公开(公告)号：US09481675B2

公开(公告)日：2016-11-01

申请号：US13394985

申请日：2010-09-10

Applicant: Christopher J Creighton ,  Leslie William Tari ,  Zhiyong Chen ,  Mark Hilgers ,  Thanh To Lam ,  Xiaoming Li ,  Michael Trzoss ,  Junhu Zhang ,  John Finn ,  Daniel Bensen

Inventor： Christopher J Creighton ,  Leslie William Tari ,  Zhiyong Chen ,  Mark Hilgers ,  Thanh To Lam ,  Xiaoming Li ,  Michael Trzoss ,  Junhu Zhang ,  John Finn ,  Daniel Bensen

IPC: C07D487/04 ,  C07D519/00 ,  C07D471/04 ,  C07D487/16 ,  C07D491/048 ,  C07D513/04

CPC classification number: C07D519/00 ,  C07D471/04 ,  C07D471/16 ,  C07D487/04 ,  C07D487/16 ,  C07D491/048 ,  C07D513/04

Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth. Compounds of Formula I are disclosed: wherein Y is N or CH; Z is N or CR5; R5 is H, a substituted or unsubstituted hydrocarbyl residue (1-3C) containing 0-2 heteroatoms selected from O, S and N, or is an inorganic residue; L is O, S, NR7, or CR8R9; R7 is H or C1-3 alkyl; R8 and R9 are each independently H or C1-3 alkyl; R2 is H, a hydrocarbyl residue (1-40C) containing 0-10 heteroatoms selected from O, S and N optionally substituted with an inorganic residue; R4 is H, an inorganic residue, or a hydrocarbyl residue (1-30C) containing 0-12 heteroatoms selected from O, S and N and containing 0-10 inorganic residues, wherein R5 and R4 together may join to form a fused ring; and R6 is selected from the group consisting of H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halo C1-5 alkyl, halo C2-5 alkenyl, halo C2-5 alkynyl, C1-5 hydroxyalkyl, C1-5 alkyl chloride, C2-5 alkenyl chloride, and C2-5 alkynyl chloride; or a pharmaceutically-acceptable salt, ester, or prodrug thereof.

Abstract translation: 新型促旋酶抑制剂和相关组合物和方法可用于阻止细菌生长。 公开了式（I）的化合物：式（I），其中Y是N或CH; Z为N或CR5; R5是H，含有0-2个选自O，S和N的杂原子的取代或未取代的烃基残基（1-3C），或是无机残基; L是O，S，NR7或CR8R9; R7是H或C1-3烷基; R 8和R 9各自独立地为H或C 1-3烷基; R2是H，含有0-10个选自O，S和N的杂原子的烃基残基（1-40℃），任选被无机残基取代; R4是H，无机残基或含有0-12个选自O，S和N的杂原子并含有0-10个无机残基的烃基残基（1-30C），其中R 5和R 4可以连接形成稠环; 并且R 6选自H，C 1-5烷基，C 2-5烯基，C 2-5炔基，卤代C 1-5烷基，卤素C 2-5烯基，卤代C 2-5炔基，C 1-5羟基烷基，C 1 -5烷基氯，C2-5烯基氯和C2-5炔基氯; 或其药学上可接受的盐，酯或前药。

公开(公告)号：US20120136014A1

公开(公告)日：2012-05-31

申请号：US13151683

申请日：2011-06-02

Applicant: Zhiyong Chen ,  Christopher J. Creghton ,  Mark Cunningham ,  John Finn ,  Mark Hilgers ,  Michael Jung ,  Lucy Aguirre Kohnen ,  Thanh Lam ,  Xiaoming Li ,  Mark Stidham ,  Les Tari ,  Michael Trzoss ,  Junhu Zhang

Inventor： Zhiyong Chen ,  Christopher J. Creghton ,  Mark Cunningham ,  John Finn ,  Mark Hilgers ,  Michael Jung ,  Lucy Aguirre Kohnen ,  Thanh Lam ,  Xiaoming Li ,  Mark Stidham ,  Les Tari ,  Michael Trzoss ,  Junhu Zhang

IPC: A61K31/517 ,  C07D401/14 ,  C07D239/72 ,  A61P31/10 ,  A61P33/00 ,  A61P31/04 ,  A61P29/00 ,  C12N9/99 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07D239/95 ,  C07D417/14

Abstract: The present disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R5, R6 and Z are as described herein. The disclosure also provides pharmaceutical compositions thereof; and methods for inhibiting DHFR activity; and methods for treating cell proliferative diseases, autoimmune disease, inflammatory disease or bacterial, fungal or parasitic infection by administering a compound of Formula I.

