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1. 发明申请

WO2005060571A3 ANTIPROTOZOAL IMIDAZOPYRIDINE COMPOUNDS 审中-公开
标题翻译：抗真菌药咪唑吡啶化合物
公开(公告)号：WO2005060571A3
公开(公告)日：2005-12-15
申请号：PCT/US2004040617
申请日：2004-12-06
申请人： MERCK & CO INC , BIFTU TESFAYE , FISHER MICHAEL H , WYVRATT MATTHEW J
发明人： BIFTU TESFAYE , FISHER MICHAEL H , WYVRATT MATTHEW J
IPC分类号： A61K31/4188 , C07D401/04 , C07D403/04 , C07D417/04 , C07D471/04
CPC分类号： C07D471/04
摘要： Compounds described by the Formula (I) or (II): or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination with one or more anticoccidieal agent(s). A composition for controlling coccidiosis in poultry comprises the compound alone, or in combination with one or more anticoccidial agent(s). Methods for the treatment and prevention of mammalian protozoal diseases, such as, for example, toxoplasmosis, malaria. African typanosomiasis, Chagas disease, and opportunistic infections comprise administering the compound alone, or in combination with one or more antiprotozoal agent(s).
摘要翻译：由式（I）或（II）表示的化合物：或其药学上可接受的盐或N-氧化物。该化合物可用于治疗和预防哺乳动物和鸟类中的原生动物疾病。用于控制家禽中球虫病的方法包括单独施用有效量的化合物，或与一种或多种抗球虫剂组合施用。用于控制家禽中球虫病的组合物包含单独的化合物，或与一种或多种抗球虫剂组合。用于治疗和预防哺乳动物原生动物疾病的方法，例如弓形体病，疟疾。非洲typanosomias，恰加斯病和机会性感染包括单独施用化合物，或与一种或多种抗原虫剂组合施用。

2. 发明申请

WO2004080390A3 ANTIPROTOZOAL IMIDAZOPYRIDINE COMPOUNDS 审中-公开
标题翻译：抗真菌药咪唑吡啶化合物
公开(公告)号：WO2004080390A3
公开(公告)日：2005-01-20
申请号：PCT/US2004006153
申请日：2004-03-02
申请人： MERCK & CO INC , WYVRATT MATTHEW J , BIFTU TESFAYE , FISHER MICHAEL H , SCHMATZ DENNIS M
发明人： WYVRATT MATTHEW J , BIFTU TESFAYE , FISHER MICHAEL H , SCHMATZ DENNIS M
IPC分类号： A61K20060101 , A61K31/429 , C07D403/04 , C07D471/04
CPC分类号： C07D471/04 , C07D519/00
摘要： Compounds described by the Formula (I): (I) or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination with one or more anticoccidial agent(s). A composition for controlling coccidiosis in poultry comprises the compound alone, or in combination with one or more anticoccidial agent(s). Methods for the treatment and prevention of mammalian protozoal diseases, such as, for example, toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, and opportunistic infections comprise administering the compound alone, or in combination with one or more antiprotozoal agent(s).
摘要翻译：由式（I）表示的化合物：（I）或其药学上可接受的盐或N-氧化物。该化合物可用于治疗和预防哺乳动物和鸟类中的原生动物疾病。控制家禽中球虫病的方法包括单独施用有效量的化合物，或与一种或多种抗球虫剂组合施用。用于控制家禽中球虫病的组合物包含单独的化合物，或与一种或多种抗球虫剂组合。用于治疗和预防哺乳动物原生动物疾病的方法，例如弓形虫病，疟疾，非洲锥虫病，恰加斯病和机会性感染包括单独施用化合物或与一种或多种抗原虫剂组合施用。

