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    A METHOD OF TREATING ANDROGEN RECEPTOR (AR)-POSITIVE BREAST CANCERS WITH SELECTIVE ANDROGEN RECEPTOR MODULATOR (SARMS)
    23.
    发明申请
    A METHOD OF TREATING ANDROGEN RECEPTOR (AR)-POSITIVE BREAST CANCERS WITH SELECTIVE ANDROGEN RECEPTOR MODULATOR (SARMS) 审中-公开
    用选择性的雄激素受体调节剂（SARMS）治疗雄激素受体（AR） - 乳腺癌的方法

    公开(公告)号：WO2014011220A2

    公开(公告)日：2014-01-16

    申请号：PCT/US2013/029667

    申请日：2013-03-07

    Applicant: GTX, INC. ,  DALTON, James, T. ,  STEINER, Mitchell, S. ,  NARAYANAN, Ramesh ,  AHN, Sunjoo

    Inventor： DALTON, James, T. ,  STEINER, Mitchell, S. ,  NARAYANAN, Ramesh ,  AHN, Sunjoo

    IPC: C07C271/02 ,  A61K31/325 ,  A61K45/06

    CPC classification number: C07C271/02 ,  A61K31/167 ,  A61K31/325 ,  A61K45/06 ,  Y02A50/395

    Abstract: This invention relates to the treatment of androgen receptor-positive breast cancer in a subject, for example a female subject. Accordingly, this invention provides methods of: a) treating a subject suffering from breast cancer; b) treating a subject suffering from metastatic breast cancer; c) treating a subject suffering from refractory breast cancer; d) treating a subject suffering from AR-positive breast cancer; e) treating a subject suffering from AR-positive refractory breast cancer; f) treating a subject suffering from AR-positive metastatic breast cancer; g) treating a subject suffering from AR-positive and ER-positive breast cancer; h) treating a subject suffering from triple negative breast cancer; i) treating a subject suffering from advanced breast cancer; j) treating a subject suffering from breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and/or fulvestrant treatments; k) treating, preventing, suppressing or inhibiting metastasis in a subject suffering from breast cancer; 1) prolonging survival of a subject with breast cancer, and/or m) prolonging the progression-free survival of a subject with breast cancer; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound, comprising administering to the subject a therapeutically effective amount of a SARM compound of this invention.

    Abstract translation: 本发明涉及治疗受试者中雄激素受体阳性乳腺癌，例如女性受试者。 因此，本发明提供了以下方法：a）治疗患有乳腺癌的受试者; b）治疗患有转移性乳腺癌的受试者; c）治疗难治性乳腺癌患者; d）治疗患有AR阳性乳腺癌的受试者; e）治疗患有AR阳性难治性乳腺癌的受试者; f）治疗患有AR阳性转移性乳腺癌的受试者; g）治疗患有AR阳性和ER阳性乳腺癌的受试者; h）治疗患有三阴性乳腺癌的受试者; i）治疗晚期乳腺癌患者; j）治疗患有SERM（他莫昔芬，托瑞米芬），芳香酶抑制剂，曲妥珠单抗（赫赛汀，阿霉素，阿曲曲坦），奥妥珠单抗（Perjeta），拉帕替尼，依西美坦（Aromasin），贝伐珠单抗（Avastin） /或氟维司群治疗; k）治疗，预防，抑制或抑制患有乳腺癌的受试者的转移; 1）延长患有乳腺癌的受试者的存活，和/或m）延长患有乳腺癌的受试者的无进展生存期; 包括向受试者施用治疗有效量的选择性雄激素受体调节剂（SARM）化合物，其包括向受试者施用治疗有效量的本发明的SARM化合物。

