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1. 发明申请

WO2004048345A3 2,5-DIKETOPIPERAZINES FOR THE TREATMENT OF OBESITY 审中-公开
标题翻译：用于治疗肥胖的2,5-二西他啶
公开(公告)号：WO2004048345A3
公开(公告)日：2004-07-15
申请号：PCT/DK0300797
申请日：2003-11-20
申请人： NOVO NORDISK AS , BOEHRINGER INGELHEIM INT
发明人： CONDE-FRIEBOES KILIAN WALDEMAR , ANKERSEN MICHAEL , SENSFUSS ULRICH , WULFF BIRGITTE SCHJELLERUP , THOEGERSEN HENNING , LUSTENBERGER PHILIPP , RUDOLF KLAUS , KRIST BERND , MUELLER STEPHAN , STENKAMP DIRK , SCHINDLER MARCUS , WIELAND HEIKE , ARNDT KIRSTEN
IPC分类号： A61P15/10 , C07D241/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/14 , A61K31/495 , C07D241/06
CPC分类号： C07D401/06 , C07D241/08 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/14
摘要： The present invention relates to novel compounds of the general formula (I) as well as any optical or geometric isomer or tautomer form thereof, or a pharmaceutically acceptable salt thereof, as agonists of melanocortin receptors, such as agonists of the MC4 receptor. The compounds may for instance be used in the treatment of obesity.
摘要翻译：本发明涉及通式（I）的新颖化合物及其任何光学或几何异构体或互变异构体形式或其药学上可接受的盐作为黑皮质素受体的激动剂，例如MC4受体的激动剂。该化合物可用于治疗肥胖症。

