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1. 发明专利

JP2012153725A Crystalline form of quinolinone-carboxamide compound 审中-公开
标题翻译：喹啉酮羧酰胺化合物的结晶形式
公开(公告)号：JP2012153725A
公开(公告)日：2012-08-16
申请号：JP2012113464
申请日：2012-05-17
申请人： Theravance Inc , セラヴァンス, インコーポレーテッド
发明人： FATHEREE PAUL R , TURNER S DEREK , GOLDBLUM ADAM , CHAO ROBERT , GENOV DANIEL
IPC分类号： C07D451/04 , A61K31/4709 , A61P1/04 , A61P1/10 , A61P43/00
CPC分类号： A61K31/46 , C07D451/04
摘要： PROBLEM TO BE SOLVED: To provide crystalline salt forms of a quinolinone-carboxamide compound which are useful as 5-HTreceptor agonists.SOLUTION: There are provided a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. There are also provided pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HTreceptor activity, and processes useful for preparing such crystalline salt forms.
摘要翻译：待解决的问题：提供可用作5-HT / 4>受体激动剂的喹啉酮 - 甲酰胺化合物的结晶盐形式。解决方案：提供1-异丙基-2-氧代-1,2-二氢喹啉-3-羧酸ä（1S，3R，5R）-8 - [（R）-2-羟基 -3-（甲磺酰基 - 甲基 - 氨基）丙基] -8-氮杂双环[3.2.1]辛-3-基}酰胺或其溶剂合物。还提供了包含这种结晶盐形式的药物组合物，使用这种结晶盐形式治疗与5-HT 4> />受体活性相关的疾病的方法，以及可用于制备这种结晶盐盐形式。版权所有（C）2012，JPO＆INPIT

2. 发明专利

JP2011001390A Use of echinocandin antifungal agent in combination with glycopeptide antibacterial agent 审中-公开
标题翻译： ECHINOCANDIN抗真菌药物与糖尿病抗菌药物联合使用
公开(公告)号：JP2011001390A
公开(公告)日：2011-01-06
申请号：JP2010227982
申请日：2010-10-07
申请人： Theravance Inc , セラヴァンス, インコーポレーテッド
发明人： KANIGA KONE
IPC分类号： A61K38/00 , A61K31/33 , A61K38/12 , A61P31/10 , A61P43/00
CPC分类号： A61K38/12 , A61K31/33 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide new methods of administering an echinocandin antifungal agent while reducing the side-effects by the agent, and to provide new methods and compositions that enhance the efficacy of such antifungal agents thereby permitting such agents to be administered in reduced amounts.SOLUTION: The invention relates to methods of administering the echinocandin antifungal agent in combination with a glycopeptide antibacterial agent having a substituent comprising at least about 8 carbon atoms. The invention also relates to methods of using the echinocandin antifungal agent combined with a predetermined glycopeptide antibacterial agent to treat fungal infections, and to compositions, kits and systems comprising the echinocandin antifungal agent and a specified glycopeptide antibacterial agent. Further, the invention relates to the use of the echinocandin antifungal agent and the glycopeptide antibacterial agent having the substituent comprising at least 8 carbon atoms in production of medicines for treating fungal infections.
摘要翻译：要解决的问题：提供施用棘皮菌素抗真菌剂同时减少药物副作用的新方法，并提供增强这些抗真菌剂的功效的新方法和组合物，从而允许以减少的量给予这些药剂解决方案：本发明涉及将棘皮菌素抗真菌剂与具有至少约8个碳原子的取代基的糖肽抗菌剂组合施用的方法。本发明还涉及使用与预定的糖肽抗菌剂组合的棘白菌素抗真菌剂治疗真菌感染的方法，以及包含棘白菌素抗真菌剂和特定糖肽抗菌剂的组合物，试剂盒和系统的方法。此外，本发明涉及棘孢菌素抗真菌剂和具有至少8个碳原子的取代基的糖肽抗菌剂在制备用于治疗真菌感染的药物中的用途。

