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111. 发明授权

US6025360A Use of theophylline for the manufacture of a medicament for the treatment of asthma 失效
标题翻译：茶碱用于制造用于治疗哮喘的药物的用途
公开(公告)号：US6025360A
公开(公告)日：2000-02-15
申请号：US652495
申请日：1996-09-06
申请人： Allan John Miller , Christopher John McDonald , Michael Court
发明人： Allan John Miller , Christopher John McDonald , Michael Court
IPC分类号： C07D473/08 , A61K31/52 , A61K31/522 , A61P11/08 , C07D473/10
CPC分类号： A61K31/52
摘要： A prophylactic treatment for the inflammatory condition associated with chronic asthma is disclosed comprising administering theophyline or pharmaceutically acceptable salts thereof to provide a mean steady state plasma level of 1 to less than 5 mg/L.
摘要翻译： PCT No.PCT / GB94 / 02657 371日期1996年9月6日 102（e）日期1996年9月6日PCT 1994年12月5日PCT公布。出版物WO95 / 15164 日期：1995年6月8日公开了与慢性哮喘相关的炎性疾病的预防性治疗，其包括施用所述茶碱或其药学上可接受的盐以提供1至小于5mg / L的平均稳态血浆水平。

112. 发明授权

US5977119A Trisubstituted thioxanthines 失效
标题翻译：三取代噻吨烷
公开(公告)号：US5977119A
公开(公告)日：1999-11-02
申请号：US931849
申请日：1997-09-15
申请人： David John Cavalla , Peter Hofer , Mark Chasin
发明人： David John Cavalla , Peter Hofer , Mark Chasin
IPC分类号： A61K31/522 , A61P11/06 , A61P25/24 , A61P25/28 , A61P29/00 , A61P37/08 , A61P43/00 , C07D473/18 , C07D473/20 , C07D473/22 , C07D473/38 , A61K31/52 , C07D239/56
CPC分类号： C07D473/18 , C07D473/20 , C07D473/22 , C07D473/38
摘要： Disclosed are compounds of the formula: ##STR1## wherein R.sup.1, R.sup.3 and R.sup.8 are independently alkyl, aryl or aralkyl, and R.sup.2 is selected from the group consisting of S and O, R.sup.6 is selected from the group consisting of S and O, provided that R.sup.2 and R.sup.6 are not both O. The compounds are effective PDE IV inhibitors and possess improved PDE IV inhibition and improved selectivity with regard to PDE III inhibition. Methods of treatment using the compounds are also disclosed.
摘要翻译：公开了下式的化合物：其中R1，R3和R8独立地是烷基，芳基或芳烷基，R2选自S和O，R6选自S和O，条件是R2和 R6不是都是O.化合物是有效的PDE IV抑制剂，并具有改善的PDE IV抑制和改善PDE III抑制的选择性。还公开了使用该化合物的治疗方法。

113. 发明授权

US5968547A Method of providing sustained analgesia with buprenorphine 失效
公开(公告)号：US5968547A
公开(公告)日：1999-10-19
申请号：US939068
申请日：1997-09-29
申请人： Robert F. Reder , Paul D. Goldenheim , Robert F. Kaiko
发明人： Robert F. Reder , Paul D. Goldenheim , Robert F. Kaiko
IPC分类号： A61F13/00 , A61K9/22 , A61K9/70 , A61K31/00 , A61K31/485 , A61P25/00 , A61P29/00
CPC分类号： A61K31/4748 , A61K31/485 , A61K9/0014 , A61K9/0019 , A61K9/7023 , A61K9/7053 , A61K9/7061
摘要： A method of effectively treating pain in humans is achieved by administering buprenorphine in accordance with first order kinetics over an initial three-day dosing interval, such that a maximum plasma concentration from about 20 pg/ml to about 1052 pg/ml is attained, and thereafter maintaining the administration of buprenorphine for at least an additional two-day dosing interval in accordance with substantially zero order kinetics, such that the patients experience analgesia throughout the at least two-day additional dosing interval.

