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1. 发明授权

US08101764B2 MCH receptor antagonists 失效
标题翻译： MCH受体拮抗剂
公开(公告)号：US08101764B2
公开(公告)日：2012-01-24
申请号：US12296557
申请日：2007-06-08
申请人： Albert Kudzovi Amegadzie , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu , Patrick Gianpietro Spinazze
发明人： Albert Kudzovi Amegadzie , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu , Patrick Gianpietro Spinazze
IPC分类号： C07D513/02
CPC分类号： C07D495/04
摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.
摘要翻译：本发明涉及式（I）的黑色素浓缩激素拮抗剂化合物：其中R1，Ra，Rb，R2，L1，R3，R4和R5如上所定义，或其药学上可接受的盐，对映体，非对映体或非对映异构体的混合物其用于治疗，肥胖和相关疾病。

2. 发明申请

US20100016350A1 NOVEL MCH RECEPTOR ANTAGONISTS 失效
标题翻译：新生儿受体拮抗剂
公开(公告)号：US20100016350A1
公开(公告)日：2010-01-21
申请号：US12296557
申请日：2007-06-08
申请人： Albert Kudzovi Amegadzie , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianlaing Lu , Patrick Gianpietro Spinazze
发明人： Albert Kudzovi Amegadzie , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianlaing Lu , Patrick Gianpietro Spinazze
IPC分类号： A61K31/4365 , C07D495/04 , A61P3/04
CPC分类号： C07D495/04
摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.
摘要翻译：本发明涉及式（I）的黑色素浓缩激素拮抗剂化合物：其中R1，Ra，Rb，R2，L1，R3，R4和R5如上所定义，或其药学上可接受的盐，对映体，非对映体或非对映异构体的混合物其用于治疗，肥胖和相关疾病。

3. 发明申请

US20120302547A1 NOVEL MCH RECEPTOR ANTAGONISTS 审中-公开
标题翻译：新生儿受体拮抗剂
公开(公告)号：US20120302547A1
公开(公告)日：2012-11-29
申请号：US13569899
申请日：2012-08-08
申请人： Macklin Brian Arnold , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu
发明人： Macklin Brian Arnold , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu
IPC分类号： A61K31/4365 , A61P3/04 , A61K31/496 , C07D495/04 , A61K31/5377
CPC分类号： C07D495/04
摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula (I) wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.
摘要翻译：本发明涉及式（I）的黑色素浓缩激素拮抗剂化合物，其中R 1，R a，R b，R 2，L 1，R 3，R 4和R 5如所定义，或其药学上可接受的盐，对映体，非对映异构体或其非对映异构体的混合物用于治疗，肥胖和相关疾病。

4. 发明授权

US08263772B2 MCH receptor antagonists 失效
标题翻译： MCH受体拮抗剂
公开(公告)号：US08263772B2
公开(公告)日：2012-09-11
申请号：US12298792
申请日：2007-06-08
申请人： Macklin Brian Arnold , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu
发明人： Macklin Brian Arnold , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu
IPC分类号： C07D515/04 , A61K31/4365
CPC分类号： C07D495/04
摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula (1): wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.
摘要翻译：本发明涉及式（1）的黑色素浓缩激素拮抗剂化合物：其中R1，Ra，Rb，R2，L1，R3，R4和R5如上定义，或其药学上可接受的盐，对映异构体，非对映体或非对映异构体的混合物其用于治疗，肥胖和相关疾病。

5. 发明申请

US20090093456A1 NOVEL MCH RECEPTOR ANTAGONISTS 失效
标题翻译：新生儿受体拮抗剂
公开(公告)号：US20090093456A1
公开(公告)日：2009-04-09
申请号：US12298792
申请日：2007-06-08
申请人： Macklin Brian Arnold , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu
发明人： Macklin Brian Arnold , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu
IPC分类号： A61K31/4365 , C07D495/04 , A61K31/5377
CPC分类号： C07D495/04
摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula (1): wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.
摘要翻译：本发明涉及式（1）的黑色素浓缩激素拮抗剂化合物：其中R1，Ra，Rb，R2，L1，R3，R4和R5如上定义，或其药学上可接受的盐，对映异构体，非对映体或非对映异构体的混合物其用于治疗，肥胖和相关疾病。

