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1. 发明授权

US08592631B2 Process for the preparation of 2-methoxymethy1-1,4-benzenediamine, its derivatives thereof and the salts thereof 有权
标题翻译： 2-甲氧基甲基-1,4-苯二胺及其衍生物及其盐的制备方法
公开(公告)号：US08592631B2
公开(公告)日：2013-11-26
申请号：US13016272
申请日：2011-01-28
申请人： John Michael Gardlik , Garry Steven Garrett , Bryan Patrick Murphy , John Michael Janusz , John August Wos
发明人： John Michael Gardlik , Garry Steven Garrett , Bryan Patrick Murphy , John Michael Janusz , John August Wos
IPC分类号： C07C209/00
CPC分类号： C07C213/02 , C07C217/76
摘要： A process for synthesizing 2-methoxymethyl-1,4-benzenediamine, its derivatives of formula (IV) and the salts thereof, which comprises a reductive amination step. The preferred final product is 2-methoxymethyl-1,4-benzenediamine of formula (IV-a). These compounds may be used as primary intermediates in compositions for dyeing keratin fibers.
摘要翻译：一种合成2-甲氧基甲基-1,4-苯二胺的方法，其式（Ⅳ）的衍生物及其盐，其包括还原胺化步骤。优选的最终产物是式（IV-a）的2-甲氧基甲基-1,4-苯二胺。这些化合物可用作用于染色角蛋白纤维的组合物中的主要中间体。

2. 发明申请

US20120142969A1 Process for the Preparation of 2-Methoxymethyl-1,4-Benzenediamine, Its Derivatives Thereof and the Salts Thereof 有权
标题翻译： 2-甲氧基甲基-1,4-苯二胺及其衍生物及其盐的制备方法
公开(公告)号：US20120142969A1
公开(公告)日：2012-06-07
申请号：US13016272
申请日：2011-01-28
申请人： John Michael GARDLIK , Garry Steven Garrett , Bryan Patrick Murphy , John Michael Janusz , John August Wos
发明人： John Michael GARDLIK , Garry Steven Garrett , Bryan Patrick Murphy , John Michael Janusz , John August Wos
IPC分类号： C07C213/02
CPC分类号： C07C213/02 , C07C217/76
摘要： A process for synthesizing 2-methoxymethyl-1,4-benzenediamine, its derivatives of formula (IV) and the salts thereof, which comprises a reductive amination step. The preferred final product is 2-methoxymethyl-1,4-benzenediamine of formula (IV-a). These compounds may be used as primary intermediates in compositions for dyeing keratin fibers.
摘要翻译：一种合成2-甲氧基甲基-1,4-苯二胺的方法，其式（Ⅳ）的衍生物及其盐，其包括还原胺化步骤。优选的最终产物是式（IV-a）的2-甲氧基甲基-1,4-苯二胺。这些化合物可用作用于染色角蛋白纤维的组合物中的主要中间体。

3. 发明授权

US07803827B2 Kv1.5 potassium channel inhibitors 失效
标题翻译： Kv1.5钾通道抑制剂
公开(公告)号：US07803827B2
公开(公告)日：2010-09-28
申请号：US12266212
申请日：2008-11-06
申请人： John Michael Janusz , Stephen Joseph Hodson , Gregory Kent Bosch , Ronald Eugene White , Benjamin E. Blass , Christopher M. Jackson , Neil T. Fairweather
发明人： John Michael Janusz , Stephen Joseph Hodson , Gregory Kent Bosch , Ronald Eugene White , Benjamin E. Blass , Christopher M. Jackson , Neil T. Fairweather
IPC分类号： A61K31/4166 , C07D233/32
CPC分类号： C07D233/38
摘要： The present invention relates to 1-N-amino-2-imidazolidinones and derivatives thereof which are effective as Kv1.5 potassium channel inhibitors providing atrial-selective antiarrhythmic agents. The present invention further relates to compositions comprising said Kv1.5 potassium channel inhibitors, and to methods for treating cardiac arrhythmia.
摘要翻译：本发明涉及作为提供心房选择性抗心律失常药物的Kv1.5钾通道抑制剂有效的1-N-氨基-2-咪唑啉酮及其衍生物。本发明还涉及包含所述Kv1.5钾通道抑制剂的组合物，以及用于治疗心律失常的方法。

