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1. 发明授权

US5547950A Oxazolidinone antimicrobials containing substituted diazine moieties 失效
标题翻译：含有取代的二嗪部分的恶唑烷酮抗微生物剂
公开(公告)号：US5547950A
公开(公告)日：1996-08-20
申请号：US332822
申请日：1994-10-31
申请人： Douglas K. Hutchinson , Michael R. Barbachyn , Steven J. Brickner , Ronald B. Gammill , Mahesh V. Patel
发明人： Douglas K. Hutchinson , Michael R. Barbachyn , Steven J. Brickner , Ronald B. Gammill , Mahesh V. Patel
IPC分类号： A61K31/395 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/495 , A61K31/496 , A61K31/551 , A61P31/00 , A61P31/04 , C07D263/20 , C07D263/24 , C07D413/10 , C07D413/12 , C07D413/14 , C07D413/00
CPC分类号： C07D263/20 , C07D413/10 , C07D413/12
摘要： A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: each n is independently 1 to 3; Y is chosen from a-n as defined herein; wherein each occurrence of said C.sub.1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR.sup.1, CO.sub.2 R.sup.1, CN, SR.sup.1, or R.sup.1 (where R.sup.1 is a hydrogen or C.sub.1-4 alkyl); X and Z are independently C.sub.1-6 alkyl, C.sub.3-12 cycloalkyl or hydrogen, or X and Z form a C.sub.0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C.sub.1-6 alkyl, F, Cl, Br, hydrogen or a C.sub.1-6 alkyl substituted with one or more of F, Cl, Br or I, preferably U and V are F and W is hydrogen; R is hydrogen, C.sub.1-12 alkyl, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and q is 0 to 4 inclusive. Oxazolidinone derivatives possessing a substituted diazine moiety bonded to the N-aryl ring are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis and Mycobacterium avium.
摘要翻译：结构式I的化合物或其药学上可接受的盐，其中：每个n独立地为1至3; Y选自本文定义的a-n; 其中所述C 1-6烷基的每次出现可以被一个或多个F，Cl，Br，I，OR1，CO 2 R 1，CN，SR 1或R 1（其中R 1是氢或C 1-4烷基）取代; X和Z独立地是C 1-6烷基，C 3-12环烷基或氢，或X和Z形成C0-3桥连基，优选X和Z是氢; U，V和W独立地是C 1-6烷基，F，Cl，Br，氢或被F，Cl，Br或I中的一个或多个取代的C 1-6烷基，优选U和V是F，W是氢; R是氢，C 1-12烷基，C 3-12环烷基，C 1-6烷氧基，被一个或多个F，Cl，Br，I或OH取代的C 1-6烷基; q为0〜4。具有与N-芳基环结合的取代的二嗪部分的恶唑烷酮衍生物是有效的抗微生物剂，其对许多人类和兽医病原体有效，包括多重耐药性葡萄球菌和链球菌，以及厌氧生物体如杀菌剂和梭菌属物种，以及耐酸生物如结核分枝杆菌和鸟分枝杆菌。

2. 发明授权

US5700799A Oxazolidinone antimicrobials containing substituted diazine moieties 失效
标题翻译：含有取代的二嗪部分的恶唑烷酮抗微生物剂
公开(公告)号：US5700799A
公开(公告)日：1997-12-23
申请号：US610031
申请日：1996-03-04
申请人： Douglas K. Hutchinson , Michael R. Barbachyn , Steven J. Brickner , Ronald B. Gammill , Mahesh V. Patel
发明人： Douglas K. Hutchinson , Michael R. Barbachyn , Steven J. Brickner , Ronald B. Gammill , Mahesh V. Patel
IPC分类号： A61K31/395 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/495 , A61K31/496 , A61K31/551 , A61P31/00 , A61P31/04 , C07D263/20 , C07D263/24 , C07D413/10 , C07D413/12 , C07D413/14 , C07D245/02
CPC分类号： C07D263/20 , C07D413/10 , C07D413/12
摘要： A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: each n is independently 1 to 3; Y is choosen from a-n as defined herein; wherein each occurrence of said C.sub.1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR.sup.1, CO.sub.2 R.sup.1, CN, SR.sup.1, or R.sup.1 (where R.sup.1 is a hydrogen or C.sub.1-4 alkyl); X and Z are independently C.sub.1-6 alkyl, C.sub.3-12 cycloalkyl or hydrogen, or X and Z form a C.sub.0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C.sub.1-6 alkyl, F, Cl, Br, hydrogen or a C.sub.1-6 alkyl substituted with one or more of F, Cl, Br or I, preferably U and V are F and W is hydrogen; R is hydrogen, C.sub.1-12 alkyl, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and q is 0 to 4 inclusive. Oxazolidinone derivatives possessing a substituted diazine moiety bonded to the N-aryl ring are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis and Mycobacterium avium.
摘要翻译：结构式I的化合物或其药学上可接受的盐，其中：每个n独立地为1至3; 从本文定义的a-n中选择Y; 其中所述C 1-6烷基的每次出现可以被一个或多个F，Cl，Br，I，OR1，CO 2 R 1，CN，SR 1或R 1（其中R 1是氢或C 1-4烷基）取代; X和Z独立地是C 1-6烷基，C 3-12环烷基或氢，或X和Z形成C0-3桥连基，优选X和Z是氢; U，V和W独立地是C 1-6烷基，F，Cl，Br，氢或被F，Cl，Br或I中的一个或多个取代的C 1-6烷基，优选U和V是F，W是氢; R是氢，C 1-12烷基，C 3-12环烷基，C 1-6烷氧基，被一个或多个F，Cl，Br，I或OH取代的C 1-6烷基; q为0〜4。具有与N-芳基环结合的取代的二嗪部分的恶唑烷酮衍生物是有效的抗微生物剂，其对许多人类和兽医病原体有效，包括多重耐药性葡萄球菌和链球菌，以及厌氧生物体如杀菌剂和梭菌属物种，以及耐酸生物如结核分枝杆菌和鸟分枝杆菌。