114. 发明授权

US5965161A Extruded multi-particulates 失效
标题翻译：挤出多颗粒
公开(公告)号：US5965161A
公开(公告)日：1999-10-12
申请号：US334209
申请日：1994-11-04
申请人： Benjamin Oshlack , Mark Chasin , Hua-Pin Huang
发明人： Benjamin Oshlack , Mark Chasin , Hua-Pin Huang
IPC分类号： A61K20060101 , A61K9/14 , A61K9/16 , A61K9/20 , A61K9/22 , A61K9/26 , A61K9/52 , A61K31/135 , A61K31/485 , A61K47/00 , A61K47/10 , A61K47/12 , A61K47/32 , A61K47/38 , A61K47/44 , A61K47/46
CPC分类号： A61K9/1635 , A61K9/1617 , A61K9/1652 , A61K9/1694 , A61K9/2018 , A61K9/2027 , A61K9/2077 , A61K9/2081 , A61K9/2095 , A61K9/145 , Y10S514/951 , Y10S514/962
摘要： A unit dose sustained-release oral dosage form containing a plurality of melt-extruded particles, each consisting essentially of a therapeutically active agent, one or more retardants, and an optional water-insoluble binder is disclosed. The particles have a length of from about 0.1 to about 12 mm and can be of varying diameters and each unit dose provides a release of therapeutically active agents over at least about 8 hours. Methods of preparing the unit doses as well as extrusion processes and methods of treatment are also disclosed.
摘要翻译：公开了包含多个熔融挤出颗粒的单位剂量持续释放口服剂型，每个主要由治疗活性剂，一种或多种阻滞剂和任选的水不溶性粘合剂组成。颗粒具有约0.1至约12mm的长度，并且可以具有不同的直径，并且每个单位剂量在至少约8小时内提供治疗活性剂的释放。还公开了制备单位剂量的方法以及挤出方法和治疗方法。

115. 发明授权

US5942241A Formulations and methods for providing prolonged local anesthesia 失效
标题翻译：提供延长局部麻醉的制剂和方法
公开(公告)号：US5942241A
公开(公告)日：1999-08-24
申请号：US793861
申请日：1997-06-16
申请人： Mark Chasin , Richard Sackler , Ronald M. Burch , Paul Goldenheim , Joseph Tigner
发明人： Mark Chasin , Richard Sackler , Ronald M. Burch , Paul Goldenheim , Joseph Tigner
IPC分类号： A61K9/107 , A61K9/00 , A61K9/14 , A61K9/16 , A61K9/52 , A61K31/135 , A61K31/415 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/465 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/54 , A61K31/55 , A61K31/57 , A61K31/715 , A61K45/06 , A61K47/02 , A61K47/34 , A61K47/36 , A61K47/42 , A61P25/02 , A61P43/00
CPC分类号： A61K31/704 , A61K31/445 , A61K31/465 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/54 , A61K31/55 , A61K31/57 , A61K31/715 , A61K45/06 , A61K47/02 , A61K47/36 , A61K9/0019 , A61K9/1647 , A61K9/0024 , Y10S514/817 , Y10S514/818 , Y10S514/93
摘要： A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible local anesthesia when implanted or injected in a patient, and a pharmaceutically acceptable, i.e., non-toxic, non-glucocorticoid augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without the augmenting agent.
摘要翻译： PCT No.PCT / US96 / 10439 Sec。 371日期：1997年6月16日 102（e）日期1996年6月16日PCT提交1996年6月7日PCT公布。公开号WO96 / 41616 日期1996年12月27日一种用于在患者中诱导持续局部局部麻醉的制剂和方法，包括含有局部麻醉剂和有效量的生物相容性，可生物降解的控制释放材料的底物，其延长局部麻醉剂从基质释放以获得植入或注射到患者中时的可逆局部麻醉，以及药学上可接受的，即无毒的非糖皮质激素增强剂，其有效地延长局部麻醉的持续时间长于可从底物获得的时间长增强剂。

116. 发明授权

US5864037A Methods for the synthesis of chemical compounds having PDE-IV inhibitory activity 失效
标题翻译：合成具有PDE-IV抑制活性的化合物的方法
公开(公告)号：US5864037A
公开(公告)日：1999-01-26
申请号：US659767
申请日：1996-06-06
申请人： Mark Chasin , David Cavalla , Peter Hofer
发明人： Mark Chasin , David Cavalla , Peter Hofer
IPC分类号： A61K31/52 , A61P11/08 , A61P29/00 , A61P43/00 , C07D473/34 , C07D473/22 , C07D473/40
CPC分类号： C07D473/34
摘要： Disclosed is a process for the preparation of a compound of Formula IV having the structure: ##STR1## wherein R.sub.6 is N(R.sub.6a)(R.sub.6b);R.sub.3 represents a C.sub.2-8, alkyl which is unbranched or branched and unsubstituted or substituted; C.sub.3-8 cycloalkyl which is unsubstituted or substituted; C.sub.4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubstituted or substituted; aryl or benzyl which is optionally unsubstituted or substituted; ar(C.sub.1-4)alkyl; a heterocyclyl group, ring optionally substituted; heterocyclyl (C.sub.1 -C.sub.4) alkyl ring optionally substituted;which comprises:(a) treating a compound of Formula I: ##STR2## with an effective amount of a dethionating agent to produce a compound of Formula II: ##STR3## (b) treating a compound of Formula II with an effective halogenating agent under conditions effective to produce a compound of Formula III: ##STR4## and (c) treating a compound of Formula III with an effective aminating agent under conditions effective to produce a compound of Formula IV.
摘要翻译：公开了制备式IV化合物的方法，其具有以下结构：其中R 6为N（R 6a）（R 6b）; R3表示C2-8烷基，其为无支链或未支链且未被取代或取代的; 未取代或取代的C 3-8环烷基; C4-8环烷基烷基，其中环烷基部分是未取代或取代的; 任选未取代或取代的芳基或苄基; 芳（C 1-4）烷基; 杂环基，任选取代的环; 任选取代的杂环基（C 1 -C 4）烷基; 其包括：（a）用有效量的去离子体处理式I的化合物：I，以产生式II的化合物：（b）用有效的卤化剂处理式II的化合物在有效产生式III化合物的条件下：（III）和（c）在有效制备式IV化合物的条件下用有效的胺化剂处理式III化合物。

