公开(公告)号：US20120220551A1

公开(公告)日：2012-08-30

申请号：US13402335

申请日：2012-02-22

Applicant: Baihua Hu ,  Kan He ,  Minsheng Zhang

Inventor： Baihua Hu ,  Kan He ,  Minsheng Zhang

IPC: A61K31/675 ,  A61P35/00 ,  C07F9/6509 ,  C07F9/58 ,  C07F9/6558

CPC classification number: C07F9/58 ,  C07F9/650952 ,  C07F9/65583

Abstract: The present invention relates to compounds represented by formula (I), which can modulate the activity of protein kinases. The invention also relates to a composition containing a compound of formula (I), and a method for synthesizing and using such compound for preventing or treating ALK or cMet mediated disorders or conditions.

Abstract translation: 本发明涉及可以调节蛋白激酶活性的由式​​（I）表示的化合物。 本发明还涉及包含式（I）化合物的组合物，以及用于合成和使用该化合物以预防或治疗ALK或cMet介导的病症或病症的方法。

公开(公告)号：US20100035957A1

公开(公告)日：2010-02-11

申请号：US12539074

申请日：2009-08-11

Applicant: John C. McKew ,  Steve Y. Tam ,  Katherine L. Lee ,  Lihren Chen ,  Paresh Thakker ,  Fuk-Wah Sum ,  Mark L. Behnke ,  Baihua Hu ,  James D. Clark ,  Wei Li ,  Valerie Clerin ,  Suzana Marusic ,  Kevin Pong

Inventor： John C. McKew ,  Steve Y. Tam ,  Katherine L. Lee ,  Lihren Chen ,  Paresh Thakker ,  Fuk-Wah Sum ,  Mark L. Behnke ,  Baihua Hu ,  James D. Clark ,  Wei Li ,  Valerie Clerin ,  Suzana Marusic ,  Kevin Pong

IPC: A61K31/405 ,  A61P9/10 ,  A61P25/28

CPC classification number: A61K31/505 ,  C07D209/14 ,  C07D209/16 ,  C07D209/20 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/08 ,  C07D491/10

Abstract: This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition diseases and disorders including asthma, stroke, atherosclerosis, multiple sclerosis, Parkinson's disease, arthritic disorders, rheumatic disorders, central nervous system damage resulting from stroke, central nervous system damage resulting from ischemia, central nervous system damage resulting from trauma, inflammation caused or potentiated by prostaglandins, inflammation caused or potentiated by leukotrienes, inflammation caused or potentiated by platelet activation factor, pain caused or potentiated by prostaglandins, pain caused or potentiated by leukotrienes, and pain caused or potentiated by platelet activation factor.

Abstract translation: 本发明提供了使用通式的取代的吲哚化合物及其药学上可接受的盐形式的方法。 本发明提供了使用化合物作为各种磷脂酶，特别是磷脂酶A2酶的活性的抑制剂的方法，以及用于医学治疗，预防和抑制疾病和病症，包括哮喘，中风，动脉粥样硬化，多发性硬化，帕金森病， 关节炎疾病，风湿病，中风引起的中枢神经系统损伤，由缺血引起的中枢神经系统损伤，由创伤引起的中枢神经系统损伤，由前列腺素引起或增强的炎症，由白细胞三烯引起或增强的炎症，血小板引起或增强的炎症 活化因子，由前列腺素引起或增强的疼痛，由白三烯引起或加剧的疼痛，以及血小板激活因子引起或增强的疼痛。

公开(公告)号：US07576215B2

公开(公告)日：2009-08-18

申请号：US11010236

申请日：2004-12-10

Applicant: Michael D. Collini ,  Robert R. Singhaus, Jr. ,  Baihua Hu ,  James W. Jetter ,  Robert L. Morris ,  David H. Kaufman ,  Christopher P. Miller ,  John W. Ullrich ,  Rayomand J. Unwalla ,  Jay E. Wrobel ,  Elaine Quinet ,  Ponnal Nambi ,  Ronald C. Bernotas ,  Merle Elloso