6. 发明申请

US20090233919A1 THIAZOLOPYRIDINONE DERIVATES AS MCH RECEPTOR ANTAGONISTS 有权
标题翻译：噻唑吡啶酮作为MCH受体拮抗剂
公开(公告)号：US20090233919A1
公开(公告)日：2009-09-17
申请号：US11721079
申请日：2005-12-16
申请人： Albert Kudzovi Amegadzie , James Peter Beck , Kevin Matthew Gardinier , Erik James Hembre , James Craig Ruble , Brian David Wakefield
发明人： Albert Kudzovi Amegadzie , James Peter Beck , Kevin Matthew Gardinier , Erik James Hembre , James Craig Ruble , Brian David Wakefield
IPC分类号： A61K31/536 , C07D513/02 , A61K31/4365 , C07D417/14 , A61K31/496 , C07D265/36 , C07D413/14 , A61K31/5377 , A61P3/04
CPC分类号： C07D513/04
摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula (I); wherein w, R1, q, p, R2, t, Ar1, L1, R3 and R4 are as defined, or a pharmaceutically acceptable salt, solvate, or enantiomer thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.
摘要翻译：本发明涉及式（I）的黑色素浓缩激素拮抗剂化合物; 其中w，R1，q，p，R2，t，Ar1，L1，R3和R4如上所定义，或其药学上可接受的盐，溶剂化物或对映异构体可用于治疗，预防或改善与肥胖相关的症状和相关疾病

7. 发明授权

US07320994B2 Triazole derivatives as tachykinin receptor antagonists 有权
标题翻译：三唑衍生物作为速激肽受体拮抗剂
公开(公告)号：US07320994B2
公开(公告)日：2008-01-22
申请号：US10512249
申请日：2003-04-22
申请人： Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , Erik James Hembre , Jian Eric Hong , Louis Nickolaus Jungheim , Brian Stephen Muehl , David Michael Remick , Michael Alan Robertson , Kenneth Allen Savin
发明人： Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , Erik James Hembre , Jian Eric Hong , Louis Nickolaus Jungheim , Brian Stephen Muehl , David Michael Remick , Michael Alan Robertson , Kenneth Allen Savin
IPC分类号： A61K31/41 , C07D249/04
CPC分类号： C07D401/04 , C07D249/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D487/04
摘要： This application relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and its use as an inhibitor of the NK-1 subtype of tachykinin receptors, as well as a process for its preparation and intermediates therefor. (I) wherein: D is a C1-C3 alkane-diyl; R1 is phenyl, which is optionally substituted with one to three substitutents independently selected from the group consisting of halo, C1-C4 alkyl, C1-C4 alkoxy, cyano, difluoromethyl, trifluoromethyl, and trifluoromethoxy; R4 is a radical selected from the group consisting of: (IA), (IB), (IC), (ID), (IE), (IF), (IG), (IH)
摘要翻译：本申请涉及式（I）化合物或其药学上可接受的盐，其药物组合物及其作为速激肽受体的NK-1亚型的抑制剂的用途，以及其制备方法及其中间体。（I）其中：D是C 1 -C 3烷烃二基; R 1是苯基，其任选地被一至三个独立地选自卤素，C 1 -C 4烷基的取代基取代， C 1 -C 4烷氧基，氰基，二氟甲基，三氟甲基和三氟甲氧基; （I），（IB），（IC），（ID），（IE），（IF），（IG），（IH）

8. 发明授权

US07902356B2 Thiazolopyridinone derivates as MCH receptor antagonists 有权
标题翻译：噻唑并吡啶酮衍生为MCH受体拮抗剂
公开(公告)号：US07902356B2
公开(公告)日：2011-03-08
申请号：US11721079
申请日：2005-12-16
申请人： Albert Kudzovi Amegadzie , James Peter Beck , Kevin Matthew Gardinier , Erik James Hembre , James Craig Ruble , Kenneth Allen Savin , Brian David Wakefield
发明人： Albert Kudzovi Amegadzie , James Peter Beck , Kevin Matthew Gardinier , Erik James Hembre , James Craig Ruble , Kenneth Allen Savin , Brian David Wakefield
IPC分类号： C07D265/36 , C07D413/00 , C07D401/00 , C07D513/02
CPC分类号： C07D513/04
摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula (I); wherein w, R1, q, p, R2, t, Ar1, L1, R3 and R4 are as defined, or a pharmaceutically acceptable salt, solvate, or enantiomer thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.
摘要翻译：本发明涉及式（I）的黑色素浓缩激素拮抗剂化合物; 其中w，R1，q，p，R2，t，Ar1，L1，R3和R4如上所定义，或其药学上可接受的盐，溶剂化物或对映异构体可用于治疗，预防或改善与肥胖相关的症状和相关疾病