2. 发明专利

DE10238865A1 New carboxamides are melanin-concentrating hormone receptor antagonists, useful for treating e.g. metabolic diseases, diabetes, eating disorders, cardiovascular disease, emotional disorders, reproductive and memory disorders 未知
公开(公告)号：DE10238865A1
公开(公告)日：2004-03-11
申请号：DE10238865
申请日：2002-08-24
申请人： BOEHRINGER INGELHEIM INT , NOVO NORDISK AS
发明人： STENKAMP DIRK , LEHMANN-LINTZ THORSTEN , MUELLER STEPHAN , RUDOLF KLAUS , LUSTENBERGER PHILLIP , ARNDT KIRSTEN , LOTZ RALF , WIELAND HEIKE , LENTER MARTIN
IPC分类号： C07C233/78 , C07D205/04 , C07D207/09 , C07D207/16 , C07D207/20 , C07D209/14 , C07D209/44 , C07D209/46 , C07D209/48 , C07D211/34 , C07D211/52 , C07D211/64 , C07D213/40 , C07D213/56 , C07D213/74 , C07D217/04 , C07D221/24 , C07D221/26 , C07D223/16 , C07D239/91 , C07D239/96 , C07D249/18 , C07D295/073 , C07D295/096 , C07D295/135 , C07D295/185 , C07D295/192 , C07D295/215 , C07D401/04 , C07D401/10 , C07D403/10 , C07D407/10 , C07D451/02 , C07D471/10 , C07D487/10 , C07D239/88 , C07D239/90 , C07D217/24 , C07D401/00 , C07D253/00 , C07D237/32 , C07D241/00 , C07D213/00 , A61K31/517 , A61K31/44 , A61K31/495
摘要： Carboxamides (I), their tautomers, diastereoisomers, enantiomers, mixtures and salts are new. Carboxamides of formula (I), their tautomers, diastereoisomers, enantiomers, mixtures and salts are new, including compounds where hydrogen atoms on carboxy or nitrogen are replaced by a group that can be cleaved in vivo. R1 and R2 = hydrogen, 1-8C alkyl or 3-7C cycloalkyl, both optionally substituted by R11, or phenyl, optionally substituted by one or more R12 and/or nitro, R1+R2 = 2-8C alkylene (particularly having one or two CH2 replaced by CH=N or CH=CH; or having one or two CH2 replaced by oxygen, sulfur, CO, C(=CH2) or NR13, provided two heteroatoms are not adjacent; having one or more hydrogen replaced by R14; or is substituted by 1 or 2 Cy, bound through single or double bonds, a single C, forming a spiro system, two adjacent C and/or N, forming a fused bicyclic system, or 3 or more C and/or N atoms, forming a bridged bicyclic system; R3 = hydrogen, 1-6C alkyl, 3-7C cycloalkyl, 3-7C cycloalkyl(1-4C)alkyl or 2-6C alkyl substituted by 1-6C alkoxy or amino, optionally substituted by 1 or 2 1-3C alkyl; X = single bond or 1-8C alkylene (particularly having 1 or 2 CH2 replaced by CH=CH, ethynyl, oxygen, S(O)x, CO or NR4, provided heteroatoms are not connected; and/or having 1 or 2 C substituted by hydroxy, omega-(hydroxy or 1-3C alkoxy) alkyl and/or 1-3C alkoxy and/or 1-6C alkyl; X+R1 or Z+R3 = heterocycle; Z = 1-4C alkylene (particularly two adjacent C may be linked by another 1-4C alkylene; one CH2 may be replaced by oxygen or NR5, or 1 or 2 C may be substituted by hydroxy, omega-(hydroxy or 1-3C alkoxy) alkyl, 1-3C alkoxy or amino(1-3C)alkyl (optionally N substituted by 1 or 2 1-3C alkyl) and/or 1 or 2 1-6C alkyl); A+Y' = carbocyclic or heterocyclic groups (Cy), and R1 with Y may form a heterocyclic group fused on Y and/or R3 with Y may form a saturated or partially unsaturated heterocycle fused on Y; A+R3 (i.e. -N(R3)CO-A-) = moiety of formula (i); Q = CR6R7, CR6=CR7, N=CR8, N=N, CONR9, CR8=N or CO; L1-L3 = R20; B' = Cy, bonded through a C atom of the carbocyclic part or fused phenyl or pyridyl or through N or C atom of the heterocyclic part; W' = single bond, oxygen, 1-4C alkylene(oxy), 2-4C alkenylene, oxy(1-4C)alkylene, 1-3C alkyleneoxy(1-3C)alkylene, (1-3C alkyl)imino, (1-3C alkyl)imino(1-4C)alkylene or 1-4C alkylene(1-3C alkyl)imino; W'-B' = W'=B' (i.e.(oxy)alkylene or alkyleneoxyalkylene); Cy = saturated 3-7 membered carbocycle; unsaturated 5-7 membered carbocycle; phenyl; saturated 4-7 membered or unsaturated 5-7 membered heterocycle containing nitrogen, oxygen or sulfur as heteroatoms; (un)saturated 5-7 membered heterocycle with 2 or more N or with one N and one O or S; aromatic 5 or 6 membered heterocycle with one or more of N, O and/or S; the 5-7 membered rings may be fused to a phenyl or pyridyl ring and/or have one CH2 replaced by CO, C(=CH2), SO or SO2; and the 6-7 membered rings may exist as bridged systems, containing imino (optionally substituted by 1-3C alkyl) or methylene, optionally substituted by 1 or 2 1-3C alkyl; and all optionally substituted on 1 or more C by R20 (also by nitro for phenyl groups) and/or by 1 or more R21 on N; R4, R5 and R16 = hydrogen, 3-7C cycloalkyl (Cyl), Cyl(1-3C)alkyl, 4-7C cycloalkenyl (Cya), Cya(1-3C)alkyl, omega-(hydroxy or 1-3C alkoxy)2-3C alkyl, or amino(1-6C)alkyl, optionally N-substituted by 1 or 2 1-3C alkyl; R6-R9 = hydrogen, 1-6C alkyl or omega-(hydroxy or 1-3C alkoxy)alkyl; also (except for R9) halo; R11 = R15O, R15OCO, R16R17N, R18R19NCO or Cy; R12 and R20 = halo, hydroxy, cyano, 1-4C alkyl, Cyl, hydroxy(1-3C)alkyl, R22-(1-3C)alkyl or R22; R13 and R17 = R16, also phenyl, phenyl(1-3C)alkyl, dioxolan-2-yl, 1-3C alkylcarbonyl, carboxy(1-3C)alkyl, 1-3C alkylcarbonylamino(2-3C)alkyl, 1-3C alkylsulfonyl or 1-3C alkylsulfonylamino(2-3C)alkyl; R14 = halo, 1-6C alkyl, R15O, R15OCO, R16R17N, R18R19NCO, R15O- or R15-OCO- (1-3C)alkyl, R16R17N(1-3C)alkyl, R18R19NCO(1-3C)alkyl or Cy-(1-3C)alkyl; R15 = hydrogen, 1-4C alkyl,

