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61. 发明授权

US08685418B2 Cyclohexylamines 有权
标题翻译：环己胺
公开(公告)号：US08685418B2
公开(公告)日：2014-04-01
申请号：US13659694
申请日：2012-10-24
申请人： Endo Pharmaceuticals, Inc.
发明人： Scott Kevin Thompson , Roger Astbury Smith , Sandeep Gupta , Tony Priestley , Nicholas James Laping , Ashis K. Saha , Sonali Rudra
IPC分类号： A61K9/00
CPC分类号： A61K31/40 , A61K31/215 , A61K31/235 , A61K31/24 , A61K31/351 , A61K31/381 , A61K45/06 , C07C63/49 , C07C65/26 , C07C219/12 , C07C219/14 , C07C2601/14 , C07D207/34 , C07D309/14 , C07D333/38 , C07D333/40 , C07D333/70 , C07D333/72 , A61K2300/00
摘要： The present application provides novel compounds and methods for preparing and using these compounds. These compounds are useful in treating pain, itch, overactive bladder and/or interstitial cystitis in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.
摘要翻译：本申请提供了用于制备和使用这些化合物的新型化合物和方法。这些化合物可用于通过向患者施用一种或多种化合物来治疗患者的疼痛，瘙痒，膀胱过度活动和/或间质性膀胱炎。所述方法包括施用式（I）化合物和TRPV1受体激活剂。在一个实施方案中，TRPV1受体激活剂是利多卡因。

62. 发明授权

US08679535B2 Sustained release matrix systems for highly soluble drugs 有权
标题翻译：用于高度可溶性药物的持续释放基质体系
公开(公告)号：US08679535B2
公开(公告)日：2014-03-25
申请号：US11729024
申请日：2007-03-27
申请人： Anand R. Baichwal , Troy W. McCall , Lirong Liu , Steve Labudzinski
发明人： Anand R. Baichwal , Troy W. McCall , Lirong Liu , Steve Labudzinski
IPC分类号： A61K9/14
CPC分类号： A61K31/554 , A61K9/167 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/205 , A61K9/2077 , A61K9/2846 , A61K9/2866
摘要： Disclosed are sustained release oral solid dosage forms comprising a therapeutically effective amount of a medicament having a solubility of more than about 10 g/l; a pH modifying agent; and a sustained release matrix comprising a gelling agent, said gelling agent comprising a heteropolysaccharide gum and a homopolysaccharide gum capable of cross-linking said heteropolysaccharide gum when exposed to an environmental fluid, said dosage form providing a sustained release of said medicament after oral administration to human patients.
摘要翻译：公开了持续释放的口服固体剂型，其包含治疗有效量的溶解度大于约10g / l的药物; pH调节剂; 以及包含胶凝剂的持续释放基质，所述胶凝剂包含杂多糖胶和能够在暴露于环境流体时交联所述杂多糖胶的均聚糖胶，所述剂型在口服给药后提供所述药物的持续释放人类病人。

63. 发明申请

US20140073782A1 Substituted Quinazoline and Pyrido-Pyrimidine Derivatives 审中-公开
标题翻译：取代喹唑啉和吡啶并嘧啶衍生物
公开(公告)号：US20140073782A1
公开(公告)日：2014-03-13
申请号：US14076765
申请日：2013-11-11
申请人： Endo Pharmaceuticals Inc.
发明人： Roger A. Smith , Scott Kevin Thompson , Subramanya Hosahalli , Mallesham Bejugam , Srinivas Nanduri , Sunil Kumar Panigrahi , Natarajan Mahalingam
IPC分类号： C07D471/04 , C07D405/04 , C07D409/04 , C07D295/155 , C07D401/14 , C07D403/04 , C07D401/04
CPC分类号： C07D239/72 , A61K31/535 , C07D239/42 , C07D295/155 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/14 , C07D471/04
摘要： The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
摘要翻译：本申请提供新的取代喹唑啉和吡啶并嘧啶化合物及其药学上可接受的盐。还提供了制备这些化合物的方法。通过向患者施用治疗有效量的一种或多种化合物，这些化合物可用于共同调节PI3K和/或mTOR活性。通过这样做，这些化合物在治疗与PI3K / AKT / mTOR途径失调相关的病症中是有效的。有利地，这些化合物表现为双重PI3K / mTOR抑制剂。可以使用这些化合物治疗各种病症，并且包括以炎症或异常细胞增殖为特征的疾病。在一个实施方案中，该疾病是癌症。

