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71. 发明申请

WO2013076590A1 BENZOTHIAZINE COMPOUNDS AS H3 RECEPTOR LIGANDS 审中-公开
标题翻译：苯扎他嗪化合物作为H3受体配体
公开(公告)号：WO2013076590A1
公开(公告)日：2013-05-30
申请号：PCT/IB2012/050219
申请日：2012-01-17
申请人： OXYGEN HEALTHCARE RESEARCH PVT. LTD , SHIRSATH, Vikas S. , PATEL, Shailesh M , SHETH, Nehal M. , SINGH, Jitendra K. , PATIL, Pawan D. , PAWAR, Anil D. , MOTIVARAS, Jitendra D.
发明人： SHIRSATH, Vikas S. , PATEL, Shailesh M , SHETH, Nehal M. , SINGH, Jitendra K. , PATIL, Pawan D. , PAWAR, Anil D. , MOTIVARAS, Jitendra D.
IPC分类号： C07D279/16 , C07D417/12 , A61K31/5415
CPC分类号： C07D279/16 , C07D417/12
摘要： The present invention provides benzothiazine derivative of formula (I), useful in the treatment of CNS disorders including cognitive disorders, ADHD, narcolepsy, pain, dementias, schizophrenia as well as obesity and sleep disorders. Pharmacological profile of these compounds includes high affinity binding with H 3 receptor along with favourable selectivity profile for other aminergic receptors. The present invention also includes 'their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions.
摘要翻译：本发明提供式（I）的苯并噻嗪衍生物，其可用于治疗CNS疾病，包括认知障碍，ADHD，发作性睡病，疼痛，痴呆，精神分裂症以及肥胖和睡眠障碍。这些化合物的药理学特征包括与H3受体的高亲和力结合以及其它胺能受体的有利选择性。本发明还包括“它们的类似物，其互变异构形式，其立体异构体，其多晶型物，其药学上可接受的盐，其药学上可接受的溶剂合物和药学上可接受的组合物。

72. 发明申请

WO2013044871A1 氯喹或氯丙嗪或其衍生物或它们的混合物在制备用于治疗和/或预防肺感染和损伤的药物中的用途审中-公开
公开(公告)号：WO2013044871A1
公开(公告)日：2013-04-04
申请号：PCT/CN2012/082480
申请日：2012-09-29
申请人：中国医学科学院基础医学研究所 , 中国人民解放军军事医学科学院军事兽医研究所
发明人：蒋澄宇 , 金宁一 , 孙阳 , 邹镇 , 李霄 , 闫毅武
IPC分类号： A61K31/4706 , A61K31/5415 , A61K31/541 , A61K9/08 , A61P31/16 , A61P11/00
CPC分类号： A61K9/08 , A61K31/4706 , A61K31/541 , A61K31/5415 , A61K31/5513 , A61K2300/00
摘要：本发明涉及氯喹治疗和氯丙嗪预防肺感染和损伤的用途。特别地，本发明涉及氯喹或氯丙嗪或其衍生物或它们的混合物以及含有它们的药物组合物在制备治疗和/或预防流感病毒引起的哺乳动物包括人的肺感染和/或肺损伤的药物中的用途。

73. 发明申请

WO2013041967A3 COMPOSITIONS AND METHODS FOR TREATING PRESBYOPIA, MILD HYPEROPIA, AND IRREGULAR ASTIGMATISM 审中-公开
公开(公告)号：WO2013041967A3
公开(公告)日：2013-03-28
申请号：PCT/IB2012/002335
申请日：2012-09-19
申请人： ALTAVISTA INSTITUTO DE INVESTIGATION MEDICA S.A.S
发明人： ABAD, Jaun, Carlos
IPC分类号： A61K31/27 , A61K31/4164 , A61K31/4174 , A61K31/4178 , A61K31/5415 , A61K45/06 , A61P27/02 , A61P27/06 , A61P27/10
摘要： The present invention is directed to compositions and methods for treating ocular conditions, including presbyopia, mild hyperopia, irregular astigmatism, hyperopic accommodative esotropia, and glaucoma. The compositions can also be used to potentiate or enhance interventions that retard, reverse, or modify the aging process of the crystalline lens and its surrounding tissues. The compositions include a cholinergic agent, such as a muscarinic acetylcholine receptor M3 agonist, and an alpha agonist having an imidazoline group or a non-steroidal anti-inflammatory agent (NSAID) having COX-2 selectivity. It has been found that an alpha agonist having an imidazoline group or non-steroidal anti-inflammatory agent (NSAID) having COX-2 selectivity in combination with a cholinergic agent, such as pilocarpine, act synergistically to improve the accommodative and focusing ability of the eye while minimizing the side effects from each compound.