3. 发明申请

WO0134632A3 ALIPHATIC HYDROXY SUBSTITUTED PIPERIDYL DIARYL PYRROLE DERIVATIVES AS ANTIPROTOZOAL AGENTS 审中-公开
标题翻译：作为抗真菌剂的二氢羟基替代哌啶衍生物衍生物
公开(公告)号：WO0134632A3
公开(公告)日：2001-09-27
申请号：PCT/US0030748
申请日：2000-11-09
申请人： MERCK & CO INC , BIFTU TESFAYE , FENG DANQING D , LIANG GUI BAI , PONPIPOM MITREE M , QIAN XIAOXIA , FISHER MICHAEL H , WYVRATT MATTHEW J , BUGIANESI ROBERT L
发明人： BIFTU TESFAYE , FENG DANQING D , LIANG GUI-BAI , PONPIPOM MITREE M , QIAN XIAOXIA , FISHER MICHAEL H , WYVRATT MATTHEW J , BUGIANESI ROBERT L
IPC分类号： C07D401/14 , C07D405/14 , A61K31/4545
CPC分类号： C07D401/14 , C07D405/14
摘要： Trisubstituted pyrroles are antiprotozal agents useful in the treatment and prevention of protozoal diseases in human an animals, including the control of coccidiosis in poultry.
摘要翻译：三取代吡咯是可用于治疗和预防人类动物体内原生动物疾病的抗替罗尔剂，包括控制家禽中的球虫病。

4. 发明申请

WO2007136603A2 AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 审中-公开
公开(公告)号：WO2007136603A2
公开(公告)日：2007-11-29
申请号：PCT/US2007011520
申请日：2007-05-11
申请人： MERCK & CO INC , BIFTU TESFAYE , CHEN PING , FENG DANQING , WEBER ANN E
发明人： BIFTU TESFAYE , CHEN PING , FENG DANQING , WEBER ANN E
IPC分类号： A61K31/498
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

5. 发明申请

WO2004103276A3 3-AMINO-4-PHENYLBUTANOIC ACID DERIVATIVES AS DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 审中-公开
公开(公告)号：WO2004103276A3
公开(公告)日：2005-08-11
申请号：PCT/US2004014642
申请日：2004-05-10
申请人： MERCK & CO INC , BIFTU TESFAYE , FENG DANQING DENNIS , LIANG GUI-BAI , QIAN XIAOXIA
发明人： BIFTU TESFAYE , FENG DANQING DENNIS , LIANG GUI-BAI , QIAN XIAOXIA
IPC分类号： A61K20060101 , A61K31/55 , A61P3/10 , C07D487/04 , C07D491/00
CPC分类号： C07D487/04
摘要： The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

6. 发明申请

WO2007097931A3 AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 审中-公开
标题翻译：氨基四氢吡喃糖苷作为二磷酸二肽酶-IV抑制剂治疗或预防糖尿病
公开(公告)号：WO2007097931A3
公开(公告)日：2007-11-22
申请号：PCT/US2007003558
申请日：2007-02-09
申请人： MERCK & CO INC , BIFTU TESFAYE , CALDWELL CHARLES G , WEBER ANN E , CHEN PING , QIAN XIAOXIA , FENG DANQING , COX JASON M
发明人： BIFTU TESFAYE , CALDWELL CHARLES G , WEBER ANN E , CHEN PING , QIAN XIAOXIA , FENG DANQING , COX JASON M
IPC分类号： A61K31/519
CPC分类号： C07D471/04 , C07D405/04 , C07D487/04
摘要： The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及结构式I的新的取代的氨基四氢吡喃，其为二肽基肽酶-IV酶的抑制剂并且可用于治疗或预防其中涉及二肽基肽酶-IV酶的疾病，例如糖尿病，特别是 2型糖尿病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗其中涉及二肽基肽酶-IV酶的疾病中的用途。

7. 发明申请

WO2006065826A3 PROCESS TO CHIRAL BETA AMINO ACID DERIVATIVES BY ASYMMETRIC HYDROGENATION 审中-公开
标题翻译：不对称加氢制备手性β氨基酸衍生物的方法
公开(公告)号：WO2006065826A3
公开(公告)日：2006-10-05
申请号：PCT/US2005045096
申请日：2005-12-12
申请人： MERCK & CO INC , BIFTU TESFAYE , SONG ZHIGUO J , ZHANG FEI , ROSNER THORSTEN , HANSEN KARL , ARMSTRONG JOSEPH D III
发明人： BIFTU TESFAYE , SONG ZHIGUO J , ZHANG FEI , ROSNER THORSTEN , HANSEN KARL , ARMSTRONG JOSEPH D III
IPC分类号： C07D243/08
CPC分类号： C07D243/08 , C07B2200/07 , C07C269/04 , C07C271/22
摘要： The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives which are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a prochiral beta amino acrylic acid derivative substrate in the presence of a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand with in situ protection of the primary amine product. The invention also relates to a novel process for the preparation of chiral beta-amino acid amides as inhibitors of the dipeptidyl peptidase-IV of structural formula III and the useful intermediates obtained therein. The products resulting from the instant process are inhibitors of dipeptidyl peptidase-IV and thereby useful for the treatment of Type 2 diabetes.
摘要翻译：本发明涉及有效制备对映异构体富集的β氨基酸衍生物的方法，其可用于不对称合成生物活性分子。该方法包括在与手性二茂铁基二膦配体络合的过渡金属前体存在下，原位保护伯胺产物，对前手性β氨基丙烯酸衍生物底物进行对映选择性氢化。本发明还涉及作为结构式III的二肽基肽酶-IV的抑制剂和其中获得的有用中间体的制备手性β-氨基酸酰胺的新方法。本方法产生的产物是二肽基肽酶-IV的抑制剂，因此可用于治疗2型糖尿病。

