公开(公告)号：US20090082390A1

公开(公告)日：2009-03-26

申请号：US12169164

申请日：2008-07-08

Applicant: Wai Ngor CHAN ,  Amanda Johns ,  Christopher Norbert Johnson ,  Riccardo Novelli ,  Roderick Alan Porter

Inventor： Wai Ngor CHAN ,  Amanda Johns ,  Christopher Norbert Johnson ,  Riccardo Novelli ,  Roderick Alan Porter

IPC: A61K31/4375 ,  C07D417/14 ,  A61K31/4245 ,  A61K31/427 ,  C07D471/04

CPC classification number: C07D413/14 ,  C07D401/14 ,  C07D413/06 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

Abstract: This invention relates to N-aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.

Abstract translation: 本发明涉及N-芳酰基环胺衍生物及其作为药物的用途，特别是作为食欲素受体拮抗剂。

公开(公告)号：US20090036442A1

公开(公告)日：2009-02-05

申请号：US11926375

申请日：2007-10-29

Applicant: Clive Leslie BRANCH ,  Wai Ngor Chan ,  Amanda Johns ,  Christopher Norbert Johnson ,  David John Nash ,  Riccardo Novelli ,  Jean-Pierre Pilleux ,  Roderick Alan Porter ,  Rachel Elizabeth Anne Stead ,  Geoffrey Stemp

Inventor： Clive Leslie BRANCH ,  Wai Ngor Chan ,  Amanda Johns ,  Christopher Norbert Johnson ,  David John Nash ,  Riccardo Novelli ,  Jean-Pierre Pilleux ,  Roderick Alan Porter ,  Rachel Elizabeth Anne Stead ,  Geoffrey Stemp

IPC: A61K31/454 ,  A61P3/04 ,  A61P43/00 ,  C07D417/14 ,  C07D401/14 ,  C07D401/06 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/4709 ,  A61K31/4545 ,  A61K31/4525

CPC classification number: C07D417/14 ,  C07D401/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D491/04

Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.

公开(公告)号：US07470710B2

公开(公告)日：2008-12-30

申请号：US10481133

申请日：2002-06-25

Applicant: Clive Leslie Branch ,  Wai Ngor Chan ,  Amanda Johns ,  Christopher Norbert Johnson ,  David John Nash ,  Riccardo Novelli ,  Jean-Pierre Pilleux ,  Roderick Alan Porter ,  Rachel Elizabeth Anne Stead ,  Geoffrey Stemp

Inventor： Clive Leslie Branch ,  Wai Ngor Chan ,  Amanda Johns ,  Christopher Norbert Johnson ,  David John Nash ,  Riccardo Novelli ,  Jean-Pierre Pilleux ,  Roderick Alan Porter ,  Rachel Elizabeth Anne Stead ,  Geoffrey Stemp

IPC: A61K31/4525 ,  A61K31/4535 ,  A61K31/454 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D407/14

CPC classification number: C07D417/14 ,  C07D401/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D491/04

Abstract: This invention relates to N-aroyl cyclic amine derivatives of formula (I), wherein X represents a bond, oxygen, NR3 or a group (CH2), wherein n represents 1, 2 or 3; Y represents CH2, CO, CH(OH), or CH2CH(OH); Het is an optionally substituted bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; Ar2 represents an optionally substituted phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S and their use as pharmaceuticals, specifically as orexin receptor antagonists.

Abstract translation: 本发明涉及式（I）的N-芳酰基环胺衍生物，其中X表示键，氧，NR 3或基团（CH 2），其中n表示1,2或3; Y表示CH 2，CO，CH（OH）或CH 2 CH（OH）; Het是含有至多4个选自N，O和S的杂原子的任选取代的双环杂芳基; Ar2表示任选取代的苯基或含有至多3个选自N，O和S的杂原子的5-或6-元杂环基，以及它们作为药物的用途，特别是作为食欲素受体拮抗剂。

公开(公告)号：US07423052B2

公开(公告)日：2008-09-09

申请号：US10481083

申请日：2002-06-25

Applicant: Wai Ngor Chan ,  Amanda Johns ,  Christopher Norbert Johnson ,  Riccardo Novelli ,  Roderick Alan Porter

Inventor： Wai Ngor Chan ,  Amanda Johns ,  Christopher Norbert Johnson ,  Riccardo Novelli ,  Roderick Alan Porter

IPC: A61K31/4525 ,  A61K31/454 ,  A61K31/4535 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

CPC classification number: C07D413/14 ,  C07D401/14 ,  C07D413/06 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

Abstract: A invention relates to N aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.

