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公开(公告)号：US08664220B2
公开(公告)日：2014-03-04
申请号：US13499052
申请日：2010-09-29
申请人： Ryan Clark , Brian Andrew Stearns , Jill Melissa Scott , Heather Renee Coate , Lucy Zhao , Thomas J. Seiders , Deborah Volkots , Jeannie Arruda , Nicholas Simon Stock , Yen Pham Truong , David Nathan Zalatan
发明人： Ryan Clark , Brian Andrew Stearns , Jill Melissa Scott , Heather Renee Coate , Lucy Zhao , Thomas J. Seiders , Deborah Volkots , Jeannie Arruda , Nicholas Simon Stock , Yen Pham Truong , David Nathan Zalatan
IPC分类号： A61K31/42 , C07D261/14
CPC分类号： C07D231/38 , C07D261/08 , C07D261/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
摘要翻译： 本文描述的是作为溶血磷脂受体拮抗剂的化合物。 还描述了包括本文所述化合物的药物组合物和药物，以及使用这些拮抗剂单独和与其它化合物组合用于治疗LPA依赖性或LPA介导的病症或疾病的方法。
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公开(公告)号：US20120289522A1
公开(公告)日：2012-11-15
申请号：US13498491
申请日：2010-10-01
申请人： Thomas J. Seiders , Lucy Zhao , Jeannie Arruda , Bowei Wang , Brian Andrew Stearns , Yen Pham Truong , Jill Melissa Scott , John Howard Hutchinson , Ryan Clark , Heather Renee Coate , Nicholas Simon Stock , Deborah Volkots
发明人： Thomas J. Seiders , Lucy Zhao , Jeannie Arruda , Bowei Wang , Brian Andrew Stearns , Yen Pham Truong , Jill Melissa Scott , John Howard Hutchinson , Ryan Clark , Heather Renee Coate , Nicholas Simon Stock , Deborah Volkots
IPC分类号： A61K31/42 , C07D261/08 , C07D413/12 , A61K31/4439 , C07D417/12 , A61P17/00 , C07D495/04 , A61K31/519 , A61P11/00 , A61P13/12 , A61P1/16 , C07D261/14 , A61K31/428
CPC分类号： C07D261/08 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/519 , C07D261/14 , C07D261/18 , C07D405/12 , C07D413/06 , C07D413/12 , C07D417/12 , C07D495/04
摘要： Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
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公开(公告)号：US08592402B2
公开(公告)日：2013-11-26
申请号：US13388502
申请日：2010-08-03
IPC分类号： A61K31/56 , A61K31/42 , C07D261/14
CPC分类号： C07D261/14 , A61K31/42 , A61K31/4427 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07F9/653
摘要： Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
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公开(公告)号：US20090306115A1
公开(公告)日：2009-12-10
申请号：US11918993
申请日：2006-04-18
IPC分类号： A61K31/506 , C07D211/76 , C07D239/08 , A61K31/4402 , A61P25/00
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。
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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。
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公开(公告)号：US20120196839A1
公开(公告)日：2012-08-02
申请号：US13388502
申请日：2010-08-03
IPC分类号： A61K31/42 , A61K31/56 , A61P29/00 , C07D261/14 , A61P35/00
CPC分类号： C07D261/14 , A61K31/42 , A61K31/4427 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07F9/653
摘要： Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
摘要翻译： 本文描述的是作为溶血磷脂受体拮抗剂的化合物。 还描述了包括本文所述化合物的药物组合物和药物，以及使用这些拮抗剂单独和与其它化合物组合用于治疗LPA依赖性或LPA介导的病症或疾病的方法。
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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。
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8.发明申请公开(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。
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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。
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10.发明授权Group 8 transition metal carbene complexes as enantionselective olefin metathesis catalysts 有权第8族过渡金属卡宾络合物作为对映选择性烯烃复分解催化剂公开(公告)号：US07683180B2
公开(公告)日：2010-03-23
申请号：US10124745
申请日：2002-04-16
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族过渡金属卡宾络合物用作烯烃交叉复分解反应的催化剂，特别涉及对映选择性反应。 还提供了这些络合物的合成及其用作催化剂的细节。
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