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公开(公告)号:US20100197907A1
公开(公告)日:2010-08-05
申请号:US12798501
申请日:2010-04-06
Applicant: David L. Berstein , Leonard W. Rozamus , Yihan Wang , Chester A. Metcalf, III
Inventor: David L. Berstein , Leonard W. Rozamus , Yihan Wang , Chester A. Metcalf, III
IPC: C07D267/00
CPC classification number: A61K45/06 , A61K31/675 , C07F9/6561
Abstract: This invention concerns a new family of phosphorus-containing compounds containing a moiety JQA- in which:A is absent or is —O—, —S— or —NR2—; Q is absent or (if A is —O—, —S— or —NR2—) Q may be —V—, —OV—, —SV—, or —NR2V—, where V is an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, such that J is linked to the cyclohexyl ring directly, through A or through VA, OVA, SVA or NR2VA; K is O or S; each occurrence of Y is independently —O—, —S—, —NR2—, or a bond linking a R5 moiety to P; each occurrence of R2 and R5 is independently an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, or H; and each occurrence of R6 is independently —PK(YR5)(YR5), —SO2(YR5) or —C(O)(YR5); so long as any R2, or R5 moiety linked directly to P is not H; wherein two R2, R5 and/or R6 moieties may be chemically linked to one another to form a ring; each occurrence of G is independently —O—, —S—, —NR2— or (M)x; each occurrence of M is independently a substituted or unsubstituted methylene moiety, and any M-M′ moiety may be saturated or unsaturated; each occurrence of x is independently an integer from 1-6; and the other variables are as defined herein.
Abstract translation: 本发明涉及一种含有部分JQA-的含磷化合物的新家族,其中:A不存在或为-O - , - S-或-NR2-; Q不存在或(如果A是-O-,-S-或-NR2-)Q可以是-V-,-OV-,-SV-或-NR2V-,其中V是脂族,杂脂族,芳基, 或杂芳基部分,使得J通过A或通过VA,OVA,SVA或NR2VA直接与环己基环连接; K为O或S; 每个出现的Y独立地是-O - , - S - , - NR2-或连接R 5部分与P的键; R 2和R 5各自独立地为脂族,杂脂族,芳基或杂芳基部分,或H; 并且每个出现的R 6独立地是-PK(YR 5)(YR 5),-SO 2(YR 5)或-C(O)(YR 5); 只要直接与P连接的任何R 2或R 5部分不是H; 其中两个R2,R5和/或R6部分可以彼此化学连接以形成环; 每次出现的G独立为-O - , - S - , - NR2-或(M)x; 每次出现的M独立地是取代或未取代的亚甲基部分,任何M-M'部分可以是饱和或不饱和的; 每次出现的x独立为1-6的整数; 其他变量如本文所定义。
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公开(公告)号:US20090149471A1
公开(公告)日:2009-06-11
申请号:US12227130
申请日:2007-05-08
Applicant: William C. Shakespeare , Wei-Sheng Huang , David C. Dalgarno , Xiaotian Zhu , R. Matthew Thomas , Yihan Wang , Jiwei Qi , Rajeswari Sundaramoorthi , Dong Zou , Chester A. Metcalf, III , Tomi k. Sawyer , Jan Antoinette C. Romero
Inventor: William C. Shakespeare , Wei-Sheng Huang , David C. Dalgarno , Xiaotian Zhu , R. Matthew Thomas , Yihan Wang , Jiwei Qi , Rajeswari Sundaramoorthi , Dong Zou , Chester A. Metcalf, III , Tomi k. Sawyer , Jan Antoinette C. Romero
IPC: A61K31/4178 , C07D403/12 , C07D417/12 , A61K31/427 , A61K31/4439 , A61K31/506 , A61P35/00 , A61K31/496
CPC classification number: C07D231/12 , C07D233/64 , C07D233/90 , C07D277/40 , C07D403/12 , C07D403/14 , C07D417/12 , C07D417/14
Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
Abstract translation: 本发明涉及以下通式的化合物:其中可变基团如本文所定义,以及其制备和用途。
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公开(公告)号:US07432277B2
公开(公告)日:2008-10-07
申请号:US11429582
申请日:2006-05-05
Applicant: Chester A. Metcalf, III , Leonard W. Rozamus , Yihan Wang , R. Mathew Thomas , Dong Zou , David L. Berstein
Inventor: Chester A. Metcalf, III , Leonard W. Rozamus , Yihan Wang , R. Mathew Thomas , Dong Zou , David L. Berstein
IPC: C07D491/06 , A61K31/395
CPC classification number: C07F9/6561 , A61K31/407 , A61K31/4745 , A61K31/675 , C07F9/6527
Abstract: This invention concerns a new family of phosphorus-containing macrocycles containing various phosphonate- and phosphonate-containing moieties.
