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1. 发明授权

US09809557B2 Prodrugs of non-steroid anti-inflammatory agents (NSAIDS) 有权
公开(公告)号：US09809557B2
公开(公告)日：2017-11-07
申请号：US14355010
申请日：2012-10-31
申请人： Claus Selch Larsen
发明人： Claus Selch Larsen , Susan Weng Larsen , Mette Agergaard Thing , Jesper Langgaard Kristensen , Henrik Jensen , Jesper Østergaard
IPC分类号： A61K31/44 , C07D235/06 , A61K47/48 , C07C219/10 , C07C219/32 , C07C229/42 , C07D487/04 , C07D233/61 , C07D235/16 , C07D235/18 , C07D213/55
CPC分类号： C07D235/06 , A61K47/54 , A61K47/545 , C07C219/10 , C07C219/32 , C07C229/42 , C07D213/55 , C07D233/61 , C07D235/16 , C07D235/18 , C07D487/04
摘要： The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.

2. 发明申请

US20100010084A1 HIGH PENETRATION PRODRUG COMPOSITIONS OF RETINOIDS AND RETINOID-RELATED COMPOUNDS 有权
标题翻译：雷诺霉素和与雷公藤相关的化合物的高渗透性原料组合物
公开(公告)号：US20100010084A1
公开(公告)日：2010-01-14
申请号：US12503739
申请日：2009-07-15
申请人： Chongxi Yu
发明人： Chongxi Yu
IPC分类号： A61K31/24 , A61K31/20 , A61K31/19 , A61K31/22 , A61K31/15 , A61K31/13 , C12Q1/02 , A61P17/00 , A61P27/02 , A61P35/04
CPC分类号： A61K47/48023 , A61K31/21 , A61K31/215 , A61K31/216 , A61K31/221 , A61K31/4453 , A61K47/54 , C07C219/10 , C07C2601/16 , C07C2602/10 , G01N33/502
摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of retinoids and retinoid-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
摘要翻译：本发明提供了能够穿过具有高穿透效率的生物屏障的类视黄醇和类视黄醇相关化合物的新型高渗透组合物（HPC）或高渗透前药（HPP）的组合物。 HPP在穿过生物屏障后能够转化为亲本活性药物或药物代谢物，因此可以对母体药物或代谢物可以进行的处理。此外，HPP能够达到母体药物可能无法进入或在目标区域提供足够浓度的区域，从而进行新的治疗。 HPP可以通过各种施用途径施用于受试者，例如局部递送至具有高浓度或系统地施用于生物受试者的病症的作用部位并以更快的速率进入总体循环。

3. 发明申请

US20070254920A1 Prodrug derivatives of acids using alcohols with homotopic hydroxy groups and methods for their preparation and use 审中-公开
标题翻译：使用具有同位羟基的醇的酸的前药衍生物及其制备和使用方法
公开(公告)号：US20070254920A1
公开(公告)日：2007-11-01
申请号：US11412207
申请日：2006-04-26
申请人： Mitchell deLong , Jill McFadden , Susan Royalty , Eric Toone , Jeffrey Yingling
发明人： Mitchell deLong , Jill McFadden , Susan Royalty , Eric Toone , Jeffrey Yingling
IPC分类号： A61K31/558 , C07D409/02 , C07D405/02 , C07D403/02
CPC分类号： C07C219/10 , C07C69/608 , C07C69/738 , C07C69/76 , C07C233/65 , C07C251/48 , C07C317/44 , C07C405/00 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2602/08 , C07C2602/24 , C07D205/095 , C07D215/56 , C07D233/78 , C07D277/06 , C07D295/116 , C07D333/56 , C07D333/64 , C07D473/30 , C07D473/34 , C07D491/056 , C07D501/34
摘要： This invention relates to novel homotopic prodrugs and medicaments and methods for their preparation, testing and use. In one embodiment, the homotopic prodrug has the general formula wherein is a biologically-active moiety comprising a carboxylic acid functional group, and Rb is a homotopically-symmetrical alcohol bonded to the biologically-active moiety through the carboxylic acid functional group to form an ester linkage, as well as optical isomers, enantiomers, pharmaceutically acceptable salts, biohydrolyzable amides, esters, and imides thereof and combinations thereof.
摘要翻译：本发明涉及新的同位素前药和药物及其制备，测试和使用的方法。在一个实施方案中，同位物前药具有以下通式：其中是包含羧酸官能团的生物活性部分，并且R bb是与生物活性部分结合的同位素对称醇，通过羧酸官能团以形成酯键，以及光学异构体，对映异构体，药学上可接受的盐，生物可水解的酰胺，酯和酰亚胺以及它们的组合。

