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1. 发明申请

WO2003016294A1 PROCESS FOR PREPARING SULTAMS 审中-公开
标题翻译：制备烟草的方法
公开(公告)号：WO2003016294A1
公开(公告)日：2003-02-27
申请号：PCT/US2002/025666
申请日：2002-08-13
申请人： MERCK & CO., INC. , LEE, Jaemoon , ASKIN, David , JENSEN, Mark, S. , ZHONG, Yong-Li
发明人： LEE, Jaemoon , ASKIN, David , JENSEN, Mark, S. , ZHONG, Yong-Li
IPC分类号： C07D279/02
CPC分类号： C07D275/02 , C07D279/02 , C07D281/02
摘要： The preparation of sultams is disclosed. In one embodiment (e.g. scheme (I)), an alkanesulfonyl halide is reacted with a haloalkylamine to obtain the corresponding N-(haloalkyl)alkanesulfonamide which is then cyclized in the presence of a deprotonating agent to give the sultam. The sultams are useful as intermediates in the preparation of naphthyridine carboxamide compounds which are HIV integrase inhibitors.
摘要翻译：披露了苏丹的准备工作。在一个实施方案中（例如方案（I）），将链烷磺酰卤与卤代烷基胺反应，得到相应的N-（卤代烷基）烷磺酰胺，然后在脱质子剂的存在下环化，得到苏丹。苏氨酸钠可用作制备作为HIV整合酶抑制剂的萘啶甲酰胺化合物的中间体。

2. 发明申请

WO2005061501A2 PROCESS FOR PREPARING HEXAHYDROPYRIMIDO[1,2-A]AZEPINE-2-CARBOXYLATES AND RELATED COMPOUNDS 审中-公开
标题翻译：制备十六氢二咪唑[1,2-A]亚甲基-2-羧酸酯及相关化合物的方法
公开(公告)号：WO2005061501A2
公开(公告)日：2005-07-07
申请号：PCT/US2004/041115
申请日：2004-12-08
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , ASKIN, David , CONLON, David , LEE, Jaemoon , PIPIK, Brenda , ZHONG, Yong-Li , KOHMURA, Yoshinori
发明人： ASKIN, David , CONLON, David , LEE, Jaemoon , PIPIK, Brenda , ZHONG, Yong-Li , KOHMURA, Yoshinori
IPC分类号： C07D487/00
CPC分类号： C07F9/6561 , C07C251/60 , C07C255/26 , C07C259/14 , C07D239/557 , C07D487/04
摘要： Processes for preparing 10-amino-3-hydroxy-4-oxo-4,6,7,8,9,10-hexahydropyrimido[1,2-a]azepine-2-carboxylates and related compounds are disclosed. The preparation of carboxamide derivatives from these carboxylates is also disclosed. The carboxamides are HIV integrase inhibitors and are useful for treating HIV infection and AIDS.
摘要翻译：公开了制备10-氨基-3-羟基-4-氧代-4,6,7,8,9,10-六氢嘧啶并[1,2-a]吖庚因-2-羧酸酯和相关化合物的方法。还公开了从这些羧酸盐制备羧酰胺衍生物。甲酰胺是HIV整合酶抑制剂，可用于治疗艾滋病毒感染和艾滋病。

3. 发明申请

WO2004087650A3 PROCESS AND INTERMEDIATES FOR THE PREPARATION OF BETA-AMINO ACID AMIDE DIPEPTIDYL PEPTIDASE-IV INHIBITORS 审中-公开
公开(公告)号：WO2004087650A3
公开(公告)日：2004-10-14
申请号：PCT/US2004/008826
申请日：2004-03-23
申请人： MERCK & CO. INC. , ANGELAUD, Remy , ARMSTRONG, Joseph, D., III , ASKIN, David , BALSELLS, Jaume , HANSEN, Karl , LEE, Jaemoon , MALIGRES, Peter, E. , RIVERA, Nelo, R. , XIAO, Yi , ZHONG, Yong-Li
发明人： ANGELAUD, Remy , ARMSTRONG, Joseph, D., III , ASKIN, David , BALSELLS, Jaume , HANSEN, Karl , LEE, Jaemoon , MALIGRES, Peter, E. , RIVERA, Nelo, R. , XIAO, Yi , ZHONG, Yong-Li
IPC分类号： C07C229/00
摘要： A novel process is provided for the preparation of chiral beta-amino acid amide inhibitors of the dipeptidyl peptidase-IV 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.

