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1. 发明授权

US08242143B2 Thiazolyl mGluR5 antagonists and methods for their use 有权
标题翻译：噻唑基mGluR5拮抗剂及其使用方法
公开(公告)号：US08242143B2
公开(公告)日：2012-08-14
申请号：US13016304
申请日：2011-01-28
申请人： Nicholas D. Cosford , Thomas J. Seiders , Joseph Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人： Nicholas D. Cosford , Thomas J. Seiders , Joseph Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号： A61P25/00 , A61K31/44 , C07D417/00
CPC分类号： C07D417/06 , C07D417/14 , C07D471/04
摘要： The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译：由于在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质，鉴定了具有药物性质特征的独特系列化合物。具体地说，通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择，其中环被选定的取代基取代，得到具有优异药物性质的化合物。本发明包括这些杂环化合物的药学上可接受的盐形式，特别是氯化物盐和三氟乙酸盐。

2. 发明申请

US20090203903A1 Thiazolyl mglur5 antagonists and methods for their use 有权
标题翻译：噻唑基mglur5拮抗剂及其使用方法
公开(公告)号：US20090203903A1
公开(公告)日：2009-08-13
申请号：US11664902
申请日：2005-10-06
申请人： Nicholas D. Cosford , Thomas J. Seiders , Joseph Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人： Nicholas D. Cosford , Thomas J. Seiders , Joseph Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号： C07D417/14 , C07D417/06
CPC分类号： C07D417/06 , C07D417/14 , C07D471/04
摘要： The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译：由于在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质，鉴定了具有药物性质特征的独特系列化合物。具体地说，通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择，其中环被选定的取代基取代，得到具有优异药物性质的化合物。本发明包括这些杂环化合物的药学上可接受的盐形式，特别是氯化物盐和三氟乙酸盐。

3. 发明申请

US20110230526A1 Thiazolyl Mglur5 Antagonists and Methods for Their Use 有权
标题翻译：噻唑基Mglur5拮抗剂及其使用方法
公开(公告)号：US20110230526A1
公开(公告)日：2011-09-22
申请号：US13016304
申请日：2011-01-28
申请人： Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人： Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号： A61K31/4439 , A61P25/00 , A61P25/22 , A61P25/24 , A61P25/28
CPC分类号： C07D417/06 , C07D417/14 , C07D471/04
摘要： The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译：由于它们在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质，鉴定了具有药物性质特征的独特系列化合物。具体地说，通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择，其中环被选定的取代基取代，得到具有优异药物性质的化合物。本发明包括这些杂环化合物的药学上可接受的盐形式，特别是氯化物盐和三氟乙酸盐。

4. 发明申请

US20120289696A1 THIAZOLYL MGLUR5 ANTAGONISTS AND METHODS FOR THEIR USE 有权
标题翻译： THIAZOLYL MGLUR5 ANTAGONISTS及其使用方法
公开(公告)号：US20120289696A1
公开(公告)日：2012-11-15
申请号：US13558537
申请日：2012-07-26
申请人： Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人： Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号： C07D417/06 , C07D417/14 , C07D471/04
CPC分类号： C07D417/06 , C07D417/14 , C07D471/04
摘要： The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译：由于在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质，鉴定了具有药物性质特征的独特系列化合物。具体地说，通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择，其中环被选定的取代基取代，得到具有优异药物性质的化合物。本发明包括这些杂环化合物的药学上可接受的盐形式，特别是氯化物盐和三氟乙酸盐。

5. 发明授权

US07879882B2 Thiazolyl mglur5 antagonists and methods for their use 有权
标题翻译：噻唑基mglur5拮抗剂及其使用方法
公开(公告)号：US07879882B2
公开(公告)日：2011-02-01
申请号：US11664902
申请日：2005-10-06
申请人： Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人： Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号： A61P25/00 , A61K31/44 , C07D417/14
CPC分类号： C07D417/06 , C07D417/14 , C07D471/04
摘要： The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译：由于它们在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质，鉴定了具有药物性质特征的独特系列化合物。具体地说，通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择，其中环被选定的取代基取代，得到具有优异药物性质的化合物。本发明包括这些杂环化合物的药学上可接受的盐形式，特别是氯化物盐和三氟乙酸盐。

