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1. 发明申请

WO2002083742A2 GROUP 8 TRANSITION METAL CARBENE COMPLEXES AS ENANTIOSELECTIVE OLEFIN METATHESIS CATALYSTS 审中-公开
标题翻译：第8组过渡金属碳复合物作为选择性烯烃METATHESIS催化剂
公开(公告)号：WO2002083742A2
公开(公告)日：2002-10-24
申请号：PCT/US2002/012165
申请日：2002-04-16
申请人： CALIFORNIA INSTITUTE OF TECHNOLOGY , GRUBBS, Robert, H. , WARD, Donald, W. , SEIDERS, Thomas, J. , GOLDBERG, Steven, D.
发明人： GRUBBS, Robert, H. , WARD, Donald, W. , SEIDERS, Thomas, J. , GOLDBERG, Steven, D.
IPC分类号： C08F
CPC分类号： C07F15/0046
摘要： The invention pertains to the use of Group 8 transition metal carbene complexes as catalysts for olefin cross- metathesis reactions, and for enantioselective reactions in particular. The synthesis of these complexes and details of their use as catalysts is also provided.
摘要翻译：本发明涉及第8族过渡金属卡宾化合物作为烯烃交换复分解反应的催化剂的制备和用途，特别涉及对映选择性反应。还提供了这些化合物的合成及其用作催化剂的细节。卡宾化合物进一步通过与金属原子键合的五元杂环配体sigma连接。该配体在与金属原子键合的碳原子相邻的环中具有两个氮，磷，氧或硫杂原子。该配体是饱和的，两个杂原子优选是具有与它们键合的苯基的氮，并且配体的另外两个远端碳原子优选是手性的。

2. 发明申请

WO2006115895A2 PHENYL ETHYNE COMPOUNDS 审中-公开
标题翻译：苯乙烯化合物
公开(公告)号：WO2006115895A2
公开(公告)日：2006-11-02
申请号：PCT/US2006014517
申请日：2006-04-18
申请人： MERCK & CO INC , COSFORD NICHOLAS D , SEIDERS THOMAS J
发明人： COSFORD NICHOLAS D , SEIDERS THOMAS J
IPC分类号： C07C255/49
CPC分类号： C07C255/50 , A01N37/34 , A01N43/40 , A01N43/54 , C07C255/51 , C07C255/53 , C07C255/58 , C07D213/65 , C07D239/42
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。

3. 发明申请

WO2007050050A3 THIAZOLYL MGLUR5 ANTAGONISTS AND METHODS FOR THEIR USE 审中-公开
标题翻译： THIAZOLYL MGLUR5 ANTAGONISTS及其使用方法
公开(公告)号：WO2007050050A3
公开(公告)日：2008-02-07
申请号：PCT/US2005035921
申请日：2005-10-06
申请人： MERCK & CO INC , COSFORD NICHOLAS D , SEIDERS THOMAS J , PAYNE JOSEPH , ROPPE JEFFREY R , HUANG DEHUA , SMITH NICHOLAS D , POON STEVE F , KING CHRIS , EASTMAN BRIAN W , WANG BOWEI , ARRUDA JEANNIE M , VERNIER JEAN-MICHEL , ZHAO XIUMIN
发明人： COSFORD NICHOLAS D , SEIDERS THOMAS J , PAYNE JOSEPH , ROPPE JEFFREY R , HUANG DEHUA , SMITH NICHOLAS D , POON STEVE F , KING CHRIS , EASTMAN BRIAN W , WANG BOWEI , ARRUDA JEANNIE M , VERNIER JEAN-MICHEL , ZHAO XIUMIN
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

