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:481437

Chemical Name: N-[2-(Cyclopentylmethylsulfanyl)-1(R)-[N-(4-methoxybenzyl)carbamoyl]ethyl]carbamic acid tert-butyl ester; N-(tert-Butoxycarbonyl)-S-(cyclopentylmethyl)-L-cyateine (4-methoxybenzyl)amide...
参考文献标题:Amino acid derivs.
文献作者:Seko,T.; Kato,M.(Ono Pharmaceutical Co.,Ltd.)
参考来源:EP 0997147; WO 9902146

新产品编号:732975

Chemical Name: 8-Chloro-10H-[1]benzofuro[3,2-b]indole-1-carboxylic acid
CAS No. 275377-99-6
项目整合开发状态: Biological Testing
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:The condensation be...
参考文献标题:Substd.benzofuranoindoles and indenoindoles as novel potassium channel openers
文献作者:Butera,J.A.; Antane,S.A.; Lennox,J.R.(Wyeth)
参考来源:EP 1135393; US 6288099; WO 0034285

SD-270

Chemical Name: 3-[2-[3-(4-Amidinophenyl)-4,5-dihydroisoxazol-5(R)-yl]acetamido]-N-(2-methylphenylsulfonyl)-L-alanine
CAS No. 223559-85-1, 223559-86-2 (trifluoroacetate)
项目整合开发状态: Preclinical
...
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

新产品编号:690261

Chemical Name: 3-(3-Hydroxy-4-methoxyphenyl)-8H-thieno[2,3-b]pyrrolizin-8-one
CAS No. 258270-07-4
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator)
合成路线:The title compound has been synthe...
参考文献标题:Derivs.of the 8H-(2,3-b)-pyrrolizine-8-one,process for their preparation and pharmaceutical compsns.containing them
文献作者:Caignard,D.-H.; Enghehard,C.; Robba,M.; Lancelot,J.-C.; Pierre,A.; Renard,P.; Rault,S.; Atassi,G.(ADIR et Cie.)
参考来源:EP 0982308; FR 2781482; JP 2000044572; US 6071945

VRC-4307

Chemical Name: N1-(2-Cyclopentylethyl)-N2-(4,5-dimethylthiazol-2-yl)-N1-(N-hydroxycarbamoylmethyl)pyrrolidine-1,2(S)-dicarboxamide
CAS No. 345890-26-8
项目整合开发状态: Preclinical
项目研究机构: Novartis (...
参考文献标题:Novel urea cpds.,compsns.and methods of use and preparation
文献作者:Patel,D.V.; Jacobs,J.W.; Lewis,J.; Ni,Z.-J.(Versicor,Inc.)
参考来源:WO 0144178

新产品编号:549463

Chemical Name: (-)-1-[2(R)-Hydroxy-3-(4-hydroxyphenyl)propyl]-4-(4-methylbenzyl)piperidin-4-ol
CAS No. 222422-59-5 (racemate), 222421-80-9 (racemic, HCl)
项目整合开发状态: Preclinical
项目研究机构: Roche (...
参考文献标题:Discovery of (R)-1-[2-hydroxy-3-(4-hydroxy-phenyl)-propyl]-4-(4-methyl-benzyl)-piperidin-4-ol: A novel NR1/2B subtype selective NMDA receptor antagonist
文献作者:Pinard,E.; Alanine,A.; Bourson,A.; Buttelmann,B.; Gill,R.; Heitz,M.-P.; Jaeschke,G.; Mutel,V.; Trube,G.; Wyler,R.
参考来源:Bioorg Med Chem Lett 2001,11(16),2173

RPR-201764

Chemical Name: 4-Chloro-N-[4-[1-(4-cyanobenzyl)-1H-imidazol-5-ylmethylamino]-1-benzopyran-8-ylcarbonyl]-L-phenylalaninamide
CAS No. 238764-04-0, 238763-08-1 (diastereomer), 238763-09-2 (diastereome...
参考文献标题:Condensed heterocyclic system derivs.,preparation,pharmaceutical compsns.containing them
文献作者:Jimonet,P.; Dereu,N.; Le Brun,A.; Baudoin,B.; Clerc,F.; El-Ahmad,Y.; Hardy,J.-C.(Aventis Pharma SA)
参考来源:EP 1054882; FR 2774987; WO 9941248

新产品编号:715573

Chemical Name: 1-[5-[4-Amino-5-(3-bromophenyl)pyrido[2,3-d]pyrimidin-7-yl]pyridin-2-yl]piperidin-4-one O-(tetrahydropyran-4-yl)oxime
CAS No. 265105-63-3
项目整合开发状态: Preclinical
项目研究机构: Abbott (...
参考文献标题:5,7-Disubstd.-4-aminopyrido[2,3-d]pyrimidine cpds.
文献作者:Stewart,A.O.; Perner,R.J.; McKie,J.A.; Zheng,G.Z.; Grillot,A.L.; Cowart,M.D.; Bhagwat,S.S.; Lee,C.-H.(Abbott Laboratories Inc.)
参考来源:WO 0023444

新产品编号:645965

Chemical Name: 2-(Benzyloxycarboxamido)-3-[4-[2-[3-methoxy-4-[3-(2-methylphenyl)ureido]phenyl]acetamidomethyl]piperidin-1-yl]propionic acid
CAS No. 247254-24-6
项目整合开发状态: Biological Testing
项目...
参考文献标题:Substd.diamines and their use as cell adhesion inhibitors
文献作者:McCarthy,C.; Morley,A.D.; Harris,N.V.(Rh鬾e-Poulenc Rorer Ltd.)
参考来源:WO 9954321

A-304470

Chemical Name: 1-[3-[4-(2,3-Dihydro-1,4-benzodioxin-6-ylsulfanyl)-3-(trifluoromethyl)phenyl]-2(E)-propenoyl]piperidine-3-carboxylic acid
CAS No. 280751-86-2 ((R)-isomer)
项目整合开发状态: Preclinical 参考文献标题:Cell adhesion-inhibiting antiinflammatory and immune-suppressive cpds.
文献作者:Lynch,J.K.; Link,J.; Zhu,G.-D.; Boyd,S.A.; Winn,M.; Pei,Z.; Gunawardana,I.W.; Liu,G.; Xin,Z.; Jae,H.-S.; Freeman,J.C.; Von Geldern,T.; Staeger,M.A.(Abbott Laboratories Inc.)
参考来源:US 6110922; WO 0039081