul Vincent Fish , Kim James , Gavin Alistair Whitlock
发明人： Usa Datta , Paul Vincent Fish , Kim James , Gavin Alistair Whitlock
IPC分类号： A61K31/541 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D417/02 , C07D413/02
CPC分类号： C07D263/16 , A61K31/421 , A61K31/422 , A61K31/4245 , C07C235/74 , C07C259/14 , C07C311/06 , C07C2601/14 , C07D205/04 , C07D211/60 , C07D211/96 , C07D231/12 , C07D233/56 , C07D249/08 , C07D263/32 , C07D263/34 , C07D271/06 , C07D271/07 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/06
摘要： Compounds of formula (I): wherein the substituents are as defined herein, and their salt, solvates, and prodrugs are procollagen C-proteinase (PCP) inhibitors useful in treating conditions mediated by PCP.
摘要翻译：式（I）化合物：其中取代基如本文所定义，其盐，溶剂合物和前药是用于治疗由PCP介导的病症的前胶原C-蛋白酶（PCP）抑制剂。

10. 发明授权

US4927819A Cyclo-octane neuroprotective agents 失效
标题翻译：环辛烷值神经保护剂
公开(公告)号：US4927819A
公开(公告)日：1990-05-22
申请号：US274436
申请日：1988-11-22
申请人： Raymond Baker , William R. Carling , Kim James , Paul D. Leeson
发明人： Raymond Baker , William R. Carling , Kim James , Paul D. Leeson
IPC分类号： A61K31/55 , A61P3/08 , A61P7/06 , A61P9/00 , A61P25/08 , A61P25/28 , C07D487/08
CPC分类号： C07D487/08
摘要： The present invention provides a compound of formula I: ##STR1## or a salt thereof, wherein: the dotted lines represent optional double bonds;R.sup.1 represents hydrogen, hydroxy, alkenyl, alkyl, aminoalkyl or hydroxyalkyl;R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently represet hydrogen, hydroxy, fluoro, alkenyl, aryl, alkyl, or alkyl substituted with aryl, amino, hydroxy, carboxy or fluoro; andR.sup.7, R.sup.8, R.sup.9 and R.sup.10 independently represent hydrogen, hydrocarbon or a heterocyclic group provided that R.sup.7, R.sup.8, R.sup.9 and R.sup.10 are not simultaneously hydrogen; orR.sup.7 and R.sup.8 and/or R.sup.9 and R.sup.10 may complete a saturated or unsaturated C.sub.4-9 hydrocarbon or heterocyclic ring; which compounds are useful as anticonvulsant agents and in the treatment and/or prevention of neurodegenerative disorders.

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