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1. 发明申请

WO2008073142A3 NOVEL INHIBITORS OF BETA-LACTAMASE 审中-公开
标题翻译： β-LACTAMASE的新型抑制剂
公开(公告)号：WO2008073142A3
公开(公告)日：2008-10-02
申请号：PCT/US2007011979
申请日：2007-05-21
申请人： MERCK & CO INC , METHLGENE INC , DININNO FRANK , HAMMOND MILTON L , DYKSTRA KEVIN , KIM SEONGKON , TAN QIANG , YOUNG KATHERINE , HERMES JEFFREY DONALD , CHEN HELEN , RAEPPEL STEPHANE , MANNION MICHAEL , GAUDETTE FREDERIC , VAISBURG ARKADII , RAHL JUBRAIL , GEORGOPAPADAKOU NAFSIKA , ZHOU NANCY Z
发明人： DININNO FRANK , HAMMOND MILTON L , DYKSTRA KEVIN , KIM SEONGKON , TAN QIANG , YOUNG KATHERINE , HERMES JEFFREY DONALD , CHEN HELEN , RAEPPEL STEPHANE , MANNION MICHAEL , GAUDETTE FREDERIC , VAISBURG ARKADII , RAHL JUBRAIL , GEORGOPAPADAKOU NAFSIKA , ZHOU NANCY Z
IPC分类号： A61P31/04 , A61K31/67 , A61K31/675 , C07F9/6539 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
CPC分类号： C07F9/655354 , C07F9/65395 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
摘要： This invention provides novel ß-lactamase inhibitors of the aryl-and heteroarylsulfonarnidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of ß-lactamases and synergize the antibacterial effects of ß-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ß-lactam antibiotics as a result of the presence of the ß-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了具有氮基阳离子或季铵基团的芳基和杂芳基磺酰基甲基膦酸酯单酯类的新型β-内酰胺酶抑制剂。该化合物抑制三种类型的β-内酰胺酶，并且与β-内酰胺类抗生素（例如，亚胺培南和头孢他啶的抗菌作用）对抗β-内酰胺抗生素通常具有抗ß-内酰胺抗生素的微生物的协同作用是由于存在β-内酰胺酶。式（I）或其药学上可接受的盐。

2. 发明专利

AU2007332968A1 Novel inhibitors of beta-lactamase 未知
公开(公告)号：AU2007332968A1
公开(公告)日：2008-06-19
申请号：AU2007332968
申请日：2007-05-21
申请人： METHLGENE INC , MERCK & CO INC
发明人： HAMMOND MILTON L , MANNION MICHAEL , CHEN HELEN , HERMES JEFFREY DONALD , GEORGOPAPADAKOU NAFSIKA , ZHOU NANCY Z , VAISBURG ARKADII , GAUDETTE FREDERIC , YOUNG KATHERINE , RAHL JUBRAIL , DININNO FRANK , KIM SEONGKON , DYKSTRA KEVIN , RAEPPEL STEPHANE , TAN QIANG
IPC分类号： A61P31/04 , A61K31/67 , A61K31/675 , C07F9/6539 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
摘要： This invention provides novel beta-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of beta-lactamases and synergize the antibacterial effects of beta-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the beta-lactam antibiotics as a result of the presence of the beta-lactamases.

3. 发明申请

WO2008073142A8 NOVEL INHIBITORS OF BETA-LACTAMASE 审中-公开
标题翻译： β-LACTAMASE的新型抑制剂
公开(公告)号：WO2008073142A8
公开(公告)日：2009-01-29
申请号：PCT/US2007011979
申请日：2007-05-21
申请人： MERCK & CO INC , METHYLGENE INC , DININNO FRANK , HAMMOND MILTON L , DYKSTRA KEVIN , KIM SEONGKON , TAN QIANG , YOUNG KATHERINE , HERMES JEFFREY DONALD , CHEN HELEN , RAEPPEL STEPHANE , MANNION MICHAEL , GAUDETTE FREDERIC , VAISBURG ARKADII , RAHL JUBRAIL , GEORGOPAPADAKOU NAFSIKA , ZHOU NANCY Z
发明人： DININNO FRANK , HAMMOND MILTON L , DYKSTRA KEVIN , KIM SEONGKON , TAN QIANG , YOUNG KATHERINE , HERMES JEFFREY DONALD , CHEN HELEN , RAEPPEL STEPHANE , MANNION MICHAEL , GAUDETTE FREDERIC , VAISBURG ARKADII , RAHL JUBRAIL , GEORGOPAPADAKOU NAFSIKA , ZHOU NANCY Z
IPC分类号： A61P31/04 , A61K31/67 , A61K31/675 , C07F9/6539 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
CPC分类号： C07F9/655354 , C07F9/65395 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
摘要： This invention provides novel ß-lactamase inhibitors of the aryl-and heteroarylsulfonarnidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of ß-lactamases and synergize the antibacterial effects of ß-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ß-lactam antibiotics as a result of the presence of the ß-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了具有氮基阳离子或季铵基团的芳基和杂芳基磺酰基甲基膦酸酯单酯类的新型β-内酰胺酶抑制剂。该化合物抑制三种类型的β-内酰胺酶，并且与β-内酰胺类抗生素（例如，亚胺培南和头孢他啶的抗菌作用）对抗β-内酰胺抗生素通常具有抗ß-内酰胺抗生素的微生物的协同作用是由于存在β-内酰胺酶。式（I）或其药学上可接受的盐。

