2,8-Diazabicyclo<3.3.0>octan-3,7-dion | 42977-13-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: 2,8-Diazabicyclo<3.3.0>octan-3,7-dion
• 英文别名: tetrahydro-pyrrolo[2,3-b]pyrrole-2,5-dione；1,3,3a,4,6,6a-Hexahydropyrrolo[2,3-b]pyrrole-2,5-dione
• CAS: 42977-13-9
• 化学式: C₆H₈N₂O₂
• 分子量: 140.142
• InChiKey: UAUKJNGCKBZPBK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.3
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  58.2
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  azane;2-(2-hydroxy-5-oxopyrrolidin-3-yl)acetic acid 、 对甲苯磺酸 以50%的产率得到
  参考文献：
  名称：

  VICTORY, P. J.;PEREZ-DE-LA-OSSA, R.;COMELLAS, L.;BORRELL, J. I.;MASCORDA,+, AFINIDAD, 48,(1991) N33, C. 149-154

  摘要：

  DOI：

文献信息

• [EN] PYRAZOLE CARBOXAMIDE COMPOUNDS FOR TREATMENT OF HBV<br/>[FR] COMPOSÉS DE PYRAZOLE CARBOXAMIDE POUR LE TRAITEMENT DU VHB
  申请人：ASSEMBLY BIOSCIENCES INC

  公开号：WO2021216642A1

  公开（公告）日：2021-10-28

  The present disclosure provides, in part, pyrazole carboxamide compounds, and pharmaceutical compositions thereof, useful for disruption of HBV core protein assembly, and methods of treating Hepatitis B (HBV) infection.

  本公开提供了吡唑羧酰胺化合物及其药物组合物，用于破坏HBV核心蛋白的组装，并治疗乙型肝炎（HBV）感染的方法。
• [EN] PROSTACYCLIN DERIVATIVES<br/>[FR] DÉRIVÉS DE PROSTACYCLINE
  申请人：CONCERT PHARMACEUTICALS INC

  公开号：WO2011003058A1

  公开（公告）日：2011-01-06

  This invention relates to novel prostacyclin derivatives and acceptable salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by prostacyclin, and in particular those diseases and conditions beneficially treated by dilators of systemic and pulmonary arterial vascular beds or by platelet aggregation inhibitors.

  本发明涉及新的前列腺素I2衍生物及其可接受的盐。该发明还提供了包含本发明化合物的组合物，以及将这些组合物用于治疗通过前列腺素I2有益治疗的疾病和状况的方法，特别是那些通过全身和肺动脉血管床扩张剂或通过血小板聚集抑制剂有益治疗的疾病和状况。
• TETRAHYDRONAPHTHALENE AND TETRAHYDROISOQUINOLINE DERIVATIVES AS ESTROGEN RECEPTOR DEGRADERS
  申请人：Arvinas, Inc.

  公开号：US20180155322A1

  公开（公告）日：2018-06-07

  The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

  本公开涉及双功能化合物，这些化合物可用作雌激素受体（目标蛋白）的调节剂。特别是，本公开涉及包含在一段至少有一种Von Hippel-Lindau配体、一种cereblon配体、凋亡抑制蛋白配体、小鼠双分钟同源2配体或其组合的双功能化合物，这些配体与相应的E3泛素连接酶结合，在另一端有一个与目标蛋白结合的部分，使得目标蛋白被置于泛素连接酶附近，以实现目标蛋白的降解（和抑制）。本公开展示了与目标蛋白降解/抑制相关的广泛药理活性。可以通过本公开的化合物和组合物治疗或预防由目标蛋白聚集或积累引起的疾病或障碍。
• DUAL MOLECULES CONTAINING A PEROXIDE DERIVATIVE, THEIR SYNTHESIS AND THERAPEUTIC USES
  申请人：COSLEDAN Frederic