74. 发明申请

WO2012162330A1 TRICYCLIC COMPOUNDS AS INHIBITORS FOR THE PRODUCTION OF BETA-AMYLOID 审中-公开
标题翻译：作为生产β-淀粉样蛋白的抑制剂的三聚化合物
公开(公告)号：WO2012162330A1
公开(公告)日：2012-11-29
申请号：PCT/US2012/039031
申请日：2012-05-23
申请人： BRISTOL-MYERS SQUIBB COMPANY , THOMPSON III, Lorin A. , SHI, Jianliang , WU, Yong-Jin , MARCIN, Lawrence R. , RAJAMANI, Ramkumar , HIGGINS, Mendi A.
发明人： THOMPSON III, Lorin A. , SHI, Jianliang , WU, Yong-Jin , MARCIN, Lawrence R. , RAJAMANI, Ramkumar , HIGGINS, Mendi A.
IPC分类号： C07D279/08 , C07D417/04 , C07D417/12 , C07D513/04 , A61K31/5415 , A61K31/542 , A61K31/55 , A61P25/28
CPC分类号： C07D279/08 , C07D417/04 , C07D417/10 , C07D417/12 , C07D513/04
摘要： Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: formula (I), wherein X is selected from the group of CH 2 , O, and NR 2 ; m = 0 or 1; R 1 at each instance is selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC 1-4 alkyl, CN, C 1 -C 6 alkyl or cycloalkyl, C 1 -C 6 alkoxy, and C2-C4 alkynyl; L is a bond, -NHCO-, -NH-, or L and Z together can be absent; Z is a C 6 -C 10 - aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, haloC 1-4 alkoxy, 4-methoxyphenyl, hydroxy, amino, C 1-4 alkylamino, C 1-4 dialkylamino, haloC 1-4 alkyl, CN, C 1 -C 6 alkyl or cycloalkyl, C 1 -C 6 alkoxy, and C 2 -C 4 alkynyl; R2 is selected from the group of hydrogen, benzyl, C 1 -C 6 alkyl or cycloalkyl, C 1 -C 6 alkoxy, acetyl, and methanesulfonyl; and R 3 , R 4 and R 5 are independently selected from hydrogen or C 1-4 alkyl.
摘要翻译：包括其药学上可接受的盐的式（I）化合物在本文中列出：式（I），其中X选自CH 2，O和NR 2; m = 0或1; 每个实例的R 1选自卤素，羟基，氨基，C 1-4烷基氨基，C 1-4二烷基氨基，卤代C 1-4烷基，CN，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基和C 2 -C 4炔基; L是键，-NHCO-，-NH-或L和Z可以不存在; Z是可以被0-3个选自卤素，卤代C 1-4烷氧基，4-甲氧基苯基，羟基，氨基，C 1 -C 10 - 芳基的取代基取代的C 6 -C 10 - 芳基或5-10元杂环基。 C 1-4烷基氨基，卤代C 1-4烷基，CN，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基和C 2 -C 4炔基; R 2选自氢，苄基，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基，乙酰基和甲磺酰基; 并且R 3，R 4和R 5独立地选自氢或C 1-4烷基。