Abstract translation: 本发明涉及含有各种含膦酸盐和膦酸盐的部分的含磷大环的新家族。
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公开(公告)号:US20070191376A1
公开(公告)日:2007-08-16
申请号:US11644849
申请日:2006-12-22
Applicant: Dong Zou , Wei-Sheng Huang , R. Thomas , Jan Romero , Jiwei Qi , Yihan Wang , Xiaotian Zhu , William Shakespeare , Rajeswari Sundaramoorthi , Chester Metcalf, , David Dalgarno , Tomi Sawyer
Inventor: Dong Zou , Wei-Sheng Huang , R. Thomas , Jan Romero , Jiwei Qi , Yihan Wang , Xiaotian Zhu , William Shakespeare , Rajeswari Sundaramoorthi , Chester Metcalf, , David Dalgarno , Tomi Sawyer
IPC: A61K31/53 , A61K31/519 , A61K31/496 , A61K31/503 , A61K31/498 , A61K31/4745 , C07D487/04
CPC classification number: C07D471/04 , C07D473/34 , C07D487/04
Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
Abstract translation: 本发明涉及以下通式的化合物:其中可变基团如本文所定义,及其制备和用途。
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公开(公告)号:US20070190106A1
公开(公告)日:2007-08-16
申请号:US11650017
申请日:2007-01-05
Applicant: David Berstein , Leonard Rozamus , Yihan Wang , Chester Metcalf
Inventor: David Berstein , Leonard Rozamus , Yihan Wang , Chester Metcalf
IPC: A61F2/00 , A61K31/675
CPC classification number: A61K45/06 , A61K31/675 , C07F9/6561
Abstract: This invention concerns a new family of phosphorus-containing compounds containing a moiety JQA- in which: A is absent or is —O—, —S— or —NR2—; Q is absent or (if A is —O—, —S— or —NR2—) Q may be —V—, —OV—, —SV—, or —NR2V—, where V is an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, such that J is linked to the cyclohexyl ring directly, through A or through VA, OVA, SVA or NR2VA; K is O or S; each occurrence of Y is independently —O—, —S—, —NR2—, or a bond linking a R5 moiety to P; each occurrence of R2 and R5 is independently an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, or H; and each occurrence of R6 is independently —PK(YR5)(YR5), —SO2(YR5) or —C(O)(YR5); so long as any R2, or R5 moiety linked directly to P is not H; wherein two R2, R5 and/or R6 moieties may be chemically linked to one another to form a ring; each occurrence of G is independently —O—, —S—, —NR2— or (M)x; each occurrence of M is independently a substituted or unsubstituted methylene moiety, and any M-M′ moiety may be saturated or unsaturated; each occurrence of x is independently an integer from 1-6; and the other variables are as defined herein.
