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11. 发明申请

US20130324606A1 Ester Derivatives of Bimatoprost Compositions and Methods 审中-公开
标题翻译：比马前列素组合物和方法的酯衍生物
公开(公告)号：US20130324606A1
公开(公告)日：2013-12-05
申请号：US13985263
申请日：2012-02-13
申请人： David F. Woodward , Jenny W. Wang , Neil J. Poloso , Todd S. Gac , Robert M. Burk , Michael E. Garst
发明人： David F. Woodward , Jenny W. Wang , Neil J. Poloso , Todd S. Gac , Robert M. Burk , Michael E. Garst
IPC分类号： C07C405/00
CPC分类号： C07C235/34 , A61K8/42 , A61Q7/00 , C07C405/00 , C07C405/0041 , C07C2601/08
摘要： Provided herein, inter alia, are prodrugs of bimatoprost, methods of using the same and compositions including the same.
摘要翻译：本文提供的是比马前列素的前药，其使用方法和包含其的组合物。

12. 发明授权

US06716876B2 Cyclopentane(ENE)heptenoic or heptanoic acids and derivatives thereof useful as therapeutic agents 失效
标题翻译：环戊烷（ENE）庚烯或庚酸及其衍生物可用作治疗剂
公开(公告)号：US06716876B2
公开(公告)日：2004-04-06
申请号：US10087867
申请日：2002-02-28
申请人： Robert M. Burk
发明人： Robert M. Burk
IPC分类号： A61K315575
CPC分类号： A61K31/5585 , A61K31/557 , A61K31/5575 , A61K31/559 , C07C405/00 , C07C405/0016 , C07C405/0041 , C07C405/0058 , Y10S514/912
摘要： The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxy-cyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.
摘要翻译：本发明涉及7- [5-羟基-2-（羟基烃基或杂原子取代的羟基烃基）-3-羟基 - 环戊基（烯基）]庚酸或庚烯酸和所述酸的衍生物，其中一个或多个所述羟基被醚基取代。本发明的化合物是有效的眼睛低血压剂，特别适用于治疗青光眼。

13. 发明授权

US06476064B1 Cyclopentane heptan(ene) acyl sulfonamide, 2-alkyl or 2-arylalkyl, or 2-heteroarylalkenyl derivatives as therapeutic agents 有权
标题翻译：环戊烷庚烷（烯）酰基磺酰胺，2-烷基或2-芳基烷基或2-杂芳基烯基衍生物作为治疗剂
公开(公告)号：US06476064B1
公开(公告)日：2002-11-05
申请号：US09880272
申请日：2001-06-13
申请人： David W. Old , Robert M. Burk
发明人： David W. Old , Robert M. Burk
IPC分类号： A61K315575
CPC分类号： C07C405/0041
摘要： The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein a hatched line represents the &agr; configuration, a triangle represents the &bgr; configuration, a straight line, e.g. at the 9, 11 or 15 position represents either the &agr; or &bgr; configuration, a dotted line represents the presence or absence of a double bond; a wavy line represents a cis or trans bond; X is O, S, NH or (CH2)n; n is 0 or an integer of from 1 to 4; Y is C1-C5 n-alkyl, C3-C7 cycloalkyl, phenyl, furanyl, thienyl, pyridinyl, thiazolyl, benzothienyl, benzofaranyl, naphthyl, or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, N(R2)2, CO2R2 and OR2; Z is (CH2)n or a covalent bond; R is C1-C6 lower alkyl or Z—CF3 or mesylate or triflate; R1 is H, R2 or COR2;and R2 is H or C1-C5 lower alkyl or 9, 11 or 15 esters thereof.
摘要翻译：本发明提供一种治疗眼高血压或青光眼的方法，其包括向具有高眼压症或青光眼的动物施用治疗有效量的由通式I表示的化合物;其中阴影线表示α构型，三角形表示β 配置，直线，例如在9,11或15位置表示α或β构型，虚线表示存在或不存在双键; 波浪线代表顺式或反式键; X为O，S，NH或（CH 2）n; n为0或1至4的整数; Y为C 1 -C 5正烷基，C 3 -C 7环烷基，苯基呋喃基，噻吩基，吡啶基，噻唑基，苯并噻吩基，苯并呋喃基，萘基或其取代的衍生物，其中取代基可以选自C 1 -C 5烷基，卤素，CF 3，CN，NO 2，N（R 2）2，CO 2 R 2 和OR 2; Z是（CH2）n或共价键; R是C1-C6低级烷基或Z-CF3或甲磺酸酯或三氟甲磺酸酯; R1是H，R2或COR2; R2是H或C1-C5低级烷基或9， 11或15个酯。