3. 发明授权

US09107921B2 Oral dosage forms for oxygen containing active agents and oxyl-containing polymers 有权
标题翻译：含氧活性剂和含氧聚合物的口服剂型
公开(公告)号：US09107921B2
公开(公告)日：2015-08-18
申请号：US14555043
申请日：2014-11-26
申请人： Chandrashekar Giliyar , Satish Kumar Nachaegari , Chidambaram Machiappan , Mahesh V. Patel , Srinivasan Venkateshwaran
发明人： Chandrashekar Giliyar , Satish Kumar Nachaegari , Chidambaram Machiappan , Mahesh V. Patel , Srinivasan Venkateshwaran
IPC分类号： A61K31/485 , A61K31/194 , A61K31/4402 , A61K45/06 , A61K31/09 , A61K31/137 , A61K9/20
CPC分类号： A61K31/485 , A61K9/0053 , A61K9/2054 , A61K31/09 , A61K31/137 , A61K31/194 , A61K31/4402 , A61K45/06 , A61K2300/00
摘要： A pharmaceutical tablet for oral administration once every 12 hours is provided. The tablet includes a first active agent that is a tri-oxy active agent, a second active agent, and a release rate controlling non-ionic oxyl-containing hydrophilic polymer. The tablet is a matrix tablet and a single-dose administration of one or more tablets to a subject under fasted conditions provides a mean Cm˜ for each of the first active agent and the second active agent that is 70% to 135% of a respective mean Cm˜ provided by administering an immediate release oral dosage form to a subject under fasted conditions every 4 to 6 hours over a 12 hour time period, wherein cumulative dosage amounts administered over the 12 hour time period of each active agent is equivalent to the respective amount of each active agent in the pharmaceutical tablet.
摘要翻译：提供每12小时一次口服给药的药片。片剂包括第一活性剂，其为三氧基活性剂，第二活性剂和释放速率控制非离子含氧基的亲水性聚合物。片剂是基质片剂，并且在禁食条件下向受试者单剂量施用一种或多种片剂，为每种第一活性剂和第二活性剂提供平均Cm〜，其为相应的70％至135％平均Cm〜通过在禁食条件下每隔4至6小时在12小时时间内向受试者施用立即释放的口服剂型，其中在每个活性剂的12小时时间段内施用的累积剂量相当于相应的药物片剂中每种活性剂的量。

4. 发明申请

US20120244215A1 HIGH-STRENGTH TESTOSTERONE UNDECANOATE COMPOSITIONS 有权
标题翻译：高强度试验机组合物
公开(公告)号：US20120244215A1
公开(公告)日：2012-09-27
申请号：US13485807
申请日：2012-05-31
申请人： Chandrashekar Giliyar , Basawaraj Chickmath , Chidambaram Nachiappan , Mahesh V. Patel , Srinivansan Venkateshwaran
发明人： Chandrashekar Giliyar , Basawaraj Chickmath , Chidambaram Nachiappan , Mahesh V. Patel , Srinivansan Venkateshwaran
IPC分类号： A61K9/48 , A61P15/08 , A61K31/568
CPC分类号： A61K31/568 , A61K9/0053 , A61K9/4858 , A61K9/4875 , A61K47/12 , A61K47/22 , A61K47/44 , G01N33/743
摘要： The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods. The capsule includes a capsule shell and a capsule fill. The capsule fill can include a solubilizer and about 14 wt % to about 35 wt % testosterone undecanoate based on the total capsule fill. The oral dosage capsule is such that when a single oral administration to a male subject of one or more capsules with a total testosterone undecanoate daily dose of about 350 mg to about 650 mg it provides a ratio of serum testosterone Cmax to serum testosterone Cave of about 2.7 or less. In yet another embodiment, a method for providing a serum concentration of testosterone within a target serum testosterone concentration Cave range for a male subject is provided.
摘要翻译：本公开涉及含有十一酸睾酮的药物组合物和口服剂量胶囊以及相关方法。胶囊包括胶囊壳和胶囊填充物。基于总胶囊填充，胶囊填充物可以包含增溶剂和约14重量％至约35重量％的十一酸睾酮。口服剂量胶囊使得当向男性受试者单次口服给予一种或多种具有总睾酮十一烷酸酯的胶囊剂，每日剂量约350mg至约650mg时，其提供血清睾酮C max与血清睾酮的比例约为 2.7以下。在另一个实施方案中，提供了一种用于在目标血清睾酮浓度范围内为男性受试者提供睾酮血清浓度的方法。