  公开号：US20120122923A1

  公开（公告）日：2012-05-17

  The invention concerns dual molecules corresponding to formula (I): in which: A represents a molecular residue with antimalarial activity of formula (IIa) or (IIIa) or a residue facilitating bioavailability; B represents a cycloalkyl group potentially substituted, or B represents a bi- or tricyclic group capable of being substituted, or B represents 2 cycloalkyl groups linked together through either a single bond or an alkylene chain; m and n represent independently of one another 0, 1 or 2; R 5 represents a hydrogen atom, an alkyl, cycloalkyl or C 1-3 -alkylene-cycloakyl group; Z 1 and Z 2 represent an alkyl radical, the group Z 1 +Z 2 +C i +C j representing a mono- or polycyclic structure, with one of the Z 1 or Z 2 being able to represent a single bond; R 1 and R 2 , identical or different, represent a hydrogen atom or a functional group capable of increasing hydrosolubility; R x and R y forming together a cyclic peroxide including 4 to 8 links and including 1 or 2 additional oxygen atoms in the cyclic structure, possibly substituted by one or more R 3 groups; as a base or a salt to be added to an acid, as a hydrate or solvate, in racemic form, isomers and their mixtures, in addition to their diasteroisomers and their mixtures. Preparation method and use as medications with antimalarial activity.

  本发明涉及与式(I)相对应的双分子，其中：A代表具有抗疟活性的分子残基，其化学式为(IIa)或(IIIa)，或者代表有助于生物利用度的残基；B代表可能被取代的环烷基团，或者B代表可能被取代的双环或三环基团，或者B代表通过单键或烷基链连接在一起的2个环烷基团；m和n分别独立地表示0、1或2；R5代表氢原子、烷基、环烷基或C1-3-烷基-环烷基团；Z1和Z2代表烷基基团，Z1+Z2+Ci+Cj代表单环或多环结构，其中Z1或Z2之一可以表示单键；R1和R2，相同或不同，代表氢原子或能增加水溶性的功能基团；Rx和Ry共同形成一个包含4到8个链的环过氧化物，包括环结构中的1或2个额外氧原子，可能被一个或多个R3基团取代；作为酸的碱或盐形式，作为水合物或溶剂合物，以外消旋形式、同分异构体及其混合物，以及它们的对映异构体及其混合物。制备方法和用作具有抗疟活性的药物。
• HYDROXY FUNCTIONAL ALKYL POLYUREA
  申请人：PPG INDUSTRIES OHIO, INC.

  公开号：US20170204289A1

  公开（公告）日：2017-07-20

  A hydroxy functional alkyl polyurea is disclosed having the formula: wherein R comprises the residue of an isocyanurate, biuret, allophonate, glycoluril, benzoguanamine, and/or polyetheramine; or R comprises the reaction product of isocyanate and alkanol amine, but the isocyanate is not HDI when the alkanol amine is diethanol amine or monomethanol amine and the isocyanate is not IPDI when the alkanol amine is monomethanol amine; wherein each R1 is independently a hydrogen, alkyl having at least 1 carbon, or a hydroxy functional alkyl having 2 or more carbons and at least one R1 is a hydroxy functional alkyl having 2 or more carbons; and n is 2-6. Further disclosed is a coating comprising: a. A film forming resin; and b. A hydroxy functional alkyl polyurea crosslinker having the formula: wherein R2 is a substituted or unsubstituted C1 to C36 alkyl group, an aromatic group, the residue of an isocyanurate, biuret, allophanate, glycoluril, benzoguanamine and/or polyetheramine wherein each R1 is independently a hydrogen, and alkyl having at least 1 carbon, or a hydroxy functional alkyl having 2 or more carbons and at least one R1 is a hydroxy functional alkyl having 2 or more carbons; and n is 2-6. Substrates coated at least in part with such a coating are also disclosed.

  揭示了具有以下化学式的羟基功能烷基聚脲：其中R包括异氰酸酯、双脲、异氰脲酸酯、甘氨酸酰胺、苯基胍胺和/或聚醚胺的残基；或者R包括异氰酸酯和烷醇胺的反应产物，但当烷醇胺为二乙醇胺或甲基乙醇胺时，异氰酸酯不是HDI，当烷醇胺为甲基乙醇胺时，异氰酸酯不是IPDI；其中每个R1独立地是氢、至少有1个碳的烷基，或具有2个或更多碳的羟基功能烷基，且至少一个R1是具有2个或更多碳的羟基功能烷基；n为2-6。还揭示了包括：a. 形成膜的树脂；和b. 具有以下化学式的羟基功能烷基聚脲交联剂：其中R2是取代或未取代的C1到C36烷基团、芳香族基团、异氰酸酯、双脲、异氰脲酸酯、甘氨酸酰胺、苯基胍胺和/或聚醚胺的残基，其中每个R1独立地是氢、至少有1个碳的烷基，或具有2个或更多碳的羟基功能烷基，且至少一个R1是具有2个或更多碳的羟基功能烷基；n为2-6。还揭示了至少部分涂有这种涂层的基材。