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1. 发明申请

WO2009016498A1 PYRIMIDINE AND PYRIDINE DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS 审中-公开
标题翻译：吡嗪和吡啶衍生物及其药物用途和组合物
公开(公告)号：WO2009016498A1
公开(公告)日：2009-02-05
申请号：PCT/IB2008/002046
申请日：2008-07-29
申请人： PFIZER INC. , SCHNUTE, Mark, E. , CARROLL, Jeffery, Neal , HANAU, Cathleen, Elizabeth , MCREYNOLDS, Matthew, David , SCHOLTEN, Jeffrey, Allen , MCDONALD, Joseph, J. , GRAPPERHAUS, Margaret, L. , MASSA, Mark, Alan , RUMINSKI, Peter, G. , SCHMIDT, Michelle, Ann , STROHBACK, Joseph, Walter , HAMPER, Bruce, Cameron , FLETCHER, Theresa, R. , ROGERS, Michael, David , O'BRIEN, Patrick, Michael , NAHRA, Joe , MORRIS, Mark, Anthony , ROARK, William, Howard
发明人： SCHNUTE, Mark, E. , CARROLL, Jeffery, Neal , HANAU, Cathleen, Elizabeth , MCREYNOLDS, Matthew, David , SCHOLTEN, Jeffrey, Allen , MCDONALD, Joseph, J. , GRAPPERHAUS, Margaret, L. , MASSA, Mark, Alan , RUMINSKI, Peter, G. , SCHMIDT, Michelle, Ann , STROHBACK, Joseph, Walter , HAMPER, Bruce, Cameron , FLETCHER, Theresa, R. , ROGERS, Michael, David , O'BRIEN, Patrick, Michael , NAHRA, Joe , MORRIS, Mark, Anthony , ROARK, William, Howard
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/14 , A61K31/44 , A61K31/506 , A61P19/00 , A61P35/00
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/14
摘要： The prsent invention relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof, processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as anti-inflammatory agents.
摘要翻译：本发明涉及式（I）的化合物及其药学上可接受的盐，制备用途的中间体，含有这些化合物的组合物和这些化合物作为抗炎剂的用途。

2. 发明申请

WO2007072150A3 PIPERIDINE DERIVATIVES 审中-公开
公开(公告)号：WO2007072150A3
公开(公告)日：2007-06-28
申请号：PCT/IB2006/003639
申请日：2006-12-16
申请人： PFIZER PRODUCTS INC. , BRUENDL, Michelle, Marie , GREENE, Keri, Lynn , JENNINGS, Rex, Allen , LAZERWITH, Scott, Edward , NAHRA, Joe , O'BRIEN, Patrick, Michael , PARA, Kimberly, Suzanne , SHEEHAN, Susan, Mary, Kult
发明人： BRUENDL, Michelle, Marie , GREENE, Keri, Lynn , JENNINGS, Rex, Allen , LAZERWITH, Scott, Edward , NAHRA, Joe , O'BRIEN, Patrick, Michael , PARA, Kimberly, Suzanne , SHEEHAN, Susan, Mary, Kult
IPC分类号： C07D211/22 , C07D401/12 , C07D405/14 , C07D495/04 , A61K31/451 , A61K31/4995 , A61P25/24 , A61P25/18 , A61P25/22
摘要： The present invention provides compounds of Formula I: and pharmaceutically acceptable salts thereof, The compounds of Formula I are useful in treating a disorder or condition selected from the group consisting of: fibromyalgia; attention deficit hyperactivity disorder (ADHD); generalized anxiety disorder; depression; and schizophrenia.

3. 发明申请

WO2003062782A1 SYSTEM FOR REMOVING VEHICLES HAVING UNSAFE TIRES FROM PUBLIC ROADWAYS 审中-公开
标题翻译：从公共道路上拆卸不安全轮胎的车辆的制度
公开(公告)号：WO2003062782A1
公开(公告)日：2003-07-31
申请号：PCT/US2003/001633
申请日：2003-01-17
申请人： O'BRIEN, John, Michael , O'BRIEN, Patrick, Michael , FOGARTY, Stacy, R.
发明人： O'BRIEN, John, Michael , O'BRIEN, Patrick, Michael , FOGARTY, Stacy, R.
IPC分类号： G01M17/02
CPC分类号： B60C11/24 , Y10T152/10027
摘要： A four step process for removing vehicles from the public roadways having worn tires including establishing a standard for end of life tire conditions (30), converting the standard to relate correspondingly to tread wear (32), providing a visual indication of end of life tread wear (34) and providing for inspection and vehicle disqualification where end of life tire wear is indicated (36).
摘要翻译：从具有磨损轮胎的公共道路中移除车辆的四步骤，包括建立寿命轮胎条件的标准（30），将标准转换为相应于胎面磨损（32），提供寿命终点的视觉指示磨损（34），并在轮胎磨损终止时提供检查和车辆取消资格（36）。