4. 发明申请

WO2007139729A8 NOVEL SULFONAMIDOMETHYLPHOSPHONATE INHIBITORS OF BETA-LACTAMASE 审中-公开
标题翻译： β-乳酸酶的新型磺酰亚胺磷酸盐抑制剂
公开(公告)号：WO2007139729A8
公开(公告)日：2008-02-28
申请号：PCT/US2007011977
申请日：2007-05-21
申请人： MERCK & CO INC , METHYLGENE INC , DININNO FRANK , HAMMOND MILTON L , DYKSTRA KEVIN , KIM SEONGKON , TAN QIANG , YOUNG KATHERINE , HERMES JEFFREY DONALD , RAEPPEL STEPHANE , MANNION MICHAEL , ZHOU NANCY Z , GAUDETTE FREDERIC , VAISBURG ARKADII , RAHIL JUBRAIL , GEORGOPAPADAKOU NAFSIKA
发明人： DININNO FRANK , HAMMOND MILTON L , DYKSTRA KEVIN , KIM SEONGKON , TAN QIANG , YOUNG KATHERINE , HERMES JEFFREY DONALD , RAEPPEL STEPHANE , MANNION MICHAEL , ZHOU NANCY Z , GAUDETTE FREDERIC , VAISBURG ARKADII , RAHIL JUBRAIL , GEORGOPAPADAKOU NAFSIKA
IPC分类号： C07F9/6539 , A61K31/662 , A61P31/04 , C07F9/655 , C07F9/6553 , C07F9/6558
CPC分类号： C07F9/655354 , C07F9/6539 , C07F9/65517 , C07F9/655345 , C07F9/65586
摘要： This invention provides novel ß-lactamase inhibitors of the aryl-and heteroaryl-sulfonamidomethylphosphonate monoester class. The compounds inhibit three classes of ß-lactamases and synergize the antibacterial effects of ß-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ß-lactam antibiotics as a result of the presence of the ß-lactamases. Formula (I) or a pro-drug or pharmaceutically acceptable salt thereof, wherein: W represents: Formula (II).
摘要翻译：本发明提供了芳基 - 和杂芳基磺酰氨基甲基膦酸酯单酯类的新型β-内酰胺酶抑制剂。该化合物抑制三种类型的β-内酰胺酶，并且与β-内酰胺类抗生素（例如，亚胺培南和头孢他啶的抗菌作用）对抗β-内酰胺抗生素通常具有抗ß-内酰胺抗生素的微生物的协同作用是由于存在β-内酰胺酶。式（I）或其前药或其药学上可接受的盐，其中：W表示：式（II）。

5. 发明申请

WO2007111864A3 GLUCAGON RECEPTOR ANTAGONIST COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE 审中-公开
公开(公告)号：WO2007111864A3
公开(公告)日：2008-10-02
申请号：PCT/US2007006806
申请日：2007-03-19
申请人： MERCK & CO INC , KIM RONALD M , PARMEE EMMA R , TAN QIANG , LINS ASHLEY ROUSE , CHANG JIANG , YANG CANGMING
发明人： KIM RONALD M , PARMEE EMMA R , TAN QIANG , LINS ASHLEY ROUSE , CHANG JIANG , YANG CANGMING
IPC分类号： A61K31/47 , C07D263/02 , C07D311/00 , C07D401/00
CPC分类号： C07D215/06 , C07C229/52 , C07C233/83 , C07C235/42 , C07C255/57 , C07C309/65 , C07C309/66 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D209/10 , C07D213/30 , C07D213/56 , C07D213/61 , C07D213/64 , C07D213/69 , C07D213/74 , C07D215/14 , C07D215/20 , C07D215/227 , C07D231/12 , C07D231/56 , C07D235/18 , C07D239/34 , C07D257/06 , C07D261/08 , C07D263/57 , C07D271/10 , C07D271/12 , C07D277/64 , C07D277/68 , C07D285/14 , C07D307/42 , C07D307/79 , C07D307/81 , C07D311/12 , C07D311/58 , C07D333/54 , C07D333/60 , C07D401/04 , C07D405/04 , C07D409/04 , C07D417/12 , C07D491/04
摘要： Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

