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    CRF receptor antagonists and methods relating thereto
    2.
    发明授权
    CRF receptor antagonists and methods relating thereto 有权
    CRF受体拮抗剂及其相关方法

    公开(公告)号：US07737154B2

    公开(公告)日：2010-06-15

    申请号：US10596648

    申请日：2004-12-20

    申请人： Zhiyong Luo ,  Deborah H Slee ,  John Williams

    发明人： Zhiyong Luo ,  Deborah H Slee ,  John Williams

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/24 ,  A61P25/22

    CPC分类号： C07D487/04

    摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure (I), including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, Y, Ar, and het are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.

    摘要翻译： 公开了CRF受体拮抗剂，其可用于治疗多种疾病，包括治疗在温血动物（例如中风）中表现出CRF分泌过高的病症。 本发明的CRF受体拮抗剂具有以下结构（I），其包括其立体异构体，前药和药学上可接受的盐，其中R1，R2，R3，Y，Ar和het如本文所定义。 还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法。

    Cancer Treatment Method
    3.
    发明申请
    Cancer Treatment Method 审中-公开
    癌症治疗方法

    公开(公告)号：US20080306097A1

    公开(公告)日：2008-12-11

    申请号：US11721675

    申请日：2005-12-16

    申请人： Stephen Rubin

    发明人： Stephen Rubin

    IPC分类号： A61K31/517 ,  A61P35/00

    CPC分类号： A61K31/517 ,  A61K31/473 ,  A61K31/513 ,  A61K45/06

    摘要： Disclosed herein is a method of treating breast cancer that has metastasized to the brain in a mammal by administration of 4-quinazolinamines and pharmaceutical compositions containing the same. In particular, the method relates to methods of treating breast cancer brain metastases which overexpress erbB2 by administration of N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine and salts and solvates thereof.

    摘要翻译： 本文公开了通过施用4-喹唑啉胺和含有它们的药物组合物来治疗哺乳动物转移至脑的乳腺癌的方法。 特别地，该方法涉及通过给予N- {3-氯-4 - [（3-氟苄基）氧基]苯基} -6- [5 - （{[2- （甲磺酰基）乙基]氨基}甲基）-2-呋喃基] -4-喹唑啉胺及其盐和溶剂化物。

    Polymorph of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2, 4-dione, maleic acid salt
    6.
    发明申请
    Polymorph of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2, 4-dione, maleic acid salt 审中-公开
    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，马来酸盐的多晶型物

    公开(公告)号：US20050080114A1

    公开(公告)日：2005-04-14

    申请号：US10935939

    申请日：2004-09-08

    申请人： Paul Blackler ,  Christine Browne ,  Timothy Coakley ,  Robert Giles ,  Gillian Morrissey

    发明人： Paul Blackler ,  Christine Browne ,  Timothy Coakley ,  Robert Giles ,  Gillian Morrissey

    IPC分类号： A61K20060101 ,  A61K31/00 ,  A61K31/4439 ,  A61P20060101 ,  A61P3/10 ,  C07D20060101 ,  C07D417/12 ,  C07D417/02

    CPC分类号： C07D417/12

    摘要： A polymorphic form of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, maleic acid salt (the “Polymorph”) characterized in that it provides: (i) an infra red spectrum containing peaks at 1763, 912, 856 and 709 cm−1; and/or (ii) a Raman spectrum containing peaks at 1762, 1284, 912 and 888 cm−1; and/or (iii) a solid-state 13C nuclear magnetic resonance spectrum containing peaks at 111.0, 113.6, 119.8, 129.1, 130.9, 131.8, 134.7, 138.7, 146.5, 152.7, 157.5, 169.5, 171.0, 178.7 ppm; and/or (iv) an X-ray powder diffraction (XRPD) pattern which gives calculated lattice spacings at 5.87, 5.30, 4.69, 4.09, 3.88, 3.61, 3.53, and 3.46 Angstroms; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound in medicine.

    摘要翻译： 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1763,912,856和709cm -1处含有峰的红外光谱; 和/或（ii）在1762,1284,912和888cm -1处含有峰的拉曼光谱; 和/或（iii）在111.0,113.6,119.8,129.1,130.9,131.8,134.7,138.7,146.5,152.7,157.5,169.5,171.0,178.7ppm处含有峰的固态13 C核磁共振光谱; 和/或（iv）在5.87,5.30,4.69,4.09,3.88,3.61,3.53和3.46埃处给出计算的晶格间距的X射线粉末衍射（XRPD）图案; 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。

    Pyrazolo [1,5-alpha] pyrimidinyl derivatives useful as corticotropin-releasing factor (CRF) receptor antagonists
    8.
    发明授权
    Pyrazolo [1,5-alpha] pyrimidinyl derivatives useful as corticotropin-releasing factor (CRF) receptor antagonists 有权
    可用作促肾上腺皮质激素释放因子（CRF）受体拮抗剂的吡唑并[1,5-a]嘧啶基衍生物

    公开(公告)号：US08088779B2

    公开(公告)日：2012-01-03

    申请号：US12067939

    申请日：2006-09-28

    申请人： Frank Hossner

    发明人： Frank Hossner

    IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00

    CPC分类号： C07D487/04

    摘要： The present invention generally relates to the polymorph Form 2 of [3-(4-methoxy-2-methyl-phenyl)-2,5-dimethyl-pyrazolo[1,5-a]pyrimidin-7-yl]-[(S)-1-(3-methyl-[1,2,4]oxa-diazol-5-yl)-propyl]amine. The present invention also relates to pharmaceutical compositions comprising the same and methods of using the same.

    摘要翻译： 本发明一般涉及[3-（4-甲氧基-2-甲基 - 苯基）-2,5-二甲基 - 吡唑并[1,5-a]嘧啶-7-基] - [（S ）-1-（3-甲基 - [1,2,4]氧杂 - 二唑-5-基） - 丙基]胺。 本发明还涉及包含其的药物组合物及其使用方法。

    CANCER TREATMENT METHOD
    10.
    发明申请
    CANCER TREATMENT METHOD 审中-公开
    癌症治疗方法

    公开(公告)号：US20110301185A1

    公开(公告)日：2011-12-08

    申请号：US13209889

    申请日：2011-08-15

    申请人： Richard Buller ,  Mark Berger ,  Clet Niyikiza

    发明人： Richard Buller ,  Mark Berger ,  Clet Niyikiza

    IPC分类号： A61K31/517 ,  A61P35/00

    CPC分类号： A61K31/7068 ,  A61K31/282 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/517 ,  A61K2300/00

    摘要： The present invention relates to a method of treating cancer in a mammal by administration of 4-quinazolinamines and at least one additional anti-neoplastic compound. In particular, the method relates to a methods of treating cancers by administration of N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine and salts and solvates thereof in combination with at least one additional anti-neoplastic compound.

    摘要翻译： 本发明涉及通过施用4-喹唑啉胺和至少一种另外的抗肿瘤化合物来治疗哺乳动物的癌症的方法。 特别地，该方法涉及通过给予N- {3-氯-4 - [（3-氟苄基）氧基]苯基} -6- [5 - （{[2-（甲磺酰基）乙基] 氨基}甲基）-2-呋喃基] -4-喹唑啉胺及其盐和溶剂化物与至少一种另外的抗肿瘤化合物的组合。