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![Polymorph B of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide](/abs-image/US/2012/09/25/US08273753B2/abs.jpg.150x150.jpg)
1.发明授权Polymorph B of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide 有权N- {2-氟-5- [3-（噻吩-2-羰基） - 吡唑并[1,5-a]嘧啶-7-基] - 苯基} -N-甲基 - 乙酰胺的多晶型B公开(公告)号：US08273753B2
公开(公告)日：2012-09-25
申请号：US13115272
申请日：2011-05-25
申请人： Luis Anglada , Albert Palomer , Antonio Guglietta
发明人： Luis Anglada , Albert Palomer , Antonio Guglietta
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D487/04
摘要： The present invention relates to a method of treating anxiety, epilepsy, sleep disorders, and insomnia, for inducing sedation-hypnosis, anesthesia, and muscle relaxation, and for modulating the necessary time to induce sleep and its duration, which comprises administering a therapeutically effective amount of Polymorph B of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide characterized by a powder X-Ray diffraction pattern containing specific peaks at 2θ=7.1° (±0.1°) and 21.4° (±0.1°) to a patient in need thereof.
摘要翻译： 本发明涉及一种治疗焦虑，癫痫，睡眠障碍和失眠的方法，用于诱导镇静催眠，麻醉和肌肉松弛，以及调节诱导睡眠所需的时间及其持续时间，其包括施用治疗有效的 N- {2-氟-5- [3-（噻吩-2-羰基） - 吡唑并[1,5-a]嘧啶-7-基] - 苯基} -N-甲基 - 乙酰胺的多晶型B的量为 对于有需要的患者，在2θ时=特征峰= 7.1°（±0.1°）和21.4°（±0.1°）的粉末X射线衍射图。
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![Halogenated pyrazolo[1,5-A]pyrimidines, processes, uses, compositions and intermediates](/abs-image/US/2013/09/10/US08530482B2/abs.jpg.150x150.jpg)
2.发明授权Halogenated pyrazolo[1,5-A]pyrimidines, processes, uses, compositions and intermediates 有权卤化吡唑并[1,5-A]嘧啶，方法，用途，组合物和中间体公开(公告)号：US08530482B2
公开(公告)日：2013-09-10
申请号：US11922602
申请日：2006-06-15
申请人： Luis Anglada , Albert Palomer , Antonio Guglietta
发明人： Luis Anglada , Albert Palomer , Antonio Guglietta
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D471/04 , A61K31/519 , C07C231/12 , C07C233/33 , C07C233/43 , C07C303/40 , C07C311/08 , C07D487/04
摘要： The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R1, X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.
摘要翻译： 本发明提供了其中R，R 1，X和Y具有不同含义的式（I）的新型卤代吡唑并[1,5-a]嘧啶及其药学上可接受的盐。 式（I）化合物可用于治疗或预防焦虑，癫痫和睡眠障碍，包括失眠，以及用于诱导镇静催眠，麻醉，睡眠和肌肉松弛。 本发明还提供了用于制备所述化合物和某些中间体以及中间体本身的合成方法。
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![Amorphous form of N-{2-fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide](/abs-image/US/2012/12/25/US08338436B2/abs.jpg.150x150.jpg)
3.发明授权Amorphous form of N-{2-fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide 有权N- {2-氟-5- [3-（噻吩-2-羰基） - 吡唑并[1,5-a]嘧啶-7-基] - 苯基} -N-甲基 - 乙酰胺的无定形形式公开(公告)号：US08338436B2
公开(公告)日：2012-12-25
申请号：US12513884
申请日：2007-11-07
申请人： Luis Anglada , Albert Palomer , Antonio Guglietta
发明人： Luis Anglada , Albert Palomer , Antonio Guglietta
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D487/04
摘要： The present invention relates to an amorphous form of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide, methods for its preparation, its use as a therapeutically active agent and pharmaceutical compositions comprising the novel form.