6. 发明申请

WO2007136577A2 GLUCAGON RECEPTOR ANTAGONIST COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：胰高血糖素受体拮抗剂化合物，含有这些化合物的组合物和使用方法
公开(公告)号：WO2007136577A2
公开(公告)日：2007-11-29
申请号：PCT/US2007011390
申请日：2007-05-11
申请人： MERCK & CO INC , KIM RONALD M , PARMEE EMMA R , TAN QIANG , YANG CANGMING , LINS ASHLEY ROUSE
发明人： KIM RONALD M , PARMEE EMMA R , TAN QIANG , YANG CANGMING , LINS ASHLEY ROUSE
IPC分类号： A61K31/47
CPC分类号： C07C233/83 , C07C235/42 , C07C323/60 , C07C323/62 , C07C2601/08 , C07C2601/14 , C07D215/14 , C07D215/227 , C07D235/16 , C07D263/56
摘要： Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译：公开了胰高血糖素受体拮抗剂化合物。这些化合物可用于治疗2型糖尿病和相关病症。药物组合物和治疗方法也包括在内。

7. 发明申请

WO2004091488A3 ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：WO2004091488A3
公开(公告)日：2005-04-07
申请号：PCT/US2004010853
申请日：2004-04-09
申请人： MERCK & CO INC , DININNO FRANK P , CHEN HELEN Y , TAN QIANG
发明人： DININNO FRANK P , CHEN HELEN Y , TAN QIANG
IPC分类号： A61K20060101 , A61K31/40 , A61K31/445 , C07D405/10
CPC分类号： C07D405/10 , C07D311/60
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
摘要翻译：本发明涉及其化合物及其衍生物，其合成及其作为雌激素受体调节剂的用途。本发明的化合物是雌激素受体的配体，因此可用于治疗或预防与雌激素功能相关的各种病症，包括：骨丢失，骨折，骨质疏松症，软骨退化，子宫内膜异位症，子宫肌瘤病，热特别是乳腺，子宫和前列腺中的LDL胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子乳腺发育症，血管平滑肌细胞增殖，肥胖症，失禁和癌症。

8. 发明专利

CA2652995A1 NOVEL INHIBITORS OF BETA-LACTAMASE 未知
公开(公告)号：CA2652995A1
公开(公告)日：2008-06-19
申请号：CA2652995
申请日：2007-05-21
申请人： MERCK & CO INC , METHYLGENE INC
发明人： KIM SEONGKON , DYKSTRA KEVIN , DININNO FRANK , HAMMOND MILTON L , GEORGOPAPADAKOU NAFSIKA , RAHL JUBRAIL , VAISBURG ARKADII , MANNION MICHAEL , GAUDETTE FREDERIC , CHEN HELEN , HERMES JEFFREY DONALD , TAN QIANG , YOUNG KATHERINE , ZHOU NANCY Z , RAEPPEL STEPHANE
IPC分类号： A61P31/04 , A61K31/67 , A61K31/675 , C07F9/6539 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
摘要： This invention provides novel .beta.-lactamase inhibitors of the aryl-and heteroarylsulfonarnidomethylphosphonate monoester class having nitrogen-bas ed cations or quarternary ammomium groups. The compounds inhibit three class es of .beta.-lactamases and synergize the antibacterial effects of .beta.-la ctam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organ isms normally resistant to the .beta.-lactam antibiotics as a result of the presence of the .beta.-lactamases. Formula (I) or pharmaceutically acceptabl e salt thereof.

