公开(公告)号：US07470694B2

公开(公告)日：2008-12-30

申请号：US11561035

申请日：2006-11-17

申请人： Colin Andrew Leach ,  Stephen Allan Smith ,  Steven James Stanway

发明人： Colin Andrew Leach ,  Stephen Allan Smith ,  Steven James Stanway

IPC分类号： A61K31/517

CPC分类号： C07D239/56 ,  C07D239/60 ,  C07D239/70 ,  C07D239/95 ,  C07D401/12 ,  C07D403/12 ,  C07D495/04

摘要： Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atheroscelerosis.

摘要翻译： 式（I）的嘧啶酮化合物：是Lp-PLA2酶的抑制剂，可用于治疗动脉粥样硬化。

公开(公告)号：US07462620B2

公开(公告)日：2008-12-09

申请号：US11456129

申请日：2006-07-07

申请人： Deirdre Mary Bernadette Hickey ,  Colin Andrew Leach ,  Ivan Leo Pinto ,  Stephen Allan Smith

发明人： Deirdre Mary Bernadette Hickey ,  Colin Andrew Leach ,  Ivan Leo Pinto ,  Stephen Allan Smith

IPC分类号： C07D239/70 ,  A61K31/517

CPC分类号： C07D239/36 ,  C07D239/70 ,  C07D239/91 ,  C07D401/12 ,  C07D403/12 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis.

摘要翻译： 式（I）化合物：是Lp-PLA2酶的抑制剂，可用于治疗，特别是治疗动脉粥样硬化。

公开(公告)号：US07429579B2

公开(公告)日：2008-09-30

申请号：US10416377

申请日：2001-11-12

申请人： Michael Stewart Hadley ,  Andrew Lightfoot ,  Gregor James MacDonald ,  Geoffrey Stemp

发明人： Michael Stewart Hadley ,  Andrew Lightfoot ,  Gregor James MacDonald ,  Geoffrey Stemp

IPC分类号： A61P25/18 ,  A61K31/55 ,  C07D223/16

CPC分类号： C07D223/16 ,  A61K31/55 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04

摘要： The invention provides compounds of formula (I): wherein: R2 and R3 independently represent various substituents; R1 and R4 independently represent H, F, Cl, Br, C1-2alkyl, C1alkoxy, OH, CN, or NO2; B represents a sulfur atom or a —CH2-group; t represents 3 or 4; and A represents an optionally substituted 5- or 6-membered aromatic heterocyclic ring, or an optionally substituted bicyclic heterocyclic ring system in which at least the ring bound to the group B in Formula (I) is aromatic; or a salt thereof. Preferably, A is selected from one of the groups (i), (ii) or (iii): wherein X1 and X2 are independently N or CR8, and X3 is NR8, O or S; Y1 and Y3 are independently N or CR9, and Y2 is NR9, O or S; Z1 is NR10, O or S, and Z2 and Z3 are independently N or CR10; R8, R9, and R10 are as herein defined, and R7 is H, a halogen atom, OH, cyano, nitro, C1-4alkyl, C1-4alkoxy, C1-4alkylenedioxy, C1-4alkanoyl, or C1-4alkylsulfonyl, an optionally substituted 3-, 4-, 5- or 6-membered cycloalkyl ring, or a group of the formula (a), (b), (c) or (d) as defined by the formulas (a), (b), (c) or (d). The compounds are modulators of dopamine D3 receptors and have potential in the treatment of psychotic conditions (e.g. schizophrenia) or substance abuse.

公开(公告)号：US20080113908A1

公开(公告)日：2008-05-15

申请号：US11461604

申请日：2006-08-01

申请人： Laura Facci ,  Stephen Drake Skaper ,  Paul Johannes Leonardus Maria Strijbos

发明人： Laura Facci ,  Stephen Drake Skaper ,  Paul Johannes Leonardus Maria Strijbos

IPC分类号： A61K38/16 ,  A61P25/28

CPC分类号： A61K38/2228

摘要： CRF receptor agonists, especially CRF receptor-1 agonists such as CRF, urocortin, sauvagine or urotensin 1, can be used for the prevention or inhibition of neuronal cell death in a mammal suffering from or susceptible to chronic neurodegenerative disease (e.g. Alzheimer's disease, Parkinson's disease or Huntington's disease), traumatic (mechanical) neuronal injury, epilepsy-associated neuronal loss, paralysis, or spinal chord injury. CRF receptor-1 agonists can also be administered to aid the prevention or inhibition of neuronal cell death in a mammal suffering from or suceptible to cerebral ischaemia (stroke). Also, where neuronal cell death is potentiated by inhibition or suppression of the PI 3-kinase signalling pathway, a treatment comprises administering to the mammal an effective amount of a CRF receptor agonist.