117. 发明授权

US5744473A PDE IV inhibitors: "bis-compounds" 失效
标题翻译： PDE IV抑制剂：“双 - 化合物”
公开(公告)号：US5744473A
公开(公告)日：1998-04-28
申请号：US714581
申请日：1996-09-16
申请人： Mark Chasin , Peter Hofer , David Cavalla
发明人： Mark Chasin , Peter Hofer , David Cavalla
IPC分类号： C07D473/24 , C07D519/00 , A61K31/44 , A61K31/505 , A61K31/52
CPC分类号： C07D473/24
摘要： Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE V inhibition. Also provided is a process of making compounds of Formula I. Compounds of the present invention are represented by Formula I: ##STR1## its pharmaceutically acceptable salts, hydrochloride salts, or prodrug forms thereof, wherein: X.sub.1a, X.sub.1b are independently selected from --NH and --N-lower alkyl; X.sub.2a, X.sub.2b are optionally present and are independently selected from S(O)n, O, CH.sub.2, and NH; P.sub.1a, P.sub.1b, P.sub.2a, P.sub.2b, P.sub.4a, and P.sub.4b are independently selected from N, or CH; R.sub.1a, R.sub.1b, R.sub.2a, R.sub.2b, R.sub.3a and R.sub.3b are independently selected from H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 branched alkyl, C.sub.3 -C.sub.6 cycloalkyl, said alkyl groups being optionally substituted with halogen, aryl or heteroaryl group(s), said aryl and heteroaryl group(s) being optionally substituted with hydroxy, alkoxy, cycloalkoxy, halogen, alkyl, or cycloalkyl; and n is an integer from 0 to 2.
摘要翻译：公开了作为有效的PDE IV抑制剂的新型化合物。与茶碱或咯利普兰相比，该化合物具有改善的PDE IV抑制，关于例如PDE V抑制具有改善的选择性。还提供了制备式I化合物的方法。本发明化合物由式I表示：其盐，盐酸盐或其前药形式，其中：X1a，X1b独立地选自-NH和-N-低级烷基; X2a，X2b任选存在并且独立地选自S（O）n，O，CH 2和NH; P1a，P1b，P2a，P2b，P4a和P4b独立地选自N或CH; R1a，R1b，R2a，R2b，R3a和R3b独立地选自H，C1-C6烷基，C3-C6支链烷基，C3-C6环烷基，所述烷基任选被卤素，芳基或杂芳基取代，所述芳基和杂芳基任选被羟基，烷氧基，环烷氧基，卤素，烷基或环烷基取代; n为0〜2的整数。

118. 发明授权

US5733571A Transdermal patch for comparative evaluations 失效
标题翻译：用于比较评估的透皮贴剂
公开(公告)号：US5733571A
公开(公告)日：1998-03-31
申请号：US583234
申请日：1996-01-05
申请人： David Sackler
发明人： David Sackler
IPC分类号： A61K9/70 , A61F13/00
CPC分类号： A61K9/7069
摘要： A transdermal patch useful for evaluating the therapeutic effectiveness of a transdermally delivered medicinal agent is disclosed. The patch includes a substantially impermeable backing layer, a delivery layer containing a medicament and a substantially impermeable blocking layer. The delivery layer is arranged between the backing and blocking layers to prevent the release of the medicament contents from the delivery layer when the transdermal patch is affixed to the skin of a mammal. In alternative embodiments, non-transdermal placebo systems such as oral dosage forms which are coated with substantially impermeable layers to create virtually identical placebos of active oral delivery systems such as tablets, capsules and osmotic tablets are disclosed. Methods of comparing the therapeutic effectiveness of active dosage forms, i.e. transdermal units containing a medicament to placebo or to comparable active agents in either similar or different delivery systems are also disclosed.
摘要翻译：公开了一种用于评估经皮递送的药物的治疗有效性的透皮贴片。贴剂包括基本上不可渗透的背衬层，包含药物的输送层和基本上不可渗透的阻挡层。递送层布置在背衬层和阻挡层之间，以防止当透皮贴片固定在哺乳动物的皮肤上时药物内容物从输送层释放。在替代实施方案中，公开了非透皮安慰剂系统，例如涂覆有基本不渗透层的口服剂型，以形成实质上相同的活性口服递送系统如安慰剂，例如片剂，胶囊和渗透片。还公开了将活性剂型的治疗有效性，即含有药物的透皮单位与安慰剂或相似或不同递送系统中的可比活性剂进行比较的方法。

