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    二氧化碳可逆保护的扩链交联剂及其制备方法与应用
    3.
    发明申请
    二氧化碳可逆保护的扩链交联剂及其制备方法与应用 审中-公开

    公开(公告)号：WO2020057047A1

    公开(公告)日：2020-03-26

    申请号：PCT/CN2019/074634

    申请日：2019-02-02

    Applicant: 中国科学院长春应用化学研究所

    Inventor： 杨小牛 ,  张波 ,  赵晓礼 ,  李肖肖 ,  田雨濛

    IPC: C07C271/02 ,  C08G18/32

    Abstract: 一种二氧化碳可逆保护的扩链交联剂及其制备方法与应用。所述二氧化碳可逆保护的扩链交联剂具有式(I)、式(II)、式(III)或式(IV)所示的化学结构，其中n、m和p均为整数，R为OCH 2 CH(CH 3 )或OCH 2 CH 2 ，1≤n≤20，1≤m≤10，1≤p≤10。所述二氧化碳可逆保护多元胺的方法在聚氨酯常见体系中都能实现低分子量的多元胺作为扩链剂制备聚氨酯，制备的聚氨酯具备很好的力学性能，拓宽了不同形式的脂肪族多元胺作为交联扩链剂在聚氨酯弹性体材料中的应用。

    NOVEL BORNEOLS, PROCESSES FOR PRODUCING THEM AND PHARMACEUTICAL USE THEREOF
    5.
    发明申请
    NOVEL BORNEOLS, PROCESSES FOR PRODUCING THEM AND PHARMACEUTICAL USE THEREOF 审中-公开
    新冰片，PROCESS FOR THEIR和制药用

    公开(公告)号：WO1997035839A1

    公开(公告)日：1997-10-02

    申请号：PCT/EP1996001324

    申请日：1996-03-27

    Applicant: SCHERING AKTIENGESELLSCHAFT ,  KLAR, Ulrich ,  GRAF, Hermann ,  BLECHERT, Siegfried ,  SACHSE, Anke

    Inventor： SCHERING AKTIENGESELLSCHAFT

    IPC: C07C271/02

    CPC classification number: C07D303/16 ,  C07C233/83 ,  C07C271/22 ,  C07C2602/42 ,  C07F7/1804

    Abstract: The disclosure relates to borneol derivatives of general formula (I) wherein: R represents a phenyl residue optionally substituted by halogen atoms, C1-C4 alkyl groups, C1-C4 alkoxy groups, C1-C6 alkoxycarbonyl groups or C1-C8 acyloxy groups; R stands for a hydrogen atom, a C1-C4 alkyl group, substituted aryl, a C1-C6 alkoxycarbonyl group or a C1-C8 acyl group; R stands for a hydrogen atom, a C1-C4 alkyl group, a C1-C4 acyl group or a tri-C1-C4 alkylsilyl group; R and R represent a hydrogen atom, a C1-C4 alkyl residue or a phenyl residue optionally substituted by halogen atoms, C1-C4 alkyl group, C1-C9 alkoxy groups, C1-C4 alkoxycarbonyl groups or C1-C8 acyloxy groups; R and R stand for a hydrogen atom, hydroxy group or a C1-C8 acyloxy group, or together represent a carbon-carbon bond or oxygen atom; or R and R and/or R and R respectively stand together for a carbonyl group, a C1-C4 alkylidene group or if required an oxirane group substituted by a C1-C3 alkyl group. Also disclosed are the salts of these derivatives with physiologically tolerable acids, their alpha -, beta - or gamma -cyclodextrin clathrates and compounds of general formula (I) encapsulated in liposomes.

    Abstract translation: Borneolderivate通式（I）中有所描述，其中R <1>表示任选被卤原子，C1-C4烷基，C1-C4烷氧基，C1-C6烷氧羰基或C 1 -C 8 - 酰氧基苯基取代; [R <2>表示一个氢原子，一个C1-C4烷基，取代的芳基，一个C1-C6烷氧基羰基或C1-C8酰基基团; [R <3>代表氢原子，C1-C4烷基，C1-C4酰基或三C1-C4烷基甲硅烷基，并且其中; [R <4>和R <7>代表氢原子，C1-C4烷基或任选地被卤素原子，C1-C4烷基，C1-C9烷氧基，C1-C4烷氧羰基或C 1 -C 8 - 酰氧基苯基取代的 且R <5>和R <6>代表氢原子，羟基或C1-C8-酰氧基或一起代表碳 - 碳键或氧原子，或R <4>和R <5>和/或R <6> 且R <7>的每个一起表示羰基，C1-C4亚烷基，或者，如果需要的话，由一个C1-C3烷基取代的环氧乙烷基团，和任选地它们的盐与生理上可接受的酸，以及它们的α - ，β - 或伽马-Cyclodextrinclathrate和 通式（I）的脂质体包裹的化合物的意思。

    HYDROXAMIC ACID-BASED BIFUNCTIONAL CHELATING COMPOUNDS
    6.
    发明申请
    HYDROXAMIC ACID-BASED BIFUNCTIONAL CHELATING COMPOUNDS 审中-公开
    基于羟基酸的双功能螯合化合物

    公开(公告)号：WO1994005627A1

    公开(公告)日：1994-03-17

    申请号：PCT/US1993008401

    申请日：1993-09-07

    Applicant: UAB RESEARCH FOUNDATION

    Inventor： UAB RESEARCH FOUNDATION ,  SAFAVY, Ahmad ,  BUCHSBAUM, Donald, J. ,  KHAZAELI, M., B.

