项目整合精选

聚焦新型临床类新产品的整合与转化. 在创新药研发领域，传统的“单一产品、单打独斗”模式正在被一种更系统化的“项目整合”思维所取代。项目整合的核心，在于将散落在研发早期、中期的创新资产，通过资金、临床资源、产业生态等多维度要素的有机组合，实现从“科学发现”到“临床价值”，再到“商业成功”的跨越。研发与商业的战略整合：从“资产思维”到“组合思维”它要求我们超越单个分子的视野，拥抱一个由技术创新、临床需求、资本支持和商业洞察共同构成的复杂网络。在这个网络中，成功的标准不再是单一的“获批上市”，而是能否通过高效的整合，将科学上的突破，转化为临床上真正可及、商业上可持续、能够惠及患者的解决方案。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，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。
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项目整合精选

IT-657

Chemical Name: 1-(2-Amino-4-fluorophenyl)-4-[(6bR,10aS)-1,2,6b,7,8,9,10,10a-octahydropyrido[3',4':4,5]pyrrolo[1,2,3-de][1,4]benzoxazin-8-yl]butan-1-one
CAS No. 313543-30-5
项目整合开发状态: Preclinical<...
参考文献标题:Novel,highly potent and selective serotonin 5-HT2A/dopamine D2 receptor antagonists as potential antipsychotics
文献作者:Boyle,K.E.; Robichaud,A.J.; Lee,T.; et al.
参考来源:221st ACS Natl Meet (April 1 2001,San Diego) 2001,Abst MEDI 98

PR-9, ME-10092

Chemical Name: N1-(2-Chloro-3,4-dimethoxybenzylideneamino)guanidine acetate
CAS No. 332395-39-8, 284042-43-9 (free base)
项目整合开发状态: Preclinical
项目研究机构: Melacure Therapeutics (Originator)
合成...
参考文献标题:Guanidine derivs.and their use in the production of a medicament for blocking xanthine oxidase/dehydrogenase
文献作者:Skottner,A.; Lundstedt,T.; Seifert,E.; Veveris,M.; Piskunova,I.; Rozhkov,E.; Wikberg,J.; Pett,C.P.; Kalvins,I.; Andrianov,V.; Semenikhina,V.; Dambrova,M.(Melacure Therapeutics)
参考来源:WO 0125192

KI-60606

Chemical Name: Hexalithium tris(trans-cyclohexane-1,2-diamine-kappaN,kappaN')[mu3-[2,4,6-tris[(1S)-1,3-di(carboxy-kappaO)propylamino]-2,4,6-tris[(1S)-1,3-dicarboxypropylamino]-1,3,5,2,4,6-triazatripho...
参考文献标题:Platinum complex conjugated to cyclotriphosphazene,its preparation,and anticancer agent comprising the same
文献作者:Lee,C.O.; Sohn,Y.S.; Baek,H.G.(Il-Yang Pharmaceutical Co.,Ltd.; Korea Institute of Science and Technology)
参考来源:EP 1082331; US 6221906; WO 0058321

新产品编号:596923

Chemical Name: 3-Chloro-N-[4-chloro-2-(5-chloropyridin-2-ylcarbamoyl)-6-methoxyphenyl]-4-[[N-(4,5-dihydro-1,3-oxazol-2-yl)-N-methylamino]methyl]-2-thiophenecarboxamide
CAS No. 229335-75-5
项目整合开发...
参考文献标题:Ortho-anthranilamide derivs.as anticoagulants
文献作者:Snider,R.M.; Liang,A.M.; Wu,S.C.; Arnaiz,D.O.; Sacchi,K.L.; Kochanny,M.J.; Phillips,G.B.; Ye,B.; Zhao,Z.; Morrissey,M.M.; Griedel,B.D.; Lee,W.; Sakata,S.T.; Karanjawala,R.E.; Chou,Y.-L.; Shaw,K.J.(Schering AG)
参考来源:EP 1040108; JP 2001526283; US 6140351; WO 9932477

