(+/-)-7-(4'-fluoro[1,1'-biphenyl]-4-yl)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-ol | 426219-17-2

• 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: (+/-)-7-(4'-fluoro[1,1'-biphenyl]-4-yl)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-ol
• 英文别名: 7-[4-(4-Fluorophenyl)phenyl]-5,6-dihydropyrrolo[1,2-c]imidazol-7-ol
• CAS: 426219-17-2；426219-30-9；426219-31-0
• 化学式: C₁₈H₁₅FN₂O
• 分子量: 294.328
• InChiKey: GIYVJBCEIATHSN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  38
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  7-(4-bromophenyl)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-ol 、 4-氟苯硼酸 、 sodium carbonate 在 三苯基膦钯 作用下， 生成 (+/-)-7-(4'-fluoro[1,1'-biphenyl]-4-yl)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-ol
  参考文献：
  名称：

  Novel imidazole derivatives, production method thereof and use thereof

  摘要：

  本发明提供一种具有类固醇C17,20-裂解酶抑制活性的化合物，用于治疗和预防前列腺癌、乳腺癌等肿瘤，以及一种有效地从其光学异构体混合物中分离出该化合物的光学活性化合物的方法，该化合物的化学式为：1其中每个符号如规范中定义，其盐或前药，以及通过使用像酞氨酸等分离剂对光学异构体混合物进行光学分离来获得光学活性化合物的方法。

  公开号：

  US20040033935A1

文献信息

• COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
  申请人：Zhang Jiazhong

  公开号：US20110263595A1

  公开（公告）日：2011-10-27

  Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC kinase protein. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC, including rheumatoid arthritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, global ischemia, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, atherosclerosis, systemic lupus erythematosis, myelopreparation for autologous transplantation, transplant rejection, glomerulonephritis, interstitial nephritis, Lupus nephritis, tubular necrosis, diabetic nephropathy, renal hypertrophy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, acute myeloid leukemia, melanoma, multiple myeloma, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastoma, neurofibromatosis, osteolytic bone metastases, brain metasteses, gastrointestinal stromal tumors, and giant cell tumors.

  描述了化合物及其盐、配方、共轭物、衍生物、形式和用途。在某些方面和实施例中，所述化合物或其盐、配方、共轭物、衍生物、形式对Fms、Kit、Flt3、TrkA、TrkB和TrkC激酶蛋白中的一个或多个具有活性。还描述了使用方法，用于治疗与Fms、Kit、Flt3、TrkA、TrkB和TrkC中的一个或多个活性相关的疾病和症状，包括类风湿性关节炎、骨关节炎、骨质疏松症、周围假体周围骨溶解、系统性硬化、脱髓鞘疾病、多发性硬化症、沙科特-玛丽-屈氏综合征、肌萎缩性侧索硬化、阿尔茨海默病、帕金森病、全球性缺血、溃疡性结肠炎、克罗恩病、免疫性血小板减少性紫癜、动脉粥样硬化、系统性红斑狼疮、自体移植的骨髓准备、移植排斥、肾小球肾炎、间质性肾炎、狼疮性肾炎、肾小管坏死、糖尿病性肾病、肾肥大、I型糖尿病、急性疼痛、炎症性疼痛、神经病性疼痛、急性髓样白血病、黑色素瘤、多发性骨髓瘤、乳腺癌、前列腺癌、胰腺癌、肺癌、卵巢癌、胶质瘤、胶质母细胞瘤、神经纤维瘤病、骨转移性溶骨病、脑转移瘤、胃肠道间质瘤和巨细胞瘤。
• Controlled release composition
  申请人：Nagahara Naoki

  公开号：US20060177509A1

  公开（公告）日：2006-08-10

  The present invention provides a controlled release composition showing release of an active ingredient (proton pump inhibitor) controlled in two or more steps at different release rates, which contains 1) a release-controlled part A capable of controlling release of the active ingredient to occur at a predetermined rate, 2) a release-controlled part B capable of controlling release of the active ingredient to occur at a predetermined rate lower than the release rate of the release-controlled part A, and where necessary, 3) a release-controlled part C capable of controlling release of the active ingredient to occur at a predetermined rate faster than the release rate of the release-controlled part B, wherein the release of the active ingredient from the release-controlled part B precedes the release of the active ingredient from the release-controlled part A (when release-controlled part C is contained, the release of the active ingredient from the release-controlled part C precedes the release of the active ingredient from the release-controlled part B).