4. 发明申请

WO2009016498A8 PYRIMIDINE AND PYRIDINE DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS 审中-公开
标题翻译：吡嗪和吡啶衍生物及其药物用途和组合物
公开(公告)号：WO2009016498A8
公开(公告)日：2010-11-11
申请号：PCT/IB2008002046
申请日：2008-07-29
申请人： PFIZER , SCHNUTE MARK E , CARROLL JEFFERY NEAL , HANAU CATHLEEN ELIZABETH , MCREYNOLDS MATTHEW DAVID , SCHOLTEN JEFFREY ALLEN , MCDONALD JOSEPH J , GRAPPERHAUS MARGARET L , MASSA MARK ALAN , RUMINSKI PETER G , SCHMIDT MICHELLE ANN , STROHBACH JOSEPH WALTER , HAMPER BRUCE CAMERON , FLETCHER THERESA R , ROGERS MICHAEL DAVID , O'BRIEN PATRICK MICHAEL , NAHRA JOE , MORRIS MARK ANTHONY , ROARK WILLIAM HOWARD
发明人： SCHNUTE MARK E , CARROLL JEFFERY NEAL , HANAU CATHLEEN ELIZABETH , MCREYNOLDS MATTHEW DAVID , SCHOLTEN JEFFREY ALLEN , MCDONALD JOSEPH J , GRAPPERHAUS MARGARET L , MASSA MARK ALAN , RUMINSKI PETER G , SCHMIDT MICHELLE ANN , STROHBACH JOSEPH WALTER , HAMPER BRUCE CAMERON , FLETCHER THERESA R , ROGERS MICHAEL DAVID , O'BRIEN PATRICK MICHAEL , NAHRA JOE , MORRIS MARK ANTHONY , ROARK WILLIAM HOWARD
IPC分类号： C07D401/04 , A61K31/44 , A61K31/506 , A61P19/00 , A61P35/00 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/14
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/14
摘要： The prsent invention relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof, processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as anti-inflammatory agents.
摘要翻译：本发明涉及式（I）的化合物及其药学上可接受的盐，制备用途的中间体，含有这些化合物的组合物，以及这些化合物作为抗炎剂的用途。

5. 发明申请

WO2006102468A2 SAFETY TIRE, METHOD OF MAKING AND METHOD OF IMPROVED TRAFFIC SAFETY WITH USE THEREOF 审中-公开
标题翻译：安全轮胎，其使用方法和改进的交通安全方法
公开(公告)号：WO2006102468A2
公开(公告)日：2006-09-28
申请号：PCT/US2006/010500
申请日：2006-03-22
申请人： O'BRIEN, John Michael , O'BRIEN, Patrick Michael
发明人： O'BRIEN, John Michael , O'BRIEN, Patrick Michael
IPC分类号： B60C11/24
CPC分类号： B60C11/24 , Y10T152/10027
摘要： A tire in which a tire manufacturer has determined the tractive capacity at numerous levels of tread wear, the tire having at least one visual warning indicator located at a tread depth corresponding to a percentage loss of tractive capacity. Also, a method of making the tire and a method improving traffic safety through use of such a tire combined with educating the consumer as to proper use of the tire.
摘要翻译：一种轮胎，其中轮胎制造商已经确定了多个胎面磨损级别的牵引能力，轮胎具有位于与牵引能力的百分比损失相对应的胎面深度处的至少一个视觉警告指示器。此外，制造轮胎的方法以及通过使用这样的轮胎提高交通安全性的方法结合教育消费者来正确使用轮胎。