3. 发明专利

JP2009256358A Cross-linked glycopeptide-cephalosporin antibiotic 审中-公开
标题翻译：交联糖蛋白抗生素抗生素
公开(公告)号：JP2009256358A
公开(公告)日：2009-11-05
申请号：JP2009144705
申请日：2009-06-17
申请人： Theravance Inc , セラヴァンス, インコーポレーテッド
发明人： MARQUESS DANIEL , LINSELL MARTIN S , TURNER DEREK S , TRAPP SEAN G , LONG DANIEL D , FATHEREE PAUL
IPC分类号： C07K7/06 , A61K38/00 , A61P31/04 , C07K9/00
CPC分类号： C07K9/008 , A61K38/00
摘要： PROBLEM TO BE SOLVED: To provide cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof, which are useful as antibiotics. SOLUTION: Provided are pharmaceutical compositions containing a specific cross-linked glycopeptide-cephalosporin compound; methods for treating bacterial infections in mammals and using such compounds; and processes and intermediates useful for preparing such compounds. When a vancomycin analogue is employed in the compounds, the binding site for crosslinking is amino acid 7 (AA-7) at position C-29. The position is also sometimes referred to as the "7d" or the "resorcinol" position of vancomycin. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供可用作抗生素的交联糖肽 - 头孢菌素化合物及其药学上可接受的盐。解决方案：提供含有特异性交联糖肽 - 头孢菌素化合物的药物组合物; 用于治疗哺乳动物细菌感染和使用这些化合物的方法; 以及可用于制备这些化合物的方法和中间体。当化合物中使用万古霉素类似物时，用于交联的结合位点是C-29位的氨基酸7（AA-7）。该位置有时也被称为万古霉素的“7d”或“间苯二酚”位置。版权所有（C）2010，JPO＆INPIT

4. 发明专利

JP2008285486A Short-acting sedative hypnotic agent for anesthesia and sedation 有权
标题翻译：短期用于麻醉和消化的消炎药
公开(公告)号：JP2008285486A
公开(公告)日：2008-11-27
申请号：JP2008126538
申请日：2008-05-13
申请人： Theravance Inc , セラヴァンス, インコーポレーテッド
发明人： JENKINS THOMAS E , AXT SABINE , BOLTON JENNIFER
IPC分类号： C07C235/06 , A61K31/16 , A61P23/00 , A61P25/20
摘要： PROBLEM TO BE SOLVED: To provide compounds, compositions, and methods useful for inducing or maintaining general anesthesia or sedation in mammals.
SOLUTION: The compounds of formula (I) and the compounds of formula (II) can be used for preparing drugs useful for inducing or maintaining anesthesia or sedation in mammals. The drugs can further comprise a therapeutic agent selected from the group consisting of another sedative hypnotic agent, an analgesic, and a paralytic agent.
COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：要解决的问题：提供可用于诱导或维持哺乳动物全身麻醉或镇静的化合物，组合物和方法。解决方案：式（I）化合物和式（II）化合物可用于制备用于诱导或维持哺乳动物麻醉或镇静的药物。药物可以进一步包含选自另一种镇静催眠剂，止痛剂和麻痹剂的治疗剂。版权所有（C）2009，JPO＆INPIT

5. 发明专利

JP2014139209A 4-[2-(2-fluorophenoxy methyl)phenyl]piperidine compounds 审中-公开
标题翻译： 4- [2-（2-氟甲氧基甲基）苯基]哌啶化合物
公开(公告)号：JP2014139209A
公开(公告)日：2014-07-31
申请号：JP2014048387
申请日：2014-03-12
申请人： Theravance Inc , セラヴァンス, インコーポレーテッド
发明人： LORI DZHIN PATTERSON , ERIC L STANGELAND , SHEILA ZIPFEL , LONG DANIEL D
IPC分类号： C07D211/22 , A61K31/451 , A61K45/00 , A61P3/04 , A61P9/00 , A61P13/10 , A61P15/10 , A61P15/12 , A61P19/02 , A61P25/04 , A61P25/14 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , C12Q1/02
CPC分类号： A61K31/4465 , C07D211/22 , C07D211/32
摘要： PROBLEM TO BE SOLVED: To provide compounds having activity as serotonin (5-HT) and norepinephrine (NE) reuptake inhibitors to treat chronic pain, such as neuropathic pain.SOLUTION: The invention relates to compounds represented by formula I, where a is 0-4; Ris independently halo or trifluoromethyl; Ris H, halogen, or alkyl; and Rare independently H, or halogen.
摘要翻译：要解决的问题：提供具有作为血清素（5-HT）和去甲肾上腺素（NE）再摄取抑制剂的作用的化合物以治疗慢性疼痛，例如神经性疼痛。解决方案：本发明涉及由式I表示的化合物，其中a为0 -4; R 1独立地为卤素或三氟甲基; R 1 H，卤素或烷基; 并且独立地为H或卤素。