Abstract translation: 本发明涉及含有部分JQA-的新的含磷化合物族,其中:A不存在或为-O - , - S-或-NR 2 - 。 Q不存在或(如果A是-O-,-S-或-NR 2 - )Q可以是-V-,-OV-,-SV-或-NR 2 V-,其中V是脂族,杂脂族,芳基或杂芳基部分,使得J通过A或通过VA,OVA,SVA或NR 2 O直接与环己基环连接 > VA; K为O或S; 每次出现的Y独立地是-O - , - S - , - NR 2 - 或 - 连接R 5部分与P的键; 每个出现的R 2和R 5独立地是脂族,杂脂族,芳基或杂芳基部分,或H; 且每次出现的R 6独立地为-PK(YR 5),(YR 5), - SO 2 - (YR 5)或-C(O)(YR 5); 只要与P直接连接的任何R“或R 5”部分不是H; 其中两个R 2,R 5和/或R 6 O 6部分可以彼此化学连接以形成环; 每次出现的G独立地为-O - , - S - , - NR 2 - 或(M)x X; 每次出现的M独立地是取代或未取代的亚甲基部分,任何M-M'部分可以是饱和或不饱和的; 每次出现的x独立地为1-6的整数; 其他变量如本文所定义。
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公开(公告)号:US20060264456A1
公开(公告)日:2006-11-23
申请号:US11494418
申请日:2006-07-27
Applicant: Chester Metcalf , Leonard Rozamus , Yihan Wang , David Berstein
Inventor: Chester Metcalf , Leonard Rozamus , Yihan Wang , David Berstein
IPC: A61K31/4745 , C07D491/14
CPC classification number: A61K45/06 , A61K31/675 , C07F9/6561
Abstract: This invention concerns a new family of phosphorus-containing compounds containing a moiety JQA- in which: A is absent or is —O—, —S— or —NR2—; Q is absent or (if A is —O—, —S— or —NR2—) Q may be —V—, —OV—, —SV—, or —NR2V—, where V is an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, such that J is linked to the cyclohexyl ring directly, through A or through VA, OVA, SVA or NR2VA; K is O or S; each occurrence of Y is independently —O—, —S—, —NR2—, or a bond linking a R5 moiety to P; each occurrence of R2 and R5 is independently an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, or H; and each occurrence of R6 is independently —PK(YR5)(YR5), —SO2(YR5) or —(O)(YR5); so long as any R2, or R5 moiety linked directly to P is not H; wherein two R2, R5 and/or R6 moieties may be chemically linked to one another to form a ring; each occurrence of G is independently —O—, —S—, —NR2— or (M)x; each occurrence of M is independently a substituted or unsubstituted methylene moiety, and any M-M′ moiety may be saturated or unsaturated; each occurrence of x is independently an integer from 1-6; and the other variables are as defined herein.
Abstract translation: 本发明涉及含有部分JQA-的新的含磷化合物族,其中:A不存在或为-O - , - S-或-NR 2 - 。 Q不存在或(如果A是-O-,-S-或-NR 2 - )Q可以是-V-,-OV-,-SV-或-NR 2 V-,其中V是脂族,杂脂族,芳基或杂芳基部分,使得J通过A或通过VA,OVA,SVA或NR 2 O直接与环己基环连接 > VA; K为O或S; 每次出现的Y独立地是-O - , - S - , - NR 2 - 或 - 连接R 5部分与P的键; 每个出现的R 2和R 5独立地是脂族,杂脂族,芳基或杂芳基部分,或H; 且每次出现的R 6独立地为-PK(YR 5),(YR 5), - SO 2 - (YR 5)或 - (O)(YR 5); 只要与P直接连接的任何R“或R 5”部分不是H; 其中两个R 2,R 5和/或R 6 O 6部分可以彼此化学连接以形成环; 每次出现的G独立地是-O - , - S - , - NR 2 - 或(M)x。 每次出现的M独立地是取代或未取代的亚甲基部分,任何M-M'部分可以是饱和或不饱和的; 每次出现的x独立为1-6的整数; 其他变量如本文所定义。
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公开(公告)号:US07091213B2
公开(公告)日:2006-08-15
申请号:US10862149
申请日:2004-06-04
Applicant: Chester A. Metcalf, lll , Leonard W. Rozamus , Yihan Wang , David L. Berstein
Inventor: Chester A. Metcalf, lll , Leonard W. Rozamus , Yihan Wang , David L. Berstein
IPC: C07D491/06 , A61K31/395 , A61P35/00 , A61P35/02
CPC classification number: A61K45/06 , A61K31/675 , C07F9/6561
Abstract: This invention concerns a new family of phosphorus-containing compounds containing a moiety JQA- in which: A is absent or is —O—, —S— or —NR2—; Q is absent or (if A is —O—, —S— or —NR2—) Q may be —V—, —OV—, —SV—, or —NR2V—, where V is an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, such that J is linked to the cyclohexyl ring directly, through A or through VA, OVA, SVA or NR2VA; K is O or S; each occurrence of Y is independently —O—, —S—, —NR2—, or a bond linking a R5 moiety to P; each occurrence of R2 and R5 is independently an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, or H; and each occurrence of R6 is independently —PK(YR5)(YR5), —SO2(YR5) or —C(O)(YR5); so long as any R2, or R5 moiety linked directly to P is not H; wherein two R2, R5 and/or R6 moieties may be chemically linked to one another to form a ring; each occurrence of G is independently —O—, —S—, —NR2— or (M)x; each occurrence of M is independently a substituted or unsubstituted methylene moiety, and any M-M′ moiety may be saturated or unsaturated; each occurrence of x is independently an integer from 1–6; and the other variables are as defined herein.
