新项目精选

近年来，药物发现已从传统的小分子化药拓展至更多元的分子类型，这些新型API在项目整合中呈现出独特的开发范式：PROTAC/分子胶降解剂：通过诱导靶蛋白泛素化降解发挥作用，而非传统“占位驱动”抑制。这类分子的项目整合需要同时考量靶点配体、E3连接酶配体及连接子的三元复合物优化，临床前到临床的转化难度显著增加。多肽/环肽药物：介于小分子与生物制品之间，兼具高选择性与口服可用性潜力。项目整合中需重点解决稳定性、递送及生产工艺放大问题。抗体-药物偶联物（ADC）：作为“生物导弹”，ADC的项目整合涉及抗体、连接子、有效载荷三部分的协同优化，需要跨学科团队的深度整合。小核酸药物（siRNA/ASO）：通过基因沉默机制发挥作用，项目整合的核心挑战在于递送系统的设计与肝外靶向能力的突破。展望未来，新型API项目的整合将呈现以下趋势：第一，AI贯穿全链条。从靶点发现、分子优化到临床开发、上市后监测，AI将成为贯穿API全生命周期的核心工具。第二，数据资产化。临床研究数据和真实世界数据将从“辅助工具”升级为“核心资产”，数据驱动的决策将成为项目整合的标准范式。第三，开放整合生态。API经济的成熟正在推动制药企业从“封闭研发”走向“开放协作”，通过API接口与外部数据源、技术平台、CRO/CDMO实现无缝对接. 而API技术——无论是数据接口还是组织协作的“应用程序接口”——正成为支撑这一整合的核心基础设施。
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新项目整合精选

ME-1036, CP-5609

Chemical Name: (1R,5S,6S)-2-[7-[1-(Carbamoylmethyl)pyridin-1-ium-3-ylcarbonyl]imidazo[5,1-b]thiazol-2-yl]-6-[1(R)-hydroxyethyl]-1-methyl-1-carba-2-penem-3-carboxylate
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:CP5609,a novel parenteral carbapenem: Synthesis and structure-activity relationships
文献作者:Shitara,E.; Yamamoto,Y.; Kano,Y.; Maruyama,T.; Takahashi,M.; Atsumi,K.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-319

NH-3

Chemical Name: 2-[4-[4-Hydroxy-3-isopropyl-5-(4-nitrophenylethynyl)benzyl]-3,5-dimethylphenoxy]acetic acid
项目整合开发状态: Preclinical
项目研究机构: University of California, San Francisco (Originator)
合...
参考文献标题:Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment
文献作者:Nguyen,N.-H.; Apriletti,J.W.; Cunha Lima,S.T.; Webb,P.; Baxter,J.D.; Scanlan,T.S.
参考来源:J Med Chem 2002,45(15),3310

新产品编号:2387747

Chemical Name: 11-Amino-11-deoxy-3-des(hexopyranosyloxy)-6-O-[N-[3-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-2(E)-propenyl]carbamoyl]-3-oxoerythromycin A 11-N,12-O-cyclic carbamate
项目整合开发状态: Biological ...
参考文献标题:6-O-Carbamoyl ketolide derivs.of erythromycin useful as antibacterials
文献作者:Henninger,T.C.; Xu,X.C.(Ortho-McNeil Pharmaceutical,Inc.)
参考来源:US 6472372; WO 0246204

新产品编号:2389329

Chemical Name: 4-[1-(2,2-Dicyclohexylacetyl)piperidin-4-ylidenemethyl]-3-fluorobenzoic acid
项目整合开发状态: Preclinical
项目研究机构: Universit鋞 des Saarlandes (Originator)
合成路线:Radical bromination of me...
参考文献标题:Synthesis and evaluation of 2'-substituted 4-(4'-carboxy- or 4'-carboxymethylbenzylidene)-N-acylpiperidines: Highly potent and in vivo active steroid 5alpha-reductase type 2 inhibitors
文献作者:Picard,F.; Barassin,S.; Mokhtarian,A.; Hartmann,R.W.
参考来源:J Med Chem 2002,45(16),3046