6. 发明专利

JP2013047267A Cross-linked glycopeptide-cephalosporin antibiotics 审中-公开
标题翻译：交联糖蛋白-CEPHALOSPORIN抗生素
公开(公告)号：JP2013047267A
公开(公告)日：2013-03-07
申请号：JP2012252018
申请日：2012-11-16
申请人： Theravance Inc , セラヴァンス, インコーポレーテッド
发明人： FATHEREE PAUL R , LINSELL MARTIN S , MARQUESS DANIEL , TRAPP SEAN G , MORAN EDMUND J , AGGEN JAMES B
IPC分类号： C07K7/06 , A61K31/546 , A61K38/00 , A61K38/14 , A61P31/04 , C07D501/00 , C07K7/64 , C07K9/00
CPC分类号： C07K7/64 , C07D501/00 , C07K9/008
摘要： PROBLEM TO BE SOLVED: To provide new antibiotics that are highly effective against antibiotic-resistant strains.SOLUTION: This invention provides a novel cross-linked glycopeptide-cephalosporin compound useful as an antibiotic and a pharmaceutically-acceptable salt thereof. This invention also provides a pharmaceutical composition containing the compound, a method of treating a bacterial infection in a mammal, and a process and intermediate useful for preparing the compound. This invention provides a novel cross-linked glycopeptide-cephalosporin compound useful as an antibiotic. The compound has a unique chemical structure in which a glycopeptide is covalently linked to a pyridinium moiety of a cephalosporin. Among other properties, the compound possesses surprising and unexpected potency against Gram-positive bacteria including methicillin-resistant Staphylococci aureus (MRSA).
摘要翻译：要解决的问题：提供对抗生素抗性菌株高度有效的新型抗生素。解决方案：本发明提供了可用作抗生素及其药学上可接受的盐的新型交联糖肽 - 头孢菌素化合物。本发明还提供含有该化合物的药物组合物，治疗哺乳动物细菌感染的方法，以及可用于制备该化合物的方法和中间体。本发明提供了可用作抗生素的新型交联糖肽 - 头孢菌素化合物。该化合物具有独特的化学结构，其中糖肽与头孢菌素的吡啶鎓部分共价连接。除其他性质外，化合物对革兰氏阳性菌（包括耐甲氧西林金黄色葡萄球菌（MRSA））具有令人惊讶和意想不到的效力。版权所有（C）2013，JPO＆INPIT

7. 发明专利

JP2011225617A BIPHENYL DERIVATIVE HAVING β2 ADRENERGIC RECEPTOR AGONIST AND MUSCARINIC RECEPTOR ANTAGONIST ACTIVITY 有权
标题翻译：具有β2ADRENERGIC受体激动剂和MUSCARINIC受体拮抗剂活性的BIPHENYL衍生物
公开(公告)号：JP2011225617A
公开(公告)日：2011-11-10
申请号：JP2011172162
申请日：2011-08-05
申请人： Theravance Inc , セラヴァンス, インコーポレーテッド
发明人： MAMMEN MATHAI , DUNHAM SARAH , HUGHES ADAM , LEE TAE WEON , HUSFELD CRAIG , STANGELAND ERIC , CHEN YAN
IPC分类号： C07D211/46 , A61K31/445 , A61K31/4468 , A61K31/452 , A61K31/4709 , A61K45/00 , A61P11/00 , A61P11/06 , A61P11/08 , A61P43/00 , C07D211/48 , C07D211/58 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D453/02 , C07D471/08 , G01N33/94
CPC分类号： C07D211/46 , A61K31/445 , A61K31/452 , C07D211/48 , C07D211/58 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/06 , C07D409/12 , C07D453/02 , C07D471/08 , G01N33/9433
摘要： PROBLEM TO BE SOLVED: To provide new biphenyl derivatives that are useful for treating pulmonary disorders.SOLUTION: There are provided biphenyl derivatives of formula I or pharmaceutically acceptable salts, solvates, or stereoisomers thereof. In formula I, R, R, R, R, R, R, R, W, a, b, and c are as defined in the specification. The biphenyl derivatives have both βadrenaline receptor agonistic activity and muscarinic receptor antagonistic activity, and such biphenyl derivatives are useful for treating pulmonary disorders (for example, chronic obstructive pulmonary disease and asthma).
摘要翻译：待解决的问题：提供可用于治疗肺部疾病的新型联苯衍生物。提供式I的联苯衍生物或其药学上可接受的盐，溶剂合物或立体异构体。在公式I中，R 1 ，R 2 ，R 3 4 ，R 5 ，R 6 ，R 7 ，W，a，b和c如说明书中所定义。联苯衍生物具有β 2 肾上腺素受体激动活性和毒蕈碱受体拮抗作用，并且这种联苯衍生物可用于治疗肺部疾病（例如慢性阻塞性肺疾病和哮喘）。版权所有（C）2012，JPO＆INPIT

