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1. 发明授权

US08530480B2 Substituted pyrimidinyl-amines as protein kinase inhibitors 有权
标题翻译：取代的嘧啶基胺作为蛋白激酶抑制剂
公开(公告)号：US08530480B2
公开(公告)日：2013-09-10
申请号：US12676411
申请日：2008-09-03
申请人： Theodore Kamenecka , Rong Jiang , Xinyi Song , Philip LoGrasso , Michael Darin Cameron , Derek R. Duckett
发明人： Theodore Kamenecka , Rong Jiang , Xinyi Song , Philip LoGrasso , Michael Darin Cameron , Derek R. Duckett
IPC分类号： A61K31/505 , A61K31/506 , C07D233/88 , C07D403/02
CPC分类号： C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D491/10
摘要： The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.
摘要翻译：本发明提供了可用作蛋白激酶抑制剂，特别是c-Jun N-末端激酶（JNK）及其药物组合物的新型取代的嘧啶基胺，以及用于治疗响应于JNK通路抑制的病症的方法。

2. 发明申请

US20080293684A1 Heterocyclic Acetophenone Potentiators of Metabotropic Glutamate Receptors 审中-公开
标题翻译：代谢型谷氨酸受体的杂环苯乙酮电位
公开(公告)号：US20080293684A1
公开(公告)日：2008-11-27
申请号：US11658546
申请日：2005-07-26
申请人： Anthony B Pinkerton , Jean-Michel Vernier , Rowena V. Cube , John H. Hutchinson , Dehua Huang , Celine Bonnefous , Steven P. Govak , Theodore Kamenecka
发明人： Anthony B Pinkerton , Jean-Michel Vernier , Rowena V. Cube , John H. Hutchinson , Dehua Huang , Celine Bonnefous , Steven P. Govak , Theodore Kamenecka
IPC分类号： A61K31/397 , C07D311/02 , A61K31/353 , A61K31/12 , C07C49/213 , C07D211/72 , A61K31/44 , A61K31/505 , C07D239/02 , C07D217/22 , A61K31/472 , A61K31/497 , C07D401/02 , C07D213/24 , A61K31/4427 , C07D471/04 , A61K31/437 , A61K31/4245 , A61P25/08 , A61P25/24 , A61P25/18 , C07D213/62 , A61K31/444 , A61K31/343 , C07D307/77 , C07D473/28 , A61K31/522 , A61K31/41 , C07D257/04 , C07D263/58 , A61K31/423 , A61K31/428 , C07D277/20 , C07D205/02 , C07D271/10 , C07D215/58 , A61K31/47 , C07D403/02 , C07D417/02 , A61K31/427
CPC分类号： C07D311/16 , C07C45/71 , C07C49/84 , C07C69/734 , C07C69/92 , C07C217/76 , C07C217/92 , C07C235/42 , C07C255/54 , C07C323/12 , C07D205/04 , C07D209/08 , C07D213/30 , C07D213/53 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/84 , C07D213/89 , C07D215/20 , C07D217/02 , C07D231/56 , C07D233/20 , C07D233/60 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/16 , C07D235/18 , C07D239/34 , C07D257/04 , C07D263/58 , C07D271/10 , C07D277/74 , C07D307/80 , C07D311/22 , C07D311/24 , C07D311/58 , C07D401/04 , C07D417/04 , C07D471/04 , C07D473/38
摘要： The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译：本发明涉及作为代谢型谷氨酸受体的增强剂（包括mGluR2受体）的化合物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及其中涉及代谢型谷氨酸受体的疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

3. 发明申请

US20080176904A1 Benzazole Potentiators of Metabotropic Glutatmate Receptors 失效
标题翻译：代谢型谷氨酸受体的苯唑增效剂
公开(公告)号：US20080176904A1
公开(公告)日：2008-07-24
申请号：US11884391
申请日：2006-02-17
申请人： Steven P. Govek , Jean-Michel Vernier , Theodore Kamenecka , John H. Hutchinson , Richard Pracitto
发明人： Steven P. Govek , Jean-Michel Vernier , Theodore Kamenecka , John H. Hutchinson , Richard Pracitto
IPC分类号： A61K31/4439 , C07D403/12 , A61K31/41 , A61P25/00 , C07D401/12
CPC分类号： C07D403/12 , C07D209/08 , C07D249/18 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/12 , C07D413/14
摘要： The present invention is directed to benzazole compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译：本发明涉及作为代谢型谷氨酸受体的增强剂（包括mGluR2受体）的苯并唑化合物，它们可用于治疗或预防与谷氨酸功能障碍相关的神经和精神疾病以及涉及代谢型谷氨酸受体的疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