    고체 카르밤 산 유도체의 제조 방법
    24.
    发明申请
    고체 카르밤 산 유도체의 제조 방법 审中-公开

    公开(公告)号：WO2012111946A3

    公开(公告)日：2012-08-23

    申请号：PCT/KR2012/001046

    申请日：2012-02-13

    Applicant: 서강대학교 산학협력단 ,  허남회 ,  이병노

    Inventor： 허남회 ,  이병노

    IPC: C07C269/04 ,  C07C271/02 ,  C07C211/63 ,  B01J2/00 ,  C07B43/04

    Abstract: 본 발명은 액체 아민 유도체와 이산화탄소를 -30 ~ 500 ℃, 0.3 ~ 100 MPa의 압력에서 반응시키는 것을 포함하는 카르밤 산 유도체 분말 제조 방법에 관한 것이다. 또한 본 발명은 상기 제조된 카르밤 산 유도체 분말을 용매에 용해한 후, 50 ~ 80 ℃에서 환류 시키고, 상기 용매를 증발시키는 것을 포함하는 카르밤 산 유도체 분말을 액체 아민 유도체와 이산화탄소로 환원시키는 방법에 관한 것이다. 본 발명에 따른 카르밤 산 유도체 분말 제조 방법은 용매를 사용하지 않고 이산화탄소와 아민을 이산화탄소와 고압 조건에서 반응시킴으로써, 부산물 없이 순수한 고체 카르밤 산 유도체 분말로 쉽게 전환시킬 수 있으며, 고체화에 필요한 시간과 에너지를 크게 절감할 수 있다. 또한, 생성된 고체 화합물들은, 필요에 따라, 액상 아민의 대체용으로 사용하거나, 카르밤 산 유도체 형태로도 사용이 가능하다.

    CYCLOOXYGENASE-2 SELECTIVE INHIBITOR COMPOUNDS COMPRISING NITRIC OXIDE ENHANCING GROUPS, COMPOSITIONS AND METHODS OF USE
    26.
    发明申请
    CYCLOOXYGENASE-2 SELECTIVE INHIBITOR COMPOUNDS COMPRISING NITRIC OXIDE ENHANCING GROUPS, COMPOSITIONS AND METHODS OF USE 审中-公开
    包含氮氧化物增强组合物的CYCLOOXYGENASE-2选择性抑制剂化合物，组合物和使用方法

    公开(公告)号：WO2007016095A3

    公开(公告)日：2008-02-28

    申请号：PCT/US2006028856

    申请日：2006-07-26

    Applicant: NITROMED INC ,  GARVEY DAVID S

    Inventor： GARVEY DAVID S

    IPC: C07C229/42 ,  A61K31/04 ,  A61K31/136 ,  A61K31/4245 ,  A61P1/04 ,  A61P7/02 ,  A61P9/14 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  C07C271/02 ,  C07D271/04 ,  C07D271/08 ,  C07D273/00 ,  C07D413/04

    CPC classification number: C07C229/42

    Abstract: The invention describes compositions and kits comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor comprising at least one nitric oxide enhancing group, or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor comprising at least one nitric oxide enhancing group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating inflammation, pain and fever; (b) treating gastrointestinal disorders and/or improving the gastrointestinal properties of COX-2 selective inhibitors; (c) facilitating wound healing; (d) treating renal and/or respiratory toxicities; (e) treating disorders resulting from elevated levels of cyclooxygenase-2; (f) improving the cardiovascular profile of COX-2 selective inhibitors; (g) treating diseases resulting from oxidative stress; (h) treating endothelial dysfunctions; (j) treating diseases caused by endothelial dysfunctions; (k) treating inflammatory disease states and/or disorders; (1) treating ophthalmic disorders; and (m) treating peripheral vascular diseases. The cyclooxygenase 2 selective inhibitors of the invention are 2(2-((2-chloro-6-fluorophenyl) amino)5-methylphenyl)acetic acid derivatives comprising at least one nitric oxide enhancing group. The nitric oxide enhancing groups are nitroxides and/or heterocyclic nitric oxide donors.

    Abstract translation: 本发明描述了包含至少一种包含至少一种一氧化氮增强基团的环氧合酶2（COX-2）选择性抑制剂或其药学上可接受的盐的组合物和试剂盒，以及包含至少一种环氧合酶2（COX-2）选择性抑制剂 包括至少一种一氧化氮增强基团和任选的至少一种一氧化氮增强化合物和/或至少一种治疗剂。 本发明还提供了（a）治疗炎症，疼痛和发烧的方法; （b）治疗胃肠道疾病和/或改善COX-2选择性抑制剂的胃肠性质; （c）促进伤口愈合; （d）治疗肾脏和/或呼吸毒性; （e）治疗由环氧合酶-2水平升高引起的疾病; （f）改善COX-2选择性抑制剂的心血管状态; （g）治疗由氧化应激引起的疾病; （h）治疗内皮功能障碍; （j）治疗由内皮功能障碍引起的疾病; （k）治疗炎性疾病状态和/或病症; （1）治疗眼科疾病; 和（m）治疗外周血管疾病。 本发明的环氧合酶2选择性抑制剂是包含至少一种一氧化氮增强基团的2（2 - （（2-氯-6-氟苯基）氨基）5-甲基苯基）乙酸衍生物。 一氧化氮增强基团是氮氧化物和/或杂环一氧化氮供体。