4. 发明申请

US20050065211A1 Ester derivatives 失效
标题翻译：酯衍生物
公开(公告)号：US20050065211A1
公开(公告)日：2005-03-24
申请号：US10983613
申请日：2004-11-09
申请人： Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
发明人： Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
IPC分类号： A61P11/00 , A61P11/06 , A61P27/16 , A61P43/00 , C07C219/10 , C07C219/14 , C07D205/04 , C07D207/08 , C07D207/12 , C07D209/52 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D239/06 , C07D451/02 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/10 , C07D498/10 , A61K31/445 , A61K31/24 , C07C229/52
CPC分类号： C07D207/08 , C07C219/10 , C07C219/14 , C07D205/04 , C07D207/12 , C07D209/52 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D239/06 , C07D451/02 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/10
摘要： This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X− signifies an anion].
摘要翻译：本发明涉及具有选择性毒蕈碱M3受体拮抗作用，副作用小，适用于吸入治疗的化合物，并且可用作通式（I）的呼吸系统疾病的治疗剂; [其中A表示由式（a0）或（b0）表示的组; Ar表示任选取代的芳基或杂芳基; B 1和B 2表示脂族烃; R 1表示氟取代的环烷基; R 2，R 3和R 4表示低级烷基，单键或与B 1键合的亚烷基，或R 2和R 3一起表示亚烷基; R 5和R 7表示氢，低级烷基或与B 2键合的单键或亚烷基; R 6表示氢，低级烷基或以-N（R 8）R 9表示的基团; 而X - 表示阴离子]。

5. 发明授权

US06846835B2 Ester derivatives 失效
标题翻译：酯衍生物
公开(公告)号：US06846835B2
公开(公告)日：2005-01-25
申请号：US10332617
申请日：2001-07-10
申请人： Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
发明人： Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
IPC分类号： A61P11/00 , A61P11/06 , A61P27/16 , A61P43/00 , C07C219/10 , C07C219/14 , C07D205/04 , C07D207/08 , C07D207/12 , C07D209/52 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D239/06 , C07D451/02 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/10 , C07D498/10 , A61K31/445 , A61K31/4465 , C07D211/04 , C07D221/02
CPC分类号： C07D207/08 , C07C219/10 , C07C219/14 , C07D205/04 , C07D207/12 , C07D209/52 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D239/06 , C07D451/02 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/10
摘要： This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X− signifies an anion].
摘要翻译：本发明涉及具有选择性毒蕈碱性M3受体拮抗作用，副作用小，适用于吸入治疗的化合物，并且可用作通式（I）的呼吸系统疾病的治疗剂; [其中A表示一组表达通式（a0）或（b0）; Ar表示任选取代的芳基或杂芳基; B 1和B 2表示脂族烃; R 1表示氟取代的环烷基; R 2，R 3和R 4表示低级烷基，单键或与B 1键合的亚烷基，或R 2和R 3一起表示亚烷基; R 5和R 7表示氢，低级烷基或与B 2键合的单键或亚烷基; R 6表示氢，低级烷基或以-N（R 8）R 9表示的基团; 而X - 表示阴离子]。

6. 发明授权

US6087346A Sigma receptor ligands and the use thereof 失效
标题翻译： Sigma受体配体及其用途
公开(公告)号：US6087346A
公开(公告)日：2000-07-11
申请号：US564362
申请日：1996-02-21
申请人： Richard A. Glennon , James B. Fischer
发明人： Richard A. Glennon , James B. Fischer
IPC分类号： C07C211/27 , C07C211/28 , C07C211/29 , C07C211/42 , C07C215/30 , C07C219/10 , C07C219/12 , C07C225/16 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/32 , C07D211/52 , C07D211/70 , C07D295/02 , C07D295/03 , C07D295/033 , C07D295/073 , C07D295/096 , C07D295/104 , C07D295/13 , C07D317/58 , A01N65/00 , A01N33/02 , C07C221/00 , C07D217/00
CPC分类号： C07D317/58 , C07C211/27 , C07C211/28 , C07C211/29 , C07C211/42 , C07C215/30 , C07C219/10 , C07C219/12 , C07C225/16 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/32 , C07D211/52 , C07D211/70 , C07D295/03 , C07D295/033 , C07D295/073 , C07D295/096 , C07D295/104 , C07D295/13 , C07C2103/18
摘要： The invention relates to methods for the treatment of central nervous system disorders, neurological disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof.
摘要翻译： PCT No.PCT / US94 / 07121 Sec。 371日期1996年2月21日 102（e）日期1996年2月21日PCT提交1994年6月23日PCT公布。公开号WO95 / 00131 日期1995年1月5日本发明涉及通过施用包含有效量的某些σ受体配体的药物组合物来治疗中枢神经系统疾病，神经障碍，胃肠道疾病，药物滥用，心绞痛，偏头痛，高血压和抑郁症的方法需要这样治疗的病人。本发明还涉及具有与σ受体高度结合的新型σ受体配体及其药物组合物。

