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

Dorzolamide hydrochloride, MK-507, L-671152, Trusopt

Chemical Name: 4(S)-(Ethylamino)-6(S)-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide hydrochloride
项目整合开发状态: Launched-1995
项目研究机构: Banyu (Originator), Merck & Co. (Origin...
参考文献标题:Thienothiopyran sulfonamide derivs.,pharmaceutical compsns.and use
文献作者:Baldwin,J.J.; Ponticello,G.S.; Christy,M.E.(Merck & Co.,Inc.)
参考来源:AU 8818387; EP 0296879; JP 1989100174; US 4797413; US 4863922

MW-60U

Chemical Name: 5-[1(R)-2,2-Dibromocyclopropyl]-2'-deoxyuridine; 1-(2-Deoxy-beta-D-ribofuranosyl)-5-[(1R)-2,2-dibromocyclopropyl]uracil; 1-(2-Deoxy-beta-D-erythro-pentofuranosyl)-5-[1(R)-2,2-dibromocyc...
参考文献标题:Synthesis and antiviral properties of (E)-5-(2-bromovinyl)-2'-deoxycytidine-related compounds
文献作者:Jones,A.; Sayers,R.; Walker,R.; De Clercq,E.
参考来源:J Med Chem 1988,31(1),268

BI-L-226

Chemical Name: 2,6-Dimethyl-4-[2-(2-thienyl)vinyl]phenol
项目整合开发状态: Biological Testing
项目研究机构: Boehringer Ingelheim (Originator)
合成路线:The reaction of 2,6-di-tert-butyllphenol (I) with hexameth...
参考文献标题:2,6-Disubstituted-4-(2-arylethenyl)phenol 5-lipoxygenase inhibitors: Development and profile of BI-L-239
文献作者:Lazer,E.S.; Farina,P.R.; Gundel,R.H.; Wegner,C.D.
参考来源:Drugs Fut 1991,16(7),641

新产品编号:1005079

Chemical Name: (+)-7(S)-Methyl-3-(2-propynyloxy)-4,5,6,7-tetrahydroisothiazolo[4,5-c]pyridine fumarate
项目整合开发状态: Biological Testing
项目研究机构: Lundbeck (Originator), Merck & Co. (Originator)
合成路...
参考文献标题:Synthesis and muscarinic receptor pharmacology of a series of 4,5,6,7-tetrahydroisothiazolo[4,5-c]pyridine bioisosteres of arecoline
文献作者:Pedersen,H.; Brauner-Osborne,H.; Ball,R.G.; Frydenvang,K.; Meier,E.; Bogeso,K.P.; Krogsgaard-Larsen,P.
参考来源:Bioorg Med Chem 1999,7(5),795

Calphostin D, UCN-1028D

Chemical Name: 4,9-Dihydroxy-1,12-bis[2(R)-hydroxypropyl]-2,6,7,11-tetramethoxy-3,10-dihydroperylene-3,10-dione
项目整合开发状态: Biological Testing
项目研究机构: Kyowa Hakko (Originator)
合成路线:The brominat...
参考文献标题:Carbene complexes in the synthesis of complex natural products: Total synthesis of the calphostins
文献作者:Merlic,C.A.; et al.
参考来源:J Am Chem Soc 2000,122(13),3224

Calphostin B, UCN-1028B

Chemical Name: 1-[2(R)-Benzyloxypropyl]-4,9-dihydroxy-12-[2(R)-hydroxypropyl]-2,6,7,11-tetramethoxy-3,10-dihydroperylene-3,10-dione
项目整合开发状态: Biological Testing
项目研究机构: Kyowa Hakko (Originator)<...
参考文献标题:Carbene complexes in the synthesis of complex natural products: Total synthesis of the calphostins
文献作者:Merlic,C.A.; et al.
参考来源:J Am Chem Soc 2000,122(13),3224

HWA-153, A-730153

Chemical Name: 7-(5-Hydroxyhexyl)-3-methyl-1-propylxanthine
项目整合开发状态: Biological Testing
项目研究机构: Hoechst Japan (Originator)
合成路线:By treating 3-methylxanthine (I) with sodium hydroxide and 1-b...
参考文献标题:
文献作者:Stefanovich,V.
参考来源:Private Communication 2002,10(9),3001

NSC-639830, IST-622

Chemical Name: 6-O-Ethoxypropionyl-3',4'-O-(exo-benzylidene)chartreusin; 10-[3,4-O-exo-Benzylidene-2-O-(alpha-D-digitalosyl)-beta-D-fucosyloxy]-6-(3-ethoxypropionyloxy)-1-methyl-5,12-dihydrobenzo[h][1...
参考文献标题:Synthesis and cytostatic activity of the antitumor antibiotic chartreusin derivatives
文献作者:Kon,K.; Sugi,H.; Tamai,K.; Ueda,Y.; Yamada,N.
参考来源:J Antibiot 1990,43(4),372

Caracasandiamide

Chemical Name: 3beta,4beta-Bis(3,4-dimethoxyphenyl)-N,N'-bis[4-[3-(3-methyl-2-butenyl)guanidino]butyl]cyclobutane-1alpha,2alpha-dicarboxamide
项目整合开发状态: Biological Testing
项目研究机构: Consiglio Nazio...
参考文献标题:Novel hypotensive agents from Verbesina caracasana.6.Synthesis and pharmacology of caracasandiamide
文献作者:Carmignani,M.; Volpe,A.R.; Delle Monache,F.; Botta,B.; Espinal,R.; De Bonnevaux,S.C.; De Luca,C.; Botta,M.; Corelli,F.; Tafi,A.; Ripanti,G.; Monache,G.D.
参考来源:J Med Chem 1999,42(16),3116

新产品编号:1006661

Chemical Name: (-)-7(R)-Methyl-3-(2-propynyloxy)-4,5,6,7-tetrahydroisothiazolo[4,5-c]pyridine fumarate
项目整合开发状态: Biological Testing
项目研究机构: Lundbeck (Originator), Merck & Co. (Originator)
合成路...
参考文献标题:Synthesis and muscarinic receptor pharmacology of a series of 4,5,6,7-tetrahydroisothiazolo[4,5-c]pyridine bioisosteres of arecoline
文献作者:Pedersen,H.; Brauner-Osborne,H.; Ball,R.G.; Frydenvang,K.; Meier,E.; Bogeso,K.P.; Krogsgaard-Larsen,P.
参考来源:Bioorg Med Chem 1999,7(5),795