Inventor： Michael D. Collini ,  Robert R. Singhaus, Jr. ,  Baihua Hu ,  James W. Jetter ,  Robert L. Morris ,  David H. Kaufman ,  Christopher P. Miller ,  John W. Ullrich ,  Rayomand J. Unwalla ,  Jay E. Wrobel ,  Elaine Quinet ,  Ponnal Nambi ,  Ronald C. Bernotas ,  Merle Elloso

IPC: C07D215/38

CPC classification number: C07D401/04 ,  C07D215/14 ,  C07D215/54 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/04 ,  C07D413/06 ,  C07D417/12

Abstract: This invention provides compounds of formula I that are useful in the treatment or inhibition of LXR mediated diseases.

Abstract translation: 本发明提供可用于治疗或抑制LXR介导的疾病的式I化合物。

公开(公告)号：US07442805B2

公开(公告)日：2008-10-28

申请号：US10947839

申请日：2004-09-23

Applicant: Baihua Hu

Inventor： Baihua Hu

IPC: C07D209/02 ,  C07D209/42 ,  A61K31/405

CPC classification number: C07D209/42 ,  C07D403/04

Abstract: The present invention relates generally to substituted sulfonamide indoles such as substituted sulfonamide indoles, and methods of using them.

Abstract translation: 本发明一般涉及取代磺酰胺吲哚如取代磺酰胺吲哚，以及使用它们的方法。

公开(公告)号：US07423044B2

公开(公告)日：2008-09-09

申请号：US10655471

申请日：2003-09-04

Applicant: Baihua Hu

Inventor： Baihua Hu

IPC: C07D239/34 ,  A61K31/505

CPC classification number: C07D471/04 ,  C07D239/34 ,  C07D239/70 ,  C07D401/04

Abstract: This invention provides compounds of Formula I having the structure: wherein: B is alkyl of 1-4 carbons or alkoxy of 1-4 carbons; R1 is aryl or Het optionally substituted with R6; R2 and R3 are each independently, alkyl of 1-4 carbons, CF3, aryl or Het substituted with R6, or R2 and R3 are combined to form a cycloalkyl or heterocyclic ring optionally substituted with alkyl, benzyl, or acyl; R4, and R5 are each independently, hydrogen, halogen, alkyl of 1-4 carbons, CO2R7, SO2NHR7, CONHR7, CN, NO2 or CF3; R6 is hydrogen, halogen, NO2, alkyl of 1-4 carbons, alkoxy of 1-4 carbons, alkylcarbonyloxy of 2-7 carbon atoms, alkylcarbonyl of 2-7 carbon atoms, CF3, or COOH; and R7 is hydrogen, alkyl of 1-4 carbons, or alkylaryl where aryl group is substituted with R6; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Abstract translation: 本发明提供具有以下结构的式I化合物：其中：B为1-4个碳的烷基或1-4个碳的烷氧基; R 1是任选被R 6取代的芳基或Het; R 2和R 3各自独立地为1-4个碳的烷基，CF 3，被R 6取代的芳基或Het 或R 2和R 3 3结合形成任选被烷基，苄基或酰基取代的环烷基或杂环; R 4和R 5各自独立地为氢，卤素，1-4个碳的烷基，CO 2 R 7， SO 2，NH 2，NH 2，NH 3，CONHR 7，CN，NO 2或CF 3 R 6是氢，卤素，NO 2，1-4个碳的烷基，1-4个碳的烷氧基，2-7个碳原子的烷基羰基氧基，2- 7个碳原子，CF 3 3或COOH; R 7是氢，1-4个碳的烷基或芳基，其中芳基被R 6取代; 或其药学上可接受的盐，其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。

公开(公告)号：US07332521B2

公开(公告)日：2008-02-19

申请号：US10947903

申请日：2004-09-23

Applicant: Baihua Hu

Inventor： Baihua Hu

IPC: A61K31/404 ,  C07D209/04

CPC classification number: C07D409/12 ,  C07D209/42

Abstract: The present invention relates generally to substituted indoles such as substituted 1H-indole-2-carboxylic acid derivatives, and methods of using them.

