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    Cyclopentane heptan(ENE)OIC acid, 2-heteroarylalkenyl derivatives as therapeutic agents
    1.
    发明授权
    Cyclopentane heptan(ENE)OIC acid, 2-heteroarylalkenyl derivatives as therapeutic agents 有权
    环戊烷庚烷（ENE）OIC酸，2-杂芳基烯基衍生物作为治疗剂

    公开(公告)号：US07906552B2

    公开(公告)日：2011-03-15

    申请号：US10916243

    申请日：2004-08-10

    申请人： Yariv Donde ,  Robert M. Burk ,  Michael E. Garst

    发明人： Yariv Donde ,  Robert M. Burk ,  Michael E. Garst

    IPC分类号： A61K31/38 ,  A61K31/5575 ,  C07D333/24 ,  C07C405/00

    CPC分类号： C07C405/00 ,  C07D333/28

    摘要： A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.

    摘要翻译： 公开了具有本文详细描述的基团的化合物或其药学上可接受的盐或其前药。 本文还公开了包含其衍生物或其衍生物的化合物或其结构或衍生物的化合物的药学上可接受的盐，四唑或前药，所述衍生物在此详细描述。 本文还公开了治疗疾病或病症的方法，包括青光眼和眼内压升高。 还公开了与其相关的药物制备的组合物和方法。

    Cyclopentane heptan(ENE)OIC acid, 2-heteroarylalkenyl derivatives as therapeutic agents
    2.
    发明授权
    Cyclopentane heptan(ENE)OIC acid, 2-heteroarylalkenyl derivatives as therapeutic agents 有权
    环戊烷庚烷（ENE）OIC酸，2-杂芳基烯基衍生物作为治疗剂

    公开(公告)号：US08168680B2

    公开(公告)日：2012-05-01

    申请号：US13023257

    申请日：2011-02-08

    申请人： Yariv Donde ,  Robert M. Burk ,  Michael E. Garst

    发明人： Yariv Donde ,  Robert M. Burk ,  Michael E. Garst

    IPC分类号： A61K31/5575 ,  C07C405/00

    CPC分类号： C07C405/00 ,  C07D333/28

    摘要： A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.

    摘要翻译： 公开了具有本文详细描述的基团的化合物或其药学上可接受的盐或其前药。 本文还公开了包含其衍生物或其衍生物的化合物或其结构或衍生物的化合物的药学上可接受的盐，四唑或前药，所述衍生物在此详细描述。 本文还公开了治疗疾病或病症的方法，包括青光眼和眼内压升高。 还公开了与其相关的药物制备的组合物和方法。

    CYCLOPENTANE HEPTAN(ENE)OIC ACID, 2-HETEROARYLALKENYL DERIVATIVES AS THERAPEUTIC AGENTS
    3.
    发明申请
    CYCLOPENTANE HEPTAN(ENE)OIC ACID, 2-HETEROARYLALKENYL DERIVATIVES AS THERAPEUTIC AGENTS 有权
    环丙沙星（ENE）OIC酸，作为治疗剂的2-异亮氨酸衍生物

    公开(公告)号：US20110130439A1

    公开(公告)日：2011-06-02

    申请号：US13023257

    申请日：2011-02-08

    申请人： Yariv Donde ,  Robert M. Burk ,  Michael E. Garst

    发明人： Yariv Donde ,  Robert M. Burk ,  Michael E. Garst

    IPC分类号： A61K31/381 ,  C07D333/28 ,  A61P27/02 ,  A61P27/06

    CPC分类号： C07C405/00 ,  C07D333/28

    摘要： A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein.Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.