新产品编号:802583

Chemical Name: 3-(3-Aminopropionamido)-4-methoxybenzenesulfonic acid 3,4,5-trimethoxyphenyl ester
CAS No. 312299-89-1
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:The reaction of...
参考文献标题:Cell proliferation inhibitors
文献作者:Barr,K.J.; Steiner,B.A.; Qun,L.; Rosenberg,S.; Sham,H.; Gwaltney,S.L.II; Imade,H.M.; Woods,K.W.(Abbott Laboratories Inc.)
参考来源:WO 0073264

A-259745

Chemical Name: 1-Methyl-5-[5-(3,4,5-trimethoxyphenyl)-4,5-dihydrooxazol-2-yl]-1H-indole
CAS No. 256934-83-5, 256935-04-3 (R-isomer), 256935-03-2 (S-isomer)
项目整合开发状态: Preclinical
项目研究机构: Abbot...
参考文献标题:Substd.oxazolines as antiproliferative agents
文献作者:Woods,K.W.; Wang,L.; Kalvin,D.M.; Barr,K.J.; Li,Q.; Liu,G.; Gwaltney,S.L.II; Claiborne,A.K.; Jae,H.-S.; Sham,H.L.(Abbott Laboratories Inc.)
参考来源:WO 0006556

新产品编号:383353

Chemical Name: 4-[2-(4-Chlorophenyl)-4-(2,4-dibutoxyphenyl)-1H-imidazol-5-yl]pyridine
CAS No. 208188-17-4 (tautomer)
项目整合开发状态: Biological Testing
项目研究机构: Merck & Co. (Originator)
合成路线:The ...
参考文献标题:Triaryl substd.imidazoles as glucagon antagonists
文献作者:Chang,L.L.(Merck & Co.,Inc.)
参考来源:EP 0959886; JP 2000514088; US 5880139; WO 9822109

IDN-5390

Chemical Name: 2-O-Acetyl-1,3-anhydro-2-C-[(1S,2S,3R,9S)-2-(benzoyloxy)-9-[3(S)-(tert-butoxycarboxamido)-2(R)-hydroxy-5-methylhexanoyloxy]-1,5-dihydroxy-4,8,11,11-tetramethyl-6-oxobicyclo[5.3.1]undeca...
参考文献标题:Synthesis and evaluation of C-seco paclitaxel analogues
文献作者:Appendino,G.; et al.
参考来源:Tetrahedron Lett 1997,38(24),4273

CRL-8299

Chemical Name: 8H-Benzo[b]pyrido[4,3,2-de]-1,7-phenanthrolin-8-one
CAS No. 294174-13-3
项目整合开发状态: Preclinical
项目研究机构: Lafon (Originator)
合成路线:The cyclization of quinoline-5,8-dione (I) with...
参考文献标题:Pharmaceutical compsn.based on polyaromatic cpds.
文献作者:Kiss,R.; Bontemps-Subielos,N.; Frydman,A.; Darro,F.; Bastide,J.; Deflourne,E.(Laboratoires L.Lafon)
参考来源:FR 2790954; WO 0055160

ONO-BB-039-02

Chemical Name: N2-[2(S)-Benzyl-3-sulfanylpropionyl]-L-glutamic acid 1-phenylamide; 4(S)-[3-Phenyl-2(S)-(sulfanylmethyl)propionamido]-5-oxo-5-(phenylamino)pentanoic acid
CAS No. 126349-24-4
项目整合开...
参考文献标题:New orally active enkephalinase inhibitors: Their synthesis,biological activity,and analgesic properties
文献作者:Senokuchi,K.; Nakai,H.; Nagao,Y.; Sakai,Y.; Katsube,N.; Kawamura,M.
参考来源:Bioorg Med Chem 1998,6(4),441