Abstract translation: 本发明一般涉及取代的吲哚如取代的1H-吲哚-2-羧酸衍生物及其使用方法。

公开(公告)号：US07268159B2

公开(公告)日：2007-09-11

申请号：US10947726

申请日：2004-09-23

Applicant: Baihua Hu ,  James Winfield Jetter

Inventor： Baihua Hu ,  James Winfield Jetter

IPC: A61K31/404 ,  C07D209/04

CPC classification number: C07D209/42 ,  C07D209/08 ,  C07D403/10 ,  C07D409/04

Abstract: The present invention relates generally to substituted indoles and methods of using them.

Abstract translation: 本发明一般涉及取代的吲哚及其使用方法。

公开(公告)号：US07101875B2

公开(公告)日：2006-09-05

申请号：US10302087

申请日：2002-11-22

Applicant: John C. McKew ,  Steve Y. Tam ,  Katherine L. Lee ,  Lihren Chen ,  Paresh Thakker ,  Fuk-Wah Sum ,  Mark Behnke ,  Baihua Hu ,  James D. Clark

Inventor： John C. McKew ,  Steve Y. Tam ,  Katherine L. Lee ,  Lihren Chen ,  Paresh Thakker ,  Fuk-Wah Sum ,  Mark Behnke ,  Baihua Hu ,  James D. Clark

IPC: A61K31/404 ,  A61K31/54 ,  A61K31/42 ,  A61K31/41 ,  A61K31/40

CPC classification number: C07D401/12 ,  C07D209/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/08 ,  C07D491/10

Abstract: This invention provides methods for treating in mammals arthritic or rheumatic disorders using substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.

Abstract translation: 本发明提供使用以下通式的取代的吲哚化合物及其药学上可接受的盐形式来治疗哺乳动物关节炎或风湿病的方法，以及使用这些化合物作为各种磷脂酶的活性抑制剂的方法，特别是磷脂酶A 2酶，并用于治疗，预防和抑制疼痛和炎症。

公开(公告)号：US06984735B2

公开(公告)日：2006-01-10

申请号：US10722782

申请日：2003-11-26

Applicant: John C. McKew ,  Steven Y. Tam ,  Katherine L. Lee ,  Lihren Chen ,  Paresh Thakker ,  Fuk-Wah Sum ,  Mark Behnke ,  Baihua Hu ,  James D. Clark ,  Wei Li

Inventor： John C. McKew ,  Steven Y. Tam ,  Katherine L. Lee ,  Lihren Chen ,  Paresh Thakker ,  Fuk-Wah Sum ,  Mark Behnke ,  Baihua Hu ,  James D. Clark ,  Wei Li

IPC: C07D215/38 ,  C07D217/12

CPC classification number: C07D401/12 ,  C07D209/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/08 ,  C07D491/10

Abstract: A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.

Abstract translation: 在没有有效量的活化剂的情况下，使亚砜与二卤代芳香族化合物反应的芳香醛的制造方法。 然后可以使用醛来制备其它化合物，例如充当cPLA抑制剂的化合物。

公开(公告)号：US20050113438A1

公开(公告)日：2005-05-26

申请号：US10947726

申请日：2004-09-23

Applicant: Baihua Hu ,  James Jetter

Inventor： Baihua Hu ,  James Jetter

IPC: A61K31/404 ,  A61K31/405 ,  C07D209/08 ,  C07D209/42 ,  C07D403/10 ,  C07D409/04 ,  C07D43/02

CPC classification number: C07D209/42 ,  C07D209/08 ,  C07D403/10 ,  C07D409/04

Abstract: The present invention relates generally to substituted indoles and methods of using them.

Abstract translation: 本发明一般涉及取代的吲哚及其使用方法。