公开(公告)号：US09701693B2

公开(公告)日：2017-07-11

申请号：US14129169

申请日：2012-06-27

Applicant: Tong-Shuang Li ,  Ernest J. Mceachern ,  David J. Vocadlo ,  Yuanxi Zhou ,  Yongbao Zhu ,  Harold G. Selnick

Inventor： Tong-Shuang Li ,  Ernest J. Mceachern ,  David J. Vocadlo ,  Yuanxi Zhou ,  Yongbao Zhu ,  Harold G. Selnick

IPC: C07D513/00 ,  C07D513/04 ,  C07H9/06 ,  C12Q1/37 ,  C12Q1/34

CPC classification number: C07D513/04 ,  C07H9/06 ,  C12Q1/34 ,  C12Q1/37 ,  G01N2333/924 ,  G01N2500/04

Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

公开(公告)号：US09126957B2

公开(公告)日：2015-09-08

申请号：US14238481

申请日：2012-08-10

Applicant: Harold G. Selnick ,  Kun Liu ,  Ernest J. McEachern ,  Yuanxi Zhou ,  Yongbao Zhu

Inventor： Harold G. Selnick ,  Kun Liu ,  Ernest J. McEachern ,  Yuanxi Zhou ,  Yongbao Zhu

IPC: A61K31/423 ,  A61K31/428 ,  C07D263/58 ,  C07D413/04 ,  C07D417/04 ,  C07D277/60 ,  C07D277/82

CPC classification number: C07D263/58 ,  A61K31/423 ,  A61K31/428 ,  C07D277/60 ,  C07D277/82 ,  C07D413/04 ,  C07D417/04

Abstract: The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.

Abstract translation: 本发明涉及用于选择性抑制糖苷酶的化合物，化合物的用途和包含该化合物的药物组合物，以及治疗与O-GlcNAC的缺乏或过度表达有关的疾病和障碍和/或O-GlcNAc的积累或缺陷的方法。

公开(公告)号：US08901087B2

公开(公告)日：2014-12-02

申请号：US13883811

申请日：2011-11-08

Applicant: Jiang Chang ,  Kun Liu ,  Ernest J. McEachern ,  Changwei Mu ,  Harold G. Selnick ,  Feng Shi ,  David J. Vocadlo ,  Yaode Wang ,  Zhongyong Wei ,  Yuanxi Zhou ,  Yongbao Zhu

Inventor： Jiang Chang ,  Kun Liu ,  Ernest J. McEachern ,  Changwei Mu ,  Harold G. Selnick ,  Feng Shi ,  David J. Vocadlo ,  Yaode Wang ,  Zhongyong Wei ,  Yuanxi Zhou ,  Yongbao Zhu

IPC: C08B37/00 ,  C07D487/02 ,  A61K31/70 ,  A61K31/425 ,  C07D513/04

CPC classification number: C07D513/04

Abstract: The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.

Abstract translation: 本发明涉及用于选择性抑制糖苷酶的化合物，化合物的用途和包含该化合物的药物组合物，以及治疗与O-GlcNAC的缺乏或过度表达有关的疾病和障碍和/或O-GlcNAc的积累或缺陷的方法。

公开(公告)号：US20130065926A1

公开(公告)日：2013-03-14

申请号：US13601357

申请日：2012-08-31

Applicant: Hassan A. PAJOUHESH ,  Ramesh KAUL ,  Yanbing DING ,  Yongbao ZHU ,  Lingyun ZHANG ,  Nagasree CHAKKA ,  Michael Edward GRIMWOOD ,  Jason TAN ,  Yuanxi ZHOU

Inventor： Hassan A. PAJOUHESH ,  Ramesh KAUL ,  Yanbing DING ,  Yongbao ZHU ,  Lingyun ZHANG ,  Nagasree CHAKKA ,  Michael Edward GRIMWOOD ,  Jason TAN ,  Yuanxi ZHOU

IPC: A61K31/445 ,  A61P29/00

CPC classification number: A61K31/5377 ,  A61K31/445 ,  A61K31/4525 ,  A61K31/453 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  C07D211/26 ,  C07D211/28 ,  C07D211/38 ,  C07D211/46 ,  C07D211/62 ,  C07D211/66 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).

