KR20030012846A - 고나도트로핀-분비 호르몬 수용체 길항제 및 이와 관련된방법 - Google Patents
고나도트로핀-분비 호르몬 수용체 길항제 및 이와 관련된방법 Download PDFInfo
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Abstract
Description
Claims (45)
- 화학식 I의 구조를 갖는 화합물, 또는 이의 입체이성질체, 프로드럭 또는 약제학적으로 허용되는 염.화학식 I상기식에서,Q는 직접 결합이거나 -(CR8aR8b)r-Z-(CR10aR10b)s- 이고;A는 O, S, 또는 NR7이고;r 및 s은 동일하거나 상이하며, 독립적으로 0, 1, 2, 3, 4, 5 또는 6 이고;n은 2, 3 또는 4 이고;Z는 직접 결합이거나, 또는 -O-, -S-, -NR9-, -SO-, -SO2-, -OSO2-, -SO2O-, -SO2NR9-, -NR9SO2-, -CO-, -COO-, -OCO-, -CONR9-, -NR9CO-, -NR9CONR9a, -OCONR9- 또는 -NR9COO- 이고;R1및 R2는 동일하거나 상이하며, 독립적으로 수소, 알킬, 치환된 알킬, 아릴, 치환된 아릴, 아릴알킬, 치환된 아릴알킬, 헤테로사이클, 치환된 헤테로사이클, 헤테로사이클알킬, 치환된 헤테로사이클알킬, -C(R1a)(=NR1b) 또는 -C(NR1aR1c)(=NR1b) 이거나;R1및 R2는 이들에 결합된 질소 원자와 함께 헤테로사이클릭 환 또는 치환된 헤테로사이클릭 환을 형성하고;R3a및 R3b는 동일하거나 상이하며, 각각 독립적으로 수소, 알킬, 치환된 알킬, 알콕시, 알킬티오, 알킬아미노, 아릴, 치환된 아릴, 아릴알킬, 치환된 아릴알킬, 헤테로사이클, 치환된 헤테로사이클, 헤테로사이클알킬, 치환된 헤테로사이클알킬, -COOR14또는 -CONR14R15이거나;R3a및 R3b는 이들에 결합된 탄소 원자와 함께 호모사이클릭 환, 치환된 호모사이클릭 환, 헤테로사이클릭 환 또는 치환된 헤테로사이클릭 환을 형성하거나;R3a및 R3b는 함께 =NR3c을 형성하거나;R3a및 이에 결합된 탄소 원자는 R1및 이에 결합된 질소 원자와 함께 헤테로사이클릭 환 또는 치환된 헤테로사이클릭 환을 형성하고;R4는 고급 알킬, 치환된 알킬, 아릴, 치환된 아릴, 헤테로사이클, 치환된 헤테로사이클, -COR11, -COOR11, -CONR12R13, -OR11, -OCOR11, -OSO2R11, -SR11, -SO2R11, -NR12R13, -NR11COR12, -NR11CONR12R13, -NR11SO2R12또는 -NR11SO2NR12R13이고;R5는 수소, 할로겐, 저급 알킬, 치환된 저급 알킬, 아릴, 치환된 아릴, 아릴알킬, 치환된 아릴알킬, 알콕시, 알킬티오, 알킬아미노, 시아노 또는 니트로이고;R6은 고급 알킬, 치환된 알킬, 아릴, 치환된 아릴, 아릴알킬, 치환된 아릴알킬, 헤테로아릴, 치환된 헤테로아릴, 헤테로아릴알킬 또는 치환된 헤테로아릴알킬이고;R7은 수소, -SO2R11, 시아노, 알킬, 치환된 알킬, 아릴, 치환된 아릴, 아릴알킬, 치환된 아릴알킬, 헤테로아릴, 치환된 헤테로아릴, 헤테로아릴알킬 또는 치환된 헤테로아릴알킬이고;R1a, R1b, R1c, R3c, R8a, R8b, R9, R9a, R10a, R10b, R11,R12, R13, R14및 R15는 동일하거나 상이하며, 각각 독립적으로 수소, 아실, 알킬, 치환된 알킬, 아릴, 치환된 아릴, 아릴알킬, 치환된 아릴알킬, 헤테로사이클, 치환된 헤테로사이클, 헤테로사이클알킬 또는 치환된 헤테로사이클알킬이거나;R1a와 R1b, R8a와 R8b, R10a와 R10b, R12와 R13, 또는 R14와 R15는 이들에 결합된 원자(들)과 함께 호모사이클릭 환, 치환된 호모사이클릭 환, 헤테로사이클릭 환 또는 치환된 헤테로사이클릭 환을 형성한다.