5. 发明申请

US20120135074A1 High-Strength Testosterone Undecanoate Compositions 审中-公开
标题翻译：高强度睾酮非特异性组合物
公开(公告)号：US20120135074A1
公开(公告)日：2012-05-31
申请号：US12957206
申请日：2010-11-30
申请人： Chandrashekar Giliyar , Basawaraj Chickmath , Chidambaram Nachiappan , Mahesh V. Patel , Srinivansan Venkateshwaran
发明人： Chandrashekar Giliyar , Basawaraj Chickmath , Chidambaram Nachiappan , Mahesh V. Patel , Srinivansan Venkateshwaran
IPC分类号： A61K9/52 , A61K9/48 , A61P15/00 , A61K31/568
CPC分类号： A61K31/568 , A61K9/148 , A61K9/4875 , A61K47/12
摘要： The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods of treatment. In one embodiment, the present invention provides for a pharmaceutical composition that includes a therapeutically effective amount of testosterone undecanoate and a solubilizer. The testosterone undecanoate is solubilized in the composition and is present in an amount such that it comprises about 14 wt % to about 35 wt % of the total composition.
摘要翻译：本公开涉及含有十一酸睾酮的药物组合物和口服剂量胶囊以及相关的治疗方法。在一个实施方案中，本发明提供了包含治疗有效量的十一酸睾酮和增溶剂的药物组合物。十一酸睾酮被溶解在组合物中，并且存在的量使得它占总组合物的约14重量％至约35重量％。

6. 发明授权

US11304960B2 Steroidal compositions 有权
公开(公告)号：US11304960B2
公开(公告)日：2022-04-19
申请号：US12350930
申请日：2009-01-08
申请人： Chandrashekar Giliyar , Nachiappan Chidambaram , Mahesh V. Patel , Srinivasan Venkateshwaran
发明人： Chandrashekar Giliyar , Nachiappan Chidambaram , Mahesh V. Patel , Srinivasan Venkateshwaran
IPC分类号： A61K31/569 , A61K9/48 , A61K31/568 , A61K9/00 , A61K47/10 , A61K47/14 , A61K47/44
摘要： Provided herein are steroid containing compositions suitable for providing therapeutically effective amounts of at least one steroid to individuals. Also provided herein are compositions comprising testosterone and/or testosterone derivatives suitable for providing therapeutically effective and safe amounts of testosterone over periods of time. Further provided are methods of treating andro- and/or testosterone deficiency in individuals by administering to the individuals compositions described herein.

7. 发明申请

US20150018324A1 TESTOSTERONE UNDECANOATE COMPOSITIONS 审中-公开
公开(公告)号：US20150018324A1
公开(公告)日：2015-01-15
申请号：US14500498
申请日：2014-09-29
申请人： Basawaraj Chickmath , Chandrashekar Giliyar , Chidambaram Nachiappan , Mahesh V. Patel , Srinivasan Venkateshwaran
发明人： Basawaraj Chickmath , Chandrashekar Giliyar , Chidambaram Nachiappan , Mahesh V. Patel , Srinivasan Venkateshwaran
IPC分类号： A61K9/28 , A61K47/38 , A61K47/10 , A61K9/20 , A61K31/568 , A61K47/36
CPC分类号： A61K9/2031 , A61K9/14 , A61K9/146 , A61K9/148 , A61K9/1652 , A61K9/1676 , A61K9/1694 , A61K9/2013 , A61K9/2018 , A61K9/205 , A61K9/2054 , A61K9/282 , A61K9/2853 , A61K9/286 , A61K9/2866 , A61K9/4866 , A61K9/4875 , A61K31/568 , A61K47/10 , A61K47/36 , A61K47/38 , A61K47/40
摘要： The present disclosure is drawn to pharmaceutical compositions and oral dosage forms containing testosterone undecanoate, as well as related methods of treatment. In one embodiment, the oral dosage form can include a therapeutically effective amount of testosterone undecanoate and a pharmaceutically acceptable carrier. The dosage form can be formulated such that, when measured using a USP Type II apparatus in 1000 mL of 8 wt % Triton X-100 in water at 37° C. and 100 rpm, the oral dosage form releases at least 20% more testosterone undecanoate after the first 120 minutes than an equivalent dose testosterone undecanoate containing oral dosage form without the pharmaceutically acceptable carrier.