7. 发明授权

US6057371A Sigma receptor ligands and the use thereof 失效
标题翻译： Sigma受体配体及其用途
公开(公告)号：US6057371A
公开(公告)日：2000-05-02
申请号：US894771
申请日：1992-06-10
申请人： Richard A. Glennon
发明人： Richard A. Glennon
IPC分类号： A61K31/13 , A61K31/135 , A61K31/16 , A61K31/18 , A61K31/19 , A61K31/215 , A61K31/275 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/495 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/55 , C07C211/08 , C07C211/17 , C07C211/27 , C07C211/28 , C07C211/29 , C07C211/30 , C07C211/42 , C07C215/52 , C07C217/16 , C07C217/60 , C07C219/10 , C07C219/12 , C07C225/16 , C07C229/38 , C07C233/04 , C07C255/58 , C07C317/32 , C07C323/32 , C07D207/12 , C07D209/48 , C07D211/14 , C07D211/36 , C07D211/46 , C07D211/52 , C07D211/70 , C07D223/16 , C07D239/42 , C07D265/30 , C07D295/02 , C07D295/03 , C07D295/033 , C07D295/06 , C07D295/073 , C07D295/096 , C07D295/108 , C07D295/192 , C07D317/58 , C07D471/08 , A01N33/02 , C07C211/00 , C07C213/00
CPC分类号： C07D209/48 , A61K31/135 , A61K31/215 , A61K31/40 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/505 , A61K31/535 , A61K31/55 , C07C211/08 , C07C211/17 , C07C211/27 , C07C211/28 , C07C211/29 , C07C211/30 , C07C211/42 , C07C215/52 , C07C217/16 , C07C217/60 , C07C219/10 , C07C219/12 , C07C225/16 , C07D207/12 , C07D211/14 , C07D211/46 , C07D211/52 , C07D211/70 , C07D223/16 , C07D239/42 , C07D265/30 , C07D295/03 , C07D295/033 , C07D295/073 , C07D295/096 , C07D295/108 , C07D295/192 , C07D317/58 , C07D471/08 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2102/08 , C07C2102/10 , C07C2102/12 , C07C2103/18
摘要： The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT.sub.1A receptors.
摘要翻译：本发明涉及通过向需要这种治疗的患者施用包含有效量的某些σ受体配体的药物组合物来治疗中枢神经系统疾病，胃肠道疾病，药物滥用，心绞痛，偏头痛，高血压和抑郁症的方法。本发明还涉及具有与σ受体高度结合的新型σ受体配体及其药物组合物。出乎意料的是，某些本发明的σ受体配体在DA，PCP和5-HT 1A受体上对σ受体具有选择性。

