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

DPC-602

Chemical Name: 1-[2-(Aminomethyl)phenyl]-N-(2'-sulfamoyl-3-fluorobiphenyl-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide hydrochloride
CAS No. 228258-45-5, 228258-87-5 (monotrifluoroacetate) 参考文献标题:Nitrogen containing heteroaromatics with ortho-substd.P1's as factor Xa inhibitors
文献作者:Bostrom,L.L.; Pinto,D.J.P.; Galemmo,R.A.Jr.; Rossi,K.A.(DuPont Pharmaceuticals Co.)
参考来源:EP 1042299; WO 9932454

A-295339

Chemical Name: 5-[4-[3-(4-Acetylpiperazin-1-yl)-3-oxo-1-propenyl]-2-chlorophenylsulfanyl]-1-methyl-1H-indole
CAS No. 280750-58-5
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:Coup...
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

BRACO-19

Chemical Name: N,N'-[9-[4-(Dimethylamino)phenylamino]acridin-3,6-diyl]bis[3-(1-pyrrolidinyl)propionamide] trihydrochloride
CAS No. 351351-75-2
项目整合开发状态: Preclinical
项目研究机构: Cancer Research Te...
参考文献标题:Therapeutic acridone and acridine cpds.
文献作者:Neidle,S.; Harrison,R.J.; Kelland,L.R.; Gowan,S.M.; Read,M.; Reszka,T.(Cancer Research Technology Ltd.)
参考来源:WO 0208193

T-0314407

Chemical Name: N-Methyl-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]benzenesulfonamide
CAS No. 293753-06-7
项目整合开发状态: Preclinical
项目研究机构: Amgen (Originator)
合成路线:Treatme...
参考文献标题:Compsns.and methods for raising HDL cholesterol levels
文献作者:Shan,B.(Tularik Inc.)
参考来源:WO 0103705

S-247

Chemical Name: 3(S)-(3-Bromo-5-chloro-2-hydroxyphenyl)-3-[N-[5-(5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-ylamino)pyridin-3-ylcarbonyl]glycylamino]propionic acid
CAS No. 247099-90-7, 280123-03-7 (ena...
参考文献标题:Heterocyclic glycyl beta-alanine derivs.as vitronectin antagonists
文献作者:Miyashiro,J.M.; Gasiecki,A.F.; Khanna,I.K.; Chandrakumar,N.S.; Desai,B.N.; Russell,M.A.; Devadas,B.; Rico,J.G.; Rogers,T.E.; Rao,S.N.; Malecha,J.W.; Ruminski,P.G.; Yu,Y.; Huff,R.(Pfizer Inc.)
参考来源:EP 1070060; JP 2002511462; WO 9952896

GW-505524B

Chemical Name: N-(4,5-Dihydro-1H-imidazol-2-ylmethyl)-N-[2-(methylsulfonyl)phenyl]amine
CAS No. 305809-45-4, 305809-46-5 (fumarate salt), 305809-64-7 (monohydrochloride)
项目整合开发状态: Preclinical 参考文献标题:Imidazoline derivs.as alpha-1A adrenoceptor ligands
文献作者:Hodson,S.J.; Navas,F.III; Bishop,M.J.; Bigham,E.C.; Garrison,D.T.; Drewry,D.H.; Speake,J.D.(Glaxo Group Ltd.)
参考来源:WO 0066563

26-Fluoroepothilone, CGP-85715

Chemical Name: (1S,3S,7S,10R,11S,12S,16R)-16-(Fluoromethyl)-7,11-dihydroxy-8,8,10,12-tetramethyl-3-[1(E)-methyl-2-(2-methylthiazol-4-yl)vinyl]-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione
CAS No....
参考文献标题:Epothilone analogs
文献作者:He,Y.; Yang,Z.; Nicolaou,C.K.; Ninkovic,S.; Pastor,J.; Roschangar,F.; Sarabia,F.; Vallberg,H.; Vourloumis,D.; Winssinger,N.; King,N.P.; Finlay,M.R.V.(Novartis AG; Scripps Research Institute)
参考来源:JP 2001504856; WO 9825929

SCH-62373

Chemical Name: 1-Benzyl-N-[2-[2-(3,4-dichlorophenyl)-4-(3,5-dimethylbenzoyl)piperazin-1-yl]-2-oxoethyl]piperidin-4-amine
CAS No. 185108-18-3
项目整合开发状态: Biological Testing
项目研究机构: Schering-Plou...
参考文献标题:Piperazino derivs.as neurokinin antagonists
文献作者:Shue,H.-J.; Shih,N.-Y.; Blythin,D.J.; Chen,X.; Tom,W.C.; Piwinski,J.J.; McCormick,K.D.(Schering Corp.)
参考来源:EP 0823906; US 5719156; WO 9634864

BMS-363131

Chemical Name: 3(R)-(1-Amidinopiperidin-3(R)-ylmethyl)-4-oxo-1-[4-(6-phenylhexanoyl)piperazin-1-ylcarbonyl]azetidine-2(S)-carboxylic acid
CAS No. 253177-55-8 (stereoisomer), 253175-00-7 (stereoisom...
参考文献标题:Amidino and guanidino azetidinone tryptase inhibitors
文献作者:Treuner,U.; Kronenthal,D.R.; Xu,Z.; Seiler,S.; Slusarchyk,W.A.; Bisacchi,G.; Randazzo,M.E.; Sutton,J.C.; Shi,Z.; Zahler,R.; Schwinden,M.D.(Bristol-Myers Squibb Co.)
参考来源:WO 9967215

SX-477

Chemical Name: 1-(4-Fluorophenyl)-4-[(8aS,12aR)-6,7,8a,9,10,11,12,12a-octahydro-5H-pyrido[3',4':4,5]pyrrolo[1,2,3-ef][1,5]benzothiazepin-11-yl]butan-1-one hydrochloride
CAS No. 313539-84-3 (free ba...
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