8. 发明申请

WO2005011581A3 HEXAHYDRODIAZEPINONES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 审中-公开
标题翻译：用于治疗或预防糖尿病的二氢芘二酮类抑制剂
公开(公告)号：WO2005011581A3
公开(公告)日：2005-04-28
申请号：PCT/US2004024052
申请日：2004-07-27
申请人： MERCK & CO INC , LIANG GUI-BAI , BIFTU TESFAYE , FENG DANQING DENNIS , WEBER ANN E
发明人： LIANG GUI-BAI , BIFTU TESFAYE , FENG DANQING DENNIS , WEBER ANN E
IPC分类号： A61K20060101 , A61K31/551 , A61P3/10 , C07D243/08 , C07D243/14 , C07D401/06 , C07D487/04
CPC分类号： C07D243/14 , C07D401/06 , C07D487/04
摘要： The present invention is directed to hexahydrodiazepinone compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DPP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及作为二肽基肽酶-IV酶抑制剂的六氢二氮杂酮化合物（“DPP-IV抑制剂”），其可用于治疗或预防其中涉及二肽基肽酶-IV酶的疾病，例如糖尿病，特别是2型糖尿病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗其中涉及二肽基肽酶-IV酶的疾病中的用途。

9. 发明申请

WO2004037169A3 BETA-AMINO HETEROCYCLIC DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 审中-公开
标题翻译：用于治疗或预防糖尿病的β-氨基间苯二酚胰蛋白酶抑制剂
公开(公告)号：WO2004037169A3
公开(公告)日：2004-08-05
申请号：PCT/US0332222
申请日：2003-10-14
申请人： MERCK & CO INC , BIFTU TESFAYE , LIANG GUI-BAI , QIAN XIAOXIA , WEBER ANN E , FENG DANQING DENNIS
发明人： BIFTU TESFAYE , LIANG GUI-BAI , QIAN XIAOXIA , WEBER ANN E , FENG DANQING DENNIS
IPC分类号： A61K20060101 , A61K31/55 , A61K31/551 , A61P3/10 , C07D243/08 , C07D307/94 , C07D401/06 , C07D403/06 , C07D405/12 , C07D405/14 , C07D491/107 , C07K5/06
CPC分类号： C07D243/08 , C07D401/06 , C07D403/06 , C07K5/06191
摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病特别是2型糖尿病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

10. 发明申请

WO2006127530A3 AMINOCYCLOHEXANES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 审中-公开
标题翻译：作为用于治疗或预防糖尿病的胰蛋白酶IV抑制剂的氨苄西林
公开(公告)号：WO2006127530A3
公开(公告)日：2009-04-23
申请号：PCT/US2006019598
申请日：2006-05-19
申请人： MERCK & CO INC , BIFTU TESFAYE , FENG DANQING , QIAN XIAOXIA , WEBER ANN E , COX JASON
发明人： BIFTU TESFAYE , FENG DANQING , QIAN XIAOXIA , WEBER ANN E , COX JASON
IPC分类号： A61K31/50 , A61K31/155 , A61K31/47
CPC分类号： C07D487/04
摘要： The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DPP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及作为二肽基肽酶-IV酶（“DPP-IV抑制剂”）的抑制剂的新型取代的氨基环己烷，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如作为糖尿病，特别是2型糖尿病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

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