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

Org-39430

Chemical Name: N-(Carboxymethyl)-3-cyclohexyl-D-alanyl-N-[5-amino-1(S)-(2-isopropoxyoxalyl)pentyl]-L-prolinamide; 7-Amino-3(S)-[N-(carboxymethyl)-3-cyclohexyl-D-alanyl-L-prolylamino]-2-oxoheptanoic ac...
参考文献标题:Thrombin inhibitors
文献作者:Adang,A.E.P.; Peters,J.A.M.; Van Boeckel,C.A.A.; Rewinkel,J.B.M.(Akzo Nobel N.V.)
参考来源:WO 9807308

ABT-839, A-228839, A-228839.25(sulfate)

Chemical Name: N-[5-[N-Butyl-N-(2-cyclohexylethyl)aminomethyl]-2'-methylbiphenyl-2-ylcarbonyl]-L-methionine
CAS No. 216234-25-2 (Li salt)
项目整合开发状态: Phase I
项目研究机构: University of Pittsburgh (O...
参考文献标题:Inhibitors of protein isoprenyl transferases
文献作者:Donner,B.G.; Janowick,D.A.; Larsen,J.J.; Rosenberg,S.H.; Hamilton,A.D.; Barr,K.J.; Sorensen,B.K.; Augeri,D.J.; Kalvin,D.M.; O'Connor,S.J.; Fakhoury,S.A.; Swenson,R.E.; Liu,G.; Sebti,S.M.; Shen,W.(University of Pittsburgh)
参考来源:EP 0986384; WO 9850029; WO 9850030; WO 9850031

SV-030

Chemical Name: 6-[2-Chloro-4-(trifluoromethyl)phenyl]-9-(dicyclopropylmethyl)-8-ethyl-9H-purine
CAS No. 219733-55-8
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:Con...
参考文献标题:Imidazopyrimidines and imidazopyridines for the treatment of neurological disorders
文献作者:Beck,J.P.; Arvanitis,A.G.; Bakthavatchalam,R.; Wilde,R.G.(DuPont Pharmaceuticals Co.)
参考来源:EP 0994877; WO 9901454

GW-4459

Chemical Name: Nalpha-[3(S)-(N-Formyl-N-hydroxyamino)-2(R)-isobutylhexanoyl]-Nomega'-nitro-N1-(2-thiazolyl)-L-argininamide
CAS No. 260270-56-2
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (O...
参考文献标题:Formamide cpds.as therapeutic agents
文献作者:Wiethe,R.W.; Andrews,R.C.; Rabinowitz,M.H.; Musso,D.L.; Chan,J.H.; McDougald,D.L.; Gaul,M.D.; Cowan,D.J.; Stanford,J.B.; Babacz,D.G.; Andersen,M.W.(Glaxo Group Ltd.)
参考来源:US 6191150; WO 0012466

SB-238039

Chemical Name: N-[4-[4-(4-Fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]pyridin-2-yl]-N-phenylamine
CAS No. 186315-03-7
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:2...
参考文献标题:Imidazole cpds.
文献作者:Adams,J.L.; Gallagher,T.F.; Sisko,J.; Peng,Z.-Q.; Osifo,I.K.; Boehm,J.C.(SmithKline Beecham plc)
参考来源:EP 0831830; JP 1999513017; US 5658903; WO 9640143

NU-3108

Chemical Name: 1-[4,8-Bis(3,4-dimethoxybenzylamino)-6-(2-hydroxypropylamino)pyrimido[5,4-d]pyrimidin-2-ylamino]-2-propanol; 1,1'-[[4,8-Bis(3,4-dimethoxybenzylamino)pyrimido[5,4-d]pyrimidine-2,6-diyl]d...
参考文献标题:Resistance-modifying agents.Part 7: 2,6-Disubstituted-4,8-dibenzylaminopyrimido[5,4-d]pyrimidines that inhibit nucleoside transport in the presence of alpha1-acid glycoprotein (AGP)
文献作者:Barlow,H.C.; Bowman,K.J.; Curtin,N.J.; Calvert,A.H.; Golding,B.T.; Huang,B.; Loughlin,P.J.; Newell,D.R.; Smith,P.G.; Griffin,RJ.
参考来源:Bioorg Med Chem Lett 2000,10(6),585

Ro-31-7453

Chemical Name: 3-(1-Methyl-1H-indol-3-yl)-4-(1-methyl-6-nitro-1H-indol-3-yl)-1H-pyrrole-2,5-dione
CAS No. 125313-92-0
项目整合开发状态: Phase II
项目研究机构: Roche (Originator)
合成路线:6-Nitroindole (I) w...
参考文献标题:Substd.pyrroles
文献作者:Davis,P.D.; Hill,C.H.; Lawton,G.(F.Hoffmann-La Roche AG)
参考来源:AU 8929658; EP 0328026; JP 1989233281; US 5057614

PT-624

Chemical Name: N2-[4-[2-(2,4-Diaminopteridin-6-yl)ethyl]benzoyl-N5-hemiphthaloyl-L-ornithine; 2-[N-[4(S)-Carboxy-4-[4-[2-(2,4-diaminopteridin-6-yl)ethyl]benzamido]butyl]carbamoyl]benzoic acid
CAS N...
参考文献标题:Analogues of the potent nonpolyglutamatable antifolate Nalpha-(4-amino-4-deoxypteroyl)-Ndelta-hemiphthaloyl-L-ornithine (PT523) with modifications in the side chain,p-aminobenzoyl moiety,or 9,10-bridge: Synthesis and in vitro antitumor activity
文献作者:Rosowsky,A.; Wright,J.E.; Vaidya,C.M.; Forsch,R.A.; Bader,H.
参考来源:J Med Chem 2000,43(8),1620

SR-3784

Chemical Name: (-)-3(R)-(2-Amino-9H-purin-9-ylmethoxy)-4-hydroxybutylphosphonic acid
CAS No. 198267-74-2
项目整合开发状态: Preclinical
项目研究机构: SRI (Originator)
合成路线:Regiospecific opening of the ch...
参考文献标题:Enantiomerically pure 2-aminopurine phosphonate nucleotide analogs as antiviral agents
文献作者:Reist,E.J.; Bradford,W.W.; Zaveri,N.T.(SRI International)
参考来源:US 5877166; WO 9741133

SR-3785

Chemical Name: 5(R)-(2-Amino-9H-purin-9-ylmethoxy)-2-hydroxy-1,2-oxaphosphorinan-2-one; 9-[(5R)-2-Hydroxy-2-oxo-1,2-oxaphosphorinan-5-yloxymethyl]-9H-purin-2-amine
CAS No. 198267-75-3
项目整合开发状态: ...
参考文献标题:Enantiomerically pure 2-aminopurine phosphonate nucleotide analogs as antiviral agents
文献作者:Reist,E.J.; Bradford,W.W.; Zaveri,N.T.(SRI International)
参考来源:US 5877166; WO 9741133