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

新产品编号:62207

Chemical Name: (2S,3S,6R,11R)-2-(Benzyloxymethyl)-3,11-dimethyl-1,7-dioxaspiro[5.5]undecane
CAS No. 153109-03-6
项目整合开发状态: Biological Testing
项目研究机构: Hokkaido University (Originator)
合成路线:T...
参考文献标题:Highly regio- and stereoselective reductions of spiroketals
文献作者:Oikawa,H.; et al.
参考来源:Tetrahedron Lett 1993,34(33),5303

NAPAP-PS

Chemical Name: 4-[2-[2(R)-[N-[1-(4-Amidinobenzyl)-2-oxo-2-(1-piperidinyl)ethyl]carbamoyl]-2-(2-naphthylsulfonamido)ethylsulfanyl]acetamido]-N-[11-(1-O-methyl-2,3,6-tri-O-sulfo-alpha-D-glucopyranosyl)(...
参考文献标题:Antithrombotic cpds.
文献作者:Van Boeckel,C.A.A.; Basten,J.E.M.; Dreef-Tromp,C.M.; Buijsman,R.C.(Akzo Nobel N.V.; Universiteit Leiden)
参考来源:WO 9965934

S-33084

Chemical Name: N-[4-[(3aR,9bS)-8-Cyano-1,2,3,3a,4,9b-hexahydro-[1]benzopyrano[3,4-c]pyrrol-2-yl]butyl]biphenyl-4-carboxamide hydrochloride
CAS No. 220647-52-9 (stereoisomer)
项目整合开发状态: Preclinica...
参考文献标题:Chromene derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:Lejeune,F.; Hautefaye,P.; Millan,M.; Dubuffet,T.; Lavielle,G.(ADIR et Cie.)
参考来源:EP 0887350; JP 1999071376; US 6090837

RU-79115

Chemical Name: 2-Propynyloxycarbamic acid 7(R)-[4-hydroxy-3-(N-methoxyethanimidoyl)-8-methyl-2-oxo-2H-1-benzopyran-7-yloxy]-8(R)-hydroxy-10(R)-methoxy-6-oxaspiro[4.5]dec-9(S)-yl ester
CAS No. 22930...
参考文献标题:Novel aromatic amides,preparation method and application as medicines
文献作者:Periers,A.-M.; Laurin,P.; Klich,M.; Musicki,B.; Haesslein,J.-L.(Aventis Pharma SA)
参考来源:FR 2773369; WO 9935155

新产品编号:84355

Chemical Name: (1R,9S,12S,13R,14S,17R,21S,23S,24R,25S,27R)-17-Ethyl-1,14-dihydroxy-23,25-dimethoxy-12-[2-[4(R)-[2(S)-hydroxy-2-(2-naphthyl)ethoxy]-3(R)-methoxycyclohex-1(R)-yl]-1(E)-methylvinyl]-13,19...
参考文献标题:Potent immunosuppressive C32-O-arylethyl ether derivatives of ascomycin with reduced toxicity
文献作者:Armstrong,H.M.; Wong,F.; Holmes,M.A.; Sinclair,P.J.; Goulet,M.T.; Dumont,F.J.; Staruch,M.J.; Koprak,S.; Peterson,L.B.; Rosa,R.; Wilusz,M.B.; Wiederrecht,G.J.; Cryan,J.G.; Wyvratt,M.J.; Parsons,W.H.
参考来源:Bioorg Med Chem Lett 1999,9(14),2089-94

PAT-5A

Chemical Name: (E)-5-[4-[1-(2-Pyridyl)pyrrolidin-2(S)-ylmethoxy]benzylidene]thiazolidine-2,4-dione maleate
CAS No. 199117-51-6, 199117-46-9 (free base), 199117-53-8 (monoHCl), 199117-54-9 (monoNa s...
参考文献标题:Heterocyclic cpds.having antidiabetic,hypolipidaemic,antihypertensive properties,process for their preparation and pharmaceutical compsns.containing them
文献作者:Rao,P.B.; Ramanujam,R.; Alla,S.R.; Lohray,V.B.; Chakrabarti,R.; Lohray,B.B.(Dr.Reddy's Research Foundation)
参考来源:US 5919782

SF-324

Chemical Name: (-)-3-(3-Amidinophenyl)-5-[5-[2-(sulfamoyl)phenyl]pyrimidin-2-ylcarbamoyl]-4,5-dihydroisoxazole-5-acetic acid methyl ester trifluoroacetate
CAS No. 193004-76-1 (free base), 193004-64...
参考文献标题:Isoxazoline,isothiazoline and pyrazoline factor Xa inhibitors
文献作者:Quan,M.L.; Wityak,J.; Galemmo,R.A.Jr.; Stouten,P.F.W.; Pruitt,J.R.(DuPont Pharmaceuticals Co.)
参考来源:EP 0874629; US 5939418; WO 9723212

新产品编号:70117

Chemical Name: N-[5-(N-Hydroxyacetamido)pentyl]-N-hydroxy-2-(3-hydroxypyridin-2-yl)-4,5-dihydrothiazole-4(S)-carboxamide
CAS No. 155880-00-5
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator...
参考文献标题:2-(Pyrid-2'-yl)-2-thiazoline-4(S)-carboxylic acid derivs.
文献作者:Peter,H.H.; Moerker,T.; Bergeron,R.J.Jr.(Novartis AG; University of Florida)
参考来源:WO 9411367

新产品编号:354877

Chemical Name: (7bR,8aS)-7-Bromo-2-[3-(4-methoxyphenyl)-2(E)-propanoyl]-6-methyl-2,5,8,8a-tetrahydro-1H-cyclopropa[c]pyrrolo[3,2-e]indol-4-one
CAS No. 205050-73-3
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Synthesis and antitumor activity of duocarmycin derivatives: Modification of segment-A of A-ring pyrrole compounds
文献作者:Amishiro,N.; Okamoto,A.; Murakata,C.; Tamaoki,T.; Okabe,M.; Saito,H.
参考来源:J Med Chem 1999,42(15),2946-60

新产品编号:114413

Chemical Name: N2-[4-[5-(Acetamidomethyl)furan-2-yl]thiazol-2-yl]-N1-(2-ethoxybenzyl)guanidine
CAS No. 168970-48-7 (tautomer)
项目整合开发状态: Preclinical
项目研究机构: Fujisawa (Originator)
合成路线:The c...
参考文献标题:Furylthiazoles and their use as H2-receptor antagonists and antimicrobials
文献作者:Katsura,Y.; Ohno,M.; Nishino,S.; Tomishi,T.; Takasugi,H.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:JP 1997507222; WO 9518126