9. 发明专利

PE20100580A1 ACTIVADORES DE GUANILATO CICLASAS SOLUBLES 未知
公开(公告)号：PE20100580A1
公开(公告)日：2010-08-29
申请号：PE2009000170
申请日：2009-02-04
申请人： MERCK & CO INC
发明人： BITTNER AMY R , SINZ CHRISTOPHER JOSEPH , CHANG JIANG , KING RONALD M , MIRC J W , PARMEE EMMA R , TAN QIANG
IPC分类号： A61K31/415 , A61K31/427 , A61K31/4418 , A61K31/4427 , A61K31/497 , A61K31/506 , A61P7/02 , A61P9/12 , A61P11/06 , A61P15/10 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14
摘要： SE REFIERE A COMPUESTOS HETEROCICLOS DE FORMULA (I) DONDE Z1 ES CH O N; A ES UN ANILLO DE FORMULA (a), (b), ENTRE OTROS, DONDE R4 ES HALOGENO, ALQUILO(C1-C6), CN, ENTRE OTROS; D1 ES CH, CR4 O N; R7 ES H, CICLOALQUILO(C3-C6), FENILO, ENTRE OTROS; L1 ES O, S, CF2, ENTRE OTROS; L2 ES (CH2)2-4, CF2, O, ENTRE OTROS; E ES ARILO(C6-C10), HETEROARILO DE 5 A 10 MIEMBROS O CICLOALQUILO(C3-C8); R5 ES ALQUILO(C1-C6), ALQUENILO(C2-C6), CICLOALQUILO(C5-C8), ENTRE OTROS; R8 ES ALQUILO(C1-C4), O-ALQUENILO(C2-C4), NO2, ENTRE OTROS; R11 ES H O ALQUILO(C1-C6). SON COMPUESTOS PREFERIDOS: ACIDO 1-[6-(2-{[4-(2-FENILETIL)BENCIL]OXI}FENIL)PIRIDIN-2-IL]-5-(TRIFLUOROMETIL)-1H-PIRAZOL-4-CARBOXILICO, ACIDO 1-[6-(2-{[4-(4-CLOROFENOXI)BENCIL]OXI}FENIL)PIRIDIN-2-IL]-5-(TRIFLUOROMETIL)-1H-PIRAZOL-4-CARBOXILICO, ACIDO 1-[6-(2-{[4-(4-OXOCICLOHEXIL)BENCIL]OXI}FENIL)PIRIDIN-2-IL]-5-(TRIFLUOROMETIL)-1H-PIRAZOL-4-CARBOXILICO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS ACTIVAN GUANILATO CICLASA SOLUBLE SIENDO UTILES EN EL TRATAMIENTO DE HIPERTENSION, ANGINA DE PECHO, INSUFICIENCIA CARDIACA, TROMBOSIS

10. 发明专利

PE05802010A1 ACTIVADORES DE GUANILATO CICLASAS SOLUBLES 未知
公开(公告)号：PE05802010A1
公开(公告)日：2010-08-29
申请号：PE0001702009
申请日：2009-02-04
申请人： MERCK & CO INC
发明人： BITTNER AMY R , SINZ CHRISTOPHER JOSEPH , CHANG JIANG , KING RONALD M , MIRC J W , PARMEE EMMA R , TAN QIANG
IPC分类号： A61K31/415 , A61K31/427 , A61K31/4418 , A61K31/4427 , A61K31/497 , A61K31/506 , A61P7/02 , A61P9/12 , A61P11/06 , A61P15/10 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14
摘要： SE REFIERE A COMPUESTOS HETEROCICLOS DE FORMULA (I) DONDE Z1 ES CH O N; A ES UN ANILLO DE FORMULA (a), (b), ENTRE OTROS, DONDE R4 ES HALOGENO, ALQUILO(C1-C6), CN, ENTRE OTROS; D1 ES CH, CR4 O N; R7 ES H, CICLOALQUILO(C3-C6), FENILO, ENTRE OTROS; L1 ES O, S, CF2, ENTRE OTROS; L2 ES (CH2)2-4, CF2, O, ENTRE OTROS; E ES ARILO(C6-C10), HETEROARILO DE 5 A 10 MIEMBROS O CICLOALQUILO(C3-C8); R5 ES ALQUILO(C1-C6), ALQUENILO(C2-C6), CICLOALQUILO(C5-C8), ENTRE OTROS; R8 ES ALQUILO(C1-C4), O-ALQUENILO(C2-C4), NO2, ENTRE OTROS; R11 ES H O ALQUILO(C1-C6). SON COMPUESTOS PREFERIDOS: ACIDO 1-[6-(2-{[4-(2-FENILETIL)BENCIL]OXI}FENIL)PIRIDIN-2-IL]-5-(TRIFLUOROMETIL)-1H-PIRAZOL-4-CARBOXILICO, ACIDO 1-[6-(2-{[4-(4-CLOROFENOXI)BENCIL]OXI}FENIL)PIRIDIN-2-IL]-5-(TRIFLUOROMETIL)-1H-PIRAZOL-4-CARBOXILICO, ACIDO 1-[6-(2-{[4-(4-OXOCICLOHEXIL)BENCIL]OXI}FENIL)PIRIDIN-2-IL]-5-(TRIFLUOROMETIL)-1H-PIRAZOL-4-CARBOXILICO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS ACTIVAN GUANILATO CICLASA SOLUBLE SIENDO UTILES EN EL TRATAMIENTO DE HIPERTENSION, ANGINA DE PECHO, INSUFICIENCIA CARDIACA, TROMBOSIS

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