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1. 发明申请

WO2004063156A1 NOVEL INDOLE DERIVATES AS FABP-4 INHIBITORS 审中-公开
标题翻译：新型吲哚衍生物作为FABP-4抑制剂
公开(公告)号：WO2004063156A1
公开(公告)日：2004-07-29
申请号：PCT/SE2004/000005
申请日：2004-01-08
申请人： BIOVITRUM AB , BARF, Tjeerd , HAMMER, Kristin , LUTHMAN, Marguerite , LEHMANN, Fredrik , RINGOM, Rune
发明人： BARF, Tjeerd , HAMMER, Kristin , LUTHMAN, Marguerite , LEHMANN, Fredrik , RINGOM, Rune
IPC分类号： C07D209/82
CPC分类号： C07D401/04 , C07D209/88 , C07D209/94 , C07D401/06 , C07D403/06 , C07D403/12 , C07D405/06 , C07D471/04
摘要： The present invention relates to novel compounds (I) wherein R0, R1, R2, R3, R4, R5, R6, R7, R8, A, B, n, X, and Y are as defined in the description and claims; and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament, which acts on the fatty acid binding protein FABP-4. The present invention relates to novel compounds (I) wherein R0, R1, R2, R3, R4, R5, R6, R7, R8, A, B, n, X, and Y are as defined in the description and claims; and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament, which acts on the fatty acid binding protein FABP-4.
摘要翻译：本发明涉及新的化合物（I），其中R 0，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，A，B，n，X和Y如说明书和权利要求中所定义; 还涉及包含该化合物的药物组合物，以及该化合物在药物中的用途以及作用于脂肪酸结合蛋白FABP-4的药物的制备。本发明涉及新的化合物（I），其中R 0，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，A，B，n，X和Y如说明书和权利要求中所定义; 还涉及包含该化合物的药物组合物，以及该化合物在药物中的用途以及作用于脂肪酸结合蛋白FABP-4的药物的制备。

2. 发明申请

WO2003043999A1 INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 审中-公开
标题翻译： 11-羟基甾体脱氢酶1型抑制剂
公开(公告)号：WO2003043999A1
公开(公告)日：2003-05-30
申请号：PCT/SE2002/002140
申请日：2002-11-22
申请人： BIOVITRUM AB , BARF, Tjeerd , EMOND, Rikard , KURZ, Guido , VALLGÅRDA, Jerk , NILSSON, Marianne , ZHANG, Lian
发明人： BARF, Tjeerd , EMOND, Rikard , KURZ, Guido , VALLGÅRDA, Jerk , NILSSON, Marianne , ZHANG, Lian
IPC分类号： C07D277/52
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/52 , C07D417/06 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds with the formula (I), and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-b-hydroxysteroid dehydrogenase type 1 enzyme.
摘要翻译：本发明涉及具有式（I）的化合物，还涉及包含该化合物的药物组合物，以及该化合物在医药中的用途以及用于制备作用于人类11-b-羟基类固醇的药物脱氢酶1型酶。

3. 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。

4. 发明申请

WO2005075471A2 THIAZOL-COMPOUNDS AS 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS 审中-公开
标题翻译：作为11-羟基脱氢酶脱氢酶1型抑制剂的噻唑化合物
公开(公告)号：WO2005075471A2
公开(公告)日：2005-08-18
申请号：PCT/SE2005/000140
申请日：2005-02-04
申请人： BIOVITRUM AB , TEDENBORG, Lars , BARF, Tjeerd , NORDIN, Sofia , VALLGÅRDA, Jerk , WILLIAMS, Meredith , KURZ, Guido
发明人： TEDENBORG, Lars , BARF, Tjeerd , NORDIN, Sofia , VALLGÅRDA, Jerk , WILLIAMS, Meredith , KURZ, Guido
IPC分类号： C07D417/12
CPC分类号： C07D277/54 , C07D417/04 , C07D417/06 , C07D417/12
摘要： The present invention relates to compounds with the formula (I), wherein R1, R2, R3, X, and Y are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.
摘要翻译：本发明涉及具有式（I）的化合物，其中R 1，R 2，R 3，X和Y如本文所定义，并且还涉及包含该化合物的药物组合物，以及该化合物在医药和用于制备作用于人类11-β-羟基类固醇脱氢酶1型酶的药物。