4. 发明授权

US6107311A Dihydrobenzofuran and related compounds useful as anti-inflammatory agents 失效
标题翻译：二氢苯并呋喃及相关化合物可用作抗炎剂
公开(公告)号：US6107311A
公开(公告)日：2000-08-22
申请号：US57685
申请日：1998-04-09
申请人： Laurence Ichih Wu , John Michael Janusz
发明人： Laurence Ichih Wu , John Michael Janusz
IPC分类号： A61K31/34 , A61K31/343 , A61K31/381 , A61K31/443 , A61K31/4433 , A61P19/02 , A61P29/00 , A61P43/00 , C07D307/79 , C07D405/06 , C07D407/06 , C07D409/06 , C07D417/06 , A61K31/44 , C07D401/06
CPC分类号： C07D307/79 , C07D405/06 , C07D409/06 , C07D417/06
摘要： A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is O or S; and(f) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.
摘要翻译：具有以下结构的化合物：其中（a）n为1至约3; （b）X选自O，S，SO或SO 2; （c）Y独立地为氢或具有1至约4个碳原子的直链，支链或环状烷基，或Y结合在一起形成约3至约7个原子的烷基环; （d）Z是氢或具有除氢以外的3至约10个原子的直链，支链或环状烷基; （e）W为O或S; 和（f）Het是包含一个或多个环的杂环基，每个环含有除氢以外的约5至约6个原子，并且其中所述基团含有至少一个选自O，N或S的杂原子。包含这样的化合物以及使用这些化合物治疗炎症或疼痛的方法。

5. 发明授权

US5972957A Dihydrobenzopyran compounds and related compounds useful as anti-inflammatory agents 失效
标题翻译：二氢苯并吡喃化合物和有用的化合物可用作抗炎剂
公开(公告)号：US5972957A
公开(公告)日：1999-10-26
申请号：US58405
申请日：1998-04-09
申请人： Laurence Ichih Wu , John Michael Janusz
发明人： Laurence Ichih Wu , John Michael Janusz
IPC分类号： C07D333/54 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/382 , A61K31/415 , A61K31/425 , A61K31/427 , A61K31/44 , A61P29/00 , A61P43/00 , C07D307/79 , C07D335/06 , C07D337/08 , C07D409/04 , C07D417/04 , C07D471/04 , C07D513/04 , A61K31/35 , C07D407/04
CPC分类号： C07D307/79 , C07D409/04 , C07D417/04 , C07D471/04 , C07D513/04
摘要： A compound having the structure: ##STR1## wherein (a) n is from about 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen; and(e) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.Pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pair using such compounds.
摘要翻译：具有以下结构的化合物：其中（a）n为约1至约3; （b）X选自O，S，SO或SO 2; （c）Y独立地为氢或具有1至约4个碳原子的直链，支链或环状烷基，或Y结合在一起形成约3至约7个原子的烷基环; （d）Z是氢或具有除氢以外的3至约10个原子的直链，支链或环状烷基; 和（e）Het是包含一个或多个环的杂环基，每个环含有除氢以外的约5至约6个原子，并且其中所述基团含有至少一个选自O，N或S的杂原子。包含这些化合物以及使用这些化合物治疗炎症或配对的方法。