Abstract translation: 本发明涉及含有部分JQA-的新的含磷化合物族,其中:A不存在或为-O - , - S-或-NR 2 - 。 Q不存在或(如果A是-O-,-S-或-NR 2 - )Q可以是-V-,-OV-,-SV-或-NR 2 V-,其中V是脂族,杂脂族,芳基或杂芳基部分,使得J通过A或通过VA,OVA,SVA或NR 2 O直接与环己基环连接 > VA; K为O或S; 每次出现的Y独立地是-O - , - S - , - NR 2 - 或 - 连接R 5部分与P的键; 每个出现的R 2和R 5独立地是脂族,杂脂族,芳基或杂芳基部分,或H; 且每次出现的R 6独立地为-PK(YR 5),(YR 5), - SO 2 - (YR 5)或-C(O)(YR 5); 只要与P直接连接的任何R“或R 5”部分不是H; 其中两个R 2,R 5和/或R 6 O 6部分可以彼此化学连接以形成环; 每次出现的G独立地是-O - , - S - , - NR 2 - 或(M)x。 每次出现的M独立地是取代或未取代的亚甲基部分,任何M-M'部分可以是饱和或不饱和的; 每次出现的x独立为1-6的整数; 其他变量如本文所定义。
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48.
公开(公告)号:US06576766B1
公开(公告)日:2003-06-10
申请号:US09554230
申请日:2000-08-17
Applicant: Manfred Weigele , Regine Bohacek , Virginia A. Jacobsen , Karina Macek , Michael G. Yang , Noriyuki H. Kawahata , Rajeswari Sundaramoorthi , Yihan Wang , Craig S. Takeuchi , George P. Luke , Chester A. Metcalf, III , William C. Shakespeare , Tomi K. Sawyer
Inventor: Manfred Weigele , Regine Bohacek , Virginia A. Jacobsen , Karina Macek , Michael G. Yang , Noriyuki H. Kawahata , Rajeswari Sundaramoorthi , Yihan Wang , Craig S. Takeuchi , George P. Luke , Chester A. Metcalf, III , William C. Shakespeare , Tomi K. Sawyer
IPC: C07D30789
CPC classification number: C07D307/92 , A61K38/00 , C07C237/22 , C07C2601/14 , C07F9/12 , C07F9/3834 , C07F9/3869 , C07F9/3873 , C07F9/3882 , C07F9/65527 , C07K5/06191
Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediate by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutic compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of formula (1) as defined herein.
Abstract translation: 本发明涉及用于抑制细胞内信号转导的化合物,特别是通过涉及含磷酸酪氨酸的蛋白质的一种或多种分子相互作用介导的细胞内信号转导。 本发明还涉及包含化合物的药物组合物和涉及化合物的药物和兽药施用的预防和治疗方法。 化合物是如本文所定义的式(1)。
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