6. 发明授权

US08609852B2 Thiazolyl mGluR5 antagonists and methods for their use 有权
标题翻译：噻唑基mGluR5拮抗剂及其使用方法
公开(公告)号：US08609852B2
公开(公告)日：2013-12-17
申请号：US13558537
申请日：2012-07-26
申请人： Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人： Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号： A61P25/00 , A61K31/55 , A61K31/54 , A61K31/505 , A61K31/44 , A61K31/47 , A61K31/445 , C07D401/00 , C07D403/00 , C07D417/00 , C07D239/02 , C07D211/00
CPC分类号： C07D417/06 , C07D417/14 , C07D471/04
摘要： The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译：由于在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质，鉴定了具有药物性质特征的独特系列化合物。具体地说，通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择，其中环被选定的取代基取代，得到具有优异药物性质的化合物。本发明包括这些杂环化合物的药学上可接受的盐形式，特别是氯化物盐和三氟乙酸盐。

7. 发明授权

US07462619B2 Pyridazine, pyrimidine and pyrazine ethyne compounds 失效
标题翻译：哒嗪，嘧啶和吡嗪乙炔化合物
公开(公告)号：US07462619B2
公开(公告)日：2008-12-09
申请号：US11097047
申请日：2005-04-01
申请人： Nicholas D. Cosford , Jeffrey R. Roppe , Lida R. Tehrani , Nicholas D. Smith , Brian Stearns , Dehua Huang , Bowei Wang , Thomas J. Seiders
发明人： Nicholas D. Cosford , Jeffrey R. Roppe , Lida R. Tehrani , Nicholas D. Smith , Brian Stearns , Dehua Huang , Bowei Wang , Thomas J. Seiders
IPC分类号： C07D401/12 , C07D239/30 , A61K31/444
CPC分类号： C07D213/16 , C07D213/30 , C07D239/26 , C07D241/12 , C07D249/08 , C07D263/32 , C07D271/06 , C07D277/22 , C07D277/24 , C07D277/40 , C07D285/01 , C07D333/08 , C07D401/06 , C07D401/12 , C07D401/14
摘要： In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring that includes at least two nitrogen atoms. The ring additionally includes four carbon atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon triple bond. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.
摘要翻译：根据本发明，提供了一类新的杂环化合物。本发明化合物含有至少两个氮原子的取代或未取代的六元杂环。该环另外包括四个碳原子。该杂环具有至少一个位于与环氮原子相邻的环位置的取代基。该环的强制取代基包括通过碳 - 碳三键与杂环连接的部分（B）。强制性取代基位于环氮原子附近。本发明化合物能够具有多种用途。例如，杂环化合物可以通过在神经系统中作为受体的激动剂和拮抗剂起作用来调节生理过程。本发明的化合物也可以作为杀虫剂和杀真菌剂。含有本发明化合物的药物组合物也具有广泛的用途。

8. 发明授权

US07365074B2 Pyridazine, pyrimidine and pyrazine ethyne compounds 失效
标题翻译：哒嗪，嘧啶和吡嗪乙炔化合物
公开(公告)号：US07365074B2
公开(公告)日：2008-04-29
申请号：US10874835
申请日：2004-06-23
申请人： Nicholas D. Cosford , Jeffrey R. Roppe , Lida R. Tehrani , Nicholas D. Smith , Brian Stearns , Dehua Huang , Bowei Wang
发明人： Nicholas D. Cosford , Jeffrey R. Roppe , Lida R. Tehrani , Nicholas D. Smith , Brian Stearns , Dehua Huang , Bowei Wang
IPC分类号： C07D401/06 , A61K31/444
CPC分类号： C07D239/26 , C07D213/16 , C07D213/30 , C07D241/12 , C07D249/08 , C07D263/32 , C07D271/06 , C07D277/22 , C07D277/24 , C07D277/40 , C07D285/01 , C07D333/08 , C07D401/06 , C07D401/12 , C07D401/14
摘要： In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted, unsaturated five, six or seven membered heterocyclic ring that includes at least one nitrogen atom and at least one carbon atom. The ring additionally includes three, four or five atoms independently selected from carbon, nitrogen, sulfur and oxygen atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon double bond, a carbon-carbon triple bond or an azo group. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.
摘要翻译：根据本发明，提供了一类新的杂环化合物。本发明的化合物含有包含至少一个氮原子和至少一个碳原子的取代的，不饱和的五，六或七元杂环。该环另外包括独立地选自碳，氮，硫和氧原子的三个，四个或五个原子。该杂环具有至少一个位于与环氮原子相邻的环位置的取代基。该环的强制取代基包括通过碳 - 碳双键，碳 - 碳三键或偶氮基与杂环连接的部分（B）。强制性取代基位于环氮原子附近。本发明化合物能够具有多种用途。例如，杂环化合物可以通过作为神经系统中受体的激动剂和拮抗剂起作用来调节生理过程。本发明的化合物也可以作为杀虫剂和杀真菌剂。含有本发明化合物的药物组合物也具有广泛的用途。