摘要翻译： 本发明涉及无定形形式的N- {2-氟-5- [3-（噻吩-2-羰基） - 吡唑并[1,5-a]嘧啶-7-基] - 苯基} -N-甲基 - 乙酰胺，其制备方法，其作为治疗活性剂的用途和包含该新型形式的药物组合物。
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![Polymorph B of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a] pyrimidin-7-yl]-phenyl}-N-methyl-acetamide](/abs-image/US/2011/10/18/US08039476B2/abs.jpg.150x150.jpg)
4.发明授权Polymorph B of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a] pyrimidin-7-yl]-phenyl}-N-methyl-acetamide 有权N- {2-氟-5- [3-（噻吩-2-羰基） - 吡唑并[1,5-a]嘧啶-7-基] - 苯基} -N-甲基 - 乙酰胺的多晶型B公开(公告)号：US08039476B2
公开(公告)日：2011-10-18
申请号：US12445170
申请日：2007-10-10
申请人： Luis Anglada , Albert Palomer , Antonio Guglietta
发明人： Luis Anglada , Albert Palomer , Antonio Guglietta
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D487/04
摘要： The present invention relates to a novel polymorph of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide, processes for its preparation, its use as a medicament, its use in the manufacture of a medicament, and pharmaceutical compositions comprising the novel polymorph.
摘要翻译： 本发明涉及N- {2-氟-5- [3-（噻吩-2-羰基） - 吡唑并[1,5-a]嘧啶-7-基] - 苯基} -N-甲基 - 乙酰胺，其制备方法，其作为药物的用途，其在制备药物中的用途以及包含该新型多晶型物的药物组合物。
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![N-[3-(3-substituted-pyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-sulfonamides, and compositions, and methods related thereto](/abs-image/US/2006/11/30/US20060270690A1/abs.jpg.150x150.jpg)
5.发明申请N-[3-(3-substituted-pyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-sulfonamides, and compositions, and methods related thereto 失效N- [3-（3-取代 - 吡唑并[1,5-a]嘧啶-7-基）苯基] - 磺酰胺及其组合物及方法公开(公告)号：US20060270690A1
公开(公告)日：2006-11-30
申请号：US10562559
申请日：2004-07-22
申请人： Luis Anglada , Albert Palomer , Marta Princep , Antonio Guglietta
发明人： Luis Anglada , Albert Palomer , Marta Princep , Antonio Guglietta
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04 , A61K31/505
摘要： The present invention relates to compounds of Formula (I): wherein R1, R2 and R3 are as defined in the claims. The compounds have specific affinity for the GABAA receptor and are therefore useful in the treatment and prevention of diseases modulated by the α1- and α2-GABAA receptors.
摘要翻译： 本发明涉及式（I）的化合物：其中R 1，R 2和R 3均如权利要求中所定义。 这些化合物对GABA A A受体具有特异性亲和力，因此可用于治疗和预防由α1 - 和α2受体调节的疾病 -GABA A 受体。
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![PYRAZOLO[1,5-A]PYRIMIDINES, PROCESSES, USES AND COMPOSITIONS](/abs-image/US/2009/10/22/US20090264448A1/abs.jpg.150x150.jpg)
公开(公告)号：US20090264448A1
公开(公告)日：2009-10-22
申请号：US12376250
申请日：2007-08-02
申请人： Luis Anglada , Albert Palomer , Antonio Guglietta
发明人： Luis Anglada , Albert Palomer , Antonio Guglietta
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention provides novel pyrazolo[1,5-a]pyrimidines which are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation.
摘要翻译： 本发明提供了可用于治疗或预防焦虑，癫痫和睡眠障碍（包括失眠）以及用于诱导镇静催眠，麻醉，睡眠和肌肉松弛的新型吡唑并[1,5-a]嘧啶。
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![7-Substituted 3-nitro-pyrazo[1,5-a] pyrimidines](/abs-image/US/2007/02/22/US20070043064A1/abs.jpg.150x150.jpg)
公开(公告)号：US20070043064A1
公开(公告)日：2007-02-22
申请号：US10563104
申请日：2004-07-22
申请人： Luis Anglada , Albert Palomer , Marta Princep , Antonio Guglietta
发明人： Luis Anglada , Albert Palomer , Marta Princep , Antonio Guglietta
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of Formula (I): wherein R1 is as defined in the claims. The compounds have specific affinity for the GABAA receptor and are therefore useful in the treatment and prevention of diseases modulated by the α1- and α2-GABAA receptors.