公开(公告)号：US20120245137A1

公开(公告)日：2012-09-27

申请号：US13496729

申请日：2010-09-17

Applicant: Hassan A. Pajouhesh ,  Robert Galemmo, JR. ,  Richard Holland ,  Yuanxi Zhou ,  Yongbao Zhu ,  Eric Simonson ,  Navjot Chahal ,  Mike Grimwood

Inventor： Hassan A. Pajouhesh ,  Robert Galemmo, JR. ,  Richard Holland ,  Yuanxi Zhou ,  Yongbao Zhu ,  Eric Simonson ,  Navjot Chahal ,  Mike Grimwood

IPC: A61K31/44 ,  C07D239/26 ,  A61K31/505 ,  C07C317/48 ,  A61K31/166 ,  C07D295/13 ,  A61K31/5375 ,  C07D205/04 ,  A61K31/397 ,  C07D265/36 ,  A61K31/538 ,  A61P25/00 ,  A61P25/08 ,  A61P25/16 ,  A61P25/24 ,  A61P25/18 ,  A61P25/06 ,  C07D213/82

CPC classification number: C07C317/44 ,  A61K31/095 ,  C07C317/14 ,  C07C317/22 ,  C07C317/28 ,  C07C317/30 ,  C07C317/32 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14

Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity, are disclosed. Specifically, a series of compounds containing aryl sulphone derivatives, as exemplified by Formula (I).

Abstract translation: 公开了有效改善由不希望的钙通道活性，特别是不需要的N型和/或T型钙通道活性表征的病症的方法和化合物。 具体而言，是一系列含有芳基砜衍生物的化合物，如式（I）所例举。

公开(公告)号：US20090281308A1

公开(公告)日：2009-11-12

申请号：US12467006

申请日：2009-05-15

Applicant: Gary J. BRIDGER ,  Ernest J. MCEACHERN ,  Renato SKERLJ ,  Dominique SCHOLS ,  Ian BAIRD ,  Al KALLER ,  Curtis HARWIG ,  Yongbao ZHU ,  Gang CHEN ,  Krystyna SKUPINSKA ,  Markus METZ

Inventor： Gary J. BRIDGER ,  Ernest J. MCEACHERN ,  Renato SKERLJ ,  Dominique SCHOLS ,  Ian BAIRD ,  Al KALLER ,  Curtis HARWIG ,  Yongbao ZHU ,  Gang CHEN ,  Krystyna SKUPINSKA ,  Markus METZ

IPC: C07D401/14 ,  C07D409/14 ,  C07D417/04 ,  C07D413/14

CPC classification number: C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: Compounds that interact with the CXCR4 receptor are described. These compounds are useful in treating, for Example, HIV infection and inflammatory conditions such as rheumatoid arthritis, as well as asthma or cancer, and are useful in methods to elevate progenitor and stem cell counts as well as methods to elevate white blood cell counts.

Abstract translation: 描述了与CXCR4受体相互作用的化合物。 这些化合物可用于治疗例如HIV感染和炎性病症如类风湿性关节炎以及哮喘或癌症，并且可用于提高祖细胞和干细胞计数的方法以及升高白细胞计数的方法。

公开(公告)号：US20140296205A1

公开(公告)日：2014-10-02

申请号：US14129177

申请日：2012-06-27

Applicant: Tong-Shuang Li ,  Ernest J. Mceachern ,  David J. Vocadlo ,  Yuanxi Zhou ,  Yongbao Zhu ,  Harold G. Selnick

Inventor： Tong-Shuang Li ,  Ernest J. Mceachern ,  David J. Vocadlo ,  Yuanxi Zhou ,  Yongbao Zhu ,  Harold G. Selnick

IPC: C07D513/04 ,  G01N33/50 ,  C12Q1/34

CPC classification number: C07D513/04 ,  C07H9/06 ,  C12Q1/34 ,  C12Q1/37 ,  G01N33/5038 ,  G01N2333/924 ,  G01N2500/04

Abstract: The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

公开(公告)号：US20120220603A1

公开(公告)日：2012-08-30

申请号：US13393369

申请日：2010-09-03

Applicant: Hassan Pajouhesh ,  Mike Grimwood ,  Yongbao Zhu ,  Yanbing Ding ,  Richard Holland

Inventor： Hassan Pajouhesh ,  Mike Grimwood ,  Yongbao Zhu ,  Yanbing Ding ,  Richard Holland

