公开(公告)号：US07084145B2

公开(公告)日：2006-08-01

申请号：US10693327

申请日：2003-10-24

Applicant: 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

Inventor： 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: A61K31/4965 ,  C07D403/00

CPC classification number: C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14

Abstract: 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.

Abstract translation: 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：US06794387B2

公开(公告)日：2004-09-21

申请号：US10099264

申请日：2002-03-14

Applicant: Charlotte Moira Norfor Allerton ,  Kevin Neil Dack ,  Mark Ian Kemp

Inventor： Charlotte Moira Norfor Allerton ,  Kevin Neil Dack ,  Mark Ian Kemp

IPC: C07D48704

CPC classification number: C07D487/04

Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, X, Y and A have the meanings given herein 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.

Abstract translation: 通式（I）的化合物：其中R 1，R 2，R 3，R 4，X，Y和A具有本文给出的用于治疗和预防性治疗 需要抑制环鸟苷3'，5'-单磷酸磷酸二酯酶（如cGMP PDE5）的医疗条件。

公开(公告)号：US06495568B1

公开(公告)日：2002-12-17

申请号：US09423359

申请日：2001-10-12

Applicant: Kevin Neil Dack ,  Gavin Alistair Whitlock

Inventor： Kevin Neil Dack ,  Gavin Alistair Whitlock

IPC: A61K31445

CPC classification number: C07D401/10 ,  C07D211/16 ,  C07D211/22 ,  C07D211/70 ,  C07D405/10 ,  C07D405/12 ,  Y02P20/55

Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diseases.

公开(公告)号：US5744488A

公开(公告)日：1998-04-28

申请号：US601013

申请日：1996-02-23

Applicant: Peter Edward Cross ,  Kevin Neil Dack ,  Roger Peter Dickinson ,  John Steele

Inventor： Peter Edward Cross ,  Kevin Neil Dack ,  Roger Peter Dickinson ,  John Steele

IPC: A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/44 ,  A61K31/4427 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P43/00 ,  C07D209/08 ,  C07D209/10 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D521/00

CPC classification number: C07D249/08 ,  C07D209/10 ,  C07D231/12 ,  C07D233/56 ,  C07D401/04 ,  C07D401/06

Abstract: Compounds of formula (I): ##STR1## and pharmaceutically acceptable salt and biolabile esters thereof, wherein R.sup.1 is H, C.sub.1 -C.sub.4 alkyl, phenyl optionally substituted by up to three substituents independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen and CF.sub.3, or is 1-imidazolyl, 3-pyridyl or 4-pyridyl; R.sup.2 is H or C.sub.1 -C.sub.4 alkyl, R.sup.3 is SO.sub.2 R.sup.4 or COR.sup.4 where R.sup.4 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.3 perfluoroalkyl(CH.sub.2).sub.p, C.sub.3 -C.sub.6 cycloalkyl(CH.sub.2).sub.p, aryl(CH.sub.2).sub.p, or heteroaryl(CH.sub.2).sub.p, p being 0, 1 or 2, or R.sup.4 may be NR.sup.5 R.sup.6 where R.sup.5 is H or C.sub.1 -C.sub.4 alkyl and R.sup.6 is C.sub.1 -C.sub.6, alkyl, C.sub.3 -C.sub.6 cycloalkyl or aryl, or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a 5- to 7-membered heterocyclic ring which may optionally incorporate a carbon-carbon double bond or a further heteroatom linkage selected from O, S, NH, N(C.sub.1 -C.sub.4 alkyl) and N(C.sub.1 -C.sub.5 alkanoyl); X is CH.sub.2 or a direct link, with the proviso that when R.sup.1 is 1-imidazolyl then X is CH.sub.2 ; m is 2, or 3; n is 0, 1 or 2, and wherein the group (CH.sub.2).sub.n NHR.sup.3 is attached at the 5-position when n is 0 or 1, or at the 5- or 4-position when n is 2. These compounds are selective TXA.sub.2 and PGH.sub.2 antagonists. Some also inhibit thromboxane synthetase.

Abstract translation: PCT No.PCT / EP94 / 02660 Sec。 371日期1996年2月23日 102（e）日期1996年2月23日PCT 1994年8月9日PCT PCT。 公开号WO95 / 06046 日期：1993年3月2日式（I）化合物：其中R 1为H，C 1 -C 4烷基，任选被至多3个独立地选自C 1 -C 4烷基的取代基取代的苯基的化合物及其药学上可接受的盐和生物不稳定酯， C4烷基，C1-C4烷氧基，卤素和CF3，或是1-咪唑基，3-吡啶基或4-吡啶基; R2是H或C1-C4烷基，R3是SO2R4或COR4，其中R4是C1-C6烷基，C1-C3全氟烷基（CH2）p，C3-C6环烷基（CH2）p，芳基（CH2）p或杂芳基（CH2） p，p为0,1或2，或者R4可以是NR5R6，其中R5是H或C1-C4烷基，R6是C1-C6，烷基，C3-C6环烷基或芳基，或R5和R6连同氮原子 它们连接形成5-至7-元杂环，其可任选地并入碳 - 碳双键或选自O，S，NH，N（C 1 -C 4烷基）和N（C 1 -C 5） 烷酰基）; X是CH 2或直链，条件是当R 1是1-咪唑基时，则X是CH 2; m为2或3; n为0,1或2，并且其中当n为0或1时，基团（CH 2）n NHR 3连接在5-位，或当n为2时在5-或4-位。这些化合物是选择性TXA2和 PGH2拮抗剂。 有些还抑制血栓素合成酶。