RS-135853

Chemical Name: (1R,3aR,4S,4aR,7R,7aR,8aS)-4-Formyl-3-isopropyl-8a-[(2R,6S,7R)-6-methoxy-7-methyl-4-(2-methyl-2-propenyl)perhydro-1,4-oxazepin-2-yloxymethyl]-7-methyl-4,4a,5,6,7,7a,8,8a-octahydro-1H-1,...
参考文献标题:Zofimarin derivs.having an oxazepan ring
文献作者:Kaneko,S.; Uchida,T.; Arai,M.; Kounosu,T.(Sankyo Co.,Ltd.)
参考来源:JP 2002161086; WO 0223541

Naphthal-NU

Chemical Name: N-(2-Chloroethyl)-N'-[2-(1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin-2-yl)ethyl]-N-nitrosourea
项目整合开发状态: Preclinical
项目研究机构: Chittaranjan National Cancer Institute (Originator)<...
参考文献标题:Evaluation of naphthal-NU,a 2-chloroethylnitrosourea derivative of naphthalimide,as a mixed-function anticancer agent
文献作者:Samanta,S.; et al.
参考来源:J Exp Clin Cancer Res 2002,21(1),87

HBJ-10

Chemical Name: 4-[(3S,5aR,8aS,12R,12aR)-Perhydro-3,12-epoxy[1,2]dioxepino[4,3-i]-2-benzopyran-3-yl]benzoic acid
项目整合开发状态: Preclinical
项目研究机构: Johns Hopkins University (Originator)
合成路线:Michae...
参考文献标题:Orally active,water-soluble antimalarial 3-aryltrioxanes: Short synthesis and preclinical efficacy testing in rodents
文献作者:Posner,G.H.; Jeon,H.B.; Ploypradith,P.; Paik,I.-H.; Borstnik,K.; Xie,S.; Shapiro,T.A.
参考来源:J Med Chem 2002,45(18),3824

新产品编号:2390911

Chemical Name: 2-(Acetoxymethyl)-4(S)-[2-[5-(benzyloxycarbonylamino)-6-oxo-2-phenyl-1,6-dihydropyrimidin-1-yl]acetamido]-2-pentenoic acid methyl ester; N-[1-[N-[3-(Acetoxymethyl)-4-methoxy-1(S)-methyl...
参考文献标题:Synthesis and in vitro studies of novel pyrimidinyl peptidomimetics as potential antimalarial therapeutic agents
文献作者:Zhu,S.; Hudson,T.H..; Kyle,D.E.; Lin,A.J.
参考来源:J Med Chem 2002,45(16),3491

新产品编号:2392493

Chemical Name: N5-(2-Chlorobenzyl)-N5-methyl-6-[6-(4-morpholinyl)pyridin-3-ylethynyl]pyrimidine-4,5-diamine
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:Reaction of 2,5-dibromopyrid...
参考文献标题:Design,synthesis,and structure-activity relationship of 6-alkynylpyrimidines as potent adenosine kinase inhibitors
文献作者:Gomtsyan,A.; DiDomenico,S.; Lee,C.H.; Matulenko,M.A.; Kim,K.; Kowaluk,E.A.; Wismer,C.T.; Mikusa,J.; Yu,H.; Kohlhaas,K.; Jarvis,M.F.; Bhagwat,S.S.
参考来源:J Med Chem 2002,45(17),3639

UK-371800

Chemical Name: 3-Ethyl-5-[5-(4-ethylpiperazin-1-ylsulfonyl)-2-[2-methoxy-1(R)-methylethoxy]pyridin-3-yl]-2-methyl-6,7-dihydro-2H-pyrazolo[4,3-d]pyrimidin-7-one
项目整合开发状态: Preclinical
项目研究机构: Pfiz...
参考文献标题:Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction
文献作者:Street,S.D.A.; Wood,A.; Bunnage,M.E.; Mathias,J.P.(Pfizer Inc.; Pfizer Ltd.)
参考来源:WO 9954333