4. 发明申请

WO2003016309A1 PROCESS FOR PREPARING 5-SULFONAMIDO-8-HYDROXY-1, 6-NAPHTHYRIDINE-7-CARBOXAMIDES 审中-公开
标题翻译：制备5-磺酰胺-8-羟基-1,6-萘啶-7-羧酸的方法
公开(公告)号：WO2003016309A1
公开(公告)日：2003-02-27
申请号：PCT/US2002/027151
申请日：2002-08-13
申请人： MERCK & CO., INC. , MALIGRES, Peter, E. , ASKIN, David
发明人： MALIGRES, Peter, E. , ASKIN, David
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , Y02P20/55
摘要： The preparation of 5-sulfonamido-8-hydroxy-1,6-naphthyridine-7-carboxamides is disclosed. A 5-halo-8-hydroxy-1,6-napthyridine-7-carboxylic acid or acid ester in which the hydroxy is derivatized with a protecting group is reacted with a sulfonamide (e.g., an alkanesulfonamide, N-alkyl alkanesulfonamide, or alkanesultam) in the presence of a copper promoter and a chelating agent, followed by deprotection of the hydroxy group, and then coupling with an amine to obtain the 5-sulfonamido-8-hydroxy-1,6-naphthyridine-7-carboxamide. Alternatively, the hydroxy-protected 5-halo-8-hydroxy-1,6-napthyridine-7-carboxylic acid (or ester) is first coupled with an amine, the resulting carboxamide reacted with a sulfonamide followed by deprotection of the hydroxy group to obtain the 5-sulfonamido-8-hydroxy-1,6-naphthyridine-7-carboxamide. The 5-sulfonamido-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and are useful for treating HIV infection, preventing HIV infection, delaying the onset of AIDS, and treating AIDS.
摘要翻译：公开了5-亚磺酰氨基-8-羟基-1,6-萘啶-7-甲酰胺的制备。将其中羟基用保护基团衍生化的5-卤代-8-羟基-1,6-萘并噻唑-7-羧酸或酸酯与磺酰胺（例如烷基磺酰胺，N-烷基烷烃磺酰胺或烷烃磺酰胺）反应）在铜促进剂和螯合剂的存在下反应，然后脱保护羟基，然后与胺偶联，得到5-亚磺酰氨基-8-羟基-1,6-萘啶-7-甲酰胺。或者，首先将羟基保护的5-卤代-8-羟基-1,6-萘并吡喃-7-羧酸（或酯）与胺偶联，得到的羧酰胺与磺酰胺反应，然后将羟基脱保护得到5-亚磺酰氨基-8-羟基-1,6-萘啶-7-甲酰胺。 5-亚磺酰氨基-8-羟基-1,6-萘啶-7-甲酰胺是HIV整合酶的抑制剂，可用于治疗HIV感染，预防艾滋病毒感染，延缓艾滋病的发病和治疗艾滋病。

