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1. 发明申请

US20080227792A1 3,4-Dihydro-1H-Isoquinoline-2-Carboxylic Acid 5-Aminopyridin-2-Yl Esters 审中-公开
标题翻译： 3,4-二氢-1H-异喹啉-2-羧酸5-氨基吡啶-2-基酯
公开(公告)号：US20080227792A1
公开(公告)日：2008-09-18
申请号：US11816299
申请日：2006-02-13
申请人： Johannes Cornelis De Jong , Poul Jacobsen
发明人： Johannes Cornelis De Jong , Poul Jacobsen
IPC分类号： A61K31/496 , A61K31/4725 , C07D401/14 , A61P3/04 , C07D403/14
CPC分类号： C07D401/14 , C07D417/14
摘要： Novel compounds of formula (I), 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：新型式（I）化合物，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。

2. 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。

3. 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。

4. 发明授权

US06316494B1 cis3, 4-chroman derivatives useful in the prevention or treatment of estrogen related diseases or syndromes 失效
标题翻译：顺式-3,4-苯并二氢吡喃衍生物，可用于预防或治疗雌激素相关疾病或综合征
公开(公告)号：US06316494B1
公开(公告)日：2001-11-13
申请号：US08958684
申请日：1997-10-27
申请人： Poul Jacobsen , Svend Treppendahl , Paul Stanley Bury , Anders Kanstrup , Lise Brown Christiansen
发明人： Poul Jacobsen , Svend Treppendahl , Paul Stanley Bury , Anders Kanstrup , Lise Brown Christiansen
IPC分类号： A61K3135
CPC分类号： C07D413/04 , C07D311/58 , Y10S514/841
摘要： The present invention relates to therapeutically active compounds of formula I a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in the prevention or treatment of estrogen related diseases or syndromes.
摘要翻译：本发明涉及式Ia的治疗活性化合物及其制备方法和包含该化合物的药物组合物。新型化合物可用于预防或治疗雌激素相关疾病或综合征。

5. 发明授权

US6043269A cis-3,4-chroman derivatives useful in the prevention or treatment of estrogen related diseases or syndromes 失效
标题翻译：可用于预防或治疗雌激素相关疾病或综合征的顺式-3,4-苯并二氢吡喃衍生物
公开(公告)号：US6043269A
公开(公告)日：2000-03-28
申请号：US958019
申请日：1997-10-27
申请人： Poul Jacobsen , Svend Treppendahl , Paul Stanley Bury , Anders Kanstrup , Lise Brown Christiansen
发明人： Poul Jacobsen , Svend Treppendahl , Paul Stanley Bury , Anders Kanstrup , Lise Brown Christiansen
IPC分类号： C07D311/58 , C07D413/04 , A61K31/40 , C07D405/10
CPC分类号： C07D413/04 , C07D311/58
摘要： The present invention relates to therapeutically active compounds of formula I ##STR1## a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in the prevention or treatment of estrogen related diseases or syndromes.
摘要翻译：本发明涉及治疗活性的式I化合物，其制备方法和包含该化合物的药物组合物。新型化合物可用于预防或治疗雌激素相关疾病或综合征。

6. 发明授权

US5994390A Trans-3,4-chroman derivatives useful in the prevention or treatment of estrogen related diseases or syndromes 失效
标题翻译：用于预防或治疗雌激素相关疾病或综合症的反式-3,4-苯并二氢吡喃衍生物
公开(公告)号：US5994390A
公开(公告)日：1999-11-30
申请号：US957821
申请日：1997-10-27
申请人： Poul Jacobsen , Svend Treppendahl , Paul Stanley Bury , Anders Kanstrup , Lise Brown Christiansen
发明人： Poul Jacobsen , Svend Treppendahl , Paul Stanley Bury , Anders Kanstrup , Lise Brown Christiansen
IPC分类号： C07D311/58 , C07D413/04 , A61K31/40 , A61K31/35 , A61K31/42 , A61K31/55
CPC分类号： C07D413/04 , C07D311/58 , Y10S514/841
摘要： The present invention relates to therapeutically active compounds of formula I ##STR1## a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in the prevention or treatment of estrogen related diseases or syndromes.
摘要翻译：本发明涉及治疗活性的式I化合物，其制备方法和包含该化合物的药物组合物。新型化合物可用于预防或治疗雌激素相关疾病或综合征。