8. 发明授权

US5196568A Compounds useful in enzymatic resolution systems and their preparation 失效
标题翻译：可用于酶解体系及其制备的化合物
公开(公告)号：US5196568A
公开(公告)日：1993-03-23
申请号：US178735
申请日：1988-04-07
申请人： Charles M. Zepp , Stephen A. Wald , David R. Dodds
发明人： Charles M. Zepp , Stephen A. Wald , David R. Dodds
IPC分类号： B01J19/24 , C07C219/10 , C07C305/04 , C07C305/10 , C07C309/65 , C07C309/66 , C07C327/32 , C07F9/09 , C12N11/02 , C12P1/00 , C12P7/40 , C12P41/00
CPC分类号： C12P41/005 , B01J19/2475 , C07C219/10 , C07C305/04 , C07C305/10 , C07C309/65 , C07C309/66 , C07C327/32 , C07F9/091 , C12N11/02 , C12P1/00 , C12P41/00 , C12P7/40 , B01J2219/00159 , B01J2219/00162 , B01J2219/00177
摘要： This invention relates to novel compositions of matter which are esters with enhanced water solubility, for use in aqueous enzymatic resolution reactions of racemic mixtures of these esters for producing the separate chiral isomers of the racemic mixture. The invention also relates to novel methods for preparing these esters. The importance of the production of the separate chiral isomers of the racemic mixtures resides in the isolation of the isomers which frequently have different biological activities. Of particular significance regarding the water soluble esters of this invention is that they are derivatized with groups which enhance their aqueous solubility and their reactivity with enzymatic resolving methods which are mediated in an aqueous environment. In addition, the importance of these compounds resides in their being useful in novel methods for facilitating the enzymatic resolution reactions of racemic mixtures of esters, which are derivatized with groups which enhance the esters' aqueous solubility, in 1) a homogeneous aqueous reaction system where an extractive phase is not present, 2) a multiphase dispersion extractive reaction where an extractive phase is present, and 3) an extractive membrane reactor where the enzyme is placed alternatively either (a) in the aqueous phase, (b) in association with the membrane, or (c) in the aqueous phase and in association with the membrane, wherein the aqueous ester phase is contacted with one side of the membrane, and where an organic extractive phase is contacted with the other side of the membrane, wherein the extractive phase serves to remove the resolving reaction product.
摘要翻译：本发明涉及物质的新型组合物，其是具有增强的水溶性的酯，用于这些酯的外消旋混合物的水性酶拆分反应中用于产生外消旋混合物的分离的手性异构体。本发明还涉及制备这些酯的新方法。外消旋混合物的分离手性异构体的生产的重要性在于分离经常具有不同生物活性的异构体。对于本发明的水溶性酯具有特别意义的是它们用增强其水溶性的基团和它们与在水性环境中介导的酶拆分方法的反应性的基团衍生化。此外，这些化合物的重要性在于它们可用于促进酯的外消旋混合物的酶拆分反应的新方法，其通过增强酯的水溶性的基团衍生化，在1）均匀的水反应体系中，其中萃取相不存在，2）存在萃取相的多相分散萃取反应，和3）提取膜反应器，其中酶在（a）在水相中交替放置，（b）与膜或（c）在水相中并与膜结合，其中酯水相与膜的一侧接触，并且其中有机萃取相与膜的另一侧接触，其中提取物相用于除去分解反应产物。

9. 发明授权

US09738593B2 Lipids and lipid nanoparticle formulations for delivery of nucleic acids 有权
公开(公告)号：US09738593B2
公开(公告)日：2017-08-22
申请号：US14732218
申请日：2015-06-05
申请人： Acuitas Therapeutics Inc.
发明人： Steven M. Ansell , Xinyao Du
IPC分类号： C07C219/06 , A61K47/18 , A61K47/22 , C07C219/08 , C07C229/16 , C07D295/13 , C08G65/333 , A61K9/127 , C07C219/10
CPC分类号： C07C229/24 , A61K9/1272 , A61K38/4846 , A61K47/18 , A61K47/22 , A61K47/24 , A61K47/28 , A61K48/0041 , C07C219/06 , C07C219/08 , C07C219/10 , C07C227/16 , C07C229/16 , C07C235/06 , C07D295/13 , C08G65/33306 , C12Y304/21022
摘要： Compounds are provided having the following structure: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6, R7, R8, R9, L1, L2, a, b, c, d and e are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.

10. 发明申请

US20150376115A1 NOVEL LIPIDS AND LIPID NANOPARTICLE FORMULATIONS FOR DELIVERY OF NUCLEIC ACIDS 有权
标题翻译：用于输送核酸的新鲜脂肪和脂质纳米颗粒配方
公开(公告)号：US20150376115A1
公开(公告)日：2015-12-31
申请号：US14732218
申请日：2015-06-05
申请人： Acuitas Therapeutics Inc.
发明人： Steven M. Ansell , Xinyao Du
IPC分类号： C07C219/06 , C07C229/16 , A61K47/22 , C07D295/13 , A61K47/18 , C08G65/333 , C07C219/08
CPC分类号： C07C229/24 , A61K9/1272 , A61K38/4846 , A61K47/18 , A61K47/22 , A61K47/24 , A61K47/28 , A61K48/0041 , C07C219/06 , C07C219/08 , C07C219/10 , C07C227/16 , C07C229/16 , C07C235/06 , C07D295/13 , C08G65/33306 , C12Y304/21022
摘要： Compounds are provided having the following structure: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6, R7, R8, R9, L1, L2, a, b, c, d and e are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.
摘要翻译：提供具有以下结构的化合物：或其药学上可接受的盐，互变异构体或立体异构体，其中R1a，R1b，R2a，R2b，R3a，R3b，R4a，R4b，R5，R6，R7，R8，R9，L1，L2， a，b，c，d和e如本文所定义。还提供了化合物作为脂质纳米颗粒制剂的组分用于递送治疗剂的用途，包含该化合物的组合物及其使用和制备方法。

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