4-(Aminomethyl)benzenesulfonamide;sulfuric acid | 5542-45-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-(Aminomethyl)benzenesulfonamide;sulfuric acid
• CAS: 5542-45-0
• 化学式: C7H12N2O6S2
• 分子量: 284.3
• InChiKey: GJQKSPOUJVHMKF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.86
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  178
• 氢给体数：
  4
• 氢受体数：
  8

文献信息

• [EN] FAP INHIBITOR<br/>[FR] INHIBITEUR DE FAP
  申请人：UNIV HEIDELBERG

  公开号：WO2019154859A1

  公开（公告）日：2019-08-15

  The present invention relates to a compound, a liposome comprising said compound, a virus-like particle comprising said compound, a pharmaceutical composition comprising or consisting of said compound, said liposome or said virus-like particle, a kit comprising or consisting of said compound, said liposome, said virus-like particle or said pharmaceutical composition and use of the compound, liposome, virus-like particle or pharmaceutical composition in the treatment of a disease characterized by overexpression of fibroblast activation protein (FAP).

  本发明涉及一种化合物，包含该化合物的脂质体，包含该化合物的病毒样颗粒，包含或由该化合物、该脂质体或该病毒样颗粒组成的药物组合物，包含或由该化合物、该脂质体、该病毒样颗粒或该药物组合物组成的试剂盒，以及在治疗由成纤维细胞激活蛋白（FAP）过表达所特征的疾病中使用该化合物、脂质体、病毒样颗粒或药物组合物。
• Orthogonally protected bifunctional amino acid
  申请人：Schering AG

  公开号：EP1717219A1

  公开（公告）日：2006-11-02

  The present invention concerns novel orthogonally protected amino acids, there production and use for the synthesis of binding compounds usable in the diagnosis and treatment of proliferative diseases, in particular tumor diseases.

  本发明涉及新型正交保护氨基酸，它们的生产和用于合成可用于诊断和治疗增殖性疾病，特别是肿瘤疾病的结合化合物。
• [EN] BICYCLIC 2,3-DIHYRDOBENZAZINE COMPOUNDS FOR USE IN THERAPY<br/>[FR] COMPOSÉS BICYCLIQUES DE 2,3-DIHYDROBENZAZINE DESTINÉS À UNE UTILISATION THÉRAPEUTIQUE
  申请人：ELARA PHARMACEUTICALS GMBH

  公开号：WO2012130306A1

  公开（公告）日：2012-10-04

  The present invention provides novel 2,3-dihydrobenzazine compounds of formula (I) and to their salts. The compounds inhibit cell proliferation and cell division and they also inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions (I) wherein X is O or S(=O)n; n is 0, 1 or 2; R1 is an optionally substituted C-bound bicyclyl comprising a first ring which is a benzene ring or a 5- or 6-membered heteroaromatic ring having either 1, 2 or 3 nitrogen atoms as heteroatom ring members or 1 oxygen or 1 sulfur atom and 0, 1 or 2 nitrogen atoms as heteroatom ring members, and a second ring, which is fused to the first ring, where the second ring is a 5-, 6- or 7-membered carbocyclic ring or a 5-, 6- or 7-membered heterocyclic ring having 1, 2 or 3 heteroatom ring members selected from oxygen, sulfur and nitrogen, where sulfur atoms, if present, may be present as S, S(O) or S(O)2 and where the saturated or unsaturated carbocyclic or heterocyclic second ring may also have 1 or 2 carbonyl groups or thiocarbonyl groups as ring members; R2 is an optionally substituted aromatic radical selected from phenyl, C-bound mono- cyclic 5- or 6-membered heteroaryl or C-bound bicyclyl comprising a first ring which is a benzene ring or a 5- or 6-membered heteroaromatic ring and a second ring, which is fused to the first ring, where the second ring is a 5-, 6- or 7-membered carbocyclic ring or a 5-, 6- or 7-membered heterocyclic ring.