    OMEGA-AMINO ACID DERIVATIVES, PROCESSES OF THEIR PREPARATION AND THEIR USE
    28.
    发明申请
    OMEGA-AMINO ACID DERIVATIVES, PROCESSES OF THEIR PREPARATION AND THEIR USE 审中-公开
    欧米茄氨基酸衍生物及其制备方法及其使用

    公开(公告)号：WO98045233A2

    公开(公告)日：1998-10-15

    申请号：PCT/CZ1998/000017

    申请日：1998-04-01

    IPC: C07C219/04 ,  A61K47/18 ,  C07C219/06 ,  C07C219/18 ,  C07C229/06 ,  C07C229/08 ,  C07C229/10 ,  C07C229/28 ,  C07C233/47 ,  C07C271/02 ,  C07C19/04 ,  C07C223/06

    CPC classification number: C07C219/06 ,  A61K9/0014 ,  A61K47/183 ,  C07C229/08 ,  C07C229/10 ,  C07C233/47 ,  C07C271/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2601/20 ,  C07C2602/08 ,  C07C2603/74

    Abstract: The invention relates to omega -amino acid derivatives of general formula (I), wherein R is H or CH3, X is H or NR R , wherein R is H, CH3, COH or COCH3 and R is H, CH3 or COO Z, wherein Z is R R NH CHR (CH2)nCOO(CH2)mCH2Y; Y is H, CH3 or NHR , wherein R is COO NH3 CH2(CH2)mOOC(CH2)nCH3, the meaning of group (CH2)m being selected from alkyls, secondary alkyls, monocycloalkyls, bicycloalkyls and tricycloalkyls having from 4 to 15 carbon atoms and n having a value of from 3 to 14. omega -Amino acid derivatives of the invention are prepared by reacting a primary or secondary or monocyclic or bicyclic or tricyclic alcohol with the reaction product of an amino acid or an N-substituted amino acid with thionyl chloride, whereafter the amino group, which has been released by an amine, reacts with carbon dioxide providing a derivative of carbamic acid, or by directly reacting a primary or secondary or monocyclic or bicyclic or tricyclic alcohol with an N-substituted amino acid in the presence of a condensing agent giving the corresponding ester of the N-substituted amino acid. Thus produced compounds of formula (I) can be used as transdermal penetration enhancers. Incorporation of from 0.1 w/w percent to 5.0 w/w percent of a compound of the invention as a transdermal penetration enhancer in the vehicle of a topically applied pharmaceutical or cosmetic composition enhances transdermal penetration of pharmaceutical agents through the human or animal skin. Included further are transdermal penetration enhancers consisting of at least one compound of formula (I).

    Abstract translation: 本发明涉及通式（I）的ω-氨基酸衍生物，其中R 1是H或CH 3，X是H或NR 2 R 3，其中R 2是H，CH 3，COH 或COCH 3和R 3是H，CH 3或COO Z，其中Z是R 2 R 3 NH + CHR 1（CH 2）n COO（CH 2）m CH 2 Y; Y是H，CH 3或NHR 4，其中R 4是COO - ，NH 3 + CH 2（CH 2）m OOC（CH 2）n CH 3，基团（CH 2）m的含义选自烷基，仲烷基 具有4至15个碳原子的单环烷基，三环烷基和n具有3至14的值。本发明的ω-氨基酸衍生物通过使伯或仲或单环或双环或三环醇与反应 氨基酸或N-取代氨基酸与亚硫酰氯的产物，之后已经被胺释放的氨基与提供氨基甲酸衍生物的二氧化碳反应，或通过使伯或仲或单环 或二环或三环醇与N-取代氨基酸在缩合剂存在下反应，得到相应的N-取代氨基酸酯。 因此产生的式（I）化合物可用作透皮渗透增强剂。 在局部应用的药物或化妆品组合物的载体中掺入0.1w / w％至5.0w / w％的作为透皮渗透促进剂的本发明化合物增强药物通过人或动物皮肤的透皮渗透。 还包括由至少一种式（I）化合物组成的透皮渗透增强剂。

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