临床前CDMO研发筛选相关化合物

CDMO是Contract Development and Manufacturing Organization的缩写，即合同定制研发生产组织。它是一种为制药企业及生物技术公司提供医药（特别是创新药）工艺研发及制备、工艺优化、放大生产、注册和验证批生产以及商业化生产等定制服务的机构. 在传统代工基础上增加了研发和工艺优化能力，是高技术壁垒的工艺研发能力与规模生产能力的深度结合. 1, 工艺开发与优化：创新性合成路线设计、工艺参数优化. 2, 中试放大：实验室工艺向规模化生产的转化 3, 注册批生产：支持客户新药申报的验证批生产. 4, 商业化生产：药品上市后的大规模生产供应. 全球医药CDMO行业保持较高景气度。根据弗若斯特沙利文预测：2026年全球CDMO市场规模：预计达1,189亿美元 2033年全球CDMO市场规模：预计达3,385亿美元. CDMO作为医药产业链专业化分工的产物，已经从单纯的CMO代工模式升级为"研发+生产"一体化的高附加值服务。当前，在多肽、ADC、CGT等新型药物赛道的驱动下，全球及中国CDMO市场保持高速增长。中国CDMO企业凭借完整的供应链体系、工程师红利和一体化服务能力，全球市占率有望持续提升，行业正从"成本优势"竞争迈向"体系优势"竞争的新阶段。
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临床前CDMO研发化合物筛选

CAS: 2127109-84-4

Ropsacitinib (PF-06826647)

中文名称:(1R,3R)-3-(氰甲基)-3-(4-(6-(1-甲基-1H-吡唑-4-基)吡唑[1,5-A]吡嗪-4-基)-1H-吡唑-1-基)环丁腈
CAS号:2127109-84-4
分子式: C20H17N9 分子量: 383.41
产品形式: Free base
研发状态: Completed
研发用途: Healthy
研究机构: Pfizer
研发日期: October 23 2019
研发阶段: Phase 1
Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO).

CAS: 212141-51-0

Vatalanib (PTK787) 2HCl

中文名称:瓦他拉尼
CAS号:212141-51-0
分子式: C20H15ClN4.2HCl 分子量: 419.73
产品形式: Dihydrochloride
研发状态: Completed
研发用途: Brain and Central Nervous System Tumors; Sarcoma
研究机构: Northwestern University; Novartis
研发日期: May-06
研发阶段: Phase 2
Vatalanib 2HCl (PTK787, ZK 222584, cpg-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3.

CAS: 211915-06-9

Dabigatran (BIBR-1048) etexilate

中文名称:达比加群酯
CAS号:211915-06-9
分子式: C34H41N7O5 分子量: 627.73
产品形式: free base
研发状态: Recruiting
研发用途: Health
研究机构: Peking University Third Hospital
研发日期: April 1 2024
研发阶段: Not Applicable
Dabigatran Etexilate (BIBR-1048) is the prodrug of dabigatran, a potent, nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombin molecule.

CAS: 21187-98-4

Gliclazide

中文名称:格列齐特
CAS号:21187-98-4
分子式: C15H21N3O3S 分子量: 323.41
产品形式: free base
研发状态: Completed
研发用途: Diabetes Mellitus Type 2
研究机构: University of Sarajevo; General Hospital Prim. Dr. Abdulah Nakas; University of Dundee; Wellcome Trust
研发日期: March 4 2019
研发阶段: Phase 1
Gliclazide(S1702, SE1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.

CAS: 211513-37-0

Dalcetrapib (JTT-705)

中文名称:CETP抑制剂
CAS号:211513-37-0
分子式: C23H35NO2S 分子量: 389.59
产品形式: free base
研发状态: Completed
研发用途: Covid19
研究机构: DalCor Pharmaceuticals; The Montreal Health Innovations Coordinating Center (MHICC); Covance
研发日期: January 11 2021
研发阶段: Phase 2
Dalcetrapib (JTT-705) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol. Phase 3.

CAS: 2114339-57-8

Amcenestrant (SAR439859)

CAS号:2114339-57-8
分子式: C31H30Cl2FNO3 分子量: 554.48
产品形式: Free Base
研发状态: Active not recruiting
研发用途: Breast Cancer
研究机构: Sanofi
研发日期: March 25 2019
研发阶段: Phase 1
Amcenestrant (SAR439859, compound 43d) is an orally available and nonsteroidal selective estrogen receptor degrader (SERD) with potential antineoplastic activity. SAR439859 is a potent estrogen receptor (ER) antagonist with EC50 of 0.2 nM for ERα degradation.