公开(公告)号：US07084145B2

公开(公告)日：2006-08-01

申请号：US10693327

申请日：2003-10-24

申请人： Robert Duncan Armour ,  Andrew Douglas Baxter ,  Justin Stephen Bryans ,  Kevin Neil Dack ,  Patrick Stephen Johnson ,  Russell Andrew Lewthwaite ,  Julie Newman ,  David James Rawson ,  Thomas Ryckmans

发明人： Robert Duncan Armour ,  Andrew Douglas Baxter ,  Justin Stephen Bryans ,  Kevin Neil Dack ,  Patrick Stephen Johnson ,  Russell Andrew Lewthwaite ,  Julie Newman ,  David James Rawson ,  Thomas Ryckmans

IPC分类号： A61K31/4965 ,  C07D403/00

CPC分类号： C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14

摘要： The invention provides compounds of formula (I), the pharmaceutically acceptable salts and solvates thereof, wherein A, B, R1, R2, and R7 are as defined herein; pharmaceutical compositions thereof; combinations thereof; and uses thereof as vasopressin V1A antagonists.

摘要翻译： 本发明提供式（I）化合物，其药学上可接受的盐和溶剂化物，其中A，B，R 1，R 2和R 7， / SUP>如本文所定义; 其药物组合物; 其组合; 并且其用作血管加压素V 1A拮抗剂。

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）

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）

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

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。

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。

公开(公告)号：US07425569B2

公开(公告)日：2008-09-16

申请号：US11870451

申请日：2007-10-11

申请人： Paul Anthony Bradley ,  Kevin Neil Dack ,  Patrick Stephen Johnson ,  Sarah Elizabeth Skerratt

发明人： Paul Anthony Bradley ,  Kevin Neil Dack ,  Patrick Stephen Johnson ,  Sarah Elizabeth Skerratt

IPC分类号： A61K31/44

CPC分类号： C07D231/18 ,  C07D401/12

摘要： Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein R1 and R3 independently represent H, C1-6alkyl, C3-8cycloalkyl, or halogen; R2 represents C1-6alkyl, CF3 or aryl; a represents 1 or 2; R4, R5, R7 and R8 independently represent H, C1-6alkyl, C1-6alkyloxy, CN or halogen, or R4 and R5, or R7 and R8, together with the ring to which they are attached form an aryl or heterocyclic fused ring system; X represents C or N; Y represents CH2 or O; R6 represents H, CN or halo provided that, when X represents N, R6 is absent. The compounds are useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.

摘要翻译： 式（I）化合物或其药学上可接受的衍生物，其中R 1和R 3独立代表H，C 1-6烷基 C 3-8环烷基或卤素; R 2表示C 1-6烷基，CF 3或芳基; a代表1或2; R 4，R 5，R 7和R 8独立地表示H，C 1-6 C 1-6烷基，C 1-6烷氧基，CN或卤素，或R 4和R 5或R 7 和它们所连接的环连接形成芳基或杂环稠环体系; X表示C或N; Y表示CH 2或O; R 6表示H，CN或卤素，条件是当X表示N时，R 6不存在。 这些化合物可用于治疗子宫内膜异位症，子宫肌瘤（平滑肌瘤），月经过多，子宫腺肌症，原发性和继发性痛经（包括性交疼痛，dyschexia和慢性盆腔疼痛症状）或慢性盆腔疼痛综合征。

公开(公告)号：US07309712B2

公开(公告)日：2007-12-18

申请号：US11592574

申请日：2006-11-03

申请人： Paul Anthony Bradley ,  Kevin Neil Dack ,  Patrick Stephen Johnson ,  Sarah Elizabeth Skerratt

发明人： Paul Anthony Bradley ,  Kevin Neil Dack ,  Patrick Stephen Johnson ,  Sarah Elizabeth Skerratt

IPC分类号： A61K31/44 ,  C07D401/00 ,  C07D231/10

CPC分类号： C07D231/18 ,  C07D401/12

摘要： Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein R1 and R3 independently represent H, C1-6alkyl, C3-8cycloalkyl, or halogen; R2 represents C1-6alkyl, CF3 or aryl; a represents 1 or 2; R4, R5, R7 and R8 independently represent H, C1-6alkyl, C1-6alkyloxy, CN or halogen, or R4 and R5, or R7 and R8, together with the ring to which they are attached form an aryl or heterocyclic fused ring system; X represents C or N; Y represents CH2 or O; R6 represents H, CN or halo provided that, when X represents N, R6 is absent. The compounds are useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.