  本发明提供了式（I）的新型2,3-二氢苯并嗪化合物及其盐。该化合物抑制细胞增殖和细胞分裂，并抑制缺氧条件下缺氧诱导因子（HIF）介导的转录和信号的激活。（I）其中X为O或S（=O）n; n为0，1或2; R1为一个可选取代的C-连接的双环，包括第一个环，该环为苯环或具有1,2或3个氮原子作为杂环原子环成员或1个氧原子或1个硫原子和0,1或2个氮原子作为杂环原子环成员的5-或6-成员杂环环，并且第二个环与第一个环融合，其中第二个环为5-,6-或7-成员碳环或5-,6-或7-成员杂环，具有1,2或3个氧、硫和氮中的杂环环成员，其中硫原子如果存在，则可以存在为S，S（O）或S（O）2，并且饱和或不饱和的碳环或杂环第二环也可以具有1或2个羰基基团或硫代羰基基团作为环成员; R2为一个可选取代的芳基，选自苯基，C-连接的单环5-或6-成员杂芳基或包括第一个环的C-连接的双环，该环为苯环或5-或6-成员杂芳环，并且第二个环与第一个环融合，其中第二个环为5-,6-或7-成员碳环或5-,6-或7-成员杂环。
• INHIBITORS OF CELL PROLIFERATION AND USES THEREOF
  申请人：Reid George

  公开号：US20110060043A1

  公开（公告）日：2011-03-10

  The present invention provides novel compounds that inhibit cell proliferation and uses of these compounds for treating, ameliorating or preventing diseases, conditions or disorders benefiting from the inhibition hyperproliferation.

  本发明提供了一种新型化合物，可抑制细胞增殖，并利用这些化合物治疗、改善或预防从抑制过度增殖中受益的疾病、病症或障碍。
• IMIDAZO [1,2-a]PYRIDINE COMPOUNDS FOR USE IN THERAPY
  申请人：Mulbaier Marcel

  公开号：US20140221354A1

  公开（公告）日：2014-08-07

  The present invention provides novel imidazo[1,2-a]pyridine compounds that are useful in therapy of diseases and disorders. The novel compounds inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularization. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders, wherein X is CH 2 , CH 2 CH 2 or C═O; R 1 is phenyl or C-bound monocyclic 5- or 6-membered heteroaryl, wherein phenyl and monocyclic 5- or 6-membered heteroaryl are unsubstituted or carry 1, 2, 3, 4 or 5 radicals R 1a which are identical or different; R 2 is phenyl or C-bound monocyclic 5- or 6-membered heteroaryl, wherein phenyl and monocyclic 5- or 6-membered heteroaryl are unsubstituted or carry 1, 2, 3, 4 or 5 radicals R 2a which are identical or different; R 3 is hydrogen, C 1 -C 6 -alkyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, fluorinated C 1 -C 2 -alkyl C(O)R 4 ; where R 1a , R 2a and R 4 are as defined in the claims and the specification.

  本发明提供了新型咪唑[1,2-a]吡啶化合物，用于治疗疾病和疾病障碍。这些新型化合物抑制缺氧条件下缺氧诱导因子（HIF）介导的转录和信号的激活。在一个方面，本发明的化合物可用于制备治疗或预防炎症性疾病、高增殖性疾病或疾病障碍、缺氧相关病理和过度血管化疾病的药物。还提供了一种药物组合物，包括本发明的化合物和第二种治疗剂或辐射，用于治疗或预防上述疾病或疾病障碍，其中X为CH2、CH2CH2或C═O；R1为苯基或C-结合的单环5-或6-成员杂环，其中苯基和单环5-或6-成员杂环未被取代或携带1、2、3、4或5个相同或不同的R1a基团；R2为苯基或C-结合的单环5-或6-成员杂环，其中苯基和单环5-或6-成员杂环未被取代或携带1、2、3、4或5个相同或不同的R2a基团；R3为氢、C1-C6-烷基、C1-C4-烷氧基-C1-C4-烷基、氟化C1-C2-烷基C(O)R4；其中R1a、R2a和R4如权利要求和说明书中所定义。