4. 发明申请

US20070149547A1 Bipyridyl amides as modulators of metabotropic glutamate receptor-5 审中-公开
标题翻译：二吡啶基酰胺作为代谢型谷氨酸受体-5的调节剂
公开(公告)号：US20070149547A1
公开(公告)日：2007-06-28
申请号：US10589407
申请日：2005-02-09
申请人： Celine Bonnefous , Theodore Kamenecka , Jean-Michel Vernier
发明人： Celine Bonnefous , Theodore Kamenecka , Jean-Michel Vernier
IPC分类号： A61K31/497 , A61K31/444 , C07D403/02 , C07D401/02
CPC分类号： C07D401/12 , C07D213/81 , C07D241/26 , C07D401/14 , C07D405/14 , C07D409/14 , C07F7/0812
摘要： The present invention is directed to novel amides such as those of Formula (I): (I) which are mGluR5 modulators useful in the treatment or prevention of diseases and conditions in which mGluR5 is involved, including but not limited to psychiatric and mood disorders such as schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders, such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal, obesity and other diseases. The invention is also directed to pharmaceutical compositions comprising these compounds. This invention further provides a method of treatment of these disorders and conditions by the administration of an effective amount of these novel amides and/or compositions containing these compounds.
摘要翻译：本发明涉及新型酰胺，例如式（I）：（I）的那些酰胺，其为可用于治疗或预防涉及mGluR5的疾病和病症的mGluR5调节剂，包括但不限于精神和心境障碍作为精神分裂症，焦虑症，抑郁症，双相性精神障碍和恐慌，以及治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律和睡眠障碍，如转移工作诱导的睡眠障碍和时差，药物成瘾，药物滥用，戒毒，肥胖等疾病。本发明还涉及包含这些化合物的药物组合物。本发明还提供了一种通过施用有效量的这些新型酰胺和/或含有这些化合物的组合物来治疗这些病症和病症的方法。

5. 发明授权

US06734311B2 Substituted amidine derivatives as inhibitors of cell adhesion 失效
标题翻译：取代的脒衍生物作为细胞粘附的抑制剂
公开(公告)号：US06734311B2
公开(公告)日：2004-05-11
申请号：US09862151
申请日：2001-05-21
申请人： William K. Hagmann , Stephen E. DeLaszlo , Theodore Kamenecka , Malcolm MacCoss
发明人： William K. Hagmann , Stephen E. DeLaszlo , Theodore Kamenecka , Malcolm MacCoss
IPC分类号： C07D20704
CPC分类号： C07D207/48 , C07D205/04
摘要： Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
摘要翻译：式I的化合物是VLA-4和/或α4β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。这些化合物可以配制成药物组合物，适用于治疗AIDS相关的痴呆，过敏性结膜炎，过敏性鼻炎，阿尔茨海默病，哮喘，动脉粥样硬化，自体骨髓移植，某些类型的毒性和免疫性肾炎，接触皮肤过敏，包括溃疡性结肠炎和克罗恩病的炎性肠病，炎症性肺病，病毒感染的炎症后遗症，脑膜炎，多发性硬化，多发性骨髓瘤，心肌炎，器官移植，牛皮癣，肺纤维化，再狭窄，视网膜炎，类风湿性关节炎，败血症关节炎，中风，肿瘤转移，葡萄膜炎和I型糖尿病。