公开(公告)号：US09233964B2

公开(公告)日：2016-01-12

申请号：US13977408

申请日：2012-01-06

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

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

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

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07482375B2

公开(公告)日：2009-01-27

申请号：US11408286

申请日：2006-04-18

Applicant: Paul Anthony Bradley ,  Kevin Neil Dack ,  Ian Roger Marsh

Inventor： Paul Anthony Bradley ,  Kevin Neil Dack ,  Ian Roger Marsh

IPC: A61K31/415 ,  C07D231/10

CPC classification number: C07D231/28 ,  C07D231/18 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06

Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6-alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii)one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be 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.

Abstract translation: 式（I）化合物或其药学上可接受的衍生物，其中：R 1表示H，C 1-6 - 烷基，C 1-6烷氧基，C 3-8环烷基或卤素; R 2表示H，C 1-6烷基（任选被R 3取代），苯基（任选被CN取代）或Het; R3表示OH，CN，Het，-R4-C1-6烷基或CONR5R6; R 4表示-CO 2 - 或-O-; R5和R6独立地表示H，C 1-6烷基（任选被OR 7取代）或C 3-8环烷基; R 7表示H或C 1-6烷基; Het表示含有（i）1-4个氮杂原子或（ii）一个或两个氮杂原子和一个氧或一个硫杂原子的五元或六元芳族杂环基，或（iii）一个或两个氧 或硫杂原子，所述杂环基团任选被一个或多个选自CN和C 1-6烷基的基团取代; R 8表示C 1-6烷基，C 1-6烷氧基，C 3-8环烷基或卤素; R 9和R 10独立地表示H，C 1-6烷基，C 1-6烷氧基，CN，CF 3或卤素; 可能有助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：US06306852B1

公开(公告)日：2001-10-23

申请号：US09556651

申请日：2000-04-24

Applicant: David James Rawson ,  Kevin Neil Dack ,  Roger Peter Dickinson ,  Kim James

Inventor： David James Rawson ,  Kevin Neil Dack ,  Roger Peter Dickinson ,  Kim James

IPC: A61P910

CPC classification number: C07D405/06 ,  C07D209/18 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: 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.

Abstract translation: 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

Applicant: David James Rawson ,  Kevin Neil Dack ,  Roger Peter Dickinson ,  Kim James

Inventor： David James Rawson ,  Kevin Neil Dack ,  Roger Peter Dickinson ,  Kim James

IPC: A61K314025

CPC classification number: C07D405/06 ,  C07D209/18 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: 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.

Abstract translation: 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：US6040309A

公开(公告)日：2000-03-21

申请号：US204789

申请日：1998-12-03

Applicant: Kevin Neil Dack ,  Roger Peter Dickinson

Inventor： Kevin Neil Dack ,  Roger Peter Dickinson

IPC: 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 classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D333/70 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D471/04

Abstract: 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.

Abstract translation: 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：US20090099209A1

公开(公告)日：2009-04-16

申请号：US12333533

申请日：2008-12-12

Applicant: Paul Anthony Bradley ,  Kevin Neil Dack ,  Ian Roger Marsh

Inventor： Paul Anthony Bradley ,  Kevin Neil Dack ,  Ian Roger Marsh

IPC: A61K31/506 ,  A61K31/4152 ,  C07D231/18 ,  C07D413/06 ,  C07D401/06 ,  C07D417/06 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/4155 ,  A61K31/433 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/422 ,  A61K31/4178 ,  C07D403/06

CPC classification number: C07D231/28 ,  C07D231/18 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06

Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; and R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be 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.

Abstract translation: 式（I）化合物或其药学上可接受的衍生物，其中：R 1表示H，C 1-6烷基，C 1-6烷氧基，C 3-8环烷基或卤素; R 2表示H，C 1-6烷基（任选被R 3取代），苯基（任选被CN取代）或Het; R3表示OH，CN，Het，-R4-C1-6烷基或CONR5R6; R 4表示-CO 2 - 或-O-; R5和R6独立地表示H，C 1-6烷基（任选被OR 7取代）或C 3-8环烷基; R 7表示H或C 1-6烷基; Het表示含有（i）1-4个氮杂原子或（ii）一个或两个氮杂原子和一个氧或一个硫杂原子的五元或六元芳族杂环基，或（iii）一个或两个氧 或硫杂原子，所述杂环基团任选被一个或多个选自CN和C 1-6烷基的基团取代; R 8表示C 1-6烷基，C 1-6烷氧基，C 3-8环烷基或卤素; 且R 9和R 10独立地表示H，C 1-6烷基，C 1-6烷氧基，CN，CF 3或卤素; 可能有助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。