6. 发明申请

WO2004014869A2 5,6-FUSED 3,4-DIHYDROPYRIMIDINE-2-ONE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：作为基质金属蛋白酶抑制剂的5,6-FUSED 3,4-二羟基嘧啶-2-酮衍生物
公开(公告)号：WO2004014869A2
公开(公告)日：2004-02-19
申请号：PCT/IB2003/003534
申请日：2003-08-04
申请人： WARNER-LAMBERT COMPANY LLC , NAHRA, Joe , O'BRIEN, Patrick, Michael , ORTWINE, Daniel, Fred
发明人： NAHRA, Joe , O'BRIEN, Patrick, Michael , ORTWINE, Daniel, Fred
IPC分类号： C07D239/00
CPC分类号： C07D231/12 , C07D233/56 , C07D239/74 , C07D239/80 , C07D249/08 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D471/04
摘要： This invention provides compounds defined by Formula (I), or a pharmaceutically acceptable salt thereof, wherein R 1 , Q, Y 3, Y 4 , Y 5 Y 6 , Y 8 , R 2 and R 4 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula (I), or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula (I), or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency, inflammatory bowel disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula (I), or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, together with another pharmaceutically active component as described in the specification
摘要翻译：本发明提供式（I）所定义的化合物或其药学上可接受的盐，其中R 1，Q，Y 3，Y 4，Y 5 Y 6，Y 8， R 2和R 4如说明书中所定义。本发明还提供包含本说明书中定义的式（I）化合物或其药学上可接受的盐以及药学上可接受的载体，稀释剂或赋形剂的药物组合物。本发明还提供了在动物中抑制MMP-13酶的方法，包括向动物施用式（I）化合物或其药学上可接受的盐。本发明还提供了治疗患者中由MMP-13酶介导的疾病的方法，其包括向患者施用单独或药物组合物中的式（I）化合物或其药学上可接受的盐。本发明还提供了治疗诸如心脏病，多发性硬化，骨关节炎和类风湿性关节炎，除了骨关节炎或类风湿性关节炎之外的关节炎，心功能不全，炎性肠病，心力衰竭，年龄相关性黄斑变性，慢性阻塞性肺疾病，哮喘，牙周疾病，牛皮癣，动脉粥样硬化和骨质疏松症，其包括向患者单独或在药物组合物中给予式（I）化合物或其药学上可接受的盐。本发明还提供组合，其包含式（I）化合物或其药学上可接受的盐以及如说明书中所述的另一种药物活性成分

7. 发明申请

WO2006061706A1 TETRAZOLYL-METHYLENE AMINO ACID DERIVATIVES 审中-公开
标题翻译：四甲基亚甲基氨基酸衍生物
公开(公告)号：WO2006061706A1
公开(公告)日：2006-06-15
申请号：PCT/IB2005/003717
申请日：2005-12-05
申请人： WARNER-LAMBERT COMPANY LLC , NAHRA, Joe , O'BRIEN, Patrick, Michael
发明人： NAHRA, Joe , O'BRIEN, Patrick, Michael
IPC分类号： C07D401/04 , C07D257/04 , A61K31/41 , A61K31/4427
CPC分类号： C07D401/04 , C07D401/06
摘要： This invention relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof; a pharmaceutical composition; a method of treating a disease mediated by an MMP-13 enzyme in a mammal; and a therapeutic combination containing at least two pharmaceutically active components, wherein R 1 , Q , W 1 , W 2 , R 2a , L 1 , and R 3 , the pharmaceutical composition, the method of treating, and the therapeutic combination are as defined in the specification.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐; 药物组合物; 治疗哺乳动物中由MMP-13酶介导的疾病的方法; 和含有至少两种药物活性成分的治疗组合，其中R 1

8. 发明申请

WO2004014366A1 HETERO BIARYL DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译： HETERO BIARYL衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：WO2004014366A1
公开(公告)日：2004-02-19
申请号：PCT/IB2003/003616
申请日：2003-08-03
申请人： WARNER-LAMBERT COMPANY LLC , BUNKER, Amy, Mae , MORRIS, Mark, Anthony , O'BRIEN, Patrick, Michael , WILSON, Michael, William
发明人： BUNKER, Amy, Mae , MORRIS, Mark, Anthony , O'BRIEN, Patrick, Michael , WILSON, Michael, William
IPC分类号： A61K31/41
CPC分类号： C07D257/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D271/10 , C07D271/107 , C07D285/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/12 , C07D409/06 , C07D413/10 , C07D417/10 , C07D417/12
摘要： This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R l , Q, S, T, U, V, and R 2 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a' pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a' compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency,,inflammatory bowel, disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically, acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, together with another pharmaceutically active, component as described in the specification.
摘要翻译：本发明提供由式I定义的化合物或其药学上可接受的盐，其中R 1，Q，S，T，U，V和R 2如说明书中所定义。本发明还提供包含本说明书中定义的式I化合物或其药学上可接受的盐以及“药学上可接受的载体，稀释剂或赋形剂”的药物组合物。本发明还提供了在动物中抑制MMP-13酶的方法，包括向动物施用式I化合物或其药学上可接受的盐。本发明还提供了治疗由患者中的MMP-13酶介导的疾病的方法，包括单独或在药物组合物中向患者施用“式I化合物或其药学上可接受的盐。本发明还提供治疗诸如心脏病，多发性硬化，骨关节炎和类风湿性关节炎，除了骨关节炎或类风湿性关节炎之外的关节炎，心功能不全，炎性肠病，疾病，心力衰竭，年龄相关性黄斑变性，慢性阻塞性肺疾病，哮喘，牙周疾病，牛皮癣，动脉粥样硬化和骨质疏松症，其包括向患者施用单独或药物组合物中的式I化合物或其药学上可接受的盐。本发明还提供了包含式I化合物或其药学上可接受的盐以及说明书中描述的另一种药学活性成分的组合。