5. 发明公开

EP1283834A1 INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 有权
标题翻译：作者11-β-羟基甾族化合物脱氢酶1型抑制剂
公开(公告)号：EP1283834A1
公开(公告)日：2003-02-19
申请号：EP01937063.4
申请日：2001-05-22
申请人： BIOVITRUM AB
发明人： BARF, Tjeerd , NILSSON, Marianne , VALLGARDA, Jerk
IPC分类号： C07D277/60 , A61K31/426 , A61P3/00 , A61P5/48 , A61P27/06 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/52 , C07D277/56 , C07D277/84 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D491/08 , C07D513/04
摘要： The present invention relates to using a compound having the formula (I) wherein T is I) thienyl, which optionally is substituted with halogen, or II) phenyl optionally substituted with halogen and/or C1-6-alkyl; E is a bond, -CH2- or -CO-; L is a bond, -CH2-, -CHR4- or -NR3-; R3 is H, C¿1-6?-alkyl, C1-6-acyl or -COR?4; R4¿ is morpholino or C¿1-6?-amido; R?6 and R7¿ are independently hydrogen or C¿1-6?-alkyl; and R?8 and R9¿ are independently hydrogen or C¿1-6?-alkyl, as well as pharmaceutically acceptable salts, hydrates and solvates thereof, in the manufacture of a medicament for the treatment or prevention of diabetes, syndrome X, obesity, glaucoma, hyperlipidemia, hyperglycemia, hyperinsulinemia, osteoporosis, tuberculosis, dementia, depression, virus diseases and inflammatory disorders.

6. 发明授权

EP1019364B1 INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 有权
标题翻译：抗蛋白酶抑制剂
公开(公告)号：EP1019364B1
公开(公告)日：2004-06-09
申请号：EP98944476.5
申请日：1998-08-24
申请人： BIOVITRUM AB
发明人： LARSEN, Scott, D. , MAY, Paul, D. , BLEASDALE, John , LILJEBRIS, Charlotta , SCHOSTAREZ, Heinrich, Josef , BARF, Tjeerd
IPC分类号： C07C235/00
CPC分类号： C07D295/215 , A61K38/00 , C07C235/74 , C07C235/80 , C07C237/52 , C07C271/02 , C07C271/22 , C07C275/24 , C07C305/24 , C07C311/06 , C07C311/13 , C07C311/37 , C07C317/50 , C07C323/59 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/66 , C07C2603/70 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/13 , C07K5/06026 , C07K5/06034 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06104 , C07K5/06113 , C07K5/06156
摘要： The present invention comprises small molecular weight, non-peptidic inhibitors of formula (I) and (II) of Protein Tyrosine Phosphatase 1 (PTP1) which are useful for the treatment and/or prevention of Non-Insulin Dependent Diabetes Mellitus (NIDDM).
摘要翻译：本发明包括可用于治疗和/或预防非胰岛素依赖性糖尿病（NIDDM）的蛋白酪氨酸磷酸酶1（PTP1）的分子量小的非肽抑制剂I和II。