6. 发明授权

US5684031A Dihydrobenzofuran and related compounds useful as anti-inflammatory agents 失效
标题翻译：二氢苯并呋喃及相关化合物可用作抗炎剂
公开(公告)号：US5684031A
公开(公告)日：1997-11-04
申请号：US595122
申请日：1996-02-01
申请人： John Michael Janusz , James Madison Ridgeway, II
发明人： John Michael Janusz , James Madison Ridgeway, II
IPC分类号： A61K31/343 , A61K31/39 , A61K31/4178 , A61P19/02 , A61P25/04 , A61P29/00 , C07D307/79 , C07D405/12 , C07D409/12 , A61K31/34
CPC分类号： C07D307/79 , C07D405/12
摘要： A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3; (b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ; (c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms; (d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen; (e) R.sub.1 is hydrogen or straight, branched or cyclic alkyl, aryl or C(.dbd.NH)--NHR.sub.4 ; and (f) R.sub.2, R.sub.3, and R.sub.4, are independently hydrogen, straight, branched or cyclic alkyl having from one to 10 carbon atoms, or aryl; R.sub.2 and R.sub.3 can be bonded together to form a ring having 5 or 6 atoms. pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.
摘要翻译：具有以下结构的化合物：其中（a）n为1至约3; （b）X选自O，S，SO或SO 2; （c）Y独立地为氢或具有1至约4个碳原子的直链，支链或环状烷基，或Y结合在一起形成约3至约7个原子的烷基环; （d）Z是氢或具有除氢以外的3至约10个原子的直链，支链或环状烷基; （e）R 1是氢或直链，支链或环状的烷基，芳基或C（= NH）-NHR 4; 和（f）R 2，R 3和R 4独立地是氢，具有1至10个碳原子的直链，支链或环状烷基或芳基; R2和R3可以结合在一起形成具有5或6个原子的环。包含这些化合物的药物组合物，以及使用这些化合物治疗炎症或疼痛的方法。

7. 发明授权

US5684002A Dihydorbenzofuran and related compounds useful as anti-inflammatory agents 失效
标题翻译：二氢苯并呋喃和相关化合物可用作抗炎剂
公开(公告)号：US5684002A
公开(公告)日：1997-11-04
申请号：US486876
申请日：1995-06-07
申请人： Michael Wiard Scherz , John Michael Janusz
发明人： Michael Wiard Scherz , John Michael Janusz
IPC分类号： C07D333/52 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61P25/04 , A61P29/00 , C07D307/79 , C07D333/54
CPC分类号： C07D307/79 , C07D333/54
摘要： A compound having the structure: ##STR1## wherein (a) W is --C(X')--NRR' or --NR--C(X')R'; (b) X and X' are independently O or S; (c) each Y is independently hydrogen or straight, branched or cyclic alkanyl having from 1 to about 3 carbon atoms, or the two Y's are bonded to form an alkanyl ring having from 3 to about 7 carbon atoms; (d) Z is unsubstituted branched or cyclic alkyl, or unsubstituted or alkanyl-substituted phenyl or benzyl, Z having from 3 to about 10 atoms other than hydrogen; (e) R and R' are each independently selected from hydrogen, hydroxy straight, branched or substituted alkyl having from 1 to about 6 carbon atoms, and cyclic alkyl having from 3 to about 7 carbon atoms; unsubstituted or substituted aryl, heteroaryl or heterocyclic groups; or R and R' are bonded together to form a ring having from from 3 to about 8 atoms wherein about 1 to about 4 atoms may be heteroatoms; pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.
摘要翻译：具有以下结构的化合物：其中（a）W是-C（X'）-NRR'或-NR-C（X'）R'; （b）X和X'独立地为O或S; （c）每个Y独立地为氢或具有1至约3个碳原子的直链，支链或环状烷基，或两个Y键合以形成具有3至约7个碳原子的烷基环; （d）Z是未取代的支链或环状烷基，或未取代的或烷基取代的苯基或苄基，Z具有除氢以外的3至约10个原子; （e）R和R'各自独立地选自氢，具有1至约6个碳原子的羟基直链，支链或取代的烷基和具有3至约7个碳原子的环状烷基; 未取代或取代的芳基，杂芳基或杂环基团; 或R和R'键合在一起形成具有3至约8个原子的环，其中约1至约4个原子可以是杂原子; 包含这些化合物的药物组合物，以及使用这些化合物治疗炎症或疼痛的方法。