- 제1항에 있어서, A는 O인 화합물.
- 제1항에 있어서, A는 S인 화합물.
- 제1항에 있어서, A는 NR7인 화합물.
- 제1항에 있어서, R1은 아릴, 치환된 아릴, 아릴알킬, 치환된 아릴알킬, 헤테로사이클, 치환된 헤테로사이클, 헤테로사이클알킬 또는 치환된 헤테로사이클알킬인 화합물.
- 제5항에 있어서, 헤테로사이클이 헤테로아릴이고, 치환된 헤테로사이클이 치환된 헤테로아릴이고, 헤테로사이클알킬이 헤테로아릴알킬이고, 치환된 헤테로사이클알킬이 치환된 헤테로아릴알킬인 화합물.
- 제7항에 있어서, R1은 헤테로아릴알킬 또는 치환된 헤테로아릴알킬인 화합물.
- 제1항에 있어서, R1은 페닐알킬 또는 치환된 페닐알킬인 화합물.
- 제1항에 있어서, R1은 벤질인 화합물.
- 제1항에 있어서, R1은 수소 또는 저급 알킬인 화합물.
- 제1항에 있어서, R2는 수소, 알킬 또는 치환된 알킬인 화합물.
- 제1항에 있어서, R2는 수소 또는 메틸인 화합물.
- 제1항에 있어서, Q는 직접 결합인 화합물.
- 제1항에 있어서, Q는 -(CR8aR8b)r-Z-(CR10aR10b)s- 인 화합물.
- 제1항에 있어서, R3a및 R3b는 각각 수소인 화합물.
- 제1항에 있어서, R3a는 수소, 알킬, 아릴 또는 아릴알킬인 화합물.
- 제1항에 있어서, R3a는 수소, 메틸, 이소부틸, 사이클로헥실, 페닐 또는 벤질인 화합물.
- 제1항에 있어서, R3b는 각각 수소인 화합물.
- 제1항에 있어서, n은 1인 화합물.
- 제1항에 있어서, n은 2인 화합물.
- 제20항에 있어서, -(R3aR3bC)n- 이 -C(R3a)(R3b)CH2- 구조를 갖는 화합물.
- 제21항에 있어서, R3a는 벤질인 화합물.
- 제21항에 있어서, R3a는 알킬인 화합물.
- 제23항에 있어서, R3a는 이소부틸 또는 사이클로헥실인 화합물.
- 제21항에 있어서, R3b는 수소 또는 메틸인 화합물.
- 제1항에 있어서, R4는 치환된 아릴 또는 치환된 헤테로사이클인 화합물.
- 제1항에 있어서, R4는 치환된 페닐인 화합물.
- 제27항에 있어서, R4는 할로겐, 알콕시, 또는 할로겐과 알콕시 둘 모두에 의해 치환된 페닐인 화합물.
- 제1항에 있어서, R5는 H, 저급 알킬 또는 치환된 저급 알킬인 화합물.
- 제1항에 있어서, R5는 수소 또는 메틸인 화합물.
- 제1항에 있어서, R6은 아릴, 치환된 아릴, 아릴알킬, 치환된 아릴알킬, 헤테로아릴, 치환된 헤테로아릴, 헤테로아릴알킬 또는 치환된 헤테로아릴알킬인 화합물.
- 제1항에 있어서, R6은 아릴알킬, 치환된 아릴알킬, 헤테로아릴알킬 또는 치환된 헤테로아릴알킬인 화합물.
