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1. 发明申请

US20150183810A1 Synthesis of Racemic Amphetamine Derivatives by Cuprate Addition Reaction with Aziridine Phosphoramidate Compounds 有权
标题翻译：通过与氮丙啶氨基磷酸酯化合物的铜酸盐加成反应合成外消旋苯丙胺衍生物
公开(公告)号：US20150183810A1
公开(公告)日：2015-07-02
申请号：US14327209
申请日：2014-07-09
申请人： Chemapotheca LLC , Harold Meckler , Brian Thomas Gregg , Jie Yang
发明人： Harold Meckler , Brian Thomas Gregg , Jie Yang
IPC分类号： C07F9/22 , C07F9/564 , C07F9/02 , C07C209/62
CPC分类号： C07F9/564 , C07C209/62 , C07F9/2458 , C07F9/2475 , C07C211/27
摘要： The invention includes processes for the synthesis of amphetamine, dexamphetamine, methamphetamine, derivatives of these, including their salts, and novel precursors and intermediates obtained thereby, by synthesizing aziridine phosphoramidate compounds in specified solvents at specified temperatures, and then converting to a novel aryl or aryl-alkyl phosphoramidate precursors using an organometallic compound such as a copper salt, where the novel aryl or aryl-alkyl phosphoramidate precursor is then easily converted to the target compounds using known reactions.
摘要翻译：本发明包括合成苯丙胺，右旋苯丙胺，甲基苯丙胺，它们的衍生物，包括它们的盐的方法，以及由此获得的新型前体和中间体，通过在指定温度下合成特定溶剂中的氮丙啶氨基磷酸酯化合物，然后转化为新的芳基或使用有机金属化合物如铜盐的芳基 - 烷基氨基磷酸酯前体，其中新的芳基或芳基 - 烷基氨基磷酸酯前体然后使用已知的反应容易地转化成目标化合物。

2. 发明申请

US20150183716A1 Synthesis of Chiral Amphetamine Derivatives by Stereospecific, Regioselective Cuprate Addition Reaction with Aziridine Phosphoramidate Compounds 有权
标题翻译：通过与氮丙啶氨基磷酸酯化合物的立体特异性，区域选择性铜酸盐加成反应合成手性苯酚衍生物
公开(公告)号：US20150183716A1
公开(公告)日：2015-07-02
申请号：US14189630
申请日：2014-02-25
申请人： Je Yang , Harold Meckler , Brian Thomas Gregg , Chemapotheca, LLC
发明人： Harold Meckler , Brian Thomas Gregg , Jie Yang
IPC分类号： C07C209/68 , C07F9/564
CPC分类号： C07F9/564 , C07B2200/07 , C07C209/62 , C07F9/2458 , C07F9/2475 , C07C211/27
摘要： The invention includes processes for the synthesis of amphetamine, dexamphetamine, methamphetamine, derivatives of these, including their salts, and novel precursors and intermediates obtained thereby, by synthesizing aziridine phosphoramidate compounds in specified solvents at specified temperatures, and then converting to a novel aryl or aryl-alkyl phosphoramidate precursors using an organometallic compound such as a copper salt, where the novel aryl or aryl-alkyl phosphoramidate precursor is then easily converted to the target compounds using known reactions,
摘要翻译：本发明包括合成苯丙胺，右旋苯丙胺，甲基苯丙胺，它们的衍生物，包括它们的盐的方法，以及由此获得的新型前体和中间体，通过在指定温度下合成特定溶剂中的氮丙啶氨基磷酸酯化合物，然后转化为新的芳基或使用有机金属化合物例如铜盐的芳基 - 烷基氨基磷酸酯前体，其中新的芳基或芳基 - 烷基氨基磷酸酯前体然后使用已知的反应容易地转化为目标化合物，

3. 发明授权

US08334266B2 Process for and intermediates in the preparation of canfosfamide and its salts 有权
标题翻译：用于制备卡非司酮及其盐的方法和中间体
公开(公告)号：US08334266B2
公开(公告)日：2012-12-18
申请号：US13429065
申请日：2012-03-23
申请人： William A. Boulanger , Steven J. Collier , Stephen A. Eastham , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernandez Abad , R. Jason Herr , Hans J. Kjaersgaard , Harold Meckler , Robert E. Polomski , Steven R. Schow , Pavel E. Zhichkin
发明人： William A. Boulanger , Steven J. Collier , Stephen A. Eastham , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernandez Abad , R. Jason Herr , Hans J. Kjaersgaard , Harold Meckler , Robert E. Polomski , Steven R. Schow , Pavel E. Zhichkin
IPC分类号： A61K38/07 , C07K38/06
CPC分类号： C07K5/0205 , A61K38/00 , C07F9/2408 , C07F9/2458 , C07K5/0215 , C07K5/0606 , C07K5/06191
摘要： A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity.
摘要翻译：一种在制备头孢噻吩及其盐的过程和中间体。一些中间体具有抗癌活性。