14. 发明申请

US20020137793A1 6-Keto prostaglandin F1alpha and analogs for treating dry eye 有权
标题翻译： 6-Keto前列腺素F1alpha和类似物用于治疗干眼症
公开(公告)号：US20020137793A1
公开(公告)日：2002-09-26
申请号：US09787788
申请日：2001-03-23
发明人： Peter G. Klimko
IPC分类号： A61K031/215 , A61K031/557 , C07C061/06 , C07C405/00
CPC分类号： C07C59/90 , A61K31/5575 , C07C405/00 , C07C405/0041
摘要： The invention relates to compositions and methods for the treatment of dry eye and related diseases utilizing 6-keto-PGF1null and its analogs, according to formula (I); wherein A,B,D,Q9, Q11, R1, X and Y have the meanings given in the description. Some of these compounds are novel.
摘要翻译：本发明涉及根据式（I），利用6-酮-PGF1α及其类似物治疗干眼症和相关疾病的组合物和方法; 其中A，B，D，Q9，Q11，R1，X和Y具有说明书中给出的含义。这些化合物中的一些是新的。

15. 发明授权

US06417228B1 13-Aza prostaglandins for the treatment of glaucoma and ocular hypertension 有权
标题翻译：用于治疗青光眼和高眼压症的13-Aza前列腺素
公开(公告)号：US06417228B1
公开(公告)日：2002-07-09
申请号：US09430513
申请日：1999-10-29
申请人： Peter G. Klimko
发明人： Peter G. Klimko
IPC分类号： A61K31215
CPC分类号： A61K31/5575 , A61K9/0048 , C07C215/44 , C07C235/22 , C07C405/0041 , C07C2601/08
摘要： 13-Aza analogs of PGF2&agr; and methods of their use in treating glaucoma and ocular hypertension are disclosed.
摘要翻译：公开了PGF2α的13-Aza类似物及其用于治疗青光眼和高眼压症的方法。

16. 发明授权

US06395787B1 Ocular hypotensive lipids 有权
标题翻译：眼部降血脂
公开(公告)号：US06395787B1
公开(公告)日：2002-05-28
申请号：US09500142
申请日：2000-02-08
申请人： David F. Woodward , Helen H. Usansky , Steven W. Andrews , Robert M. Burk , June Chen , Achim H-P. Krauss , Cherukury Madhu
发明人： David F. Woodward , Helen H. Usansky , Steven W. Andrews , Robert M. Burk , June Chen , Achim H-P. Krauss , Cherukury Madhu
IPC分类号： A61K315575
CPC分类号： A61K9/0048 , C07C405/0041
摘要： Compounds of Formula 1, where the symbols are as defined in the specification, are useful as ocular hypotensive agents but do not exert their activity through the FP prostaglandin receptor. In particular the compound PGF2&agr; 1-ethanolamide, having the formula was discovered to be present in mammalian tissue as a naturally occurring substance, was synthesized in a substantially pure form and was found to be effective for lowering intraocular pressure in the mammalian eye, but not acting through the FP receptor through which many ocular hypotensive prostaglandins act.
摘要翻译：化学式1的化合物，其中符号如说明书中所定义，可用作眼部降压药，但不通过FP前列腺素受体发挥其活性。特别是具有发现存在于该药物中的福尔马林的化合物PGF2α1-乙醇酰胺作为天然存在的物质的哺乳动物组织以基本上纯的形式被合成，并被发现对于降低哺乳动物眼睛中的眼内压而言是有效的，但不能通过多种眼部低血压前列腺素起作用的FP受体起作用。

17. 发明授权

US6160129A Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents 有权
标题翻译：环戊烷庚（烯）酸，2-杂芳基烯基衍生物作为治疗剂
公开(公告)号：US6160129A
公开(公告)日：2000-12-12
申请号：US243344
申请日：1999-02-01
申请人： Robert M. Burk
发明人： Robert M. Burk
IPC分类号： C07D333/28 , A61K31/34 , A61K31/38 , A61K31/557 , A61K31/5575 , A61K31/5585 , A61P27/06 , C07C405/00 , C07D277/30 , C07D307/02 , C07D307/06 , C07D307/56 , C07D307/68 , C07D333/16 , C07D333/24 , C07D333/38
CPC分类号： C07D333/28 , A61K31/557 , A61K31/5575 , A61K31/5585 , A61K31/559 , C07C405/00 , C07C405/0016 , C07C405/0041 , C07C405/0058 , C07D333/24 , C07D333/38
摘要： The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The compounds used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate .alpha. configuration; the solid triangle is used to indicate .beta. configuration; dashed bonds represent a double bond, or a single bond; R is a substituted heteroaryl radical having at least two pendant substituents selected from the group consisting of C.sub.1 to C.sub.6 alkyl; halogen; trifluoromethyl; COR.sup.1 ; COCF.sub.3 ; SO.sub.2 NR.sup.1 ; NO.sub.2 and CN or at least one cyano group; R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2 ; Y is .dbd.O or represents 2 hydrogen radicals and the 9, 11 or 15 lower alkyl esters thereof; provided, however, when said heteroaryl radical is a dichlorothienyl radical, the compound is not a 1-carboxylic acid or amide thereof. Certain of the compounds represented by Formula I are novel and comprise another aspect of the present invention.
摘要翻译：本发明涉及使用F型前列腺素衍生物作为眼部低血压。根据本发明使用的化合物由下式I表示：其中波浪线附着物指示α（α）或β（β）构型; 阴影线段表示alpha配置; 实心三角形用于指示beta配置; 虚线键代表双键或单键; R是具有至少两个选自C 1至C 6烷基的侧基取代基的取代的杂芳基; 卤素; 三氟甲基 COR1; COCF3; SO2NR1; NO 2和CN或至少一个氰基; R 1是氢或具有至多6个碳原子的低级烷基，X选自-OR 1和-N（R 1）2; Y为= O或代表2个氢原子及其9,11或15个低级烷基酯; 但是，当所述杂芳基为二氯噻吩基时，该化合物不是1-羧酸或其酰胺。某些由式I表示的化合物是新的并且包括本发明的另一方面。