5. 发明申请

WO2005087768A1 HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：艾滋病毒整合抑制剂
公开(公告)号：WO2005087768A1
公开(公告)日：2005-09-22
申请号：PCT/US2005/007772
申请日：2005-03-09
申请人： MERCK & CO., INC. , HAN, Wei , EGBERTSON, Melissa , WAI, John, S. , ZHUANG, Linghang , RUZEK, Rowena, D. , PERLOW, Debra, S. , ISAACS, Richard, C., A. , CAMERON, Mark , FOSTER, Bruce, S. , DOLLING, Ulf, H. , HOERRNER, R., Scott , OBLIGADO, Vanessa, E. , NEILSON, Lou, Anne , KIM, Boyoung , PAYNE, Linda, S. , MORRISETTE, Matthew, M. , WILLIAMS, Peter, D. , PYE, Philip, J. , ANGELAUD, Remy , MANCHENO, Danny, E. , ASKIN, David
发明人： HAN, Wei , EGBERTSON, Melissa , WAI, John, S. , ZHUANG, Linghang , RUZEK, Rowena, D. , PERLOW, Debra, S. , ISAACS, Richard, C., A. , CAMERON, Mark , FOSTER, Bruce, S. , DOLLING, Ulf, H. , HOERRNER, R., Scott , OBLIGADO, Vanessa, E. , NEILSON, Lou, Anne , KIM, Boyoung , PAYNE, Linda, S. , MORRISETTE, Matthew, M. , WILLIAMS, Peter, D. , PYE, Philip, J. , ANGELAUD, Remy , MANCHENO, Danny, E. , ASKIN, David
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein a, R¿1?, R¿2?, R¿3?, R¿4? and R¿5? are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：式I的羟基（四或六） - 氢化萘啶二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂：（I）其中a，R 1，R 2，R 3，R 4，和R？在本文中定义。这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。这些化合物被用作抗HIV感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

6. 发明申请

WO2004080402A2 POTASSIUM SALT OF AN HIV INTEGRASE INHIBITOR 审中-公开
标题翻译：艾滋病毒整合抑制剂的钾盐
公开(公告)号：WO2004080402A2
公开(公告)日：2004-09-23
申请号：PCT/US2004/006968
申请日：2004-03-08
申请人： MERCK & CO. INC. , PALUCKI, Michael , ASKIN, David , ANGELICO, Vincent, J. , WENSLOW, Robert, M., Jr.
发明人： PALUCKI, Michael , ASKIN, David , ANGELICO, Vincent, J. , WENSLOW, Robert, M., Jr.
IPC分类号： A61K
CPC分类号： C07D471/04
摘要： A potassium salt of Compound A is disclosed, wherein Compound A is of formula (I): Compound A is an HIV integrase inhibitor useful for preventing or treating HIV infection, for delaying the onset of AIDS, and for treating AIDS.
摘要翻译：公开了化合物A的钾盐，其中化合物A具有式（I）：化合物A是可用于预防或治疗HIV感染，延迟AIDS发作和用于治疗AIDS的HIV整合酶抑制剂。

7. 发明申请

WO1996028440A1 REDUCTIVE ALKYLATION PROCESS FOR THE PREPARATION N-(2-(R)-HYDROXY-1-(S)-INDANYL)-2(R)-PHENYLMETHYL-4(S)-HYDROXY-5-(1-(4-(3-PYRIDYLMETHYL)-2(S)-N'-(t-BUTYLCARBOXAMIDO)-PIPERAZINYL))-PENTANEAMIDE (=COMPOUND J OR L-735,524) 审中-公开
标题翻译：制备N-（2-（R） - 羟基-1-（S） - 茚满）-2（R） - 苯基甲基-4（S） - 羟基-5-（1-（4-（3 - 吡咯烷基）-2（S）-N' - （叔丁氧羰基） - 哌嗪基）） - 戊胺（=化合物J或L-735,524）
公开(公告)号：WO1996028440A1
公开(公告)日：1996-09-19
申请号：PCT/US1996002646
申请日：1996-03-11
申请人： MERCK & CO., INC.
发明人： MERCK & CO., INC. , ASKIN, David , CIANCIOSI, Steven, J. , HOERRNER, Robert, S.
IPC分类号： C07D401/06
CPC分类号： C07D401/06
摘要： A process of reductive amination efficiently yields an HIV protease inhibitor. The invention described herein concerns the final bond-forming step in the synthesis of the HIV protease inhibitor (J). In the invention, the penultimate intermediate (1) is converted to (J) via introduction of a 3-picolyl moiety in the form of 3-pyridinecarboxaldehyde (2) via a reductive alkylation. A process for synthesizing compound (J) of structure (3) comprising the steps of: (a) reacting for at least 5 minutes in suitable solvent one equivalent of the compound having structure (4) with excess 3-pyridine carboxaldehyde in the presence of excess reducing agent, at a temperature range of between about -78 DEG C and about 90 DEG C; (b) to give compound (J) or hydrate thereof.
摘要翻译：还原胺化的过程有效地产生了HIV蛋白酶抑制剂。本文描述的发明涉及HIV蛋白酶抑制剂（J）的合成中的最终的结合形成步骤。在本发明中，通过经由还原性烷基化引入3-吡啶甲醛（2）形式的3-吡啶甲基部分，将倒数第二中间体（1）转化为（J）。一种用于合成结构（3）的化合物（J）的方法，包括以下步骤：（a）在合适的溶剂中反应至少5分钟，其中一当量的具有结构（4）的化合物与过量的3-吡啶甲醛在存在下在约-78℃至约90℃的温度范围内的过量还原剂; （b）得到化合物（J）或其水合物。