  本发明提供了一种控制释放组合物，该组合物显示出活性成分（质子泵抑制剂）在不同的释放速率下控制释放，其中包括1）能够控制活性成分以预定速率释放的释放控制部分A，2）能够控制活性成分以比释放控制部分A更低的预定速率释放的释放控制部分B，必要时还包括3）能够控制活性成分以比释放控制部分B更快的预定速率释放的释放控制部分C，其中活性成分从释放控制部分B的释放先于从释放控制部分A的释放（当包含释放控制部分C时，从释放控制部分C的释放先于从释放控制部分B的释放）。
• Release-Control Composition
  申请人：Ishida Hajime

  公开号：US20090053308A1

  公开（公告）日：2009-02-26

  The present invention relates to a controlled release capsule preparation for oral administration, which contains (i) a granule containing a physiologically active substance which is a compound represented by the formula: wherein n is an integer of 1 to 3, and Ar is an aromatic ring optionally having substituent(s), or a salt thereof, and a hydrophilic polymer, and coated with an enteric coating agent and the like, and (ii) a fluidizer. According to the present invention, a controlled release composition for oral administration of an imidazole derivative, which has steroid C 17,20 -lyase inhibiting activity and which has remarkably improved sustainability of the blood concentration, is provided.

  本发明涉及一种口服控释胶囊制剂，其包含（i）一种颗粒，其中包含一种生理活性物质，该物质是由以下公式表示的化合物：其中n是1至3的整数，Ar是一种芳香环，可以具有取代基，或其盐，以及一种亲水性聚合物，并涂有肠溶涂层剂等；（ii）一种流动剂。根据本发明，提供了一种具有类固醇C17,20-裂解酶抑制活性并具有显着改善血浓度持久性的咪唑衍生物口服控释组合物。
• GNRH AGONIST COMBINATION DRUGS
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1424080A1

  公开（公告）日：2004-06-02

  In the field of pharmaceuticals, it is intended to provide drugs whereby the preventive and therapeutic effects of a GnRH agonist on various diseases can be enhanced and QOL can be improved. More specifically, combination of drugs characterized in that the GnRH agonist is combined with a chemical selected from among SERM, SARM, sex hormone synthesis inhibitors, receptor-type tyrosine kinase inhibitors, bone metabolism regulators, drugs for immunotherapy, cytokine/chemokine inhibitors and endothelin receptor antagonists. Owing to these combinations, excellent effects of enhancing the preventive and therapeutic effects of the GnRH agonist on various diseases and relieving side effects can be established. Furthermore, QOL can be improved thereby.

  在制药领域，旨在提供可增强 GnRH 激动剂对各种疾病的预防和治疗效果并改善 QOL 的药物。更具体地说，药物组合，其特征在于 GnRH 促效剂与选自 SERM、SARM、性激素合成抑制剂、受体型酪氨酸激酶抑制剂、骨代谢调节剂、免疫治疗药物、细胞因子/凝血因子抑制剂和内皮素受体拮抗剂的化学物质相结合。通过这些联合用药，GnRH 促效剂在增强对各种疾病的预防和治疗效果以及缓解副作用方面可以取得良好的效果。此外，还能改善 QOL。
• RELEASE CONTROL COMPOSITIONS
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1607092A1

  公开（公告）日：2005-12-21

  A controlled release composition for oral administration, which comprises a physiologically active substance which is a compound represented by the formula: wherein n is an integer of 1 to 3, and Ar is an aromatic ring which may be substituted, or a salt thereof, and a hydrophilic polymer, or a controlled release composition for oral administration, wherein a core containing the physiologically active substance is coated with a coating layer containing a polymer, is provided.

  一种用于口服的控释组合物，它包含一种生理活性物质，该物质是由式表示的化合物： 其中 n 为 1 至 3 的整数，Ar 为可被取代的芳香环、 或其盐，以及一种亲水性聚合物，或一种口服控释组合物，其中含有生理活性物质的芯部被一层含有聚合物的包衣层包覆。