4. 发明申请

US20120238772A1 PROCESS FOR AND INTERMEDIATES IN THE PREPARATION OF CANFOSFAMIDE AND ITS SALTS 有权
标题翻译：在制备氰氟虫及其盐的过程和中间体
公开(公告)号：US20120238772A1
公开(公告)日：2012-09-20
申请号：US13429065
申请日：2012-03-23
申请人： William A. Boulanger , Steven J. Collier , Stephen A. Eastham , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernández Abad , R. Jason Herr , Hans J. Kjaersgaard , Harold Meckler , Robert E. Polomski , Steven R. Schow , Pavel E. Zhichkin
发明人： William A. Boulanger , Steven J. Collier , Stephen A. Eastham , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernández Abad , R. Jason Herr , Hans J. Kjaersgaard , Harold Meckler , Robert E. Polomski , Steven R. Schow , Pavel E. Zhichkin
IPC分类号： C07F9/24 , C07C323/59
CPC分类号： C07K5/0205 , A61K38/00 , C07F9/2408 , C07F9/2458 , C07K5/0215 , C07K5/0606 , C07K5/06191
摘要： A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity.
摘要翻译：一种在制备头孢噻吩及其盐的过程和中间体。一些中间体具有抗癌活性。

5. 发明授权

US08067605B2 Process for production of piperidine derivatives 有权
公开(公告)号：US08067605B2
公开(公告)日：2011-11-29
申请号：US12956601
申请日：2010-11-30
申请人： Harold Meckler , Benjamin J. Littler , Prasad Raje , Michael Van Brundt , Paul Vogt
发明人： Harold Meckler , Benjamin J. Littler , Prasad Raje , Michael Van Brundt , Paul Vogt
IPC分类号： C07D211/22
CPC分类号： C07D211/14 , C07D211/22
摘要： Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III: The processes involve reacting a compound of formula Ia, IIa or IIIa with isobutyrate or an isobutyrate equivalent.

6. 发明授权

US07498345B2 Process for production of piperidine derivatives 失效
标题翻译：哌啶衍生物的制备方法
公开(公告)号：US07498345B2
公开(公告)日：2009-03-03
申请号：US10943276
申请日：2004-09-17
申请人： Harold Meckler , Benjamin J. Littler , Prasad Raje , Michael Van Brunt , Paul F. Vogt
发明人： Harold Meckler , Benjamin J. Littler , Prasad Raje , Michael Van Brunt , Paul F. Vogt
IPC分类号： A61K31/445
CPC分类号： C07D211/14 , C07D211/22
摘要： Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III: The processes involve reacting a compound of formula Ia, IIa or IIIa with isobutyrate or an isobutyrate equivalent.
摘要翻译：公开了制备式I，II或III的哌啶衍生物化合物的方法：该方法包括使式Ia，IIa或IIIa的化合物与异丁酸酯或异丁酸酯当量反应。

7. 发明申请

US20060135409A1 Process for and intermediates in the preparation of canfosfamide and its salts 失效
标题翻译：用于制备卡非司酮及其盐的方法和中间体
公开(公告)号：US20060135409A1
公开(公告)日：2006-06-22
申请号：US11018391
申请日：2004-12-21
申请人： William Boulanger , Steven Collier , Stephen Eastham , Dennis Edie , Ronan Guevel , Pedro Abad , R. Herr , Hans Kjaersgaard , Harold Meckler , Robert Polomski , Steven Schow , Pavel Zhichkin
发明人： William Boulanger , Steven Collier , Stephen Eastham , Dennis Edie , Ronan Guevel , Pedro Abad , R. Herr , Hans Kjaersgaard , Harold Meckler , Robert Polomski , Steven Schow , Pavel Zhichkin
IPC分类号： A61K38/05 , C07K5/06
CPC分类号： C07K5/0205 , A61K38/00 , C07F9/2408 , C07F9/2458 , C07K5/0215 , C07K5/0606 , C07K5/06191
摘要： A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity.
摘要翻译：一种在制备头孢噻吩及其盐的过程和中间体。一些中间体具有抗癌活性。