3. 发明专利

CA2506843A1 2,5-DIKETOPIPERAZINES FOR THE TREATMENT OF OBESITY 未知
公开(公告)号：CA2506843A1
公开(公告)日：2004-06-10
申请号：CA2506843
申请日：2003-11-20
申请人： NOVO NORDISK AS , BOEHRINGER INGELHEIM INT
发明人： RUDOLF KLAUS , STENKAMP DIRK , SCHINDLER MARCUS , LUSTENBERGER PHILIPP , MUELLER STEPHAN , KRIST BERND , THOGERSEN HENNING , ANKERSEN MICHAEL , SENSFUSS ULRICH , WULFF BIRGITTE SCHJELLERUP , CONDE-FRIEBOES KILIAN WALDEMAR , ARNDT KIRSTEN , WIELAND HEIKE
IPC分类号： A61P15/10 , C07D241/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/14 , C07D241/06 , A61K31/495
摘要： The present invention relates to novel compounds of the general formula (I) as well as any optical or geometric isomer or tautomer form thereof, or a pharmaceutically acceptable salt thereof, as agonists of melanocortin receptors, such as agonists of the MC4 receptor. The compounds may for instance be used in the treatment of obesity.

4. 发明专利

AU2003281978A8 Compounds for use in treating obesity 未知
公开(公告)号：AU2003281978A8
公开(公告)日：2004-06-18
申请号：AU2003281978
申请日：2003-11-20
申请人： NOVO NORDISK AS , BOEHRINGER INGELHEIM INT
发明人： WULFF BIRGITTE SCHJELLERUP , THOGERSEN HENNING , LUSTENBERGER PHILIPP , RUDOLF KLAUS , KRIST BERND , MULLER STEPHAN , STENKAMP DIRK , SCHINDLER MARCUS , WIELAND HEIKE , ARNDT KIRSTEN , CONDE-FRIEBOES KILIAN WALDEMAR , ANKERSEN MICHAEL , SENSFUSS ULRICH
IPC分类号： A61P15/10 , C07D241/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/14 , C07D241/00
摘要： Described herein are novel and useful compounds of the general formula Compounds of this invention can advantageously exhibit melanocortin receptor agonist activity. New and useful compounds comprising such a chemical structure and methods of modulating melanocortin receptor activity in a subject (and promoting, inducing, and/or enhancing the treatment or prevention of related diseases) by administering such a compound or composition also are described.

5. 发明专利

AU2003281978A1 COMPOUNDS FOR USE IN TREATING OBESITY 未知
公开(公告)号：AU2003281978A1
公开(公告)日：2004-06-18
申请号：AU2003281978
申请日：2003-11-20
申请人： NOVO NORDISK AS
发明人： WULFF BIRGITTE SCHJELLERUP , THOGERSEN HENNING , LUSTENBERGER PHILIPP , RUDOLF KLAUS , KRIST BERND , MULLER STEPHAN , STENKAMP DIRK , SCHINDLER MARCUS , WIELAND HEIKE , ARNDT KIRSTEN , CONDE-FRIEBOES KILIAN WALDEMAR , ANKERSEN MICHAEL , SENSFUSS ULRICH
IPC分类号： A61P15/10 , C07D241/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/14 , C07D241/00
摘要： Described herein are novel and useful compounds of the general formula Compounds of this invention can advantageously exhibit melanocortin receptor agonist activity. New and useful compounds comprising such a chemical structure and methods of modulating melanocortin receptor activity in a subject (and promoting, inducing, and/or enhancing the treatment or prevention of related diseases) by administering such a compound or composition also are described.

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