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

Ro-32-6168

Chemical Name: 1-[N-(4-Hydroxysuccinyl)-L-aspartyl-L-glutamyl-L-(2-methyl)phenyl-alanyl-L-(3-methyl)valyl-L-leucylamino]propylboronic acid; N-(3-Carboxypropanoyl)-L-aspartyl-L-glutamyl-2-methyl-L-phen...
参考文献标题:Antiviral peptide derivs.
文献作者:Attwood,M.R.; Hurst,D.N.; Jones,P.S.; Kay,P.B.; Raynham,T.M.; Wilson,F.X.(F.Hoffmann-La Roche AG)
参考来源:JP 2000508344; WO 9822496

DPP-CNDAC

Chemical Name: (R)-4-Amino-1-[5-O-[[2,3-bis(hexadecanoyloxy)propoxy]hydroxyphosphinyl]-2-cyano-2-deoxy-beta-D-arabinofuranosyl]-2(1H)-pyrimidinone monosodium salt; (R)-1-[5-O-[[2,3-Bis(hexadecanoyloxy...
参考文献标题:Nucleosides and nucleotides.150.Enzymatic synthesis of 5'-phosphatidyl derivatives of 1-(2-C-cyano-2-deoxy-beta-D-arabino-pentofuranosyl)cytosine (CNDAC) and their notable antitumor effects in mice
文献作者:Shuto,S.; et al.
参考来源:Bioorg Med Chem Lett 1996,6(9),1021

ZK-805623

Chemical Name: 3,3'-[(3,5-Difluoro-4-methyl-2,6-pyridinediyl)bis(oxy)]benzenecarboximidamide
CAS No. 183299-91-4 (mono(trifluoroacetate) salt)
项目整合开发状态: Biological Testing
项目研究机构: Berlex (Ori...
参考文献标题:Benzamidine derivs.their preparation and their use as anti-coagulants
文献作者:Buckman,B.O.; Davey,D.D.; Guilford,W.J.; Morrissey,M.M.; Ng,H.P.; Phillips,G.B.; Wu,S.C.; Xu,W.(Berlex Laboratories,Inc.)
参考来源:EP 0813525; US 5691364; WO 9628427

BILA-2157, BILA-2157-BS

Chemical Name: 2(R)-(2-Aminothiazol-4-ylmethyl)-N4-(cyclohexylmethyl)-N1-[1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]-N4-[N-methyl-N-[2-(2-pyridyl)ethyl]carbamoylmethyl]succinamide
C...
参考文献标题:Discovery of non-peptidic P2-P3 butanediamide renin inhibitors with high oral efficacy
文献作者:Simoneau,B.; Lavall閑,P.; Anderson,P.C.; Bailey,M.; Bantle,G.; Berthiaume,S.; Chabot,C.; Fazal,G.; Halmos,T.; Ogilvie,W.W.; Poupart,M.A.; Thavonekham,B.; Xin,Z.; Thibeault,D.; Bolger,G.; Panzenbeck,M.; Winquist,R.; Jung,G.L.
参考来源:Bioorg Med Chem 1999,7(3),489

SQ-094

Chemical Name: 4-[6-(4,6-Diphenyl-2-pyridinyloxy)-2,2-dimethylhexylamino]-4-oxo-3-(3-pyridinylcarboxamido)butanoic acid
CAS No. 206263-67-4 ([(S)-isomer])
项目整合开发状态: Biological Testing
项目研究机构:...
参考文献标题:Radiopharmaceuticals for imaging infection and inflammation
文献作者:Rajopadhye,M.; Harris,T.D.; Barrett,J.A.; Cheesman,E.H.(DuPont Pharmaceuticals Co.)
参考来源:WO 9815295

PNU-144113

Chemical Name: 4-(3,4-Difluorobenzamido)ethyl]-[3(S)-isobutyl-2-oxo-1-(2-phenylethyl)pyrrolidin-3-yl]butyrohydroxamic acid
CAS No. 196951-03-8 ((R*,S*)-isomer)
项目整合开发状态: Biological Testing
项目...
参考文献标题:Hydroxamic acid derivs.for use with the treatment of diseases related to connective tissue degradation
文献作者:Jacobsen,E.J.(Pharmacia & Upjohn AB)
参考来源:EP 0898562; JP 2000506163; US 5712300; WO 9732846

CI-1030, PD-172760

Chemical Name: 7-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]-3,4-dihydro-2H-1,4-benzoxazin-3-one
CAS No. 200195-01-3
项目整合开发状态: Phase I
项目研究机构: Pfizer (Originator)
合成路线:3-Hydroxy-4-nitrobenzal...
参考文献标题:Benzoxazinone dopamine D4 receptor antagonists
文献作者:Belliotti,T.; Wise,L.D.; Wustrow,D.J.(Pfizer Inc.)
参考来源:EP 0906294; WO 9745419

CP-467688

Chemical Name: N-[2-[6-[4'-(Trifluoromethyl)biphenyl-2-ylcarboxamido]-1,2,3,4-tetrahydroisoquinolin-2-yl]ethyl]carbamic acid methyl ester hydrochloride
CAS No. 208590-81-2 (free base)
项目整合开发状态: ...
参考文献标题:Apo B-secretion/MTP inhibitory amides
文献作者:Chang,G.; Quallich,G.J.(Pfizer Inc.)
参考来源:EP 0944602; JP 2000505810; WO 9823593

Ro-60-0869

Chemical Name: cis-7-Ethyl-6-hydroxy-8-methoxy-2-methyl-1,2,3,3a,4,9b-hexahydro-5H-benzo[e]isoindol-5-one
CAS No. 204650-27-1, 204650-28-2 (fumarate(1:1))
项目整合开发状态: Preclinical
项目研究机构: Roche ...
参考文献标题:Tricyclic benzo[e]isoindoles and benzo[h]isoquinolines
文献作者:Stadler,H.; B,M.; Wichmann,J.(F.Hoffmann-La Roche AG)
参考来源:EP 0958285; JP 2000507965; WO 9830546

WAY-140288

Chemical Name: N-[4-[3-(Dimethylaminomethyl)-10,11-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-10-ylcarbonyl]-2-methoxyphenyl]biphenyl-2-carboxamide
CAS No. 200878-87-1
项目整合开发状态: Preclinical
...
参考文献标题:Tricyclic benzazepine vasopressin antagonists
文献作者:Albright,J.D.; Venkatesan,A.M.; Dusza,J.P.; Sum,F.-W.(American Cyanamid Co.)
参考来源:JP 2000510154; US 5753648; WO 9749707