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1. 发明授权

US07279470B2 Compounds and uses thereof for decreasing activity of hormone-sensitive lipase 失效
标题翻译：用于降低激素敏感性脂肪酶活性的化合物及其用途
公开(公告)号：US07279470B2
公开(公告)日：2007-10-09
申请号：US10319885
申请日：2002-12-13
申请人： Soren Ebdrup , Johannes Cornelis de Jong , Poul Jacobsen , Holger Claus Hansen , Per Vedso
发明人： Soren Ebdrup , Johannes Cornelis de Jong , Poul Jacobsen , Holger Claus Hansen , Per Vedso
IPC分类号： C07D401/12 , C07D401/14 , A61K31/496 , A61K31/4523
CPC分类号： C07D207/404 , C07C39/367 , C07C233/25 , C07C233/26 , C07C233/60 , C07C307/06 , C07C311/04 , C07C311/17 , C07C311/21 , C07C311/29 , C07C311/40 , C07C317/22 , C07C323/20 , C07C2601/14 , C07D209/08 , C07D209/32 , C07D209/48 , C07D211/88 , C07D213/61 , C07D213/63 , C07D213/64 , C07D213/643 , C07D213/68 , C07D213/69 , C07D213/70 , C07D213/74 , C07D213/75 , C07D213/84 , C07D215/20 , C07D215/22 , C07D217/24 , C07D231/12 , C07D231/16 , C07D233/54 , C07D233/56 , C07D235/18 , C07D235/26 , C07D237/14 , C07D239/22 , C07D241/18 , C07D241/44 , C07D249/04 , C07D249/08 , C07D249/18 , C07D253/04 , C07D257/04 , C07D261/12 , C07D263/52 , C07D277/24 , C07D277/68 , C07D285/01 , C07D295/205 , C07D295/26 , C07D307/16 , C07D307/52 , C07D307/89 , C07D311/16 , C07D311/18 , C07D333/16 , C07D333/32 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D471/06 , C07D491/10
摘要： Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.
摘要翻译：使用化合物抑制激素敏感性脂肪酶，包含化合物的药物组合物，使用这些化合物和组合物的治疗方法以及新化合物。本发明化合物是激素敏感性脂肪酶的抑制剂，并且可用于治疗和/或预防需要激素敏感性脂肪酶活性降低的医学病症。

2. 发明授权

US07067517B2 Use of compounds for decreasing activity of hormone-sensitive lipase 失效
标题翻译：使用化合物降低激素敏感性脂肪酶的活性
公开(公告)号：US07067517B2
公开(公告)日：2006-06-27
申请号：US10319212
申请日：2002-12-13
申请人： Soren Ebdrup , Johannes Cornelis de Jong , Poul Jacobsen , Holger Claus Hansen , Per Vedso
发明人： Soren Ebdrup , Johannes Cornelis de Jong , Poul Jacobsen , Holger Claus Hansen , Per Vedso
IPC分类号： A61K31/44 , C07D401/04
CPC分类号： C07D207/404 , C07C39/367 , C07C233/25 , C07C233/26 , C07C233/60 , C07C307/06 , C07C311/04 , C07C311/17 , C07C311/21 , C07C311/29 , C07C311/40 , C07C317/22 , C07C323/20 , C07C2601/14 , C07D209/08 , C07D209/32 , C07D209/48 , C07D211/88 , C07D213/61 , C07D213/63 , C07D213/64 , C07D213/643 , C07D213/68 , C07D213/69 , C07D213/70 , C07D213/74 , C07D213/75 , C07D213/84 , C07D215/20 , C07D215/22 , C07D217/24 , C07D231/12 , C07D231/16 , C07D233/54 , C07D233/56 , C07D235/18 , C07D235/26 , C07D237/14 , C07D239/22 , C07D241/18 , C07D241/44 , C07D249/04 , C07D249/08 , C07D249/18 , C07D253/04 , C07D257/04 , C07D261/12 , C07D263/52 , C07D277/24 , C07D277/68 , C07D285/01 , C07D295/205 , C07D295/26 , C07D307/16 , C07D307/52 , C07D307/89 , C07D311/16 , C07D311/18 , C07D333/16 , C07D333/32 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D471/06 , C07D491/10
摘要： Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.
摘要翻译：使用化合物抑制激素敏感性脂肪酶，包含化合物的药物组合物，使用这些化合物和组合物的治疗方法以及新化合物。本发明化合物是激素敏感性脂肪酶的抑制剂，并且可用于治疗和/或预防需要激素敏感性脂肪酶活性降低的医学病症。