64. 发明申请

US20130085148A1 Pyridine Derivatives 有权
标题翻译：吡啶衍生物
公开(公告)号：US20130085148A1
公开(公告)日：2013-04-04
申请号：US13632006
申请日：2012-09-30
申请人： Endo Pharmaceuticals Inc.
发明人： Roger Astbury Smith , Nicholas James Laping , Raghava Reddy Kethiri , Chandregowda Venkateshappa , Bheemashankar Kulkarni , Purushottam Dewang , Rajendra Kristam , Rajesh Devraj
IPC分类号： A61K31/444 , C07D417/06 , A61K31/4439 , A61K31/497 , C07D401/14 , A61P5/26 , C07D417/14 , C07D413/06 , C07D417/08 , A61K31/4725 , A61P35/00 , C07D401/06 , C07D409/14
CPC分类号： C07D417/06 , C07D213/30 , C07D213/84 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D417/04 , C07D417/14
摘要： The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.
摘要翻译：本申请提供了新颖的吡啶化合物及其药学上可接受的盐或前药。还提供了制备这些化合物的方法。通过向患者施用治疗有效量的一种或多种化合物，这些化合物可用于抑制CYP17活性。通过这样做，这些化合物在治疗与CPY17活性相关的病症中是有效的。可以使用这些化合物治疗多种病症，并且包括以异常细胞增殖为特征的疾病。在一个实施方案中，该疾病是癌症，例如前列腺癌。

65. 发明授权

US07501452B2 Treatment of xerostomia 有权
标题翻译：口腔干燥症的治疗
公开(公告)号：US07501452B2
公开(公告)日：2009-03-10
申请号：US11605983
申请日：2006-11-29
申请人： Janice Mary Troha , Victoria Jean Abbas , Gary Joseph Rosenthal , Wren Henderson Schauer
发明人： Janice Mary Troha , Victoria Jean Abbas , Gary Joseph Rosenthal , Wren Henderson Schauer
IPC分类号： A61K31/195
CPC分类号： A61K31/198 , A61K9/006 , A61K9/06 , A61K31/381 , A61K31/426 , A61K33/04 , A61K47/10
摘要： Xerostomia is treated with a sulfur-containing antioxidant, such as N-acetylcysteine. Delivery compositions including polyoxyalkylene block copolymers may be used, which may be formulated to exhibit reverse-thermal viscosity behavior.
摘要翻译：口干燥剂用含硫抗氧化剂如N-乙酰半胱氨酸处理。可以使用包括聚氧化烯嵌段共聚物的递送组合物，其可以配制成表现出反向热粘性行为。

66. 发明申请

US20080262013A1 OXYMORPHONE CONTROLLED RELEASE FORMULATIONS 审中-公开
标题翻译：臭氧控制释放配方
公开(公告)号：US20080262013A1
公开(公告)日：2008-10-23
申请号：US12167859
申请日：2008-07-03
申请人： Huai-Hung Kao , Anand R. Baichwal , Troy McCall , David Lee
发明人： Huai-Hung Kao , Anand R. Baichwal , Troy McCall , David Lee
IPC分类号： A61K31/485 , A61P29/00
CPC分类号： A61K31/485 , A61K9/0053 , A61K9/2009 , A61K9/2018 , A61K9/205 , A61K9/2054 , A61K9/209 , A61K47/02 , A61K47/10 , A61K47/26 , A61K47/36 , A61K47/38
摘要： The invention pertains to a method of relieving pain by administering a controlled release pharmaceutical tablet containing oxymorphone which produces a mean minimum blood plasma level 12 to 24 hours after dosing, as well as the tablet producing the sustained pain relief.
摘要翻译：本发明涉及一种减轻疼痛的方法，该方法是通过施用含有羟吗啡酮的控释药物片剂，其在给药后12至24小时产生平均最低血浆水平，以及产生持续疼痛缓解的片剂。

67. 发明申请

US20080069881A1 Abuse-resistant controlled-release opioid dosage form 审中-公开
标题翻译：滥用耐药阿片类药物剂型
公开(公告)号：US20080069881A1
公开(公告)日：2008-03-20
申请号：US11901232
申请日：2007-09-14
申请人： Frank Caruso , Huai-Hung Kao
发明人： Frank Caruso , Huai-Hung Kao
IPC分类号： A61K31/485 , A61K9/14 , A61P25/36
CPC分类号： A61K31/485 , A61K9/0002 , A61K9/0053 , A61K9/20 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/48 , A61K9/4858 , A61K9/4866 , A61K31/46 , A61K2300/00
摘要： Abuse-resistant, controlled release opioid tablets are a combination containing an opioid antagonist such as naloxone at a level above that needed to suppress the euphoric effect of the opioid, if the combination were crushed to break the controlled release properties causing the opioid and opioid antagonist to be released as an immediate release product as a single dose. The controlled release nature of the tablet prevents the accumulation of orally effective amounts of opioid antagonist when taken normally. The opioid antagonist is contained in a controlled-release matrix and released, over time, with the opioid.
摘要翻译：滥用耐药的控制释放阿片类药物是含有阿片样物质拮抗剂如纳洛酮的组合，其水平高于抑制阿片样物质的欣快作用所需的水平，如果组合被粉碎以破坏控制释放性质，导致阿片样物质和阿片样物质拮抗剂作为单次剂量的即时释放产品释放。片剂的控制释放性质可防止口服有效量的阿片样物质拮抗剂在正常服用时积聚。阿片类拮抗剂包含在控释基质中，随着时间的推移与阿片样物质一起释放。