摘要翻译： 本发明涉及式（I）的化合物：其中R 1如权利要求中所定义。 这些化合物对GABA A A受体具有特异性亲和力，因此可用于治疗和预防由α1 - 和α2受体调节的疾病 -GABA A 受体。
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![N-[3-(3-substituted-pyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-sulfonamides, and compositions, and methods related thereto](/abs-image/US/2011/05/24/US07947688B2/abs.jpg.150x150.jpg)
8.发明授权N-[3-(3-substituted-pyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-sulfonamides, and compositions, and methods related thereto 失效N- [3-（3-取代 - 吡唑并[1,5-a]嘧啶-7-基）苯基] - 磺酰胺及其组合物及方法公开(公告)号：US07947688B2
公开(公告)日：2011-05-24
申请号：US10562559
申请日：2004-07-22
申请人： Luis Anglada , Albert Palomer , Marta Princep , Antonio Guglietta
发明人： Luis Anglada , Albert Palomer , Marta Princep , Antonio Guglietta
IPC分类号： A61P21/02 , A61P25/08 , C07D487/04 , A61K31/519 , C07D279/02 , C07D267/04 , A61K31/541 , A61K31/554
CPC分类号： C07D487/04 , A61K31/505
摘要： The present invention relates to compounds of Formula (I): wherein R1, R2 and R3 are as defined in the claims. The compounds have specific affinity for the GABAA receptor and are therefore useful in the treatment and prevention of diseases modulated by the α1- and α2-GABAA receptors.
摘要翻译： 本发明涉及式（I）的化合物：其中R 1，R 2和R 3如权利要求中所定义。 该化合物对GABA A受体具有特异性亲和力，因此可用于治疗和预防由α1-和α2-GABA A受体调节的疾病。
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公开(公告)号：US20100087451A1
公开(公告)日：2010-04-08
申请号：US12445170
申请日：2007-10-10
申请人： Luis Anglada , Albert Palomer , Antonio Guglietta
发明人： Luis Anglada , Albert Palomer , Antonio Guglietta
IPC分类号： A61K31/519 , C07D487/04 , A61P25/00 , A61P21/02
CPC分类号： C07D487/04
摘要： The present invention relates to a novel polymorph of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide, processes for its preparation, its use as a medicament, its use in the manufacture of a medicament, and pharmaceutical compositions comprising the novel polymorph.
摘要翻译： 本发明涉及N- {2-氟-5- [3-（噻吩-2-羰基） - 吡唑并[1,5-a]嘧啶-7-基] - 苯基} -N-甲基 - 乙酰胺，其制备方法，其作为药物的用途，其在制备药物中的用途以及包含该新型多晶型物的药物组合物。
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![Halogenated Pyrazolo[1,5-A]Pyrimidines, Processes, Uses, Compositions and Intermediates](/abs-image/US/2009/04/30/US20090111848A1/abs.jpg.150x150.jpg)
10.发明申请Halogenated Pyrazolo[1,5-A]Pyrimidines, Processes, Uses, Compositions and Intermediates 有权卤代吡唑并[1,5-A]嘧啶，方法，用途，组合物和中间体公开(公告)号：US20090111848A1
公开(公告)日：2009-04-30
申请号：US11922602
申请日：2006-06-15
申请人： Luis Anglada , Albert Palomer , Antonio Guglietta
发明人： Luis Anglada , Albert Palomer , Antonio Guglietta
IPC分类号： A61K31/437 , C07D487/04 , C07C211/27 , A61P21/02
CPC分类号： C07D471/04 , A61K31/519 , C07C231/12 , C07C233/33 , C07C233/43 , C07C303/40 , C07C311/08 , C07D487/04
摘要： The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R1, X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.
摘要翻译： 本发明提供了其中R，R 1，X和Y具有不同含义的式（I）的新型卤代吡唑并[1,5-a]嘧啶及其药学上可接受的盐。 式（I）化合物可用于治疗或预防焦虑，癫痫和睡眠障碍，包括失眠，以及用于诱导镇静催眠，麻醉，睡眠和肌肉松弛。 本发明还提供了用于制备所述化合物和某些中间体以及中间体本身的合成方法。
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