3. 发明申请

US20060160851A1 Substituted piperidine carbamates 审中-公开
标题翻译：取代的哌啶氨基甲酸酯
公开(公告)号：US20060160851A1
公开(公告)日：2006-07-20
申请号：US11301166
申请日：2005-12-12
申请人： Soren Ebdrup , Per Vedso , Poul Jacobsen , Flemming Nielsen , Johannes Cornelis de Jong
发明人： Soren Ebdrup , Per Vedso , Poul Jacobsen , Flemming Nielsen , Johannes Cornelis de Jong
IPC分类号： A61K31/4545 , C07D401/02
CPC分类号： C07D211/34 , C07D211/44 , C07D211/66 , C07D211/88 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Novel substituted piperidine carbamates, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which modulation of the activity of hormone sensitive lipase is beneficial.
摘要翻译：新型取代的哌啶氨基甲酸酯，包含它们的药物组合物及其用于治疗和/或预防与激素敏感性脂肪酶相关的疾病和病症的用途。更具体地，这些化合物可用于治疗和/或预防激素敏感性脂肪酶的活性调节有益的疾病和病症。

4. 发明申请

US20060160819A1 Substitued piperazine carbamates 审中-公开
标题翻译：取代的哌嗪氨基甲酸酯
公开(公告)号：US20060160819A1
公开(公告)日：2006-07-20
申请号：US11299637
申请日：2005-12-12
申请人： Holger Hansen , Johannes Cornelis de Jong , Poul Jacobsen , Soren Ebdrup
发明人： Holger Hansen , Johannes Cornelis de Jong , Poul Jacobsen , Soren Ebdrup
IPC分类号： A61K31/497 , C07D403/14 , A61K31/496
CPC分类号： C07D213/74 , C07D213/65 , C07D213/75 , C07D213/76 , C07D213/80 , C07D233/54 , C07D401/12 , C07D401/14 , C07D405/04 , C07D473/34
摘要： Novel piperazines, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which modulation of lipolysis, such as decreased lipolysis is beneficial.
摘要翻译：新颖的哌嗪，包含它们的药物组合物及其用于治疗和/或预防与激素敏感性脂肪酶相关的疾病和病症的用途。更具体地说，这些化合物可用于治疗和/或预防脂肪分解调节如脂肪分解降低有益的疾病和病症。