Abstract translation: 本发明涉及N芳酰基环胺衍生物及其作为药物的用途，特别是作为食欲素受体拮抗剂。

公开(公告)号：US07416853B2

公开(公告)日：2008-08-26

申请号：US11603741

申请日：2006-11-22

Applicant: Colin H. MacPhee ,  David Graham Tew

Inventor： Colin H. MacPhee ,  David Graham Tew

IPC: G01N33/573

CPC classification number: C12N9/20 ,  A61K38/005 ,  C12N9/18 ,  C12Q1/44 ,  G01N33/6893 ,  G01N2800/323 ,  G01N2800/324 ,  Y10S435/81

Abstract: The enzyme Lp-PLA2 in purified form, an isolated nucleic acid molecule encoding Lp-PLA2, the use of an inhibitor of the enzyme Lp-PLA2 in therapy and a method of screening compounds to identify those compounds.

Abstract translation: 纯化形式的酶Lp-PLA 2 2，编码Lp-PLA 2的分离的核酸分子，使用酶Lp-PLA2的抑制剂 在治疗和筛选化合物鉴定那些化合物的方法。

公开(公告)号：US07405217B2

公开(公告)日：2008-07-29

申请号：US11557998

申请日：2006-11-09

Applicant: Clive Leslie Branch ,  Christopher Norbert Johnson ,  David John Nash ,  Geoffrey Stemp

Inventor： Clive Leslie Branch ,  Christopher Norbert Johnson ,  David John Nash ,  Geoffrey Stemp

IPC: A61K31/495 ,  A61K31/496 ,  C07D241/04 ,  C07D417/12

CPC classification number: C07D413/10 ,  C07D241/04 ,  C07D417/06

Abstract: This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals.

Abstract translation: 本发明涉及N-芳酰基环状氨基衍生物及其作为药物的用途。

公开(公告)号：US07399837B2

公开(公告)日：2008-07-15

申请号：US11076395

申请日：2005-10-20

Applicant: Robert S. Ames ,  Edward Robert Appelbaum ,  Irwin M. Chaiken ,  Richard M. Cook ,  Mitchell Stuart Gross ,  Stephen Dudley Holmes ,  Lynette Jane McMillan ,  Timothy Wayne Theisen

Inventor： Robert S. Ames ,  Edward Robert Appelbaum ,  Irwin M. Chaiken ,  Richard M. Cook ,  Mitchell Stuart Gross ,  Stephen Dudley Holmes ,  Lynette Jane McMillan ,  Timothy Wayne Theisen

IPC: C07K16/00

CPC classification number: C07K16/244 ,  A61K2039/505 ,  C07K2317/24 ,  C07K2317/55 ,  C07K2319/00

Abstract: Chimeric, humanized and other IL-5 mAbs, derived from high affinity neutralizing mAbs, pharmaceutical compositions containing same, methods of treatment and diagnostics are provided.

Abstract translation: 提供衍生自高亲和力中和mAb的嵌合，人源化和其它IL-5mAb，含有其的药物组合物，治疗方法和诊断。

公开(公告)号：US07375105B2

公开(公告)日：2008-05-20

申请号：US10488650

申请日：2002-09-05

Applicant: David Kenneth Dean ,  Andrew Kenneth Takle ,  David Matthew Wilson

Inventor： David Kenneth Dean ,  Andrew Kenneth Takle ,  David Matthew Wilson

IPC: A61K31/5377 ,  A61K31/4545 ,  A61K31/443 ,  C07D413/14 ,  C07D211/32 ,  C07D405/04

CPC classification number: C07D405/04 ,  C07D405/14

Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. Wherein X is O, CH2 CO, S or NH, or the moiety X—R1 is hydrogen; Y1 and Y2 independently represent CH or N; Ar is a mono- or fused bicyclic aromatic or heteroaromatic group which may be optionally substituted; one of X1 and X2 is selected from O, S or NR11 and the other is CH, wherein R11 is hydrogen, C1-6alkyl, aryl or arylC1-6alkyl.