8. 发明授权

US09145366B2 Process for preparing [(3-hydroxypyridine-2-carbonyl)amino]alkanoic acids, esters and amides 有权
标题翻译：制备[（3-羟基吡啶-2-羰基）氨基]链烷酸，酯和酰胺的方法
公开(公告)号：US09145366B2
公开(公告)日：2015-09-29
申请号：US13488554
申请日：2012-06-05
申请人： Christopher M. Lanthier , Boris Gorin , Jan Oudenes , Craig Edward Dixon , Alan Qingbo Lu , James Densmore Copp , John Michael Janusz
发明人： Christopher M. Lanthier , Boris Gorin , Jan Oudenes , Craig Edward Dixon , Alan Qingbo Lu , James Densmore Copp , John Michael Janusz
IPC分类号： C07D211/72 , C07D211/84 , C07D213/62 , C07D213/78 , C07D213/79 , C07D213/81 , C07D213/803
CPC分类号： C07D213/81 , C07D213/79 , C07D213/803
摘要： Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.
摘要翻译：公开了制备[（3-羟基吡啶-2-羰基）氨基] - 链烷酸，衍生物，特别是5-芳基取代和5-杂芳基取代的[（3-羟基吡啶-2-羰基）氨基}乙酸的方法。还公开了制备[（3-羟基吡啶-2-羰基） - 氨基]乙酸的前药的方法，例如[（3-羟基吡啶-2-羰基）氨基}乙酸酯和{[3-羟基吡啶-2 - 羰基]氨基}乙酸酰胺。所公开的化合物可用作脯氨酰羟化酶抑制剂或用于治疗需要脯氨酰羟化酶抑制的条件。

9. 发明申请

US20120309977A1 PROCESS FOR PREPARING [(3-HYDROXYPYRIDINE-2-CARBONYL)AMINO]ALKANOIC ACIDS, ESTERS AND AMIDES 有权
标题翻译：制备[（3-羟基吡啶-2-羰基）氨基]亚烷基酸，酯和胺的方法
公开(公告)号：US20120309977A1
公开(公告)日：2012-12-06
申请号：US13488554
申请日：2012-06-05
申请人： Christopher M. Lanthier , Boris Gorin , Jan Oudenes , Craig Edward Dixon , Alan Quigbo Lu , James Densmore Copp , John Michael Janusz
发明人： Christopher M. Lanthier , Boris Gorin , Jan Oudenes , Craig Edward Dixon , Alan Quigbo Lu , James Densmore Copp , John Michael Janusz
IPC分类号： C07D213/81 , C07D405/10 , C07D213/79
CPC分类号： C07D213/81 , C07D213/79 , C07D213/803
摘要： Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]aminolacetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.
摘要翻译：公开了制备[（3-羟基吡啶-2-羰基）氨基] - 链烷酸，衍生物，特别是5-芳基取代的和5-杂芳基取代的[（3-羟基吡啶-2-羰基）氨基乙酸）的方法。是制备[（3-羟基吡啶-2-羰基） - 氨基]乙酸的前药的方法，例如[（3-羟基吡啶-2-羰基）氨基}乙酸酯和{[3-羟基吡啶-2-羰基 ]氨基}乙酸酰胺，所公开的化合物可用作脯氨酰羟化酶抑制剂或用于治疗需要脯氨酰羟化酶抑制的条件。

10. 发明授权

US07504517B2 Kv1.5 potassium channel inhibitors 失效
标题翻译： Kv1.5钾通道抑制剂
公开(公告)号：US07504517B2
公开(公告)日：2009-03-17
申请号：US11765359
申请日：2007-06-19
申请人： John Michael Janusz , Stephen Joseph Hodson , Gregory Kent Bosch , Ronald Eugene White , Benjamin E. Blass , Christopher M. Jackson , Neil T. Fairweather
发明人： John Michael Janusz , Stephen Joseph Hodson , Gregory Kent Bosch , Ronald Eugene White , Benjamin E. Blass , Christopher M. Jackson , Neil T. Fairweather
IPC分类号： C07D233/38 , A61K31/4166
CPC分类号： C07D233/38
摘要： The present invention relates to 1-N-amino-2-imidazolidinones and derivatives thereof which are effective as Kv1.5 potassium channel inhibitors providing atrial-selective antiarrhythmic agents. The present invention further relates to compositions comprising said Kv1.5 potassium channel inhibitors, and to methods for treating cardiac arrhythmia.
摘要翻译：本发明涉及作为提供心房选择性抗心律失常药物的Kv1.5钾通道抑制剂有效的1-N-氨基-2-咪唑啉酮及其衍生物。本发明还涉及包含所述Kv1.5钾通道抑制剂的组合物，以及用于治疗心律失常的方法。

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