18. 发明授权

US5164412A 5-Hetero-6-oxo-PGE-derivatives 失效
标题翻译： 5-HETERO-6-OXO-PGE-DERIVATIVES
公开(公告)号：US5164412A
公开(公告)日：1992-11-17
申请号：US681669
申请日：1991-04-08
申请人： Yoshitaka Konishi , Masanori Kawamura
发明人： Yoshitaka Konishi , Masanori Kawamura
IPC分类号： C07C405/00
CPC分类号： C07C405/0016 , C07C405/00 , C07C405/0025 , C07C405/0041
摘要： A Derivative of 5-hetero-6-oxo-PGE A derivative of 5-hetero-6-oxo-PGE of the formula: ##STR1## wherein R.sup.1 is (1) a group of the formula: COOR11(2) hydroxymethylcarbonyl,(3) hydroxymethyl or(4) a group of the formula:CO--AA wherein AA is an amino acid-residue,Z is oxygen, sulfur or a group of the formula: NR21 wherein R21 is hydrogen or alkyl of C1--4;R2 is a single-bond or alkylene of C1--4;R3 isi) alkyl of C1-7,ii) cycloalkyl of C4-7 or cycloalkyl of C4-7 substituted by alkyl of C1-7,iii) phenyl, phenoxy, phenyl or phenoxy substituted by one group selected from alkyl of C1-4, halogen and trihalomethyl, is single-bond or a double bond.Possess PG-like activity, especially cytoprotection, and therefore are useful for treatment for and/or prevention of cytodamage.

20. 发明授权

US5006539A Prostaglandins 失效
标题翻译：前列腺素
公开(公告)号：US5006539A
公开(公告)日：1991-04-09
申请号：US319052
申请日：1989-03-06
申请人： Robert L. Jones , Norman H. Wilson
发明人： Robert L. Jones , Norman H. Wilson
IPC分类号： C07C59/74 , A61K31/16 , A61K31/17 , A61K31/195 , A61K31/215 , A61K31/557 , A61P7/02 , A61P11/08 , A61P29/00 , C07C43/315 , C07C45/44 , C07C51/00 , C07C59/325 , C07C59/353 , C07C59/62 , C07C59/80 , C07C59/86 , C07C67/00 , C07C69/608 , C07C69/716 , C07C69/738 , C07C229/28 , C07C229/32 , C07C231/00 , C07C233/05 , C07C233/65 , C07C235/06 , C07C235/20 , C07C235/46 , C07C237/24 , C07C239/00 , C07C275/26 , C07C275/28 , C07C335/16 , C07C401/00 , C07C405/00 , C07D213/55 , C07D277/62 , C07D307/00 , C07D493/00 , C07D493/08
CPC分类号： C07D493/08 , C07C255/00 , C07C405/0041 , C07C405/0091 , C07C43/315 , C07C45/44 , C07C59/62
摘要： Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1]heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.1 is a 6-carboxyhex-2-enyl group or a modification thereof as defined herein; A is an unbranched or branched aliphatic hydrocarbon group with a chain length between the points of attachment to the divalent cyclic group and to the group NR.sup.2 R of 1 to 5 carbon atoms or such a group substituted by an aromatic group; R.sup.2 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups; and R is a group --CO.NR.sup.3 R.sup.4, --CS.NR.sup.3 R.sup.4, --CNH.NR.sup.3 R.sup.4, --CO.R.sup.4 or --CO.R.sup.4 in which R.sup.3 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups, and R.sup.4 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly by an aromatic group or groups and/or through an oxygen or sulphur atom either by an aromatic group or by an aliphatic hydrocarbon group substituted directly by an aromatic group or groups. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.

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