6. 发明申请

US20080312286A1 Indanone Potentiators of Metabotropic Glutamate Receptors 审中-公开
标题翻译：代谢型谷氨酸受体的茚酮电位器
公开(公告)号：US20080312286A1
公开(公告)日：2008-12-18
申请号：US11658490
申请日：2005-07-26
申请人： Anthony B. Pinkerton , Jean-Michel Vernier , Rowena Cube , John Hutchinson , Celine Bonnefous , Theodore Kamenecka
发明人： Anthony B. Pinkerton , Jean-Michel Vernier , Rowena Cube , John Hutchinson , Celine Bonnefous , Theodore Kamenecka
IPC分类号： C07D257/04 , A61K31/41 , C07C307/02 , A61K31/18 , C07C233/02 , A61K31/454 , C07D401/02 , A61K31/192 , C07C65/00 , C07D213/80 , A61K31/44 , A61K31/343 , C07D307/78 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/08
CPC分类号： C07C233/91 , C07C59/90 , C07C65/40 , C07C311/51 , C07C2601/08 , C07C2602/08 , C07D257/04 , C07D307/79 , C07D401/04
摘要： The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译：本发明涉及作为代谢型谷氨酸受体的增强剂（包括mGluR2受体）的化合物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及其中涉及代谢型谷氨酸受体的疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

7. 发明授权

US07960417B2 Benzazole potentiators of metabotropic glutamate receptors 失效
标题翻译：代谢型谷氨酸受体的苯唑增强剂
公开(公告)号：US07960417B2
公开(公告)日：2011-06-14
申请号：US11884391
申请日：2006-02-17
申请人： Steven P. Govek , Jean-Michel Vernier , Theodore Kamenecka , John H. Hutchinson , Richard Pracitto
发明人： Steven P. Govek , Jean-Michel Vernier , Theodore Kamenecka , John H. Hutchinson , Richard Pracitto
IPC分类号： A61K31/41 , A61K31/4192 , C07D403/12 , C07D249/20 , C07D249/18
CPC分类号： C07D403/12 , C07D209/08 , C07D249/18 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/12 , C07D413/14
摘要： The present invention is directed to benzazole compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译：本发明涉及作为代谢型谷氨酸受体的增强剂（包括mGluR2受体）的苯并唑化合物，它们可用于治疗或预防与谷氨酸功能障碍相关的神经和精神疾病以及涉及代谢型谷氨酸受体的疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

8. 发明申请

US20070060618A1 Alkyne derivatives as tracers for metabotropic glutamate receptor binding 审中-公开
标题翻译：炔基衍生物作为代谢型谷氨酸受体结合的示踪剂
公开(公告)号：US20070060618A1
公开(公告)日：2007-03-15
申请号：US10532634
申请日：2003-10-24
申请人： Nicholas David Cosford , Steven Govck , Terence Hamill , Theodore Kamenecka , Thomas Seiders , Jeffrey Roppe , Celine Bonnefous , Donald Burns , Matthew Braun , Dennis Dean , Joseph Simeone
发明人： Nicholas David Cosford , Steven Govck , Terence Hamill , Theodore Kamenecka , Thomas Seiders , Jeffrey Roppe , Celine Bonnefous , Donald Burns , Matthew Braun , Dennis Dean , Joseph Simeone
IPC分类号： A61K31/444 , A61K31/4439 , A61K31/426 , A61K51/00 , C07D417/14
CPC分类号： C07D417/14 , A61K51/04 , A61K51/0453 , A61K51/0455 , C07B2200/05 , C07D213/22 , C07D213/65 , C07D277/30 , C07D417/06
摘要： The present invention is directed to isotopically labeled alkyne derivative compounds, particularly 11C, 13C, 14C, 18F, 15O, 13N, 35S, 2H, and 3H labeled compounds. In particular, the present invention is directed to 11C, 13C, 14C, 18F, 15O, 13N, 35S, 2H, and 3H labeled heterocyclic alkynes and methods of their preparation. The present invention further includes a method of use of the 11C, 18F, 15O, or 13N labeled heterocyclic alkyne compounds as tracers in positron emission tomography (PET) imaging, particularly in the study of metabolic conditions in mammals, specifically conditions modulated by metabotropic glutamate receptors subtype 5 (mGluR5).
摘要翻译：本发明涉及同位素标记的炔衍生物，特别是11 C，13 C，14 C，18 C以上 F，15，O，N，N，S，S，H，和H 3， SUP> H标记化合物。特别地，本发明涉及至少11 C，13 C，14 C，18 F， SUP> 15 O，13 N，35 S，2 H，H 3和H 3 H标记杂环炔烃及其制备方法。本发明进一步包括使用“11”，“18”，“15”或“13” N标记的杂环炔化合物作为正电子发射断层扫描（PET）成像中的示踪剂，特别是在哺乳动物的代谢条件的研究中，特别是由代谢型谷氨酸受体亚型5（mGluR5）调节的条件。