5. 发明申请

US20100267721A1 Heterocyclic H3 Antagonists 失效
标题翻译：杂环H3拮抗剂
公开(公告)号：US20100267721A1
公开(公告)日：2010-10-21
申请号：US12663103
申请日：2008-05-19
申请人： Rolf Hohlweg , Jane Marie Lundbeck , Johannes Cornelis de Jong
发明人： Rolf Hohlweg , Jane Marie Lundbeck , Johannes Cornelis de Jong
IPC分类号： A61K31/5377 , C07D401/14 , A61K31/4545 , C07D413/14 , A61K31/497 , C07D403/04 , A61K31/501 , A61P3/04 , A61P1/16 , A61P3/06 , A61P3/10 , A61P9/00 , A61P11/06 , A61P19/02 , A61P25/28 , A61P1/12 , A61P35/00
CPC分类号： C07D405/14 , C07D401/04 , C07D401/14 , C07D413/10 , C07D413/14
摘要： Compound of formula (I) wherein W, X, Y, Z is —C(R′)═ or N; R1 is hydrogen or alkyl, V is N or C (i.e. carbon), A is a bond or an alkylene linker with 1 to 3 carbon atoms, with the proviso that when A is a bond, V must be CH, R is ethyl, propyl, a branched C3-6 alkyl or a cyclic C3-8 alkyl, m and n is 1-3, D is heteroaryl optionally substituted with halogen, hydroxy, cyano, alkyl, cycloalkyl, alkoxy, —(CH2)o—(C═O)p—NR2R3, or D is aryl optionally substituted with one or more of the groups independently selected from hydrogen, halogen, hydroxy, cyano, alkyl, cycloalkyl, haloalkyl, alkoxy, haloalkoxy, alkylsulfonyl, alkylsulfinyl, heterocyclyl, heterocyclylalkyl, heterocyclyl-alkoxy, heterocyclylcarbonyl, alkylcarbonyl, alkoxycarbonyl, alkylcarboxy, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylcarbonylamino, alkylcarbonylaminoalkyl, arylcarbonylamino, aryl-carbonylaminoalkyl, heteroarylcarbonylamino or heteroarylcarbonylaminoalkyl, —(CH2)0—(C═O)p—NR2R3, wherein o is 0-3, p is 0 or 1, and R2 and R3 independently are hydrogen, alkyl or cycloalkyl; or R2 and R3, can together with the attached nitrogen form a heterocyclyl group, and salts and solvates thereof have binding affinity for the histamine H3 receptor.
摘要翻译：式（I）化合物，其中W，X，Y，Z为-C（R'）=或N; R1是氢或烷基，V是N或C（即碳），A是具有1至3个碳原子的键或亚烷基接头，条件是当A是键时，V必须是CH，R是乙基，丙基，支链C 3-6烷基或环C 3-8烷基，m和n为1-3，D为任选被卤素，羟基，氰基，烷基，环烷基，烷氧基， - （CH 2）o - （C ≡O）p-NR2R3，或D是任选被一个或多个独立地选自氢，卤素，羟基，氰基，烷基，环烷基，卤代烷基，烷氧基，卤代烷氧基，烷基磺酰基，烷基亚磺酰基，杂环基，杂环基烷基，杂环基 - 烷基羰基，烷氧基羰基，烷氧基烷基，烷基羰基氨基，烷基羰基氨基烷基，芳基羰基氨基，芳基 - 羰基氨基烷基，杂芳基羰基氨基或杂芳基羰基氨基烷基， - （CH2）O-（C = O）p-NR2R3，其中o为0 -3，p为0或1，R2和R3独立地为氢，烷基o 环烷基或R 2和R 3可以与连接的氮一起形成杂环基，其盐和溶剂合物对组胺H3受体具有结合亲和力。

6. 发明授权

US06927214B1 Non-peptide GLP-1 agonists 失效
标题翻译：非肽GLP-1激动剂
公开(公告)号：US06927214B1
公开(公告)日：2005-08-09
申请号：US09483504
申请日：2000-01-14
申请人： Min Teng , Larry Kenneth Truesdale , Dilip Bhumralkar , Dan Kiel , Michael D. Johnson , Christine Thomas , Anker Steen Jorgensen , Peter Madsen , Preben Houlberg Olesen , Liselotte Bjerre Knudsen , Ingrid Vivika Petterson , Johannes Cornelis de Jong , Carsten Behrens , Janos Tibor Kodra , Jesper Lau
发明人： Min Teng , Larry Kenneth Truesdale , Dilip Bhumralkar , Dan Kiel , Michael D. Johnson , Christine Thomas , Anker Steen Jorgensen , Peter Madsen , Preben Houlberg Olesen , Liselotte Bjerre Knudsen , Ingrid Vivika Petterson , Johannes Cornelis de Jong , Carsten Behrens , Janos Tibor Kodra , Jesper Lau
IPC分类号： C07D215/20 , C07D215/36 , C07D241/44 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D417/12 , C07D491/10 , C07D495/04 , A61K31/33 , A61K31/495 , C07D239/00 , C07D241/36
CPC分类号： C07D491/10 , C07D215/20 , C07D215/36 , C07D241/44 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D417/12 , C07D495/04
摘要： Novel non-peptide GLP-1 agonists, pharmaceutical compositions comprising them, use of the non-peptide GLP-1 agonists for the preparation of pharmaceutical compositions and methods for the treatment and/or prevention of disorders and diseases wherein an activation of the human GLP-1 receptor is beneficial, especially metabolic disorders such as IGT, Type 1 diabetes, Type 2 diabetes and obesity.
摘要翻译：新型非肽GLP-1激动剂，包含它们的药物组合物，使用非肽GLP-1激动剂来制备用于治疗和/或预防疾病和疾病的药物组合物和方法，其中人GLP -1受体是有益的，特别是代谢疾病如IGT，1型糖尿病，2型糖尿病和肥胖。

