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1. 发明申请

WO2009037220A1 TRICYCLIC HETEROCYCLIC DERIVATIVES 审中-公开
标题翻译：三元杂环衍生物
公开(公告)号：WO2009037220A1
公开(公告)日：2009-03-26
申请号：PCT/EP2008/062229
申请日：2008-09-15
申请人： N.V. ORGANON , GROVE, Simon James Anthony , KIYOI, Takao , MISTRY, Ashvinkumar Dhirubhai , RAY, Peter, Christopher , WISHART, Grant
发明人： GROVE, Simon James Anthony , KIYOI, Takao , MISTRY, Ashvinkumar Dhirubhai , RAY, Peter, Christopher , WISHART, Grant
IPC分类号： C07D491/052 , A61K31/40 , A61P25/00
CPC分类号： C07D491/052
摘要： The present invention relates to a tricyclic heterocyclic derivative of Formula (I) wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular for the treatment of serotonin-mediated disorders such as obesity, schizophrenia and cognitive dysfunction.
摘要翻译：本发明涉及式（I）的三环杂环衍生物，其中变量如说明书中所定义。本发明还涉及包含这些化合物的药物组合物及其在治疗中的用途，特别是用于治疗5-羟色胺介导的障碍，例如肥胖，精神分裂症和认知功能障碍。

2. 发明申请

WO2010103001A1 TRICYCLIC HETEROCYCLIC DERIVATIVES 审中-公开
标题翻译：三元杂环衍生物
公开(公告)号：WO2010103001A1
公开(公告)日：2010-09-16
申请号：PCT/EP2010/052976
申请日：2010-03-09
申请人： N.V. ORGANON , DAVIES, Keneth , KIYOI, Takao , MISTRY, Ashvinkumar Dhirubhai , RAY, Peter, Christopher , REID, Mark , WISHART, Grant
发明人： DAVIES, Keneth , KIYOI, Takao , MISTRY, Ashvinkumar Dhirubhai , RAY, Peter, Christopher , REID, Mark , WISHART, Grant
IPC分类号： C07D209/62 , A61K31/403 , A61P25/00
CPC分类号： C07D209/62
摘要： The present invention relates to a tricyclic heterocyclic derivative according to Formula (I), wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to pharmaceutical compositions comprising said tricyclic heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of serotonin mediated disorders, such as obesity.
摘要翻译：本发明涉及式（I）的三环杂环衍生物，其中变量如说明书中所定义，或其药学上可接受的盐或溶剂合物。本发明还涉及包含所述三环杂环衍生物的药物组合物及其在治疗中的用途，例如用于治疗或预防5-羟色胺介导的障碍，例如肥胖症。

3. 发明申请

WO2008020081A1 6-SUBSTITUTED ISOQUINOLINE DERIVATIVES AS ROCK-1 INHIBITORS 审中-公开
标题翻译： 6取代的异喹啉衍生物作为ROCK-1抑制剂
公开(公告)号：WO2008020081A1
公开(公告)日：2008-02-21
申请号：PCT/EP2007/058593
申请日：2007-08-17
申请人： N.V. ORGANON , RAY, Peter, Christopher , LAATS, Steven , MORPHY, John, Richard , SHERBORNE, Brad
发明人： RAY, Peter, Christopher , LAATS, Steven , MORPHY, John, Richard , SHERBORNE, Brad
IPC分类号： C07D217/22 , C07D217/24 , A61K31/472 , A61P9/10 , A61P27/06
CPC分类号： C07D217/22 , C07D217/24
摘要： The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH 2 ; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R 1 is H, when Y is NH 2 ; or R 1 is H, (C 1-4 )alk yl or halogen, when Y is OH; R 2 and R 3 are independently H, (C 1-4 )alkyl or halogen; R 4 is H or (C 1-6 )alkyl, optionally substituted with halogen, (C 3-7 )cycloalkyl, (C 6-10 )aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C 6-10 )aryl and heterocyclic ring being optionally substituted with (C 1-4 )alkyl, (C 1-4 )alkyloxy or halogen; R 5 is H or (C 1-4 )alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH, n is 0 and m+o =2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such as glaucoma, hypertension and atherosclerosis.
摘要翻译：本发明涉及具有通式I的6-取代的异喹啉衍生物，其中X是O，S或NH; Y是OH或NH 2; m为0,1或2; n为0或1; o为0或1; R 1是H，当Y是NH 2时; 或者R 1是H，（C 1-4）烷基或卤素，当Y是OH时; R 2和R 3独立地是H，（C 1-4烷基）烷基或卤素; R 4是H或（C 1-6 - ）烷基，任选被卤素，（C 3-7）环烷基取代，（C 1 -C 6）（C 6-10）芳基或饱和的5-或6-元杂环，其包含1-3个独立地选自O，S和N的杂原子，芳基和杂环任选被（C 1-4烷基）烷基，（C 1-4-4烷基）烷氧基或卤素取代; R 5是H或（C 1-4烷基）烷基; 或其药学上可接受的盐，条件是其中X为O，Y为OH，n为0且m + o = 2的式I化合物排除于包含该化合物的药物组合物中，以及使用的所述6-取代的异喹啉衍生物用于制备用于治疗ROCK-1相关疾病如青光眼，高血压和动脉粥样硬化的药物。