Abstract translation: 本公开提供式I化合物或其药学上可接受的盐，其中R 5，R 6和Z如本文所述。 本公开还提供其药物组合物; 和抑制DHFR活性的方法; 以及通过给予式I化合物治疗细胞增殖性疾病，自身免疫疾病，炎性疾病或细菌，真菌或寄生虫感染的方法。

公开(公告)号：US20100137283A1

公开(公告)日：2010-06-03

申请号：US12697513

申请日：2010-02-01

Applicant: Klaus Ruprecht Dress ,  Qiyue Hu ,  Ted William Johnson ,  Michael Bruno Plewe ,  Steven Paul Tanis ,  Huichun Zhu ,  Junhu Zhang

Inventor： Klaus Ruprecht Dress ,  Qiyue Hu ,  Ted William Johnson ,  Michael Bruno Plewe ,  Steven Paul Tanis ,  Huichun Zhu ,  Junhu Zhang

IPC: A61K31/55 ,  C12N9/99 ,  A61K31/551 ,  A61K31/5377 ,  A61K31/437 ,  C07D471/14

CPC classification number: C07D491/14 ,  C07D471/14

Abstract: The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIV”) integrase enzyme.

Abstract translation: 本发明涉及式（I）化合物及其药学上可接受的盐和溶剂合物，它们的合成及其作为人免疫缺陷病毒（“HIV”）整合酶的调节剂或抑制剂的用途。

公开(公告)号：US20070004768A1

公开(公告)日：2007-01-04

申请号：US11470301

申请日：2006-09-06

Applicant: Qiyue Hu ,  Atsuo Kuki ,  Michael Plewe ,  Dawn Nowlin ,  Hai Wang ,  Junhu Zhang

Inventor： Qiyue Hu ,  Atsuo Kuki ,  Michael Plewe ,  Dawn Nowlin ,  Hai Wang ,  Junhu Zhang

IPC: A61K31/4745 ,  C07D471/14 ,  C07D491/14

CPC classification number: C07D471/04 ,  C07D471/12 ,  C07D471/14

Abstract: Bicyclic hydroxamate compounds represented by the Formula I: are described. The bicyclic hydroxamate compounds and compositions containing those compounds may be used to inhibit or modulate an enzyme activity of HIV Integrase and to treat HIV mediated diseases and conditions.

Abstract translation: 描述由式I表示的双环氧肟酸酯化合物。 双环异羟肟酸酯化合物和含有这些化合物的组合物可用于抑制或调节HIV整合酶的酶活性并治疗HIV介导的疾病和病症。

公开(公告)号：US09732083B2

公开(公告)日：2017-08-15

申请号：US13496188

申请日：2012-03-14

Applicant: Daniel Bensen ,  Zhiyong Chen ,  John Finn ,  Thanh To Lam ,  Suk Joong Lee ,  Xiaoming Li ,  Douglas W. Phillipson ,  Leslie William Tari ,  Michael Trzoss ,  Junhu Zhang ,  Felice C. Lightstone ,  Toan B. Nguyen ,  Sergio E. Wong ,  Paul Aristoff ,  Michael Jung

Inventor： Daniel Bensen ,  Zhiyong Chen ,  John Finn ,  Thanh To Lam ,  Suk Joong Lee ,  Xiaoming Li ,  Douglas W. Phillipson ,  Leslie William Tari ,  Michael Trzoss ,  Junhu Zhang ,  Felice C. Lightstone ,  Toan B. Nguyen ,  Sergio E. Wong ,  Paul Aristoff ,  Michael Jung

IPC: C07D487/04 ,  C07D487/14

CPC classification number: C07D487/04 ,  C07D487/14

Abstract: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors.Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

公开(公告)号：US09634273B2

公开(公告)日：2017-04-25

申请号：US13813628

申请日：2011-05-13

Applicant: Bai Yang ,  Weili Yu ,  Hao Zhang ,  Junhu Zhang ,  Haotong Wei ,  Zhanxi Fan

Inventor： Bai Yang ,  Weili Yu ,  Hao Zhang ,  Junhu Zhang ,  Haotong Wei ,  Zhanxi Fan