7. 发明授权

US5532236A [1,2,4]triazolo[4,3-a]quinoxaline compounds 失效
标题翻译： [1,2,4]三唑并[4,3-a]喹喔啉化合物
公开(公告)号：US5532236A
公开(公告)日：1996-07-02
申请号：US237518
申请日：1994-05-03
申请人： Poul Jacobsen , Flemming E. Nielsen , Lone Jeppesen
发明人： Poul Jacobsen , Flemming E. Nielsen , Lone Jeppesen
IPC分类号： A61K31/495 , A61P21/02 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/28 , C07D487/04 , C07D487/14 , A61K31/505 , A61K31/54 , C07D417/14
CPC分类号： C07D487/04
摘要： The present invention relates to [1,2,4]triazolo[4,3-a quinoxaline derivatives of formula I ##STR1## wherein one of R.sup.1 and R.sup.2 is a 5- or 6-membered nitrogen-containing heterocyclic ring which is optionally substituted with one, two or three substituents, wherein each substituent is independently phenyl or C.sub.1-6 -alkyl, or one of R.sup.1 and R.sup.2 is a fused ring system comprising a 5- or 6-membered nitrogen-containing heterocyclic ring and a benzene, pyridine, pyrimidine or pyrazine ring, wherein the fused ring system is optionally substituted with phenyl or C.sub.1-6 -alkyl; and the other of R.sup.1 and R.sup.2 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, halogen, NO.sub.2, NH.sub.2, CN, CF.sub.3, COC.sub.1-6 -alkyl or SO.sub.2 NR'R", wherein R' and R" are independently hydrogen or C.sub.1-6 -alkyl; and X is O or S; and pharmaceutically acceptable salts thereof. The compounds have affinity for the AMPA receptors and are antagonists in connection with this type of receptors which makes them useful in the treatment of CNS ailments, especially in the treatment of any of the numerous indications caused by hyperactivity of excitatory amino acids.
摘要翻译：本发明涉及式Ⅰ化合物[1,2,4]三唑并[4,3-a喹喔啉衍生物，其中R 1和R 2之一为5-或6-元含氮杂环，其中任选地被一个，两个或三个取代基取代，其中每个取代基独立地是苯基或C 1-6 - 烷基，或者R 1和R 2中的一个是包含5或6元含氮杂环的稠环体系和苯，吡啶，嘧啶或吡嗪环，其中稠环体系任选被苯基或C 1-6 - 烷基取代; R 1和R 2中的另一个为氢，C 1-6 - 烷基，C 1-6 - 烷氧基，卤素，NO 2，NH 2，CN，CF 3，COC 1-6 - 烷基或SO 2 NR'R“ '独立地是氢或C 1-6 - 烷基; X为O或S; 及其药学上可接受的盐。这些化合物对AMPA受体具有亲和力，并且是与这种类型的受体有关的拮抗剂，这使得它们可用于治疗CNS疾病，特别是在治疗由兴奋性氨基酸的多动症引起的许多适应症中的任何一种。

8. 发明授权

US5504085A Triazolo quinoxalines and their preparation and use 失效
标题翻译：三氮唑喹喔啉及其制备和使用
公开(公告)号：US5504085A
公开(公告)日：1996-04-02
申请号：US285598
申请日：1994-08-03
申请人： Poul Jacobsen , Flemming E. Nielsen
发明人： Poul Jacobsen , Flemming E. Nielsen
IPC分类号： A61K31/495 , A61P25/00 , C07D487/04 , C07D241/52
CPC分类号： C07D487/04
摘要： Quinoxaline compounds represented by formulas I or II, ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-6 -alkyl, halogen, NO.sub.2, NH.sub.2, CN, CF.sub.3, SO.sub.2 NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1-6 -alkyl, or COR.sup.6 wherein R.sup.6 is C.sub.1-6 -alkyl; and R.sup.3 is hydrogen, C.sub.1-6 -alkyl or CF.sub.3, compositions thereof and methods of preparing the compounds are described.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.
摘要翻译：由式I或II表示的喹喔啉化合物，其中R 1和R 2独立地是氢，C 1-6 - 烷基，卤素，NO 2，NH 2，CN，CF 3，SO 2 NR 4 R 5，其中R 4和R 5 独立地是氢或C 1-6 - 烷基，或COR 6，其中R 6是C 1-6 - 烷基; 和R 3为氢，C 1-6 - 烷基或CF 3，其组成和制备该化合物的方法。该化合物可用于治疗由兴奋性神经递质的多动症引起的适应症。

9. 发明授权

US5109001A Fused 2,3-dihydroxydiazolo compounds and their preparation and use 失效
标题翻译：熔融的2,3-二羟基二唑化合物及其制备和使用
公开(公告)号：US5109001A
公开(公告)日：1992-04-28
申请号：US570819
申请日：1990-08-22
申请人： Poul Jacobsen , Flemming E. Nielsen , Tage Honore , Jorgen Drejer
发明人： Poul Jacobsen , Flemming E. Nielsen , Tage Honore , Jorgen Drejer
IPC分类号： A61K31/00 , A61K31/495 , A61K31/55 , A61P25/00 , A61P43/00 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D517/04
CPC分类号： C07D487/04 , C07D495/04 , C07D513/04 , C07D517/04
摘要： Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.2 is hydrogen, NO.sub.2, NH.sub.2, CN, halogen, or SO.sub.2 NH.sub.2 ;--X--Y--Z-- is selected from .dbd.N-Se--N.dbd., .dbd.N--O--N.cuberoot., .dbd.N--S--N.dbd.;wherein R.sup.3 is hydrogen, lower alkyl, or CF.sub.3.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

10. 发明申请

US20060148799A1 Substituted p-phenyl carbamates 审中-公开
标题翻译：取代的对苯基氨基甲酸酯
公开(公告)号：US20060148799A1
公开(公告)日：2006-07-06
申请号：US11301092
申请日：2005-12-12
申请人： Johannes de Jong , Soren Ebdrup , Poul Jacobsen
发明人： Johannes de Jong , Soren Ebdrup , Poul Jacobsen
IPC分类号： A61K31/537 , A61K31/445 , C07D211/52 , C07D265/30
CPC分类号： C07D295/155 , C07D211/40 , C07D211/88 , C07D295/14
摘要： Novel substituted p-phenyl 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：新型取代的对苯基氨基甲酸酯，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。

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