9. 发明授权

US07179804B2 Tachykinin receptor antagonists 有权
标题翻译：速激肽受体拮抗剂
公开(公告)号：US07179804B2
公开(公告)日：2007-02-20
申请号：US10512248
申请日：2003-04-22
申请人： Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , Erik James Hembre , Jian Eric Hong , Louis Nickolaus Jungheim , Michael Alan Robertson , Kenneth Allen Savin
发明人： Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , Erik James Hembre , Jian Eric Hong , Louis Nickolaus Jungheim , Michael Alan Robertson , Kenneth Allen Savin
IPC分类号： A61K31/4192 , A61K31/4406 , A61K31/4409 , A61K31/497 , A61K31/541 , A61K31/5377 , C07D261/08 , C07D413/06 , C07D417/14 , C07F7/10
CPC分类号： C07D249/06 , C07D249/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/06 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/14
摘要： The present invention relates to selective NK-1 receptor antagonists of Formula (I); or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins
摘要翻译：本发明涉及式（I）的选择性NK-1受体拮抗剂; 或其药学上可接受的盐，用于治疗与过速的速激肽相关的病症

10. 发明授权

US08049013B2 5- [4-(azetidin-3-yloxy)-phenyl]-2-phenyl-5H-thiazolo[5,4-C] pyridin-4-one derivatives and their use as MCH receptor antagonists 失效
标题翻译： 5- [4-（氮杂环丁烷-3-基氧基） - 苯基] -2-苯基-5H-噻唑并[5,4-C]吡啶-4-酮衍生物及其作为MCH受体拮抗剂
公开(公告)号：US08049013B2
公开(公告)日：2011-11-01
申请号：US12515432
申请日：2007-11-15
申请人： Kevin Matthew Gardinier , David Joseph Garmene , Erik James Hembre , Michael Brunavs , Helen Jane Szekeres
发明人： Kevin Matthew Gardinier , David Joseph Garmene , Erik James Hembre , Michael Brunavs , Helen Jane Szekeres
IPC分类号： C07D513/02
CPC分类号： C07D513/04
摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula I: wherein “-----” is absent or is optionally a bond; q is 1 or 2; R1 is independently selected from hydrogen, —C1-C2 alkyl, halo, hydroxy, —C1-C2 haloalkyl, —C1-C3 alkoxy, cyano, —O—C3-C4 cycloalkyl, and —OC1-C2 haloalkyl; R2 is selected from the group consisting of hydrogen, —C1-C3 alkyl, hydroxy, —C1-C3 alkoxy, cyano, —C1-C2 haloalkyl, —OC1-C2 haloalkyl, and halo; R3 is selected from the group consisting of hydrogen, —C1-C4 alkyl, —C2-C4 haloalkyl, —C2-C4 alkylOH, —C3-C6 cycloalkyl, —CH2C3-C6 cycloalkyl, —C2-C4 alkyl-O—C1-C4 alkyl, —C(O)C1-C4 alkyl, —C(O)C1-C4 haloalkyl, —CH2-thiazole, phenyl, benzyl, tetrahydrothiopyranyl, and tetrahydropyranyl, wherein the cycloalkyl, tetrahydrothiopyranyl, tetrahydropyranyl and thiazolyl group is optionally substituted with one or two groups independently selected from the group consisting of halo, hydroxy, C1-C2 alkyl, and —C1-C2 haloalkyl; or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture thereof, useful in the treating, preventing or ameliorating of symptoms associated with obesity and related diseases.
摘要翻译：本发明涉及式I的黑色素浓缩激素拮抗剂化合物：其中“-----”不存在或任选地是键; q为1或2; R 1独立地选自氢，-C 1 -C 2烷基，卤素，羟基，-C 1 -C 2卤代烷基，-C 1 -C 3烷氧基，氰基，-O-C 3 -C 4环烷基和-OC 1 -C 2卤代烷基; R 2选自氢，-C 1 -C 3烷基，羟基，-C 1 -C 3烷氧基，氰基，-C 1 -C 2卤代烷基，-OC 1 -C 2卤代烷基和卤素; R 3选自氢，-C 1 -C 4烷基，-C 2 -C 4卤代烷基，-C 2 -C 4烷基OH，-C 3 -C 6环烷基，-CH 2 C 3 -C 6环烷基，-C 2 -C 4烷基-O- C4烷基，-C（O）C1-C4烷基，-C（O）C1-C4卤代烷基，-CH2-噻唑，苯基，苄基，四氢噻喃基和四氢吡喃基，其中环烷基，四氢噻喃基，四氢吡喃基和噻唑基任选被取代具有一个或两个独立地选自卤素，羟基，C 1 -C 2烷基和-C 1 -C 2卤代烷基的基团; 或其药学上可接受的盐，对映异构体，非对映体或其混合物，其可用于治疗，预防或改善与肥胖症和相关疾病相关的症状。

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