7. 发明授权

US08344001B2 Heterocyclic H3 antagonists 失效
标题翻译：杂环H3拮抗剂
公开(公告)号：US08344001B2
公开(公告)日：2013-01-01
申请号：US12663103
申请日：2008-05-19
申请人： Rolf Hohlweg , Jane Marie Lundbeck , Johannes Cornelis de Jong
发明人： Rolf Hohlweg , Jane Marie Lundbeck , Johannes Cornelis de Jong
IPC分类号： A61K31/44
CPC分类号： C07D405/14 , C07D401/04 , C07D401/14 , C07D413/10 , C07D413/14
摘要： Compound of formula (I) wherein W, X, Y, Z is —C(R1)═ or N; R1 is hydrogen or alkyl, V is N or C (i.e. carbon), A is a bond or an alkylene linker with 1 to 3 carbon atoms, with the proviso that when A is a bond, V must be CH, R is ethyl, propyl, a branched C3-6 alkyl or a cyclic C3-8 alkyl, m and n is 1-3, D is heteroaryl optionally substituted with halogen, hydroxy, cyano, alkyl, cycloalkyl, alkoxy, —(CH2)0—(C═O)p—NR2R3, or D is aryl optionally substituted with one or more of the groups independently selected from hydrogen, halogen, hydroxy, cyano, alkyl, cycloalkyl, haloalkyl, alkoxy, haloalkoxy, alkylsulfonyl, alkylsulfinyl, heterocyclyl, heterocyclylalkyl, heterocyclyl-alkoxy, heterocyclylcarbonyl, alkylcarbonyl, alkoxycarbonyl, alkylcarboxy, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylcarbonylamino, alkylcarbonylaminoalkyl, arylcarbonylamino, aryl-carbonylaminoalkyl, heteroarylcarbonylamino or heteroarylcarbonylaminoalkyl, —(CH2)0—(C═O)p—NR2R3, wherein o is 0-3, p is 0 or 1, and R2 and R3 independently are hydrogen, alkyl or cycloalkyl; or R2 and R3, can together with the attached nitrogen form a heterocyclyl group, and salts and solvates thereof have binding affinity for the histamine H3 receptor.
摘要翻译：式（I）的化合物，其中W，X，Y，Z是-C（R 1）=或N; R1是氢或烷基，V是N或C（即碳），A是具有1至3个碳原子的键或亚烷基接头，条件是当A是键时，V必须是CH，R是乙基，丙基，支链C 3-6烷基或环C 3-8烷基，m和n是1-3，D是任选被卤素，羟基，氰基，烷基，环烷基，烷氧基， - （CH 2）O-（C ≡O）p-NR2R3，或D是任选被一个或多个独立地选自氢，卤素，羟基，氰基，烷基，环烷基，卤代烷基，烷氧基，卤代烷氧基，烷基磺酰基，烷基亚磺酰基，杂环基，杂环基烷基，杂环基 - 烷基羰基，烷氧基羰基，烷氧基烷基，烷基羰基氨基，烷基羰基氨基烷基，芳基羰基氨基，芳基 - 羰基氨基烷基，杂芳基羰基氨基或杂芳基羰基氨基烷基， - （CH2）O-（C = O）p-NR2R3，其中o为0 -3，p为0或1，R2和R3独立地为氢，烷基o 环烷基或R 2和R 3可以与连接的氮一起形成杂环基，其盐和溶剂合物对组胺H3受体具有结合亲和力。

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