摘要翻译： CRF受体激动剂，特别是CRF受体-1激动剂如CRF，尿皮质素，sauvagine或尿激肽1可用于预防或抑制患有或易患慢性神经变性疾病的哺乳动物（例如阿尔茨海默病，帕金森病 疾病或亨廷顿氏病），创伤性（机械性）神经​​元损伤，癫痫相关神经元损失，麻痹或脊髓损伤。 还可以施用CRF受体-1激动剂以帮助预防或抑制患有或可感受到脑缺血（中风）的哺乳动物的神经元细胞死亡。 此外，通过抑制或抑制PI3-激酶信号通路来增强神经元细胞死亡，治疗包括向哺乳动物施用有效量的CRF受体激动剂。

公开(公告)号：US20070161560A1

公开(公告)日：2007-07-12

申请号：US11549189

申请日：2006-10-13

申请人： John Davis ,  Martin Gunthorpe ,  Julie Egerton ,  Darren Smart

发明人： John Davis ,  Martin Gunthorpe ,  Julie Egerton ,  Darren Smart

IPC分类号： A61K48/00 ,  A61K38/17 ,  C12Q1/68 ,  G01N33/567

CPC分类号： A61K38/177 ,  G01N33/566 ,  G01N33/6872 ,  G01N2500/00

摘要： The use of VR4 polypeptides and polynucleotides in the design of protocols for the treatment of diseases of cartilage, such as hyaline-, fibro- and elastic-cartilage, or diseases of tissues where such cartilage is found including diseases or disorders affecting the larynx, auditory canal, intervertebral discs, ligaments, tendons and joint capsules, bone development including osteoporosis, diseases involving joint destruction and also pain linked to rheumatoid arthritis and osteoarthritis.

摘要翻译： 在设计用于治疗软骨疾病的方案中使用VR4多肽和多核苷酸，例如透明，纤维和弹性软骨，或发现这种软骨的组织疾病，包括影响喉部的疾病或障碍，听觉 运动，椎间盘，韧带，腱和关节囊，骨发育，包括骨质疏松症，涉及关节破坏的疾病，以及与类风湿性关节炎和骨关节炎相关的疼痛。

公开(公告)号：US07199137B2

公开(公告)日：2007-04-03

申请号：US10380891

申请日：2001-09-19

申请人： David Kenneth Dean ,  Andrew Kenneth Takle ,  David Matthew Wilson

发明人： David Kenneth Dean ,  Andrew Kenneth Takle ,  David Matthew Wilson

IPC分类号： A61K31/4439 ,  C07D401/04

CPC分类号： C07D401/04 ,  A61K49/0021 ,  C07D401/14 ,  C07D405/14

摘要： Novel compounds (I) 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 Ar is a group of formula a) or b).

摘要翻译： 新型化合物（I）及其作为药物特别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激酶抑制剂的用途，其中Ar是式a）或b）的基团。

公开(公告)号：US20070059721A1

公开(公告)日：2007-03-15

申请号：US11316490

申请日：2005-12-21

申请人： David Michalovich ,  Rabinder Prinjha

发明人： David Michalovich ,  Rabinder Prinjha

IPC分类号： C12Q1/68 ,  C07H21/04 ,  C12P21/06 ,  C07K14/705 ,  C07K16/28 ,  C40B30/06

CPC分类号： C12N9/2497 ,  C07K14/47

摘要： MAGI polypeptides, polynucleotides, antibodies, and methods for producing the same by recombinant techniques are disclosed. Also disclosed are methods for utilizing MAGI polypeptides and polynucleotides in diagnostic assays.

摘要翻译： 公开了MAGI多肽，多核苷酸，抗体以及通过重组技术制备其的方法。 还公开了在诊断测定中利用MAGI多肽和多核苷酸的方法。

公开(公告)号：US07169924B2

公开(公告)日：2007-01-30

申请号：US10398977

申请日：2001-10-05

申请人： Richard Leonard Elliott ,  Deirdre Mary Bernadette Hickey ,  Robert John Ife ,  Colin Andrew Leach ,  Ivan Leo Pinto ,  Stephen Allan Smith

发明人： Richard Leonard Elliott ,  Deirdre Mary Bernadette Hickey ,  Robert John Ife ,  Colin Andrew Leach ,  Ivan Leo Pinto ,  Stephen Allan Smith