119. 发明授权

US5656295A Controlled release oxycodone compositions 失效
标题翻译：对照释放羟考酮组合物
公开(公告)号：US5656295A
公开(公告)日：1997-08-12
申请号：US618344
申请日：1996-03-19
申请人： Benjamin Oshlack , Mark Chasin , John Joseph Minogue , Robert Francis Kaiko
发明人： Benjamin Oshlack , Mark Chasin , John Joseph Minogue , Robert Francis Kaiko
IPC分类号： A61K9/20 , A61K9/22 , A61K31/485 , A61K9/26
CPC分类号： A61K9/2013 , A61K31/485 , A61K9/2027 , A61K9/2054
摘要： A method for substantially reducing the range in daily dosages required to control pain in approximately 90% of patients is disclosed whereby an oral solid controlled release dosage formulation having from about 10 to about 40 mg of oxycodone or a salt thereof is administered to a patient. The formulation provides a mean maximum plasma concentration of oxycodone from about 6 to about 60 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration from about 3 to about 30 ng/ml from about 10 to about 14 hours after repeated "q12h" (i.e., every 12 hour) administration through steady-state conditions. Another embodiment is directed to a method for substantially reducing the range in daily dosages required to control pain in substantially all patients by administering an oral solid controlled release dosage formulation comprising up to about 160 mg of oxycodone or a salt thereof, such that a mean maximum plasma concentration of oxycodone up to about 240 ng/ml from a mean of up to about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration up to about 120 ng/ml from about 10 to about 14 hours after repeated "q12h" (i.e., every 12 hour) administration through steady-state conditions are achieved. Controlled release oxycodone formulations for achieving the above are also disclosed.
摘要翻译：公开了一种用于大大减少约90％患者中控制疼痛所需的日剂量范围的方法，其中向患者施用具有约10至约40mg羟可待酮或其盐的口服固体控释剂量制剂。所述制剂提供给药后平均约2至约4.5小时约6至约60ng / ml的羟考酮的平均最大血浆浓度，并且平均最小血浆浓度为约3至约30ng / ml，约10 通过稳态条件重复“q12h”（即每12小时）至约14小时。另一个实施方案涉及通过施用包含高达约160mg羟考酮或其盐的口服固体控制释放剂量制剂来显着降低在基本上所有患者中控制疼痛所需的日剂量范围的方法，使得平均最大值在给药后平均高达约2至约4.5小时，羟考酮的血浆浓度高达约240ng / ml，重复“q12h”后约10至约14小时的平均最小血浆浓度高达约120ng / ml “（即每12小时一次）通过稳态条件实现。还公开了用于实现上述目标的控释羟考酮制剂。

120. 发明授权

US5508043A Controlled release matrix for pharmaceuticals 失效
标题翻译：药物控制释放基质
公开(公告)号：US5508043A
公开(公告)日：1996-04-16
申请号：US391837
申请日：1995-02-21
申请人： Thinnayam N. Krishnamurthy
发明人： Thinnayam N. Krishnamurthy
IPC分类号： A61K47/36 , A61K20060101 , A61K9/00 , A61K9/02 , A61K9/16 , A61K9/20 , A61K9/22 , A61K9/26 , A61K9/48 , A61K9/52 , A61K47/02 , A61K47/04 , A61K47/10 , A61K47/14
CPC分类号： A61K9/02 , A61K9/1611 , A61K9/1617 , A61K9/1652 , Y10S424/15 , Y10S514/965 , Y10S514/966
摘要： The controlled release of therapeutically active agents is achieved from a controlled release matrix of sodium alginate and a calcium salt. When the composition is to be administered rectally, the matrix is combined with a therapeutically active agent and a suitable suppository base. When the composition is to be administered orally, the matrix further includes a higher aliphatic alcohol.
摘要翻译：治疗活性剂的控制释放由藻酸钠和钙盐的控释基质获得。当组合物要直肠给药时，将基质与治疗活性剂和合适的栓剂基质组合。当组合物要口服给药时，基质还包括高级脂族醇。

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