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1. 发明申请

WO2005048916A3 TETRAHYDROSPIRO-BETA-CARBOLINE-1,3 '-PYRROLIDINE DERIVATIVES AND THEIR USE IN GHSR-RELATED DISORDERS 审中-公开
标题翻译：四氢呋喃 - 吡咯烷-1,3'-吡咯烷衍生物及其在GHS相关疾病中的用途
公开(公告)号：WO2005048916A3
公开(公告)日：2007-12-13
申请号：PCT/SE2004001688
申请日：2004-11-18
申请人： BIOVITRUM AB , BRANDT PETER , BREMBERG ULF , CROSSLEY ROGER , GRAFFNER NORDBERG MALIN , JENMALM JENSEN ANNIKA , RINGBERG ERIK , WARD TERRY
发明人： BRANDT PETER , BREMBERG ULF , CROSSLEY ROGER , GRAFFNER NORDBERG MALIN , JENMALM JENSEN ANNIKA , RINGBERG ERIK , WARD TERRY
IPC分类号： C07D471/14 , A61K20060101 , A61K31/407 , A61K31/438 , A61K31/4747 , A61P3/04 , A61P3/10 , A61P5/08 , A61P9/04 , A61P9/10 , A61P35/00 , C07D209/00 , C07D221/00 , C07D317/00 , C07D471/00 , C07D471/18 , C07D471/20 , C07D471/22 , C07D491/00 , C07D491/14 , C07D491/20 , C07D491/22
CPC分类号： C07D471/20 , C07D491/20
摘要： The present invention relates to compounds of Formula (I): Formula (I) wherein R 3 -R 8 , X, and Y are as described herein, processes for preparing the compounds, pharmaceutical compositions comprising the compounds, and use of the compounds and compositions in the prophylaxis or treatment of a GHSR receptor-related disorder. Examples of such disorders are obesity and related disorders such as diabetes type II, dyslipidemia and the metabolic syndrome Prader-Willi syndrome, cardiovascular diseases such as atherosclerotic vascular disease, angina pectoris, myocardial infarction and stroke, acromegaly and cancer, in particular breast, lung, prostate, thyroid and endocrine pituary carcinomas.
摘要翻译：本发明涉及式（I）的化合物：式（I）其中R 3，R 3，X和Y如本文所述，制备方法化合物，包含该化合物的药物组合物，以及该化合物和组合物在预防或治疗GHSR受体相关病症中的用途。这种障碍的例子是肥胖症和相关疾病，例如II型糖尿病，血脂异常和代谢综合征Prader-Willi综合征，心血管疾病如动脉粥样硬化性血管疾病，心绞痛，心肌梗死和中风，肢端肥大症和癌症，特别是乳腺，肺，前列腺，甲状腺和内分泌腺癌。

