SC-77964 | 226396-02-7

• 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: SC-77964
• 英文别名: 1-cyclopropyl-N-hydroxy-4-{4-[4-(trifluoromethoxy)phenoxy]phenylsulfonyl}piperidine-4-carboxamide hydrochloride；1-cyclopropyl-N-hydroxy-4-[[4-[4-(trifluoromethoxy)phenoxy]-phenyl]sulfonyl]-4-piperidine-carboxamide, monohydrochloride；1-cyclopropyl-N-hydroxy-4-[4-[4-(trifluoromethoxy)phenoxy]phenyl]sulfonylpiperidine-4-carboxamide;hydrochloride
• CAS: 226396-02-7
• 化学式: C₂₂H₂₃F₃N₂O₆S*ClH
• 分子量: 536.957
• InChiKey: BVIDCXUUODTSPR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.08
• 重原子数：
  35
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  114
• 氢给体数：
  3
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  1-cyclopropyl-N-(oxan-2-yloxy)-4-[4-[4-(trifluoromethoxy)phenoxy]phenyl]sulfonylpiperidine-4-carboxamide 在 盐酸 作用下， 以 1,4-二氧六环 、 甲醇 为溶剂， 反应 2.5h， 以81%的产率得到SC-77964
  参考文献：
  名称：

  Orally Active MMP-1 Sparing α-Tetrahydropyranyl and α-Piperidinyl Sulfone Matrix Metalloproteinase (MMP) Inhibitors with Efficacy in Cancer, Arthritis, and Cardiovascular Disease

  摘要：

  alpha-Sulfone-alpha-piperidine and alpha-tetrahydropyranyl hydroxamates were explored that are potent inhibitors of MMP's-2, -9, and -13 that spare MMP-1, with oral efficacy in inhibiting tumor growth in mice and left-ventricular hypertrophy in rats and in the bovine cartilage degradation ex vivo explant system. alpha-Piperidine 19v (SC-78080/SD-2590) was selected for development toward the initial indication of cancer, while alpha-piperidine and alpha-tetrahydropyranyl hydroxamates 19w (SC-77964) and 9l (SC-77774), respectively, were identified as backup compounds.

  DOI：

  10.1021/jm100669j

文献信息

• Method of using a COX-2 inhibitor and a TACE inhibitors as a combination therapy
  申请人：Pharmacia Corporation

  公开号：US20040122011A1

  公开（公告）日：2004-06-24

  The present invention provides compositions and methods to treat, prevent or inhibit a neoplasia, a neoplasia-related disorder, pain, inflammation, an inflammatory-related disorder, a vaso-occlusive event or a vaso-occlusive-related disorder in a mammal using a combination of a COX-2 inhibitor and a TACE inhibitor.

  本发明提供了一种使用COX-2抑制剂和TACE抑制剂的组合物和方法，以治疗、预防或抑制哺乳动物中的肿瘤、肿瘤相关疾病、疼痛、炎症、炎症相关疾病、血管闭塞性事件或血管闭塞性相关疾病。
• Exemestane as chemopreventing agent
  申请人：——

  公开号：US20040024044A1

  公开（公告）日：2004-02-05

  The present invention concerns the use of aromatase inhibitor exemestane, either alone or in combination with other therapeutic agents in the chemoprevention of estrogen dependent cancer in mammals, including humans, at increased risk of the disease.

  本发明涉及芳香化酶抑制剂依西美坦（exemestane）单独或与其他治疗剂联合用于哺乳动物（包括人类）雌激素依赖性癌症的化学预防。
• Methods for treating estrogen-dependent disorders
  申请人：——

  公开号：US20040082557A1

  公开（公告）日：2004-04-29

  A method of preventing and/or treating estrogen-dependent disorders selected from endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, fibrocystic breast disease and fibrocystic mastopathy, is disclosed which is comprised of administering to a female mammal in need of such treatment an effective amount of aromatase inactivator exemestane, alone or in combination with additional therapeutic agents. The present invention also relates to a method for treating infertility in a female mammal in need of the infertility treatment, comprising administering an effective amount of exemestane to the mammal.

  本发明公开了一种预防和/或治疗雌激素依赖性疾病的方法，该方法选自子宫内膜异位症、子宫肌瘤、功能失调性子宫出血、子宫内膜增生症、多囊卵巢疾病、纤维囊性乳腺疾病和纤维囊性乳腺病，其包括向需要此类治疗的雌性哺乳动物施用有效量的芳香化酶灭活剂依西美坦，单独或与其他治疗剂联合使用。本发明还涉及一种治疗需要不孕症治疗的雌性哺乳动物不孕症的方法，包括向哺乳动物施用有效量的依西美坦。
• Combination therapy including a matrix metalloproteinase inhibitor and an antineoplastic agent
  申请人：McKearn P. John

  公开号：US20050058725A1

  公开（公告）日：2005-03-17

  The present invention provides methods to treat or prevent neoplasia disorders in a mammal using a combination of a matrix metalloproteinase inhibitor and an antineoplastic agent.

  本发明提供了使用基质金属蛋白酶抑制剂和抗肿瘤剂组合治疗或预防哺乳动物肿瘤疾病的方法。
• USE OF A MATRIX METALLAPROTEINASE INHIBITOR AND RADIATION AS A COMBINED TREATMENT OF NEOPLASIA
  申请人：G.D. SEARLE & CO.

  公开号：EP1140178A2

  公开（公告）日：2001-10-10