IPC: A61K31/495 ,  C07D295/15 ,  A61K31/496 ,  A61P25/00 ,  C12N5/02 ,  A61P25/16 ,  A61P25/24 ,  A61P25/18 ,  A61P25/06 ,  C07D241/08 ,  A61P25/08

CPC classification number: C07D241/08 ,  C07D211/34 ,  C07D295/15 ,  C07D403/06 ,  C07D413/06

Abstract: Compounds of formula (I) which are useful in ameliorating conditions characterized by unwanted sodium and/or calcium channel activity, particularly unwanted NaV 1.7, NaV 1.8, or CaV 3.2 channel activity are disclosed. Specifically, a series of compounds containing piperidine or piperazine linked through an amide, isoxazole or similar linker to an aryl ring are described and are shown to be useful for the treatment of pain or epilepsy. A is selected from Formulae (i) or (ii).

Abstract translation: 公开了可用于改善由不希望的钠和/或钙通道活性，特别是不需要的NaV 1.7，NaV 1.8或CaV 3.2通道活性表征的特征的式（I）化合物。 具体地说，描述了一系列含有通过酰胺，异恶唑或类似连接物与芳基环连接的哌啶或哌嗪的化合物，并被证明可用于治疗疼痛或癫痫。 A选自式（i）或（ii）。

公开(公告)号：US07863293B2

公开(公告)日：2011-01-04

申请号：US11936047

申请日：2007-11-06

Applicant: Gary J. Bridger ,  Ernest J. McEachern ,  Renato Skerlj ,  Dominique Schols ,  Ian Baird ,  Al Kaller ,  Curtis Harwig ,  Yongbao Zhu ,  Gang Chen ,  Krystyna Skupinska

Inventor： Gary J. Bridger ,  Ernest J. McEachern ,  Renato Skerlj ,  Dominique Schols ,  Ian Baird ,  Al Kaller ,  Curtis Harwig ,  Yongbao Zhu ,  Gang Chen ,  Krystyna Skupinska

IPC: C07D401/02 ,  A61K31/44

CPC classification number: C07D413/14 ,  C07D213/38 ,  C07D213/61 ,  C07D213/65 ,  C07D213/69 ,  C07D213/70 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D213/80 ,  C07D213/82 ,  C07D213/89 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D451/04 ,  C07D471/06

Abstract: The present invention relates to compounds that bind to chemokine receptors, and having the formula wherein each A, X, Y, R1, R2 and R3 are substituents. The present invention also relates to methods of using such compounds, such as in treating HIV infection and inflammatory conditions such as rheumatoid arthritis. Furthermore, the present invention relates to methods to elevate progenitor and stem cell counts, as well as methods to elevate white blood cell counts, using such compounds.

Abstract translation: 本发明涉及结合趋化因子受体的化合物，具有下式，其中每个A，X，Y，R 1，R 2和R 3是取代基。 本发明还涉及使用这些化合物的方法，例如用于治疗HIV感染和炎性病症如类风湿性关节炎。 此外，本发明涉及使用这些化合物提高祖细胞和干细胞计数的方法以及升高白细胞计数的方法。

公开(公告)号：US07790747B2

公开(公告)日：2010-09-07

申请号：US11453221

申请日：2006-06-14

Applicant: Yuanxi Zhou ,  Elyse Bourque ,  Yongbao Zhu ,  Jonathan Langille ,  Markus Metz ,  Wen Yang ,  Ernest J. McEachern ,  Curtis Harwig ,  Ian R. Baird ,  Tong-Shuang Li ,  Renato T. Skerlj

Inventor： Yuanxi Zhou ,  Elyse Bourque ,  Yongbao Zhu ,  Jonathan Langille ,  Markus Metz ,  Wen Yang ,  Ernest J. McEachern ,  Curtis Harwig ,  Ian R. Baird ,  Tong-Shuang Li ,  Renato T. Skerlj

IPC: A61K31/4545 ,  C07D409/14

CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

Abstract: The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. These compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).

Abstract translation: 本发明涉及趋化因子受体结合化合物，药物组合物及其用途。 更具体地，本发明涉及趋化因子受体活性的调节剂，优选CCR5的调节剂。 这些化合物表现出对人体免疫缺陷病毒（HIV）感染靶细胞的保护作用。