7. 发明授权

EP1283834B1 INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 有权
标题翻译：作者11-β-羟基甾族化合物脱氢酶1型抑制剂
公开(公告)号：EP1283834B1
公开(公告)日：2009-09-16
申请号：EP01937063.4
申请日：2001-05-22
申请人： BIOVITRUM AB
发明人： BARF, Tjeerd , NILSSON, Marianne , VALLGARDA, Jerk
IPC分类号： C07D277/60 , A61K31/426 , A61P3/00 , A61P5/48 , A61P27/06 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/52 , C07D277/56 , C07D277/84 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D491/08 , C07D513/04
摘要： The present invention relates to using a compound having the formula (I) wherein T is I) thienyl, which optionally is substituted with halogen, or II) phenyl optionally substituted with halogen and/or C1-6-alkyl; E is a bond, -CH2- or -CO-; L is a bond, -CH2-, -CHR4- or -NR3-; R3 is H, C¿1-6?-alkyl, C1-6-acyl or -COR?4; R4¿ is morpholino or C¿1-6?-amido; R?6 and R7¿ are independently hydrogen or C¿1-6?-alkyl; and R?8 and R9¿ are independently hydrogen or C¿1-6?-alkyl, as well as pharmaceutically acceptable salts, hydrates and solvates thereof, in the manufacture of a medicament for the treatment or prevention of diabetes, syndrome X, obesity, glaucoma, hyperlipidemia, hyperglycemia, hyperinsulinemia, osteoporosis, tuberculosis, dementia, depression, virus diseases and inflammatory disorders.

8. 发明公开

EP1461325A1 INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 有权
标题翻译： 11-β-羟基类固醇脱氢酶1型抑制剂
公开(公告)号：EP1461325A1
公开(公告)日：2004-09-29
申请号：EP02789090.4
申请日：2002-11-22
申请人： BIOVITRUM AB
发明人： BARF, Tjeerd , EMOND, Rikard , KURZ, Guido , VALLG RDA, Jerk , NILSSON, Marianne , ZHANG, Lian
IPC分类号： C07D277/52
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/52 , C07D417/06 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds with the formula (I), and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-b-hydroxysteroid dehydrogenase type 1 enzyme.
摘要翻译：本发明涉及具有式（I）的化合物，还涉及包含该化合物的药物组合物，以及该化合物在药物中的用途以及用于制备作用于人类11-β-羟基类固醇的药物的用途脱氢酶1型酶。

9. 发明公开

EP1283833A1 INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 审中-公开
标题翻译： 11-β-羟基类固醇脱氢酶1型抑制剂
公开(公告)号：EP1283833A1
公开(公告)日：2003-02-19
申请号：EP01938885.9
申请日：2001-05-22
申请人： BIOVITRUM AB
发明人： BARF, Tjeerd , NILSSON, Marianne , KURZ, Guido , VALLGARDA, Jerk
IPC分类号： C07D277/52 , A61K31/426 , A61P3/00 , A61P5/48 , A61P27/06 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/52 , C07D277/56 , C07D277/84 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D491/08 , C07D513/04
摘要： The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.
摘要翻译：本发明涉及具有式（I）的化合物以及包含该化合物的药物组合物，其制备方法，以及该化合物在药物中的用途以及制备作用于人的药物的用途 11-β-羟基类固醇脱氢酶1型酶。

10. 发明公开

EP1283831A1 INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 审中-公开
标题翻译： 11-β-羟基类固醇脱氢酶1型抑制剂
公开(公告)号：EP1283831A1
公开(公告)日：2003-02-19
申请号：EP01934781.4
申请日：2001-05-22
申请人： BIOVITRUM AB
发明人： BARF, Tjeerd , EMOND, Rikard , KURZ, Guido , VALLG RDA, Jerk , NILSSON, Marianne
IPC分类号： C07D277/52 , A61K31/426 , A61P3/00 , A61P5/48 , A61P27/06 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/52 , C07D277/56 , C07D277/84 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D491/08 , C07D513/04
摘要： The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of thecompounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.
摘要翻译：本发明涉及具有式（II）的化合物，还涉及包含所述化合物的药物组合物，其制备方法，以及该化合物在药物中的用途以及用于制备作用于人11的药物的用途 -β-羟基类固醇脱氢酶1型酶。

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