8. 发明申请

WO1995021162A1 PROCESS FOR MAKING HIV PROTEASE INHIBITORS 审中-公开
标题翻译：制备HIV蛋白酶抑制剂的方法
公开(公告)号：WO1995021162A1
公开(公告)日：1995-08-10
申请号：PCT/US1995001232
申请日：1995-01-30
申请人： MERCK & CO., INC.
发明人： MERCK & CO., INC. , ROSSEN, Kai , ASKIN, David , REIDER, Paul , VARSOLONA, Richard, J. , VOLANTE, Ralph
IPC分类号： C07D241/04
CPC分类号： C07D401/06 , C07D241/04 , C07D491/04
摘要： A process for racemization of optically pure or enriched piperazine-2-tert-butylcarboxamide and its derivatives comprising reacting the optically pure or enriched piperazine compound with a racemizing agent selected from a strong base, an anhydrous metal salt or a carboxylic acid, in a solvent at a temperature range of between room temperature and 250 DEG C. The piperazine carboxamide derivatives are key intermediates in the preparation of HIV protease inhibitor compounds, including Compound J.
摘要翻译：光学纯的或富含的哌嗪-2-叔丁基甲酰胺及其衍生物的外消旋化方法，包括使光学纯的或富集的哌嗪化合物与选自强碱，无水金属盐或羧酸的外消旋剂在溶剂中反应在室温至250℃的温度范围内。哌嗪甲酰胺衍生物是制备HIV蛋白酶抑制剂化合物的关键中间体，包括化合物J.

9. 发明申请

WO1995002584A2 PROCESS FOR MAKING HIV PROTEASE INHIBITORS 审中-公开
标题翻译：制备HIV蛋白酶抑制剂的方法
公开(公告)号：WO1995002584A2
公开(公告)日：1995-01-26
申请号：PCT/US1994007706
申请日：1994-07-11
申请人： MERCK & CO., INC.
发明人： MERCK & CO., INC. , ASKIN, David , VOLANTE, Ralph, P. , ENG, Kan, K.
IPC分类号： C07D263/52
CPC分类号： C07D263/52 , C07D413/06
摘要： Intermediates of structural formula (IV) can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.
摘要翻译：结构式（IV）的中间体可以通过缩水甘油或其活化衍生物与酰胺反应来制备。该方法和中间体可用于合成HIV蛋白酶抑制剂化合物。

10. 发明申请

WO1996036629A1 PROCESS FOR MAKING HIV PROTEASE INHIBITORS 审中-公开
标题翻译：制备HIV蛋白酶抑制剂的方法
公开(公告)号：WO1996036629A1
公开(公告)日：1996-11-21
申请号：PCT/US1996006846
申请日：1996-05-14
申请人： MERCK & CO., INC.
发明人： MERCK & CO., INC. , ASKIN, David , SAGER, Jess, W. , ROSSEN, Kai , VOLANTE, Ralph, P. , REIDER, Paul, J.
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , C07D241/04 , C07D413/14
摘要： A process for making a clinically efficacious HIV protease inhibitor Compound J eliminates one step in its synthesis, by an improved, alternative synthesis of the 2(S)-4-picolyl-2-piperazine-t-butyl-carboxamide intermediate.
摘要翻译：制备临床有效的HIV蛋白酶抑制剂化合物J的方法通过改进的替代合成2（S）-4-吡啶甲基-2-哌嗪叔丁基甲酰胺中间体来消除其合成中的一个步骤。

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