9. 发明授权

US5736560A Substituted pyridines useful as modulators of acetylcholine receptors 失效
公开(公告)号：US5736560A
公开(公告)日：1998-04-07
申请号：US488122
申请日：1995-06-07
申请人： Nicholas D. Cosford , Jean-Michel Vernier
发明人： Nicholas D. Cosford , Jean-Michel Vernier
IPC分类号： A61K31/44 , A61K31/55 , A61P25/04 , A61P25/28 , A61P43/00 , C07D213/38 , C07D213/48 , C07D213/61 , C07D213/82 , C07D401/06 , C07F7/08 , C07D401/02
CPC分类号： C07D401/06 , C07D213/38 , C07F7/0814
摘要： In accordance with the present invention, there is provided a class of pyridine compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors, and are useful for a variety of therapeutic applications, such as the treatment of Alzheimer's disease and other disorders involving memory loss and/or dementia (including AIDS dementia); disorders of attention and focus (such as attention deficit disorder); disorders of extrapyramidal motor function such as Parkinson's disease, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, panic, anxiety and psychosis; substance abuse including withdrawal syndromes and substitution therapy; neuroendocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders of nociception and control of pain; autonomic disorders including dysfunction of gastrointestinal motility and function such as inflammatory bowel disease, irritable bowel syndrome, diarrhea, constipation, gastric acid secretion and ulcers; pheochromocytoma; cardiovascular dysfunction including hypertension and cardia arrhythmias, comedication in surgical procedures, and the like.

10. 发明授权

US5686473A Substituted pyridines useful as modulators of acetylcholine receptors 失效
标题翻译：取代的吡啶可用作乙酰胆碱受体的调节剂
公开(公告)号：US5686473A
公开(公告)日：1997-11-11
申请号：US480405
申请日：1995-06-07
申请人： Nicholas D. Cosford , Jean-Michel Vernier
发明人： Nicholas D. Cosford , Jean-Michel Vernier
IPC分类号： A61K31/44 , A61K31/55 , A61P25/04 , A61P25/28 , A61P43/00 , C07D213/38 , C07D213/48 , C07D213/61 , C07D213/82 , C07D401/06 , C07F7/08 , C07D213/02
CPC分类号： C07D401/06 , C07D213/38 , C07F7/0814
摘要： In accordance with the present invention, there is provided a class of pyridine compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors, and are useful for a variety of therapeutic applications, such as the treatment of Alzheimer's disease and other disorders involving memory loss and/or dementia (including AIDS dementia); disorders of attention and focus (such as attention deficit disorder); disorders of extrapyramidal motor function such as Parkinson's disease, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, panic, anxiety and psychosis; substance abuse including withdrawal syndromes and substitution therapy; neuroendocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders of nociception and control of pain; autonomic disorders including dysfunction of gastrointestinal motility and function such as inflammatory bowel disease, irritable bowel syndrome, diarrhea, constipation, gastric acid secretion and ulcers; pheochromocytoma; cardiovascular dysfunction including hypertension and cardia arrhythmias, comedication in surgical procedures, and the like.
摘要翻译：根据本发明，提供了一类作为乙酰胆碱受体调节剂的吡啶化合物。本发明的化合物从其结合位点取代乙酰胆碱受体配体。本发明化合物可用作乙酰胆碱受体的激动剂，部分激动剂，拮抗剂或变构调节剂，并且可用于各种治疗应用，例如治疗阿尔茨海默氏病和涉及记忆丧失和/或痴呆的其它病症（包括AIDS痴呆） ; 注意力集中障碍（如注意力缺陷障碍）; 锥体外系运动功能紊乱，如帕金森病，亨廷顿疾病，吉列斯·杜列特综合征和迟发性运动障碍; 情绪和情绪障碍如抑郁，恐慌，焦虑和精神病; 药物滥用，包括戒断综合征和替代治疗; 神经内分泌障碍和食物摄入异常，包括贪食症和厌食症; 伤害感受障碍和疼痛控制; 自主神经障碍包括胃肠蠕动功能障碍和功能障碍，如炎性肠病，肠易激综合征，腹泻，便秘，胃酸分泌和溃疡; 嗜铬细胞瘤心血管功能障碍，包括高血压和贲门节律不正，外科手术中的喜剧等。

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