2. 发明申请

WO2004020418A1 2,4- DIAMINO QUINAZOLINE AND PYRIDOPYRIMIDINE ESTER DERIVATIVES AS DIHYDROFOLATE REDUCTASE INHIBITORS 审中-公开
标题翻译： 2,4-二氨基喹唑啉和吡咯烷酮衍生物作为二氢叶酸还原酶抑制剂
公开(公告)号：WO2004020418A1
公开(公告)日：2004-03-11
申请号：PCT/GB2003/003714
申请日：2003-08-27
申请人： MELACURE THERAPEUTICS AB , PETT, Christopher, Phineas , HALLBERG, Anders , GRAFFNER-NORDBERG, Malin , BOMAN, Arne , SEIFERT, Elisabeth
发明人： HALLBERG, Anders , GRAFFNER-NORDBERG, Malin , BOMAN, Arne , SEIFERT, Elisabeth
IPC分类号： C07D239/95
CPC分类号： C07D239/95
摘要： The invention provides novel compounds of the formula 11: wherein R 1 , R 2 , R 3 and R 4 are independently hydrogen or a group that liberates the free amine in vivo , for example -CO-alkyl, preferably -CO-C 1 -C 3 alkyl or pivalate; or -COhaloalkyl, preferably -CO-C 1 -C 3 haloalkyl, most preferably -CO-C 1 -C 3 chloroalkyl; wherein W is; and @ denotes the points of attachment and wherein the ester can be located in either direction; wherein n and m are independently 0-5; wherein one but not both of X and Y can be nitrogen, or X is C-A and/or Y is C-B; wherein A and B are independently selected from hydrogen, alkyl optionally substituted with a halogen, an electron donor group such as amino, alkylamino, dialkylamino or hydroxy, or an electron acceptor group such as nitro, cyano, trihaloalkyl or amido, alkoxy or halogen; and pharmacologically acceptable salts thereof. Provided that when R 1 to R 4 are hydrogen, both X and Y are C-H, n is 1 and -(CH 2 ) n - is attached to the bridging oxygen of the ester group W, then m cannot be 0 or 1.
摘要翻译：本发明提供式11的新化合物：其中R 1，R 2，R 3和R 4独立地为氢或在体内释放游离胺的基团，例如-CO-烷基，优选-CO-C 1 -C 3烷基或特戊酸酯; 或-CO卤代烷基，优选-CO-C 1 -C 3卤代烷基，最优选-CO-C 1 -C 3氯代烷基; 其中W是; 和@表示连接点，并且其中酯可以位于任一方向上; 其中n和m独立地为0-5; 其中X和Y中的一个但不是二者可以是氮，或X是C-A和/或Y是C-B; 其中A和B独立地选自氢，任选被卤素取代的烷基，电子给体基团如氨基，烷基氨基，二烷基氨基或羟基，或电子受体基团如硝基，氰基，三卤代烷基或酰胺基，烷氧基或卤素; 及其药理学上可接受的盐。假设当R1至R4为氢时，X和Y均为C-H，n为1， - （CH2）n-连接到酯基W的桥连氧上，则m不能为0或1。

3. 发明申请

WO2009003681A1 DPP-IV INHIBITORS 审中-公开
标题翻译： DPP-IV抑制剂
公开(公告)号：WO2009003681A1
公开(公告)日：2009-01-08
申请号：PCT/EP2008/005370
申请日：2008-07-01
申请人： SANTHERA PHARMACEUTICALS (SCHWEIZ) AG , BIOVITRUM AB , NORDHOFF, Sonja , ROSENBAUM, Claudia , RUMMEY, Christian , FEURER, Achim , BULAT, Stephan , GRAFFNER NORDBERG, Malin , GUSTAVSSON, Anna-Lena , HOFFMANN-ENGER, Barbara
发明人： NORDHOFF, Sonja , ROSENBAUM, Claudia , RUMMEY, Christian , FEURER, Achim , BULAT, Stephan , GRAFFNER NORDBERG, Malin , GUSTAVSSON, Anna-Lena , HOFFMANN-ENGER, Barbara
IPC分类号： C07D401/06 , A61K31/505 , A61P3/10
CPC分类号： C07D401/06
摘要： The invention relates to compounds of formula (I) wherein R 1 , R 2 , R 3 and n have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3和n具有在说明书和权利要求书中引用的含义。所述化合物可用作DPP-IV抑制剂。本发明还涉及这种化合物的制备以及其作为药物的生产和使用。