IPC: H01L21/00 ,  H01L51/42 ,  H01L51/00

CPC classification number: H01L51/426 ,  H01L51/0003 ,  H01L51/0038 ,  H01L51/4213 ,  Y02E10/549

Abstract: Provided is a method for producing a highly efficient organic/inorganic hybrid solar cell using fully aqueous phase-synthesized semiconductor nanocrystals and conducting polymer. The method mainly includes three steps: synthesizing nanocrystals in an aqueous phase, synthesizing a conjugated polymer precursor in an aqueous phase, and producing a device of solar cell. The nanocrystal material required for producing a solar cell by the method is widely available, diversified and size-controlled, and the used conjugated polymer has regulated molecular structure and molecular weight, which contributes to increase the absorption of sunlight. The processing of cell device can be performed at room temperature in air, and has advantages of no pollution, short processing period, and low cost. A method for producing an organic/inorganic hybrid solar cell is developed, which succeeds in introducing the high quality nanocrystals synthesized in an aqueous phase and is an eco-friendly and pollution-free technology for producing a solar cell.

公开(公告)号：US20100324074A1

公开(公告)日：2010-12-23

申请号：US12919216

申请日：2009-02-28

Applicant: Junhu Zhang

Inventor： Junhu Zhang

IPC: A61K31/519 ,  C07D487/04 ,  A61P35/00 ,  A61P35/02

CPC classification number: C07D487/04

Abstract: The present invention is directed to low molecular weight and orally bioavailable 3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the tyrosine kinase MET. The invention is also directed to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract translation: 本发明涉及低分子量和口服生物可利用的3H- [1,2,3]三唑并[4,5-d]嘧啶衍生物，其可用于治疗细胞增殖性疾病，用于治疗与MET活性相关的疾病，以及 用于抑制酪氨酸激酶MET。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。

公开(公告)号：US20070232644A1

公开(公告)日：2007-10-04

申请号：US11574869

申请日：2005-08-26

Applicant: Klaus Dress ,  Jon Kuehler ,  Michael Plewe ,  Anle Yang ,  Junhu Zhang

Inventor： Klaus Dress ,  Jon Kuehler ,  Michael Plewe ,  Anle Yang ,  Junhu Zhang

IPC: A61K31/44 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions comprising compounds of formula (I), and their methods of use in treating HIV-infected mammals.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐或溶剂化物，包含式（I）化合物的药物组合物及其用于治疗HIV感染的哺乳动物的方法。

公开(公告)号：US07135482B2

公开(公告)日：2006-11-14

申请号：US10699068

申请日：2003-10-30

Applicant: Qiyue Hu ,  Ted William Johnson ,  Atsuo Kuki ,  Michael Bruno Plewe ,  Dawn Marie Nowlin ,  Hai Wang ,  Junhu Zhang

Inventor： Qiyue Hu ,  Ted William Johnson ,  Atsuo Kuki ,  Michael Bruno Plewe ,  Dawn Marie Nowlin ,  Hai Wang ,  Junhu Zhang

IPC: A61K31/44

CPC classification number: C07D471/04 ,  C07D471/12 ,  C07D471/14

Abstract: Bicyclic hydroxamate compounds represented by the Formula I: are described. The bicyclic hydroxamate compounds and compositions containing those compounds may be used to inhibit or modulate an enzyme activity of HIV Integrase and to treat HIV mediated diseases and conditions.

Abstract translation: 描述由式I表示的双环氧肟酸酯化合物。 双环异羟肟酸酯化合物和含有这些化合物的组合物可用于抑制或调节HIV整合酶的酶活性并治疗HIV介导的疾病和病症。

公开(公告)号：US08598184B2

公开(公告)日：2013-12-03

申请号：US12919216

申请日：2009-02-28

Applicant: Junhu Zhang

Inventor： Junhu Zhang

IPC: C07D487/04 ,  A61K31/519 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: The present invention is directed to low molecular weight and orally bioavailable 3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the tyrosine kinase MET. The invention is also directed to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract translation: 本发明涉及低分子量和口服生物可利用的3H- [1,2,3]三唑并[4,5-d]嘧啶衍生物，其可用于治疗细胞增殖性疾病，用于治疗与MET活性相关的疾病，以及 用于抑制酪氨酸激酶MET。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。