- 제1항에 있어서, R6은 벤질 또는 치환된 벤질인 화합물.
- 제1항에 있어서, R6은 2개의 할로겐으로 치환된 벤질인 화합물.
- 제1항에 있어서, Q는 결합이고, R4는 치환된 아릴 또는 헤테로사이클인 화합물.
- 제1항에 있어서, R1은 -CH2(헤테로아릴) 또는 -CH2CH2(헤테로아릴)인 화합물.
- 제1항에 있어서, R1및 R2는 이들에 결합된 질소 원자와 함께 헤테로사이클릭 환 또는 치환된 헤테로사이클릭 환을 형성하는 화합물.
- 제1항의 화합물 및 약제학적으로 허용되는 담체 또는 희석제를 포함하는 약제학적 조성물.
- 유효량의 제1항의 화합물 또는 제38항의 약제학적 조성물을 고나도트로핀-분비 호르몬을 길항시킬 필요가 있는 피험체에게 투여함을 포함하여, 당해 피험체에서 고나도트로핀-분비 호르몬을 길항시키는 방법.
- 유효량의 제1항의 화합물 또는 제38항의 약제학적 조성물을 성-호르몬 관련 증상의 치료를 필요로 하는 피험체에게 투여함을 포함하여, 당해 피험체에서 성-호르몬 관련 증상을 치료하는 방법.
- 제40항에 있어서, 성-호르몬 관련 증상이 암, 양성 전립선 비대증 또는 자궁 근종인 방법.
- 제41항에 있어서, 암이 전립선암, 자궁암, 유방암 또는 뇌하수체 성선자극세포 선종인 방법.
- 제41항에 있어서, 성-호르몬 관련 증상이 자궁내막증, 다낭성 난소 질환, 자궁 유섬유종 또는 성조발증인 방법.
- 유효량의 제1항의 화합물 또는 제38항의 약제학적 조성물을 피임을 필요로 하는 피험체에게 투여함을 포함하여, 당해 피험체를 피임시키는 방법.
- 유효량의 제1항의 화합물 또는 제38항의 약제학적 조성물을 홍반성 루푸스, 과민성 대장 증후군, 월경전 증후군, 다모증, 단신증 또는 수면 장애의 치료를 필요로 하는 피험체에게 투여함을 포함하여, 당해 피험체의 홍반성 루푸스, 과민성 대장 증후군, 월경전 증후군, 다모증, 단신증 또는 수면 장애를 치료하는 방법.
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US6872728B2 (en) | 2005-03-29 |
US20070208049A1 (en) | 2007-09-06 |
NO20023525D0 (no) | 2002-07-24 |
US6608197B2 (en) | 2003-08-19 |
ES2383954T3 (es) | 2012-06-27 |
US7179815B2 (en) | 2007-02-20 |
AU767585B2 (en) | 2003-11-20 |
ATE548357T1 (de) | 2012-03-15 |
MXPA02006848A (es) | 2002-12-13 |
US20040048884A1 (en) | 2004-03-11 |
US7462625B2 (en) | 2008-12-09 |
US20020132820A1 (en) | 2002-09-19 |
HK1051042A1 (en) | 2003-07-18 |
EP1255738B1 (en) | 2012-03-07 |
PT1255738E (pt) | 2012-06-19 |
CY1112815T1 (el) | 2016-02-10 |
EP1255738A2 (en) | 2002-11-13 |
JP2003520856A (ja) | 2003-07-08 |
CA2398018C (en) | 2011-10-18 |
AU3797501A (en) | 2001-08-07 |
CA2398018A1 (en) | 2001-08-02 |
KR100814269B1 (ko) | 2008-03-18 |
WO2001055119A3 (en) | 2002-02-14 |
DK1255738T3 (da) | 2012-06-25 |
US20050234082A1 (en) | 2005-10-20 |
JP4931314B2 (ja) | 2012-05-16 |
NO20023525L (no) | 2002-07-24 |
WO2001055119A2 (en) | 2001-08-02 |
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