8. 发明申请

US20120322780A1 STEROIDAL COMPOSITIONS 有权
标题翻译： STEROIDAL组合物
公开(公告)号：US20120322780A1
公开(公告)日：2012-12-20
申请号：US13592258
申请日：2012-08-22
申请人： Chandrashekar Giliyar , Nachiappan Chidambaram , Mahesh V. Patel , Srinivasan Venkateshwaran
发明人： Chandrashekar Giliyar , Nachiappan Chidambaram , Mahesh V. Patel , Srinivasan Venkateshwaran
IPC分类号： A61K31/568 , A61P5/26
CPC分类号： A61K31/569 , A61K9/0053 , A61K9/4858 , A61K9/4866 , A61K9/4875 , A61K31/568 , A61K47/10 , A61K47/14 , A61K47/44
摘要： Provided herein are steroid containing compositions suitable for providing therapeutically effective amounts of at least one steroid to individuals. Also provided herein are compositions comprising testosterone and/or testosterone derivatives suitable for providing therapeutically effective and safe amounts of testosterone over periods of time. Further provided are methods of treating andro- and/or testosterone deficiency in individuals by administering to the individuals compositions described herein.
摘要翻译：本文提供了适用于向个体提供治疗有效量的至少一种类固醇的含甾族化合物的组合物。本文还提供包含适于在一段时间内提供治疗有效和安全量的睾酮的睾酮和/或睾酮衍生物的组合物。还提供了通过给予本文所述的个体组合物来治疗个体中的和/或睾酮缺乏症的方法。

9. 发明授权

US06569463B2 Solid carriers for improved delivery of hydrophobic active ingredients in pharmaceutical compositions 有权
标题翻译：用于改善药物组合物中疏水性活性成分递送的固体载体
公开(公告)号：US06569463B2
公开(公告)日：2003-05-27
申请号：US09800593
申请日：2001-03-06
申请人： Mahesh V. Patel , Feng-Jing Chen
发明人： Mahesh V. Patel , Feng-Jing Chen
IPC分类号： A61K916
CPC分类号： A61K47/14 , A61K9/1617 , A61K9/1676 , A61K9/4858 , A61K9/5015 , A61K9/5026 , A61K9/5078 , A61K9/5084 , A61K31/352 , A61K31/4709 , A61K31/496 , A61K31/5383 , A61K31/5513 , A61K31/568 , A61K31/7048 , A61K47/10 , B82Y5/00 , Y02A50/463 , Y10S977/906 , Y10S977/927
摘要： The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutrionals, cosmeceuticals and diagnostic agents.
摘要翻译：本发明提供用于改善递送其中所含的各种药物活性成分或单独施用的固体药物组合物。在一个实施方案中，固体药物组合物包括固体载体，固体载体包括底物和基材上的包封涂层。包封涂层可以包括药物活性成分，亲水性表面活性剂，亲脂性表面活性剂和甘油三酯的不同组合。在另一个实施方案中，固体药物组合物包括固体载体，固体载体由药物活性成分，亲水性表面活性剂，亲脂性表面活性剂和甘油三酸酯的不同组合形成。本发明的组合物可用于改善递送亲水或疏水性药物活性成分，例如药物，营养成分，药妆和诊断剂。

10. 发明授权

US06514986B2 Chiral fluoroquinolone arginine salt forms 失效
公开(公告)号：US06514986B2
公开(公告)日：2003-02-04
申请号：US09802793
申请日：2001-03-09
申请人： Noel J. de Souza , Shivkumar Agarwal , Mahesh V. Patel , Satish B. Bhawsar , Rupinder K. Beri , Ravindra D. Yeole , Nitin Shetty
发明人： Noel J. de Souza , Shivkumar Agarwal , Mahesh V. Patel , Satish B. Bhawsar , Rupinder K. Beri , Ravindra D. Yeole , Nitin Shetty
IPC分类号： C07D45506
CPC分类号： C07D215/233 , A61K31/4745 , A61K45/06 , C07B2200/07 , C07C279/14 , C07D401/04 , C07D401/14 , C07D455/04 , C07D471/04 , C07D471/08
摘要： The invention relates to the new arginine salt forms of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating antimicrobial infections.

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