WO2007050050A2 THIAZOLYL MGLUR5 ANTAGONISTS AND METHODS FOR THEIR USE 审中-公开
标题翻译： THIAZOLYL MGLUR5 ANTAGONISTS及其使用方法
公开(公告)号：WO2007050050A2
公开(公告)日：2007-05-03
申请号：PCT/US2005/035921
申请日：2005-10-06
申请人： MERCK & CO., INC. , COSFORD, Nicholas, D. , SEIDERS, Thomas, J. , PAYNE, Joseph , ROPPE, Jeffrey, R. , HUANG, Dehua , SMITH, Nicholas, D. , POON, Steve, F. , KING, Chris , EASTMAN, Brian, W. , WANG, Bowei , ARRUDA, Jeannie, M. , VERNIER, Jean-Michel , ZHAO, Xiumin
发明人： COSFORD, Nicholas, D. , SEIDERS, Thomas, J. , PAYNE, Joseph , ROPPE, Jeffrey, R. , HUANG, Dehua , SMITH, Nicholas, D. , POON, Steve, F. , KING, Chris , EASTMAN, Brian, W. , WANG, Bowei , ARRUDA, Jeannie, M. , VERNIER, Jean-Michel , ZHAO, Xiumin
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，选择由亚乙炔连接到吡啶环的3位或嘧啶环的5位的1,3-噻唑-2-基环成员，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. 发明申请

WO2006115895A3 PHENYL ETHYNE COMPOUNDS 审中-公开
公开(公告)号：WO2006115895A3
公开(公告)日：2006-11-02
申请号：PCT/US2006/014517
申请日：2006-04-18
申请人： MERCK & CO., INC. , COSFORD, Nicholas, D. , SEIDERS, Thomas, J.
发明人： COSFORD, Nicholas, D. , SEIDERS, Thomas, J.
IPC分类号： C07C255/50 , C07D239/08 , C07D213/62 , A61K31/275 , A61K31/435 , A61K31/505
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.

6. 发明申请

WO02083742A3 GROUP 8 TRANSITION METAL CARBENE COMPLEXES AS ENANTIOSELECTIVE OLEFIN METATHESIS CATALYSTS 审中-公开
标题翻译：第8族过渡金属碳烯配合物作为对映体烯烃分解催化剂
公开(公告)号：WO02083742A3
公开(公告)日：2002-12-19
申请号：PCT/US0212165
申请日：2002-04-16
申请人： CALIFORNIA INST OF TECHN , GRUBBS ROBERT H , WARD DONALD W , SEIDERS THOMAS J , GOLDBERG STEVEN D
发明人： GRUBBS ROBERT H , WARD DONALD W , SEIDERS THOMAS J , GOLDBERG STEVEN D
IPC分类号： C07F15/00 , C08F4/06 , C08F4/80 , C07F9/70 , C07F9/90 , C07F9/94 , C07F15/02 , C07F15/04 , C07F15/06 , C07F17/02
CPC分类号： C07F15/0046
摘要： The invention pertains to the preparation and use of Group 8 transition metal carbene compounds as catalysts for olefin cross- metathesis reactions, and for enantioselective reactions in particular. The synthesis of these compounds and details of their use as catalysts is also provided. The carbene compounds are further ligated by a five-membered heterocycle ligand sigma bonded to the metal atom. This ligand has two nitrogen, phosphorus, oxygen or sulfur heteroatoms in the ring adjacent to the carbon atom bonded to the metal atom. This ligand is saturated, the two heteroatoms are preferably nitrogen with phenyl groups bonded to them, and the other two distal carbon atoms of the ligand are preferably chiral.
摘要翻译：本发明涉及第8族过渡金属卡宾化合物作为烯烃交叉复分解反应催化剂以及特别是对映选择性反应的制备和用途。还提供了这些化合物的合成及其作为催化剂使用的细节。卡宾化合物通过与金属原子键合的五元杂环配体σ进一步连接。该配体在与金属原子键合的碳原子相邻的环中具有两个氮，磷，氧或硫杂原子。该配体是饱和的，两个杂原子优选是具有与它们键合的苯基的氮，并且配体的另外两个远端碳原子优选是手性的。

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