9. 发明申请

US20070027321A1 Bipyridyl amines and ethers as modulators of metabotropic glutamate receptor-5 审中-公开
标题翻译：联吡啶胺和醚作为代谢型谷氨酸受体-5的调节剂
公开(公告)号：US20070027321A1
公开(公告)日：2007-02-01
申请号：US10570068
申请日：2004-08-27
申请人： Theodore Kamenecka , Jean-Michel Vernier , Celine Bonnefous , Steven Govek , John Hutchinson
发明人： Theodore Kamenecka , Jean-Michel Vernier , Celine Bonnefous , Steven Govek , John Hutchinson
IPC分类号： A61K31/4743 , C07D471/02 , C07D401/02 , C07D417/14
CPC分类号： C07D213/74 , C04B35/632 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/04
摘要： The present invention is directed to novel bipyridyl amine and ether compounds such as those of Formula (I): (I) (where R?1#191, R?2#191, R?3#191, X and Y are as defined herein) which are mGluR5 modulators useful in the treatment or prevention of diseases and conditions in which mGluR5 is involved, including but not limited to psychiatric and mood disorders such as schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders, such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal, obesity and other diseases. The invention is also directed to pharmaceutical compositions comprising these compounds. This invention further provides a method of treatment of these disorders and conditions by the administration of an effective amount of these novel bipyridyl amine and/or ether compounds and/or compositions containing these compounds.
摘要翻译：本发明涉及新型联吡啶胺和醚化合物，例如式（I）的那些：（I）（其中R 1＃191，R 2＃191，R 3＃191，X和Y如上所定义）这是mGluR5调节剂，其可用于治疗或预防涉及mGluR5的疾病和病症，包括但不限于精神和心境障碍如精神分裂症，焦虑，抑郁，双相情感障碍和恐慌，以及在治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律和睡眠障碍，如转移工作诱导的睡眠障碍和时差，药物成瘾，药物滥用，药物戒断，肥胖症等疾病。本发明还涉及包含这些化合物的药物组合物。本发明还提供了通过施用有效量的这些新型联吡啶胺和/或醚化合物和/或含有这些化合物的组合物来治疗这些病症和病症的方法。

10. 发明申请

US20060069088A1 Benzoxazinyl-amidocyclopentyl-heterocyclic modulators of chemokine receptors 有权
标题翻译：趋化因子受体的苯并恶嗪基酰胺基环戊基 - 杂环调节剂
公开(公告)号：US20060069088A1
公开(公告)日：2006-03-30
申请号：US11129512
申请日：2005-05-13
申请人： Stephen Goble , Sander Mills , Lihu Yang , Alexander Pasternak , Celine Bonnefous , Theodore Kamenecka , Jean-Michel Vernier , John Hutchinson , Essa Hu , Steven Govek
发明人： Stephen Goble , Sander Mills , Lihu Yang , Alexander Pasternak , Celine Bonnefous , Theodore Kamenecka , Jean-Michel Vernier , John Hutchinson , Essa Hu , Steven Govek
IPC分类号： A61K31/542 , A61K31/538 , A61K31/519 , C07D498/02 , C07D487/02 , C07D491/02
CPC分类号： C07D413/08 , C07D413/14 , C07D417/14
摘要： Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.
摘要翻译：通过使用苯并恶嗪的环氮通过酰胺部分连接到苯并恶嗪基的环戊基化合物，并进一步被杂环部分取代，由式I表示的化合物：

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