8. 发明专利

JP2011219500A Biphenyl compound useful as muscarinic receptor antagonist 审中-公开
标题翻译：联苯化合物有效作为MUSCARINIC受体拮抗剂
公开(公告)号：JP2011219500A
公开(公告)日：2011-11-04
申请号：JP2011171399
申请日：2011-08-04
申请人： Theravance Inc , セラヴァンス, インコーポレーテッド
发明人： MAMMEN MATHAI , JI YU-HUA , MU YONGQI , HUSFELD CRAIG , LI LI
IPC分类号： C07D211/60 , A61K31/4545 , A61K31/573 , A61K45/00 , A61P11/00 , A61P29/00 , A61P43/00 , C07D211/62
摘要： PROBLEM TO BE SOLVED: To provide a new muscarinic receptor antagonist that has high efficacy and reduced systemic side effects when administered by inhalation.SOLUTION: A compound represented by formula (I) is provided. The compound represented by formula (I) is a muscarinic receptor antagonist. A pharmaceutical composition containing such a compound, a method for preparing such a compound and an intermediate, and a method for treating lung disorders using such a compound are also provided.
摘要翻译：待解决的问题：提供一种新的毒蕈碱受体拮抗剂，其通过吸入给药时具有高效力和降低的全身副作用。解决方案：提供由式（I）表示的化合物。由式（I）表示的化合物是毒蕈碱受体拮抗剂。还提供含有这种化合物的药物组合物，这种化合物的制备方法和中间体，以及使用这种化合物治疗肺病的方法。版权所有（C）2012，JPO＆INPIT

9. 发明专利

JP2011016848A DIARYLMETHYL COMPOUND AND RELATED COMPOUND HAVING β2 ADRENERGIC RECEPTOR AGONIST ACTIVITY AND MUSCARINIC RECEPTOR ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有β2ADRENERGIC受体激动剂活性和MUSCARINIC受体拮抗剂活性的二异喹啉化合物及相关化合物
公开(公告)号：JP2011016848A
公开(公告)日：2011-01-27
申请号：JP2010233130
申请日：2010-10-15
申请人： Theravance Inc , セラヴァンス, インコーポレーテッド
发明人： MAMMEN MATHAI , HUGHES ADAM
IPC分类号： C07D207/09 , A61K31/40 , A61K31/4709 , A61K45/00 , A61P11/00 , A61P11/06 , A61P11/08 , A61P43/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14
CPC分类号： C07D401/12 , C07D207/04 , C07D207/09 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14
摘要： PROBLEM TO BE SOLVED: To provide a new diarylmethyl compound and related compounds useful for treating pulmonary disorders.SOLUTION: There are provided compounds represented by formula (I), or a pharmaceutically acceptable salt, or solvate or stereoisomer thereof. The compounds have both of βadrenergic receptor agonist activity and muscarinic receptor antagonist activity. The compounds are useful for treating pulmonary disorders (for example, chronic obstructive pulmonary disease and asthma).
摘要翻译：要解决的问题：提供新的二芳基甲基化合物和可用于治疗肺部疾病的相关化合物。解决方案：提供由式（I）表示的化合物或其药学上可接受的盐或溶剂合物或立体异构体。该化合物具有β-肾上腺素能受体激动剂活性和毒蕈碱受体拮抗剂活性。该化合物可用于治疗肺部疾病（例如慢性阻塞性肺疾病和哮喘）。

10. 发明专利

JP2008231109A Glycopeptide antibiotic composition containing cyclodextrin 审中-公开
标题翻译：含有CYCLODEXTRIN的甘氨酸抗生素组合物
公开(公告)号：JP2008231109A
公开(公告)日：2008-10-02
申请号：JP2008097622
申请日：2008-04-03
申请人： Theravance Inc , セラヴァンス, インコーポレーテッド
发明人： JUDICE J KEVIN , SHAW JENG-PYNG , MU YONGQI , CONNER MICHAEL W , PACE JOHN L
IPC分类号： A61K38/00 , A61K47/40 , A61K9/00 , A61K9/02 , A61K9/14 , A61K9/19 , A61K9/20 , A61K9/48 , A61K47/06 , A61K47/12 , A61K47/26 , A61K47/48 , A61K51/08 , A61P31/04 , C07F9/38 , C07K1/113 , C07K9/00
CPC分类号： B82Y5/00 , A61K9/0014 , A61K9/0019 , A61K9/0095 , A61K9/02 , A61K9/19 , A61K9/2018 , A61K9/4858 , A61K31/724 , A61K38/14 , A61K47/06 , A61K47/12 , A61K47/26 , A61K47/40 , A61K47/6951 , C07K9/008
摘要： PROBLEM TO BE SOLVED: To provide a new pharmaceutical composition containing a glycopeptide antibiotic reducing undesirable characteristics. SOLUTION: The composition contains a cyclodextrin and a lipidated glycopeptide antibiotic or pharmaceutically acceptable salt thereof. The pharmaceutical composition contains aqueous cyclodextrin carrier, a therapeutically effective amount of a lipidated glycopeptide antibiotic or pharmaceutically acceptable salt thereof. The composition optionally contains water, or may be a powder or a freeze-dried powder. COPYRIGHT: (C)2009,JPO&INPIT

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