IPC分类号： C07D239/70 ,  A61K31/517 ,  A61P9/01

CPC分类号： C07D239/36 ,  C07D239/70 ,  C07D239/91 ,  C07D401/12 ,  C07D403/12 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： Compound of formula (I): are disclosed in which: R1 is an aryl group, optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from C(1-6)alkyl, C(1-6)alkoxy, C(1-6)alkylthio, hydroxy, halogen, CN, and mono to perfluoro-C(1-4)alkyl; R2 is halogen, C(1-3)alkyl, C(1-3)alkoxy, hydroxyC(1-3)alkyl, C(1-3)alkylthio, C(1-3)alkylsulphinyl, aminoC(1-3)alkyl, mono- or di-C(1-3)alkylaminoC(1-3)alkyl, C(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkoxyC(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkylsulphonylaminoC(1-3)alkyl, C(1-3)alkylcarboxy, C(1-3)alkylcarboxyC(1-3)alkyl, and R3 is hydrogen, halogen, C(1-3)alkyl, or hydroxyC(1-3)alkcyl; or R2 and R3 together with the pyrimidone ring carbon atoms to which they are attached form a fused 5-or 6-membered carbocyclic ring; or R2 and R3 together with the pyrimidone ring carbon atoms to which they are attached form a fused benzo or heteroaryl ring ring optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from halogen, C(1-4)alkyl, cyano, C(1-6)alkoxy, C(1-6)alkylthio or mono to perfluoro-C(1-4)alkyl; R4 is hydrogen, C(1-6)alkyl which may be unsubstituted or substituted by 1, 2 or 3 substituents selected from hydroxy, halogen, OR7, COR7, carboxy, COOR7, CONR9R10, NR9R10, NR7COR8, mono- or di-(hydroxyC(1-6)alkyl) amino and N-hydroxyC(1-6)alkyl-N—C(1-6)allkylamino; or R4 is Het-C(0-4)alkyl in which Het is a 5- to 7- membered heterocyclyl ring comprising N and optionally O or S, and in which N may be substituted by COR7, COOR7, CONR9R10, or C(1-6)alkyl optionally substituted by 1, 2 or 3 substituents selected from hydroxy, halogen, OR7, COR7, carboxy, COOR7, CONR9R10 or NR9R10, for instance, piperidinyl-4-yl, pyrrolidin-3-yl; R5 is an aryl or a heteroaryl ring optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selectd from C(1-6)alkyl, C(1-6)alkoxy, C(1-6)alkylthio, arylC(1-6)alkoxy, hydroxy, halogen, CN, COR7, carboxy, COOR7, NR7COR8, CONR9R10, SO2NR9R10, NR7SO2R8, NR9R10, mono to perfluoro-C(1-4)alkyl and mono to perfluoro-C(1-4)alkoxy; R6 is an aryl or a heteroaryl ring which is further optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from C(1-18)alkyl, C(1-18)alkoxy, C(1-6)alkylthio, C(1-6)alkylsulfonyl, arylC(1-6)alkoxy, hydroxy, halogen, CN, COR7, carboxy, COOR7, CONR9R10, NR7COR8, SO2NR9R10, NR7SO2R8, NR9R10, mono to perfluoro-C(1-4)alkyl and mono to perfluoro-C(1-4)alkoxy, or C(5-10)alkyl; These compound are useful for treating diseases associated with abnormal activity of the phospholipase A2 enzyme, for example athereosclosis.

公开(公告)号：US07115616B2

公开(公告)日：2006-10-03

申请号：US10776876

申请日：2004-02-11

申请人： Ashley Edward Fenwick ,  Deirdre Mary Bernadette Hickey ,  Robert John Ife ,  Colin Andrew Leach ,  Ivan Leo Pinto ,  Stephen Allan Smith

发明人： Ashley Edward Fenwick ,  Deirdre Mary Bernadette Hickey ,  Robert John Ife ,  Colin Andrew Leach ,  Ivan Leo Pinto ,  Stephen Allan Smith

IPC分类号： C07D473/00 ,  C07D239/02 ,  A61K31/505 ,  A61P9/10

CPC分类号： C07D239/56 ,  C07D401/14 ,  C07D403/06

摘要： Pyrimidinone compounds of formula (10 are inhibitors of the enzyme Lp-PLA2 and of use in therapy, in particular for treating atherosclerosis.

摘要翻译： 式（10）的嘧啶酮化合物是Lp-PLA 2酶的抑​​制剂，并且在治疗中尤其用于治疗动脉粥样硬化。

公开(公告)号：US20060205641A1

公开(公告)日：2006-09-14

申请号：US10668846

申请日：2003-09-23

申请人： Graham Smith ,  Philip Hayes ,  Darren Smart ,  John Davis ,  Rosemary Kelsell

发明人： Graham Smith ,  Philip Hayes ,  Darren Smart ,  John Davis ,  Rosemary Kelsell

IPC分类号： A61K38/17 ,  C07K14/705 ,  C07H21/04 ,  C12P21/06

CPC分类号： C07K14/705

摘要： VANILREP4 polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing VANILREP4 polypeptides and polynucleotides in diagnostic assays.

摘要翻译： VANILREP4多肽和多核苷酸以及通过重组技术产生此类多肽的方法。 还公开了在诊断测定中利用VANILREP4多肽和多核苷酸的方法。