75. 发明申请

WO2012130306A1 BICYCLIC 2,3-DIHYRDOBENZAZINE COMPOUNDS FOR USE IN THERAPY 审中-公开
标题翻译：双酚2,3-二羟基苯并嗪化合物用于治疗
公开(公告)号：WO2012130306A1
公开(公告)日：2012-10-04
申请号：PCT/EP2011/054959
申请日：2011-03-30
申请人： ELARA PHARMACEUTICALS GMBH , JANSSEN, Bernd , THOMSON, Douglas , MÜLBAIER, Marcel , ALONSO, Jorge , ENCINAS-LOPEZ, Arantxa , WENDT, Bernd , SCHULTES, Christoph
发明人： JANSSEN, Bernd , THOMSON, Douglas , MÜLBAIER, Marcel , ALONSO, Jorge , ENCINAS-LOPEZ, Arantxa , WENDT, Bernd , SCHULTES, Christoph
IPC分类号： C07D413/04 , C07D417/04 , C07D419/04 , A61K31/538 , A61K31/5415 , A61P29/00
CPC分类号： C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D498/04
摘要： The present invention provides novel 2,3-dihydrobenzazine compounds of formula (I) and to their salts. The compounds inhibit cell proliferation and cell division and they also inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions (I) wherein X is O or S(=O)n; n is 0, 1 or 2; R 1 is an optionally substituted C-bound bicyclyl comprising a first ring which is a benzene ring or a 5- or 6-membered heteroaromatic ring having either 1, 2 or 3 nitrogen atoms as heteroatom ring members or 1 oxygen or 1 sulfur atom and 0, 1 or 2 nitrogen atoms as heteroatom ring members, and a second ring, which is fused to the first ring, where the second ring is a 5-, 6- or 7-membered carbocyclic ring or a 5-, 6- or 7-membered heterocyclic ring having 1, 2 or 3 heteroatom ring members selected from oxygen, sulfur and nitrogen, where sulfur atoms, if present, may be present as S, S(O) or S(O) 2 and where the saturated or unsaturated carbocyclic or heterocyclic second ring may also have 1 or 2 carbonyl groups or thiocarbonyl groups as ring members; R 2 is an optionally substituted aromatic radical selected from phenyl, C-bound mono- cyclic 5- or 6-membered heteroaryl or C-bound bicyclyl comprising a first ring which is a benzene ring or a 5- or 6-membered heteroaromatic ring and a second ring, which is fused to the first ring, where the second ring is a 5-, 6- or 7-membered carbocyclic ring or a 5-, 6- or 7-membered heterocyclic ring.
摘要翻译：本发明提供新的式（I）的2,3-二氢苯并嗪化合物及其盐。这些化合物抑制细胞增殖和细胞分裂，并且还在低氧条件下（I）抑制缺氧诱导因子（HIF）介导的转录和信号传导的活化，其中X是O或S（= O）n; n为0,1或2; R1是任选取代的C结合的双环，其包含第一环，其是苯环或具有1,2或3个氮原子作为杂原子环成员或1个氧或1个硫原子的5或6元杂芳环和0 ，1或2个氮原子作为杂原子环成员，和第二个环，其与第一个环稠合，其中第二个环是5-，6-或7-元碳环或5-，6-或7 含有1,2或3个选自氧，硫和氮的杂原子环成员的杂环，其中硫原子（如果存在）可以S，S（O）或S（O）2存在，其中饱和或不饱和的碳环或杂环第二环也可以具有1或2个羰基或硫代羰基作为环成员; R2是任选取代的芳基，其选自苯基，C-结合的单环5-或6-元杂芳基或C结合的双环，其包含第一环，其是苯环或5-或6-元杂芳环，第二个环与第一个环融合，其中第二个环是5-，6-或7-元的碳环或5-，6-或7-元杂环。

76. 发明申请

WO2012072977A8 FORMULATIONS COMPRISING METHYLTHIONINIUM CHLORIDE 审中-公开
标题翻译：包含甲基氯化铵的配方
公开(公告)号：WO2012072977A8
公开(公告)日：2012-09-20
申请号：PCT/GB2011001662
申请日：2011-11-30
申请人： WISTA LAB LTD , KHAN KARRAR AHMAD
发明人： KHAN KARRAR AHMAD
IPC分类号： A61K9/14 , A61K9/20 , A61K31/5415 , A61P25/28
CPC分类号： A61K31/5415 , A61K9/1652 , A61K9/20 , A61K9/2054 , A61K9/2095 , A61K9/4866 , C07D279/18
摘要： Solid dosage forms of methylthioninium chloride (MTC) further comprise at least one diluent suitable for direct compression. The MTC exists in a substantially pure and stable polymorphic form. The solid dosage forms may preferably be prepared by direct compression methods.
摘要翻译：甲基硫堇（MTC）的固体剂型还包含至少一种适于直接压制的稀释剂。 MTC以基本上纯且稳定的多晶型形式存在。固体剂型可优选通过直接压制方法制备。

77. 发明申请

WO2012072977A3 FORMULATIONS COMPRISING METHYLTHIONIUM CHLORIDE 审中-公开
标题翻译：包含甲基氯化铝的配方
公开(公告)号：WO2012072977A3
公开(公告)日：2012-08-16
申请号：PCT/GB2011001662
申请日：2011-11-30
申请人： WISTA LAB LTD , KHAN KARRAR AHMAD
发明人： KHAN KARRAR AHMAD
IPC分类号： A61K9/14 , A61K9/20 , A61K31/5415 , A61P25/28
CPC分类号： A61K31/5415 , A61K9/1652 , A61K9/20 , A61K9/2054 , A61K9/2095 , A61K9/4866 , C07D279/18
摘要： Solid dosage forms of methylthioninium chloride (MTC) further comprise at least one diluent suitable for direct compression. The MTC exists in a substantially pure and stable polymorphic form. The solid dosage forms may preferably be prepared by direct compression methods.
摘要翻译：甲基硫堇（MTC）的固体剂型还包含至少一种适于直接压制的稀释剂。 MTC以基本上纯且稳定的多晶型形式存在。固体剂型可优选通过直接压制方法制备。