Abstract translation: 化合物及其作为药物的用途，特别是用作治疗神经创伤性疾病，癌症，慢性神经变性，疼痛，偏头痛和心脏肥大的Raf激酶抑制剂。 其中X是O，CH 2 CO，S或NH，或者X-R 1部分是氢; Y 1和Y 2独立地表示CH或N; Ar是可以任选取代的单或二稠合双环芳族或杂芳族基团; X 1和X 2之一选自O，S或NR 11，另一个是CH，其中R 11， / SUP>是氢，C 1-6烷基，芳基或芳基C 1-6烷基。

公开(公告)号：US20080108615A1

公开(公告)日：2008-05-08

申请号：US11928762

申请日：2007-10-30

Applicant: David Dean ,  Andrew Takle ,  David Wilson

Inventor： David Dean ,  Andrew Takle ,  David Wilson

IPC: A61K31/5377 ,  C07D413/14 ,  C07D401/14 ,  C07D401/02 ,  A61K31/497 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/4439 ,  A61P35/00

CPC classification number: C07D401/04 ,  C07D401/14

Abstract: The present invention relates to compounds of formula (I): pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, use as Raf Kinase Inhibitors and treatment methods for neurotraumatic diseases and cancer.

Abstract translation: 本发明涉及式（I）化合物：其药学上可接受的盐，相应的药物组合物，用作Raf激酶抑制剂和治疗神经损伤疾病和癌症的方法。

公开(公告)号：US07358366B2

公开(公告)日：2008-04-15

申请号：US11458471

申请日：2006-07-19

Applicant: Paul David James Blackler ,  Robert Gordon Giles ,  Stephen Moore ,  Michael John Sasse

Inventor： Paul David James Blackler ,  Robert Gordon Giles ,  Stephen Moore ,  Michael John Sasse

IPC: C07D417/12

CPC classification number: C07D417/12

Abstract: A polymorphic form of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, maleic acid salt (the “Polymorph”) characterised in that it provides: (i) an infra red spectrum containing peaks at 1752, 1546, 1154, 621, and 602 cm−1; and/or (ii) a Raman spectrum containing peaks at 1751, 1243 and 602 cm−1; and/or (iii) a solid-state nuclear magnetic resonance spectrum containing peaks at 111.9, 114.8, 119.6, 129.2, 134.0, 138.0, 144.7, 153.2, 157.1, 170.7, 172.0, and 175.0 ppm; and/or (iv) an X-ray powder diffraction (XRPD) pattern which gives calculated lattice spacings of 6.46, 5.39, 4.83, 4.68, 3.71, 3.63, 3.58, and 3.48 Angstroms; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound in medicine.

Abstract translation: 5- [4- [2-（N-甲基-N-（2-吡啶基）氨基）乙氧基]苄基]噻唑烷-2,4-二酮，马来酸盐（“多晶型”）的多晶形式，其特征在于 它提供：（i）在1752,1546,1154,621和602cm -1处含有峰的红外光谱; 和/或（ii）在1751,1243和602cm -1处含有峰的拉曼光谱; 和/或（iii）在111.9,114.8,119.6,129.2,134.0,138.0,144.7,153.2,157.1,170.7,172.0和175.0ppm处含有峰的固态核磁共振光谱; 和/或（iv）X射线粉末衍射（XRPD）图案，其给出计算的晶格间距为6.46,5.39,4.83,4.68,3.73,3.63,3.58和3.48埃; 制备这种化合物的方法，含有这种化合物的药物组合物和这种化合物在医药中的用途。