    摘要翻译： 公开了具有本文详细描述的基团的化合物或其药学上可接受的盐或其前药。 本文还公开了包含其衍生物或其衍生物的化合物或其结构或衍生物的化合物的药学上可接受的盐，四唑或前药，所述衍生物在此详细描述。 本文还公开了治疗疾病或病症的方法，包括青光眼和眼内压升高。 还公开了与其相关的药物制备的组合物和方法。

    Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents
    5.
    发明授权
    Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents 有权
    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：US07183310B2

    公开(公告)日：2007-02-27

    申请号：US10915933

    申请日：2004-08-10

    申请人： Yariv Donde ,  Robert M. Burk ,  Michael E. Garst

    发明人： Yariv Donde ,  Robert M. Burk ,  Michael E. Garst

    IPC分类号： A61K31/38 ,  C07D333/16

    CPC分类号： C07D333/28

    摘要： A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.

    摘要翻译： 公开了具有本文详细描述的基团的化合物或其药学上可接受的盐或其前药。 本文还公开了包含其衍生物或其衍生物的化合物或其结构或衍生物的化合物的药学上可接受的盐，四唑或前药，所述衍生物在此详细描述。 本文还公开了治疗疾病或病症的方法，包括青光眼和眼内压升高。 还公开了与其相关的药物制备的组合物和方法。

    Interphenylene 7-oxabicyclic [2.2.1] heptane oxazoles as prostaglandin F2a antagonists
    8.
    发明授权
    Interphenylene 7-oxabicyclic [2.2.1] heptane oxazoles as prostaglandin F2a antagonists 有权
    2-亚麻基7-氧杂双环[2.2.1]庚烷恶唑作为前列腺素F2a拮抗剂

    公开(公告)号：US06407250B1

    公开(公告)日：2002-06-18

    申请号：US09661771

    申请日：2000-09-14

    申请人： Robert M. Burk ,  Yariv Donde ,  Michael E. Garst

    发明人： Robert M. Burk ,  Yariv Donde ,  Michael E. Garst

    IPC分类号： C07D41304

    CPC分类号： C07D493/08

    摘要： The present invention provides novel compounds represented by the general formula I. wherein m is an integer of from 1 to 3; n is 0 or an integer of from 1 to 4; R is selected from the group consisting of CO2H, CO2 R6, CH2OH, CH2O R6  and CONR3R4; R1 and R2 are independently selected from the group consisting of H, R6, C1-C6 alkenyl, C1-C6 alkynyl, C3-C7 cycloalkyl, C4-C12 alkylcycloalkyl, C6-C10 aryl, C7-C12 alkyl aryl radicals and heteroatom-substituted derivatives thereof, wherein one or more of the hydrogen or carbon atoms in said radicals is replaced with a halogen, nitrogen or sulfur-containing radical; R3 and R4 are selected from the group consisting of H and R6; and X is selected from the group consisting of R6, hydroxy, N(R6)2, CON(R6)2, SR6, sulfoxy, sulfone, halogen, COOR6, NO2, CN and OR6, wherein R6 is C1-C6 alkyl, and pharmaceutically acceptable salts thereof. The novel compounds are PGF2&agr; antagonists, useful in pharmaceutical compositions for treating PGF2&agr;-mediated disease responses such as inflammatory reactions relating to rheumatoid arthritis and psoriasis, reproductive disorders, bronchoconstrictive disorders (asthma), excessive bone breakdown (osteoporosis), peptic ulcers, heart disease, platelet aggregation and thrombosis.

    摘要翻译： 本发明提供由通式Ⅰ表示的新型化合物，其中m为1〜3的整数，n为0或1〜4的整数; R选自CO 2 H，CO 2 R 6，CH 2 OH， CH2O R6和CONR3R4; R1和R2独立地选自H，R6，C1-C6烯基，C1-C6炔基，C3-C7环烷基，C4-C12烷基环烷基，C6-C10芳基，C7-C12烷基芳基 基团和杂原子取代的衍生物，其中所述基团中的一个或多个氢原子或碳原子被卤素，氮或含硫基团取代; R 3和R 4选自H和R 6; 和X选自R6，羟基，N（R6）2，CON（R6）2，SR6，磺氧基，砜，卤素，COOR6，NO2，CN和OR6，其中R6是C1-C6烷基， 其可接受的盐。 新型化合物是PGF2α拮抗剂，可用于治疗PGF2α介导的疾病反应的药物组合物，例如与类风湿性关节炎和牛皮癣相关的炎性反应，生殖障碍，支气管收缩性疾病（哮喘），过度骨分解（骨质疏松症），消化性溃疡，心脏病 ，血小板聚集和血栓形成。

    Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents
    9.
    发明授权
    Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents 有权
    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：US07863319B2

    公开(公告)日：2011-01-04

    申请号：US11623417

    申请日：2007-01-16

    申请人： Yariv Donde ,  Robert M. Burk ,  Michael E. Garst

    发明人： Yariv Donde ,  Robert M. Burk ,  Michael E. Garst

    IPC分类号： A61K31/381 ,  C07D333/28

    CPC分类号： C07D333/28

    摘要： A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.

    摘要翻译： 公开了具有本文详细描述的基团的化合物或其药学上可接受的盐或其前药。 本文还公开了包含其衍生物或其衍生物的化合物或其结构或衍生物的化合物的药学上可接受的盐，四唑或前药，所述衍生物在此详细描述。 本文还公开了治疗疾病或病症的方法，包括青光眼和眼内压升高。 还公开了与其相关的药物制备的组合物和方法。

    2,3,4-substituted cyclopentanones as therapeutic agents
    10.
    发明授权
    2,3,4-substituted cyclopentanones as therapeutic agents 有权
    2,3,4-取代环戊酮作为治疗剂

    公开(公告)号：US07101906B2

    公开(公告)日：2006-09-05

    申请号：US10991284

    申请日：2004-11-16

    申请人： Yariv Donde ,  Robert M. Burk ,  Michael E. Garst ,  Jeremiah H. Nguyen

    发明人： Yariv Donde ,  Robert M. Burk ,  Michael E. Garst ,  Jeremiah H. Nguyen

    IPC分类号： A61K31/881 ,  C07D333/56 ,  C07D333/62

    CPC分类号： C07D333/62 ,  C07C405/0025 ,  C07D333/56

    摘要： Disclosed herein are compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, wherein a dashed line represents the presence or absence of a bond; Y is a carboxylic acid, sulfonic acid, or phosphonic acid functional group; or an amide or ester thereof comprising from 0 to 12 carbon atoms; or Y is hydroxymethyl or an ether thereof comprising from 0 to 12 carbon atoms; or Y is a tetrazolyl functional group; A is —(CH2)6—, cis —CH2—CH═CH—(CH2)3—, or —CH2—C≡C—(CH2)3— wherein 1 or 2 carbons may be substituted with S or O; B is hydrogen, C1-6 hydrocarbyl, CN, CO2H, or —(CH2)mX(CH2)pH, wherein m is at least 1 and the sum of m and p is from 1 to 5; X is S or O; J is H, CH3, or CF3; D is a covalent bond, CH2, O, or S; and E is an aromatic heterobicyclic ring system which may have substituents comprising up to 6 non-hydrogen atoms each. Methods, compositions, and medicaments related thereto are also disclosed.

    摘要翻译： 本文公开了包含其药学上可接受的盐或其前药的化合物，其中虚线表示存在或不存在键; Y是羧酸，磺酸或膦酸官能团; 或其包含0至12个碳原子的酰胺或酯; 或Y是含有0至12个碳原子的羟甲基或其醚; 或Y为四唑基官能团; A是 - （CH 2 CH 2）6 - ，顺式-CH 2 -CH-CH-（CH 2 CH 2） ）3 - 或 - CH 2-C≡C-（CH 2）3 - 其中1或 2个碳可以被S或O取代; B是氢，C 1-6烃基，CN，CO 2 H或 - （CH 2 CH 2）m H 其中m至少为1，m和p之和为1至5; X是S或O; J是H，CH 3或CF 3; D是共价键，CH 2，O或S; 并且E是芳族杂双环系统，其可以具有各自包含多达6个非氢原子的取代基。 还公开了与之相关的方法，组合物和药物。