68. 发明申请

US20070281017A1 Sustained release oxycodone composition with acrylic polymer and metal hydroxide 审中-公开
标题翻译：缓释羟考酮组合物与丙烯酸聚合物和金属氢氧化物
公开(公告)号：US20070281017A1
公开(公告)日：2007-12-06
申请号：US11447714
申请日：2006-06-06
申请人： Huai-Hung Kao , Sou-Chan Chang , Yadi Zeng , Fai Jim
发明人： Huai-Hung Kao , Sou-Chan Chang , Yadi Zeng , Fai Jim
IPC分类号： A61K31/485 , A61K9/22 , A61K9/14
CPC分类号： A61K9/2027 , A61K9/2009
摘要： The invention is a controlled release composition comprising a therapeutic amount of an active ingredient in a controlled release matrix. The matrix comprises a combination of a pharmaceutically acceptable acrylic polymer and a metal hydroxide. The amount of metal hydroxide, relative to a given amount of acrylic polymer, is selected for and corresponds to a pre-determined release rate for said active ingredient. The compound is preferably used to provide controlled release dosage of oxycodone through a matrix of ammonio methacrylic polymer and magnesium hydroxide.
摘要翻译：本发明是一种控释组合物，其包含治疗量的受控释放基质中的活性成分。基质包含药学上可接受的丙烯酸类聚合物和金属氢氧化物的组合。选择相对于给定量的丙烯酸类聚合物的金属氢氧化物的量，并对应于所述活性成分的预定释放速率。该化合物优选用于通过氨基甲基丙烯酸聚合物和氢氧化镁的基质提供羟考酮的控制释放剂量。

69. 发明申请

US20070134328A1 OXYMORPHONE CONTROLLED RELEASE FORMULATIONS 有权
公开(公告)号：US20070134328A1
公开(公告)日：2007-06-14
申请号：US11680432
申请日：2007-02-28
申请人： Huai-Hung Kao , Anand Baichwal , Troy McCall , David Lee
发明人： Huai-Hung Kao , Anand Baichwal , Troy McCall , David Lee
IPC分类号： A61K31/485 , A61K9/22
CPC分类号： A61K31/485 , A61K9/0053 , A61K9/2009 , A61K9/2018 , A61K9/205 , A61K9/2054 , A61K9/209 , A61K47/02 , A61K47/10 , A61K47/26 , A61K47/36 , A61K47/38
摘要： The invention pertains to a method of relieving pain by administering a controlled release pharmaceutical tablet containing oxymorphone which produces a mean minimum blood plasma level 12 to 24 hours after dosing, as well as the tablet producing the sustained pain relief.

70. 发明申请

US20030124174A1 Method for treating non-neuropathic pain 审中-公开
标题翻译：治疗非神经性疼痛的方法
公开(公告)号：US20030124174A1
公开(公告)日：2003-07-03
申请号：US10045341
申请日：2001-10-25
申请人： Endo Pharmaceuticals, Inc
发明人： Bradley Stuart Galer
IPC分类号： A61K009/70 , A61K031/24
CPC分类号： A61K9/7023 , A61K31/167
摘要： A method including topically administering an effective amount of local anesthetic to a patient is disclosed. The method is effective for inducing analgesia for treating non-neuropathic pain. Non-neuropathic pain suitable for treatment according to the invention includes pain associated with sports injuries; sprains; strains; soft-tissue injury; repetitive motion injury; carpal tunnel syndrome; injury to tendons, ligament, and muscles; conditions such as fibromyalgia, bursitis, castrochondritis, myofascial pain, and pain associated with arthritis, inflammation, contusions, post-surgical pain, and nociceptive pain. Preferably, the lidocaine is applied via a transdermal patch applied near the locus of pain.
摘要翻译：公开了一种包括向患者局部施用有效量的局部麻醉剂的方法。该方法对于诱导止痛治疗非神经性疼痛是有效的。适用于根据本发明治疗的非神经性疼痛包括与运动损伤相关的疼痛; 扭伤菌株软组织损伤; 重复性运动损伤; 腕管综合症; 对肌腱，韧带和肌肉的损伤; 诸如纤维肌痛，滑囊炎，硬骨炎，肌筋膜疼痛和与关节炎相关的疼痛，炎症，挫伤，手术后疼痛和伤害性疼痛等疾病。优选地，利多卡因通过施加在疼痛位置附近的透皮贴剂施用。

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