8. 发明申请

US20060047171A1 Catalytic hydrogenation of nitriles to produce capsaicinoid derivatives and amine compounds, and methods for purifying and obtaining the polymorphs thereof 审中-公开
标题翻译：腈类催化氢化制备辣椒素衍生物和胺化合物，以及纯化和获得其多晶型物的方法
公开(公告)号：US20060047171A1
公开(公告)日：2006-03-02
申请号：US10927493
申请日：2004-08-27
申请人： Harold Meckler , Karl Popp , Bingidimi Mobele , Paul Isbester , Bruce Elder , Paul Vogt , Benjamin Littler , Stephen Eastham , David Reed , Luckner Ulysse , Michael Uttley
发明人： Harold Meckler , Karl Popp , Bingidimi Mobele , Paul Isbester , Bruce Elder , Paul Vogt , Benjamin Littler , Stephen Eastham , David Reed , Luckner Ulysse , Michael Uttley
IPC分类号： A61K31/16 , C07C233/24
CPC分类号： C07C235/34 , C07C231/12
摘要： Processes for preparing an amine compound by catalytically hydrogenating a precursor nitrile compound. In a particular aspect, the present hydrogenation process occurs in a dipolar organic solvent in the presence of a palladium/carbon catalyst and a strong anhydrous protic acid. In a further aspect, the preferred embodiment relates to a process for deprotecting a compound to produce an amine compound. In yet a further aspect, the preferred embodiment relates to amine products produced by the present processes. These amine products may be used for a variety of purposes.
摘要翻译：通过催化氢化前体腈化合物制备胺化合物的方法。在一个特定方面，本发明的氢化方法在钯/碳催化剂和强无水质子酸的存在下在偶极有机溶剂中进行。在另一方面，优选的实施方案涉及使化合物脱保护以制备胺化合物的方法。在另一方面，优选实施方案涉及通过本方法制备的胺产物。这些胺产物可用于各种目的。

9. 发明申请

US20060063933A1 Process for production of carebastine 失效
公开(公告)号：US20060063933A1
公开(公告)日：2006-03-23
申请号：US10944309
申请日：2004-09-17
申请人： Harold Meckler , Benjamin Littler , Prasad Raje , Michael Van Brunt , Paul Vogt
发明人： Harold Meckler , Benjamin Littler , Prasad Raje , Michael Van Brunt , Paul Vogt
IPC分类号： C07D211/52 , A61K31/445 , C07D211/54
CPC分类号： C07D211/46
摘要： Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III:

10. 发明授权

US5096919A Pyrrolylphenyl-substituted hydroxamic acid derivatives 失效
标题翻译：吡咯基苯基取代的异羟肟酸衍生物
公开(公告)号：US5096919A
公开(公告)日：1992-03-17
申请号：US439731
申请日：1989-11-20
申请人： Jan W. F. Wasley , Karl O. Gelotte , Harold Meckler
发明人： Jan W. F. Wasley , Karl O. Gelotte , Harold Meckler
IPC分类号： C07D207/32 , C07D207/325 , C07D207/327
CPC分类号： C07D207/325 , C07D207/327
摘要： Disclosed are the pyrrolylphenyl-substituted hydroxamic acid derivatives of the formula ##STR1## wherein R represents hydrogen, lower alkyl, halogen or lower alkoxy; R.sub.1 and R.sub.2 independently represent hydrogen, lower alkyl or aryl; Y represents a direct bond, lower alkylene, lower alkenylene, lower alkadienylene, (thio, sulfinyl or sulfonyl)-lower alkylene or oxy-lower alkylene; Z represents ##STR2## wherein R.sub.3 represents hydrogen or acyl; R.sub.4 represents lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, aryl or aryl-lower alkyl; or Z represents ##STR3## wherein R.sub.3 represents hydrogen or acyl; R.sub.5 represents lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, aryl, aryl-lower alkyl, amino or N-(mono- or di-lower alkyl)-amino; R.sub.6 and R.sub.7 represent hydrogen or lower alkyl; and pharmaceutically acceptable salts thereof provided that R.sub.3 represents hydrogen; which are useful as selective lipoxygenase inhibitors, methods for preparation thereof, pharmaceutical compositions comprising said compounds, and a method of inhibiting lipoxygenase and of treating diseases in mammals which are responsive to lipoxygenase inhibition using said compounds and pharmaceutical compositions comprising said compounds of the invention.
摘要翻译：公开了式（I）的吡咯基苯基取代的异羟肟酸衍生物，其中R表示氢，低级烷基，卤素或低级烷氧基; R1和R2独立地表示氢，低级烷基或芳基; Y表示直接键，低级亚烷基，低级亚烯基，低级亚烷基亚芳基，（硫代，亚磺酰基或磺酰基） - 低级亚烷基或氧 - 低级亚烷基; Z代表（a）其中R3代表氢或酰基; R 4表示低级烷基，C 3 -C 7 - 环烷基，芳基或芳基 - 低级烷基; 或Z表示（b）其中R3表示氢或酰基; R 5表示低级烷基，C 3 -C 7 - 环烷基，芳基，芳基 - 低级烷基，氨基或N-（单 - 或二 - 低级烷基） - 氨基; R6和R7代表氢或低级烷基; 其药学上可接受的盐，其中R3表示氢; 其可用作选择性脂氧合酶抑制剂，其制备方法，包含所述化合物的药物组合物，以及抑制脂氧合酶的方法，以及使用所述化合物和包含本发明化合物的药物组合物治疗对脂氧合酶抑制作用有抑制作用的哺乳动物疾病的方法。

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