摘要翻译： 式（I）化合物或其药学上可接受的衍生物，其中R 1和R 3独立代表H，C 1-6烷基 C 3-8环烷基或卤素; R 2表示C 1-6烷基，CF 3或芳基; a代表1或2; R 4，R 5，R 7和R 8独立地表示H，C 1-6 C 1-6烷基，C 1-6烷氧基，CN或卤素，或R 4和R 5或R 7 和它们所连接的环连接形成芳基或杂环稠环体系; X表示C或N; Y表示CH 2或O; R 6表示H，CN或卤素，条件是当X表示N时，R 6不存在。 这些化合物可用于治疗子宫内膜异位症，子宫肌瘤（平滑肌瘤），月经过多，子宫腺肌症，原发性和继发性痛经（包括性交疼痛，dyschexia和慢性盆腔疼痛症状）或慢性盆腔疼痛综合征。

公开(公告)号：US6040309A

公开(公告)日：2000-03-21

申请号：US204789

申请日：1998-12-03

申请人： Kevin Neil Dack ,  Roger Peter Dickinson

发明人： Kevin Neil Dack ,  Roger Peter Dickinson

IPC分类号： A61K31/00 ,  A61K31/38 ,  A61K31/381 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/425 ,  A61K31/427 ,  A61K31/435 ,  A61K31/4353 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/495 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/50 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P13/00 ,  A61P13/08 ,  A61P13/12 ,  A61P15/00 ,  A61P15/10 ,  C07D333/70 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D471/04 ,  C07D521/00 ,  C07D333/64

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D333/70 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D471/04

摘要： Compounds of formula I, ##STR1## wherein X represents O or S(O).sub.m ;R.sup.1 and R.sup.2 independently represent phenyl, naphthyl or heteroaryl; each of which is optionally fused and optionally substituted;Y represents a bond, O, (CH.sub.2).sub.n, O(CH.sub.2).sub.n, (CH.sub.2).sub.n O, or CH(C.sub.1-6 alkyl)O;R.sup.3 represents H or C.sub.1-6 alkyl;m represents 0, 1, or 2; andn represents 1, or 2;and pharmaceutically acceptable salts thereof, are useful in therapy, in particular in the treatment of restenosis, renal failure and pulmonary hypertension.

摘要翻译： 式I化合物，其中X表示O或S（O）m; R1和R2独立地表示苯基，萘基或杂芳基; 各自任选地被稠合并任选地被取代; Y表示键，O，（CH 2）n，O（CH 2）n，（CH 2）n O或CH（C 1-6烷基）O; R 3表示H或C 1-6烷基; m表示0,1或2; n表示1或2; 其药学上可接受的盐可用于治疗，特别是治疗再狭窄，肾衰竭和肺动脉高压。

公开(公告)号：US09233964B2

公开(公告)日：2016-01-12

申请号：US13977408

申请日：2012-01-06

申请人： Søren Christian Schou ,  Daniel Rodriguez Greve ,  Simon Feldbæk Nielsen ,  Jens Bjørn Jensen ,  Kevin Neil Dack

发明人： Søren Christian Schou ,  Daniel Rodriguez Greve ,  Simon Feldbæk Nielsen ,  Jens Bjørn Jensen ,  Kevin Neil Dack

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04 ,  A61K31/5377 ,  A61K45/06

CPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

摘要： The invention relates to compounds of general Formula (I), Wherein R1, R2, R3, R4, R5, m, n are defined herein, and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.

摘要翻译： 本发明涉及通式（I）的化合物，其中R1，R2，R3，R4，R5，m，n如本文所定义，及其药学上可接受的盐，前体药物，水合物或溶剂化物，单独使用或组合使用 与治疗中的一种或多种其它药物活性化合物一起作为用于预防，治疗或改善疾病及其并发症的JAK激酶和蛋白酪氨酸激酶抑制剂，包括例如牛皮癣，特应性皮炎，酒渣鼻，狼疮，多发性硬化，类风湿性关节炎 ，I型糖尿病，哮喘，癌症，自身免疫性甲状腺疾病，溃疡性结肠炎，克罗恩病，阿尔茨海默氏病，白血病，眼睛疾病如糖尿病性视网膜病变和黄斑变性以及其他自身免疫性疾病和免疫抑制在器官中是理想的适应症 移植。