9. 发明申请

WO2003032999A1 ALKYNE MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译： ALKYNE MATRIX金属蛋白酶抑制剂
公开(公告)号：WO2003032999A1
公开(公告)日：2003-04-24
申请号：PCT/IB2002/003057
申请日：2002-08-02
申请人： WARNER-LAMBERT COMPANY LLC , BUNKER, Amy, Mae , HARTER, William, Glen , HICKS, James, Lester , O'BRIEN, Patrick, Michael , PHAM, Ly, Thi , PICARD, Joseph, Armand , ROARK, William, Howard
发明人： BUNKER, Amy, Mae , HARTER, William, Glen , HICKS, James, Lester , O'BRIEN, Patrick, Michael , PHAM, Ly, Thi , PICARD, Joseph, Armand , ROARK, William, Howard
IPC分类号： A61K31/549
CPC分类号： C07D213/40 , C07C233/87 , C07C235/42 , C07C255/57 , C07C255/60 , C07C311/46 , C07C317/32 , C07D213/56 , C07D213/64 , C07D213/81 , C07D213/82 , C07D215/233 , C07D231/12 , C07D233/56 , C07D249/04 , C07D249/08 , C07D279/02 , C07D285/16 , C07D285/24 , C07D291/08 , C07D401/06 , C07D495/04 , C07D513/04 , C07D515/04
摘要： A compound of Formula (I) or a pharmaceutical acceptable salt thereof, or a tautomer thereof, wherein G 1 , G 2 , and B are as defined in the application, are selective inhibitors of MMP-13. The compounds are useful for treating diseases mediated by MMP-13, including cancer and arthritis.
摘要翻译：式（I）化合物或其药学上可接受的盐或其互变异构体，其中G1，G2和B如本申请中所定义，是MMP-13的选择性抑制剂。该化合物可用于治疗由MMP-13介导的疾病，包括癌症和关节炎。

10. 发明申请

WO2002064568A1 PYRIDINE MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：吡啶基金属蛋白酶抑制剂
公开(公告)号：WO2002064568A1
公开(公告)日：2002-08-22
申请号：PCT/IB2002/000345
申请日：2002-02-04
申请人： WARNER-LAMBERT COMPANY , BARVIAN, Nicole, Chantel , CONNOR, David, Thomas , O'BRIEN, Patrick, Michael , ORTWINE, Daniel, Fred , PATT, William, Chester , SHULER, Kevon, Ray , WILSON, Michael, William
发明人： BARVIAN, Nicole, Chantel , CONNOR, David, Thomas , O'BRIEN, Patrick, Michael , ORTWINE, Daniel, Fred , PATT, William, Chester , SHULER, Kevon, Ray , WILSON, Michael, William
IPC分类号： C07D213/80
CPC分类号： C07D213/80 , C07D213/81 , C07D213/82 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D405/14 , C07D409/14
摘要： Selective MMP-13 inhibitors are pyridine derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: R 1 and R 2 independently are hydrogen, halo, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, NO 2 , NR 4 R 5 , CN, or CF 3 ; E is independently O or S; A and B independently are OR 4 or NR 4 R 5 ; R 4 and R 5 independently are H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, (CH 2 ) n aryl, (CH 2 ) n cycloalkyl, (CH 2 ) n heteroaryl, or R 4 and R 5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6.
摘要翻译：选择性MMP-13抑制剂是式（I）的吡啶衍生物或其药学上可接受的盐，其中：R 1和R 2独立地是氢，卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基， C 2 -C 6烯基，C 2 -C 6炔基，NO 2，NR 4 R 5，CN或CF 3; E独立地为O或S; A和B分别是OR 4或NR 4 R 5; R 4和R 5独立地是H，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，（CH 2）n芳基，（CH 2）n环烷基，（CH 2）n杂芳基或R 4 和R 5与它们所连接的氮原子一起形成含有3至8元环的碳原子并且任选地含有选自O，S或NH的杂原子，并且任选地被取代或未取代; n为0〜6。

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