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。
如有产品相关项目调研推广服务, 请致函联系我们

客户展示

新项目整合精选

CP-060

Chemical Name: 3-[3-[N-[2-(1,3-Benzodioxol-5-yloxy)ethyl]-N-methylamino]propyl]-2-(3,5-di-tert-butyl-4-hydroxyphenyl)thiazolidin-4-one
项目整合开发状态: Biological Testing
项目研究机构: Chugai (Originator) 参考文献标题:Novel calcium antagonists with both calcium overload inhibition and antioxidant activity.1.2-(3,5-Di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones
文献作者:Kato,T.; Ozaki,T.; Tamura,K.; Suzuki,Y.; Akima,M.; Ohi,N.
参考来源:J Med Chem 1998,41(22),4309

新产品编号:1084179

Chemical Name: 8(S)-(Bromomethyl)-6-(4-methoxycinnamoyl)-2-methyl-4-[N-[4-(piperidin-1-yl)piperidin-1-yl]carbamoyloxy]-3,6,7,8-tetrahydrobenzo[1,2-b:4,3-b']dipyrrole-1-carboxylic acid methyl ester hyd...
参考文献标题:DC-89 deriv.
文献作者:Amishiro,N.; Nagamura,S.; Saito,H.; Kobayashi,E.; Okamoto,A.; Gomi,K.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0702014; US 5670492; WO 9526964

新产品编号:1085761

Chemical Name: 8(S)-(Bromomethyl)-6-(4-methoxycinnamoyl)-2-methyl-4-[N-(4-methylpiperazin-1-yl)carbamoyloxy]-3,6,7,8-tetrahydrobenzo[1,2,b:4,3-b']dipyrrole-1-carboxylic acid methyl ester hydrobromide<...
参考文献标题:DC-89 deriv.
文献作者:Amishiro,N.; Nagamura,S.; Saito,H.; Kobayashi,E.; Okamoto,A.; Gomi,K.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0702014; US 5670492; WO 9526964

PD-166285

Chemical Name: 6-(2,6-Dichlorophenyl)-2-[4-[2-(diethylamino)ethoxy]phenylamino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:The reac...
参考文献标题:2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones.Structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity
文献作者:Klutchko,S.R.; Hamby,J.M.; Boschelli,D.H.; Wu,Z.; Kraker,A.J.; Amar,A.M.; Hartl,B.G.; Shen,C.; Klohs,W.D.; Steinkampf,R.W.; Driscoll,D.L.; Nelson,J.M.; Elliott,W.L.; Roberts,B.J.; Stoner,C.L.; Vincent,P.W.; Dykes,D.J.; Panek,R.L.; et al.
参考来源:J Med Chem 1998,41(17),3276

DMP-802

Chemical Name: 3-[2-[3-(4-Amidinophenyl)-4,5-dihydroisoxazol-5(R)-yl]acetamido]-2(S)-(3,5-dimethylisoxazol-4-ylsulfonamido)propionic acid mesylate
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squ...
参考文献标题:Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action
文献作者:Olson,R.E.; Sielecki,T.M.; Wityak,J.; Pinto,D.J.; Batt,D.G.; Frietze,W.E.; Liu,J.; Tobin,A.E.; Orwat,M.J.; Di Meo,S.V.; Houghton,G.C.; Lalka,G.K.; Mousa,S.A.; Racanelli,A.L.; Hausner,E.A.; Kapil,R.P.; Rabel,S.R.; et al.
参考来源:J Med Chem 1999,42(7),1178

PD-159790

Chemical Name: N-(1-Ethylpiperidin-3-yl)-N-[6-iodo-2-(trifluoromethyl)quinazolin-4-yl]amine
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:The cyclization of 2-amino-5-iodobenz...
参考文献标题:Quinazolines as inhibitors of endothelin converting enzyme
文献作者:Ahn,K.; Cheng,X.-M.; Doherty,A.M.; Elslager,E.F.; Kornberg,B.; Lee,C.; Leonard,D.; Nikam,S.S.; Werbel,L.M.(Pfizer Inc.)
参考来源:EP 0799221; JP 1998510834; US 5658902; WO 9619474

PGE-5428060

Chemical Name: (1''R,5''S,6''S)-7-[4-[4(S)-[3-Carboxy-6-[1(R)-hydroxyethyl]-1-methyl-1-carba-2-penem-2-ylsulfanyl]pyrrolidin-2(S)-ylcarbonyl]piperazin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroqui...
参考文献标题:Preparation and antimicrobial assessment of 2-thioether-linked quinolonyl-carbapenems
文献作者:Hershberger,P.M.; Switzer,A.G.; Yelm,K.E.; Coleman,M.C.; Devries,C.A.; Rourke,F.J.; Davis,B.W.; Kraft,W.G.; Twinem,T.L.; Koenigs,P.M.; Paule,S.M.; Siehnel,R.J.; Zoutendam,P.H.; Imbus,R.; Demuth,T.P.Jr.
参考来源:J Antibiot 1998,51(9),857-871

新产品编号:1087343

Chemical Name: [6-Methoxy-2-(4-methoxyphenyl)benzo[b]thien-3-yl](3,4,5-trimethoxyphenyl)methanone
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator), Baylor University (Codevelopment), Nati...
参考文献标题:Novel benzothiophene cpds.and methods
文献作者:Carlson,D.G.; Cullinan,G.J.; Fahey,K.J.; Jackson,W.T.; Roehm,N.W.; Spaethe,S.M.(Eli Lilly and Company)
参考来源:EP 0732331; JP 1999501932; WO 9628156

MOL-174

Chemical Name: (3S,6R,8aR)-6-amino-N-[(1S)-4-{[amino(imino)methyl]amino}-1-(1,3-benzothiazol-2-ylcarbonyl)butyl]-6-benzyl-5-oxooctahydro-3-indolizinecarboxamide; (3S,6S,8aR)-2-[Nalpha-(6-Amino-6-benzy...
参考文献标题:Secondary structure peptide mimetics: Design,synthesis,and evaluation of beta-strand mimetic thrombin inhibitors
文献作者:Boatman,P.D.; Ogbu,C.O.; Eguchi,M.; Kim,H.O.; Nakanishi,H.; Cao,B.; Shea,J.P.; Kahn,M.
参考来源:J Med Chem 1999,42(8),1367

新产品编号:1088925

Chemical Name: 3-[4-(5-Methyl-4-phenylpyrazol-1-yl)piperidin-1-ylmethyl]benzonitrile
项目整合开发状态: Biological Testing
项目研究机构: Merck Sharp & Dohme (Originator)
合成路线:N-Boc-4-Hydroxypiperidine (I) w...
参考文献标题:4-N-Linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors
文献作者:Moore,K.W.; Bonner,K.; Jones,E.A.; Emms,F.; Leeson,P.D.; Marwood,R.; Patel,S.; Rowley,M.; Thomas,S.; Carling,R.W.
参考来源:Bioorg Med Chem Lett 1999,9(9),1285