4. 发明申请

WO2005048916A2 NOVEL BETA-CARBOLINES AS GROWTH HORMONE SECRETAGOGUE RECEPTOR (GHSR) ANTAGONISTS 审中-公开
标题翻译：作为生长激素分泌受体（GHSR）拮抗剂的新型β-CARBOLINS
公开(公告)号：WO2005048916A2
公开(公告)日：2005-06-02
申请号：PCT/SE2004/001688
申请日：2004-11-18
申请人： BIOVITRUM AB , BRANDT, Peter , BREMBERG, ULF , CROSSLEY, Roger , GRAFFNER NORDBERG, Malin , JENMALM JENSEN, Annika , RINGBERG, Erik , WARD, Terry
发明人： BRANDT, Peter , BREMBERG, ULF , CROSSLEY, Roger , GRAFFNER NORDBERG, Malin , JENMALM JENSEN, Annika , RINGBERG, Erik , WARD, Terry
IPC分类号： A61K
CPC分类号： C07D471/20 , C07D491/20
摘要： The present invention relates to compounds of Formula (I): Formula (I) wherein R 3 -R 8 , X, and Y are as described herein, processes for preparing the compounds, pharmaceutical compositions comprising the compounds, and use of the compounds and compositions in the prophylaxis or treatment of a GHSR receptor-related disorder. Examples of such disorders are obesity and related disorders such as diabetes type II, dyslipidemia and the metabolic syndrome Prader-Willi syndrome, cardiovascular diseases such as atherosclerotic vascular disease, angina pectoris, myocardial infarction and stroke, acromegaly and cancer, in particular breast, lung, prostate, thyroid and endocrine pituary carcinomas.
摘要翻译：本发明涉及式（I）化合物：式（I）其中R 3 -R 8，X和Y如本文所述，制备化合物的方法，包含该化合物的药物组合物和使用化合物和组合物在预防或治疗GHSR受体相关病症中的作用。这种障碍的例子是肥胖症和相关疾病，例如II型糖尿病，血脂异常和代谢综合征Prader-Willi综合征，心血管疾病如动脉粥样硬化性血管疾病，心绞痛，心肌梗死和中风，肢端肥大症和癌症，特别是乳腺，肺，前列腺，甲状腺和内分泌腺癌。

5. 发明申请

WO2006122931A1 BETA-CARBOLINE DERIVATIVES AND THERI USE AS GHSR MODULATORS 审中-公开
标题翻译：测定碳氢化合物衍生物，并作为GHSR调节剂使用
公开(公告)号：WO2006122931A1
公开(公告)日：2006-11-23
申请号：PCT/EP2006/062343
申请日：2006-05-16
申请人： BIOVITRUM AB , GRAFFNER NORDBERG, Malin , BARF, Tjeerd , MOTT, Andrew
发明人： GRAFFNER NORDBERG, Malin , BARF, Tjeerd , MOTT, Andrew
IPC分类号： C07D471/20 , A61K31/438 , A61P3/04
CPC分类号： C07D471/20
摘要： The present invention relates to compounds of Formula (I): wherein R 1 to R 3 are as described herein, processes for preparing the compounds, pharmaceutical compositions comprising the compounds, and use of the compounds and compositions in the prophylaxis or treatment of a GHSR receptor-related disorder. Examples of such disorders are obesity and related disorders such as diabetes type II, dyslipidemia and the metabolic syndrome Prader-Willi syndrome, cardiovascular diseases such as atherosclerotic vascular disease, angina pectoris, myocardial infarction and stroke, intestinal inflammation that is associated with inflammatory bowel diseases (IBD) such as Crohn's disease and ulcerative colitis, acromegaly and cancer, in particular breast, lung, prostate, thyroid and endocrine pituary carcinomas.
摘要翻译：本发明涉及式（I）化合物：其中R 1至R 3如本文所述，制备化合物的方法，包含该化合物的药物组合物和化合物和组合物在预防或治疗GHSR受体相关病症中的用途。这种障碍的实例是肥胖症和相关疾病，例如II型糖尿病，血脂异常和代谢综合征Prader-Willi综合征，心血管疾病如动脉粥样硬化性血管疾病，心绞痛，心肌梗塞和中风，与炎症性肠病相关的肠道炎症（IBD）如克罗恩病和溃疡性结肠炎，肢端肥大症和癌症，特别是乳腺癌，肺癌，前列腺癌，甲状腺和内分泌性胰腺癌。

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