78. 发明申请

WO2012061907A3 OSTEOCLAST ACTIVITY 审中-公开
公开(公告)号：WO2012061907A3
公开(公告)日：2012-05-18
申请号：PCT/BE2011/000064
申请日：2011-11-10
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN , GUNST, Jan , OWEN, Helen , VAN DEN BERGHE, Greet , VANHOREBEEK, Lise
发明人： GUNST, Jan , OWEN, Helen , VAN DEN BERGHE, Greet , VANHOREBEEK, Lise
IPC分类号： A61K31/13 , A61K31/436 , A61K31/5415 , A61P19/00
摘要： The invention relates to medicaments and novel methods of treating metabolic bone diseases, and more particularly for treating or preventing Critical Illness Related Metabolic Bone Disease or of critical illness induced Osteopenia [ICD-10 M85.8, ICD-9 733.90, DiseasesDB 29870 or MeSH D001851] secondary to ICU Admission by sufficient autophagy inducing compound to inhibit or suppressing critical illness [MeSH Descriptor: C23.550.291.625] enhanced osteoclastogenesis or increased osteoclast differentiation. The disclosed therapeutic methods include administering of a autophagy activating compound to a mammal to: (1) treat or prevent a bone degenerative disorder; (2) slow bone deterioration; (3) restore lost bone; (4) maintain bone mass and/or bone quality or (5) inhibit bone resorption in particularly by inhibiting or reducing a process by which osteoclasts break down bone and release the minerals resulting in a transfer of calcium from bone fluid to the blood. The invention also provides methods for administering the autophagy activating compound to treat a bone disorder of hyperresorption of bone and/or enhanced activation of osteoclasts.

79. 发明申请

WO2012033983A2 CANDESARTAN PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译： CANDESARTAN药物组合物
公开(公告)号：WO2012033983A2
公开(公告)日：2012-03-15
申请号：PCT/US2011050938
申请日：2011-09-09
申请人： REDDYS LAB LTD DR , REDDYS LAB INC DR , SUSEENDHARNATH AMARNATH , JOSHI VENKATESH MADHAVACHARYA , BEERAM SUNIL REDDY , VOBALABOINA VENKATESWARLU , BHAGWATWAR HARSHAL PRABHAKAR , CHAWLA MANISH
发明人： SUSEENDHARNATH AMARNATH , JOSHI VENKATESH MADHAVACHARYA , BEERAM SUNIL REDDY , VOBALABOINA VENKATESWARLU , BHAGWATWAR HARSHAL PRABHAKAR , CHAWLA MANISH
IPC分类号： A61K9/20 , A61K9/28 , A61K31/41 , A61K31/5415 , A61K47/38
CPC分类号： A61K31/4184 , A61K9/2013 , A61K9/2054 , A61K9/2095 , A61K45/06
摘要： Oral pharmaceutical compositions comprising candesartan or its pharmaceutically acceptable salts, esters, solvates, hydrates, enantiomers, polymorphs, or their mixtures, and processes for preparing the same are described. Also described are pharmaceutical formulations comprising compositions containing candesartan or an ester thereof, processes for preparing the formulations, and methods of use, treatment, and administration involving the formulations.
摘要翻译：描述了包含坎地沙坦或其药学上可接受的盐，酯，溶剂合物，水合物，对映异构体，多晶型物或它们的混合物的口服药物组合物，以及制备它们的方法。还描述了包含含有坎地沙坦或其酯的组合物的药物制剂，制备该制剂的方法以及涉及该制剂的使用，治疗和施用方法。

80. 发明申请

WO2012009542A2 METHODS FOR ALLEVIATING CHRONIC PAIN AND IMPROVING PERFORMANCE OF CATTLE UNDERGOING DEHORNING OR CASTRATION 审中-公开
标题翻译：缓解慢性疼痛的方法和提高嗅觉抑制效果的方法
公开(公告)号：WO2012009542A2
公开(公告)日：2012-01-19
申请号：PCT/US2011044017
申请日：2011-07-14
申请人： UNIV KANSAS STATE , COETZEE JOHANN F , KUKANICH STANLEY P
发明人： COETZEE JOHANN F , KUKANICH STANLEY P
IPC分类号： A61K31/5415
CPC分类号： A61K31/5415 , A01K17/00 , A23K20/10 , A23K20/168 , A23K50/10 , A23K50/60 , A61K31/19 , A61K31/197 , A61K2300/00
摘要： Methods of improving performance, increasing weight gain, and decreasing incidence of disease in ruminant and pre-ruminant animals, such as cattle, after undergoing painful processing procedures, such as castration and dehorning, are provided. Veterinary formulations for use in methods of the invention are also provided. The formulations comprise a compound selected from the group consisting of meloxicam, gabapentin, the pharmaceutically acceptable salts thereof, and combinations thereof. Methods of treating pathological pain in cattle are also provided.
摘要翻译：提供了在经过痛苦的加工过程如阉割和阉割之后改善反刍动物和反刍动物如牛的性能，增加体重增加和降低发病率的方法。还提供了用于本发明方法的兽用制剂。制剂包含选自美洛昔康，加巴喷丁，其药学上可接受的盐及其组合的化合物。还提供了治疗牛的病理性疼痛的方法。

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