4. 发明申请

WO2007065916A1 ISOQUINOLINE DERIVATIVES 审中-公开
标题翻译：异喹啉衍生物
公开(公告)号：WO2007065916A1
公开(公告)日：2007-06-14
申请号：PCT/EP2006/069392
申请日：2006-12-06
申请人： N.V. ORGANON , RAY, Peter, Christopher
发明人： RAY, Peter, Christopher
IPC分类号： C07D401/12 , A61K31/47
CPC分类号： C07D401/12
摘要： The invention relates to isoquinoline derivatives having the general Formula (I) wherein X is O, S or NH; Y is OH or NH 2 ; m is 0, 1 or 2; n is 1 or 2; R 1 is H, when Y is NH 2 ; or R 1 is H, (C 1-4 )alkyl or halogen, when Y is OH; R 2 and R 3 are independently H, (C 1-4 )alkyl or halogen; R is H or (C 1-6 )alkyl, optionally substituted with OH, (C 1-4 )- alkyloxy, (C 1-4 )alkyloxycarbonyl, (C 3-7 )cycloalkyl, which may optionally comprise a heteroatom selected from O and S, (C 6-10 )aryl, (C 6-10 )aryloxy or a 5- or 6-membered heteroaryl group comprising 1-3 heteroatoms independently selected from O, N and S, each aryl or heteroaryl group being optionally substituted with 1-3 substituents independently selected from (C 1-4 )alkyl, (C 1-4 )alkyloxy, (C 1-4 )alkylsulfonyl and halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of the isoquinoline derivatives in the treatment of ROCK-I related disorders such as hypertension, atherosclerosis and glaucoma.
摘要翻译：本发明涉及具有通式（I）的异喹啉衍生物，其中X为O，S或NH; Y是OH或NH 2; m为0,1或2; n为1或2; R 1是H，当Y是NH 2时; 或者R 1是H，（C 1-4）烷基或卤素，当Y是OH时; R 2和R 3独立地是H，（C 1-4烷基）烷基或卤素; R是H或（C 1-6）烷基，任选被OH取代，（C 1-4烷基） - 烷氧基，（C 1-4 - （C 3-7）环烷基，其可以任选地包含选自O和S的杂原子，（C 1-6-10）芳基，（C 1 -C 6）芳基氧基或含有1-3个独立地选自O，N和S的杂原子的5或6元杂芳基，每个芳基或杂芳基任选被1-3个独立选择的取代基取代（C 1-4）烷基，（C 1-4烷基）烷氧基，（C 1-4烷基）烷基磺酰基和卤素; 或其药学上可接受的盐用于包含其的药物组合物以及异喹啉衍生物在治疗ROCK-1相关疾病如高血压，动脉粥样硬化和青光眼中的用途。

5. 发明申请

WO2004007501A1 BIOLOGICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：生物活性化合物
公开(公告)号：WO2004007501A1
公开(公告)日：2004-01-22
申请号：PCT/GB2003/002957
申请日：2003-07-15
申请人： AMURA THERAPEUTICS LIMITED , QUIBELL, Martin , RAY, Peter, Christopher , WATTS, John Paul
发明人： QUIBELL, Martin , RAY, Peter, Christopher , WATTS, John Paul
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Compounds of general formula (I) wherein: Z = CR 3 R 4 , where R 3 and R 4 are independently chosen from C O-7 -alkyl P 1 = CR 5 R 6 , P 2 = O, CR 7 R 8 or NR 9 , Y = CR 10 R 11 -C(O) or CR 10 R 11 -C(S) or CR 10 R 11 -S(O) or CR 10 R 11 -SO 2 (X) o =.CR 16 R 17 (W) n = 0, S, C(O), S(O) or S(O) 2 -or NR 18 (V) m = C(O), C(S), S(O), S(O) 2 , S(O) 2 NH, OC(O), NHC(O), NHS(O), NHS(O) 2 , OC(O)NH, C(O)NH or CR 19 R 20 , C=N-C(O)-OR 19 or C=N-C(O)-NHR 19 , U = a stable. 5- to 7-membered monocyclic or a stable 8- to 11-membered bicyclic ring which is either saturated or unsaturated, and which includes zero to four heteroatoms and their salts, hydrates, solvates, complexes and prodrugs are inhibitors of cathepsin K and other cysteine protease inhibitors and are useful as therapeutic agents, .for example in osteoporosis, Paget's disease gingival diseases such as gingivitis and periodontitis, hypercalaemia of malignancy, metabolic bone disease, diseases involving matrix or cartilage degradation, in particular osteoarthritis and rheumatoid arthritis and neoplastic diseases. The compounds are also useful for validating therapeutic target compounds.
摘要翻译：通式（I）的化合物，其中：Z = CR 3 R 4，其中R 3和R 4独立地选自CO-7-烷基P1 = CR 5 R 6， R 2 = O，CR 7 R 8或NR 9，Y = CR 10 R 11 -C（O）或CR 10 R 11 -C（S）（O）或CR 10 R 11 -SO 2（X）o = CR 16 R 17（W）n = 0，S，C（O） S（O）或S（O）2 - 或NR 18（V）m = C（O），C（S），S（O），S（O）2，S（O）2 NH，OC O），NHC（O），NHS（O），NHS（O）2，OC（O）NH，C（O）NH或CR 19 R 20，C = NC（O） >或C = NC（O）-NHR 19，U =稳定的。 5-至7-元单环或饱和或不饱和的稳定的8至11元双环，并且其包括0至4个杂原子及其盐，水合物，溶剂化物，复合物和前药是组织蛋白酶K等的抑制剂半胱氨酸蛋白酶抑制剂，并且可用作治疗剂，例如骨质疏松症，佩吉特氏病牙龈疾病如牙龈炎和牙周炎，恶性高钙血症，代谢性骨病，涉及基质或软骨降解的疾病，特别是骨关节炎和类风湿性关节炎和肿瘤性疾病。所述化合物也可用于验证治疗性目标化合物。

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