    IPC: C07C271/02

    CPC classification number: C07C259/06 ,  A61K51/1093 ,  A61K2121/00 ,  A61K2123/00 ,  C07K5/022

    Abstract: The present disclosure details the preparation of hydroxamic-acid based bifunctional chelators and their use in conjugating metal ions to proteins and nucleic acids for tumor or tissue imaging or therapy purposes. Some preferred aspects of the disclosure involve the preparation of trisuccin, chemical name N-((tris)(2-N-benzyloxyaminocarbonylethyl)) methylsuccinamic acid, which is a hydroxamic acid/succinate based structure that is particularly useful for binding radionuclides such as 99mTc, 186Re and 67Cu.

    Abstract translation: 本公开详细描述了基于异羟肟酸的双功能螯合剂的制备及其在将金属离子与用于肿瘤或组织成像或治疗目的的蛋白质和核酸结合的用途。 本公开的一些优选方面涉及制备三羟色胺，化学名称N - （（三（（三（（（N） - 三苄基氧基氨基羰基乙基））甲基琥珀酸，其是特别可用于结合放射性核素如99mTc的异羟肟酸/ ，186Re和67Cu。

    SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
    9.
    发明申请
    SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 审中-公开
    选择性雄激素受体降解物（SARD）配体及其使用方法

    公开(公告)号：WO2017214634A1

    公开(公告)日：2017-12-14

    申请号：PCT/US2017/037063

    申请日：2017-06-12

    Applicant: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

    Inventor： NARAYANAN, Ramesh ,  MILLER, Duane ,  PONNUSAMY, Thamarai ,  HWANG, Dong-Jin ,  HE, Yali

    IPC: A61K31/325 ,  C07C271/02

    Abstract: This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors, R -isomers, and non-hydroxylated and/or non-chiral propanamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

    Abstract translation: 本发明涉及吡咯，吡唑，咪唑，三唑和基于吗啉的选择性雄激素受体降解剂（SARD）化合物，包括杂环酰苯胺环及其合成前体，R- 异构体和非羟基化和/或非手性丙酰胺，以及其在治疗前列腺癌，晚期前列腺癌，去势抵抗性前列腺癌，三阴性乳腺癌，表达雄激素受体的其他癌症，雄激素性脱发或其他 高雄激素性皮肤病，肯尼迪氏病，肌萎缩性侧索硬化症（ALS），腹主动脉瘤（AAA）和子宫肌瘤，以及降低包括致病性或抗性突变在内的雄激素受体全长（AR-FL） （AR-SV）和AR的致病性聚谷氨酰胺（polyQ）多态性。

    METHOD FOR PREPARING SOLID CARBAMIC ACID DERIVATIVES
    10.
    发明申请
    METHOD FOR PREPARING SOLID CARBAMIC ACID DERIVATIVES 审中-公开
    制备固体碳酸衍生物的方法

    公开(公告)号：WO2012111946A2

    公开(公告)日：2012-08-23

    申请号：PCT/KR2012001046

    申请日：2012-02-13

    Applicant: UNIV SOGANG IND UNIV COOP FOUN ,  HUR NAM HWI ,  LEE BYEONG NO

    Inventor： HUR NAM HWI ,  LEE BYEONG NO

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

    CPC classification number: C07C209/46 ,  C07B43/00 ,  C07C269/04 ,  C07D295/13 ,  C07C271/02

    Abstract: The present invention relates to a method for preparing solid carbamic acid derivative powder which comprises a step of reacting liquid amine derivatives with carbon dioxides at -30 to 500 ? under 0.3 to 100 MPa. In addition, the invention relates to a method for reducing carbamic acid derivative powder with the liquid amine derivatives and carbon dioxides which comprises the steps of: dissolving the prepared carbamic acid derivative powder in a solvent; refluxing the resultant at 50 to 80 ?; and evaporating the solvent. The method for preparing a carbamic acid derivative powder according to the invention enables easy conversion into pure solid carbamic acid derivative powder without by-products and can remarkably reduce time and energy required for solidification by reacting carbon dioxides and amines with carbon dioxides in high pressure conditions without the use of a solvent. In addition, the prepared solid compounds can be used as a liquid amine substitute or used in a carbamic acid derivative form as necessary.

    Abstract translation: 本发明涉及一种制备固体氨基甲酸衍生物粉末的方法，该方法包括使液体胺衍生物与二氧化碳在-30至500℃反应的步骤， 0.3〜100MPa。 此外，本发明涉及一种用液体胺衍生物和二氧化碳还原氨基甲酸衍生物粉末的方法，包括以下步骤：将制备的氨基甲酸衍生物粉末溶解在溶剂中; 将所得物在50〜80℃下回流; 并蒸发溶剂。 根据本发明的制备氨基甲酸衍生物粉末的方法能够容易地转化成纯的固体氨基甲酸衍生物粉末而不产生副产物，并且可以显着地减少二氧化碳和胺与二氧化碳在高压条件下反应而固化所需的时间和能量 而不使用溶剂。 此外，所制备的固体化合物可以根据需要用作液体胺替代物或以氨基甲酸衍生物形式使用。

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