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

Eliprodil hydrochloride

依利罗地 Chemical Name: (?-1-(4-Chlorophenyl)-2-[4-(4-fluorobenzyl)-1-piperidinyl]ethanol hydrochloride; (?-alpha-(4-Chlorophenyl)-4-[(4-fluorophenyl)methyl]piperidine-1-ethanol hydrochloride
CAS No. ...
参考文献标题:1-Phenyl-2-piperidino propanol derivs.,their preparation and medicines containing them
文献作者:Wick,A.; Frost,J.; Gaudilliere,B.; Bertin,J.; Dupont,R.; Rousseau,J.(Sanofi-Synthabo )
参考来源:EP 0109317

Eplivanserin, SR-46349

依利色林Chemical Name: 1(Z)-[2-(Dimethylamino)ethoxyimino]-1-(2-fluorophenyl)-3-(4-hydroxyphenyl)-2(E)-propene; 1-(2-Fluorophenyl)-3-(4-hydroxyphenyl)-2(E)-propenone (Z)-O-[2-(dimethylamino)ethyl]oxime 参考文献标题:Propenone oxime ethers,method for their preparation and pharmaceutical compsns.containing them
文献作者:Congy,C.; Labeeuw,B.; Gueule,P.; Rinaldi,M.(Sanofi-Synthabo)
参考来源:EP 0373998; FR 2639942; JP 1990262552

Icotidine trihydrochloride, SK&F-93319(free base), SK&F-93319-A3

依可替丁 Chemical Name: 2-[4-(3-Methoxypyridin-2-yl)butylamino]-5-(6-methylpyridin-3-ylmethyl)pyrimidin-4(1H)-one trihydrochloride
CAS No. 71351-65-0, 71351-79-6 (free base)
项目整合开发状态: Biological Te...
参考文献标题:Pyridylalkylpyrimidone cpds.,process for preparin
文献作者:Durant,G.J.; Brown,T.H.; Ganellin,C.R.(SmithKline Beecham plc)
参考来源:EP 0017679

Edotreotide yttrium, Yttrium (90Y) edotreotide, Octreother, DOTATOC-[90Y], SMT-487-[90Y], [90Y]-SMT-487

依多曲肽 Chemical Name: [N-[2-[4,7-Bis[(carboxy-kappaO)methyl]-10-(carboxymethyl)-1,4,7,10-tertaazacyclododec-1-yl-kappaN1,kappaN4,kappaN10]acetyl]-D-phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lys...
参考文献标题:Direct synthesis of [DOTA-DPhe]-octreotide and [DOTA-DPhe1,Tyr3]-octreotide (SMT487): Two conjugates for systemic delivery of radiotherapeutical nuclides to somatostatin receptor positive tumors in man
文献作者:Albert,R.; Smith-Jones,P.; Stolz,B.; Simeon,C.; Knecht,,H.; Bruns,C.; Pless,J.
参考来源:Bioorg Med Chem Lett 1998,8(10),1207

Ebselen, DR-3305, PZ-51, Harmokisane

依布硒Chemical Name: 2-Phenyl-1,2-benzisoselenazol-3(2H)-one
CAS No. 60940-34-3
项目整合开发状态: Discontinued
项目研究机构: Aventis Pharma (Originator), Daiichi Pharmaceutical (Licensee)
合成路线:The neutral...
参考文献标题:2-Phenyl-1,2-benzisoselenazol-3(2H)-one containing pharmaceutical preparations and process for the treatment or rheumatic diseases
文献作者:Renson,M.; Etschenberg,E.; Winkelmann,J.(A.Nattermann & Cie.GmbH)
参考来源:DE 3027073; EP 0044971; JP 8256427; US 4352799

Epalrestat, Ono-2235, Kinedak

依帕司他Chemical Name: (Z,E)-5-(2-Methyl-3-phenyl-2-propenylidene)-4-oxo-2-thioxothiazolidine-3-acetic acid; (Z,E)-3-(Carboxymethyl)-5-(beta-methylcinnamylidene)rhodanine; (Z,E)-5-(beta-Methylcinnamylide...
参考文献标题:Rhodanine derivs.,process for their preparation,
文献作者:Hiroshi,T.; Tetsuya,M.; Takeshi,M.; Akio,A.; Masanori,K.; Fumio,H.; Tadao,T.; Masaki,H.(Ono Pharmaceutical Co.,Ltd.)
参考来源:EP 0047109; US 4464382

Etravirine, TMC-125, R-165335

依曲韦林Chemical Name: 4-[6-Amino-5-bromo-2-(4-cyanophenylamino)pyrimidin-4-yloxy]-3,5-dimethylbenzonitrile
CAS No. 269055-15-4
项目整合开发状态: Phase II
项目研究机构: Janssen (Originator), Tibotec-Virco (Or...
参考文献标题:HIV replication inhibiting pyrimidines
文献作者:Heeres,J.; De Corte,B.; Kukla,M.J.; Van Aken,K.J.A.; Janssen,P.A.J.; Ludovici,D.W.; De Jonge,M.R.; Kavash,R.W.; Ho,C.Y.; Koymans,L.M.H.(Janssen Pharmaceutica NV)
参考来源:EP 1002795; WO 0027825

Technetium (99mTc) exametazime, [99mTc]-HMPAO, HMPAO-[99mTc], Ceretec

依沙美肟钛-99Tc,[[3,3'-[(2,2-二甲基-1,3-丙二二基)di(亚氨基-kN)]双[2-丁酮] di(oximato-kN)](3-)]oxo-, (SP-5-15)-(9CI)Chemical Name: [[(?-(3RS,3'RS)-3,3'-[(2,2-Dimethyltrimethylene)diimino][di-2-butanone]dioximato](3-)-...
参考文献标题:Complexes of technetium-99m with propylene amine oximes
文献作者:Nowotnik,D.P.; Canning,L.R.; Neirinckx,R.D.; Piper,I.M.(Amersham plc)
参考来源:EP 0194843; JP 1986225159; US 4789736

Efavirenz, L-743725((+)-enantiomer), DMP-266, L-741211(racemate), L-743726, Stocrin, Sustiva

依法韦仑Chemical Name: (S)-(-)-6-Chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-2,4-dihydro-1H-3,1-benzoxazin-2-one
CAS No. 154598-52-4
项目整合开发状态: Launched-1998
项目研究机构: Banyu (Orphan Drug), Br...
参考文献标题:Benzoxazinones as inhibitors of HIV reverse transcriptase
文献作者:Young,S.D.; Tran,L.O.; Britcher,S.F.; Lumma,W.C.Jr.; Payne,L.S.(Merck & Co.,Inc.)
参考来源:EP 0582455; JP 1994184124; WO 9403440

Esorubicin hydrochloride, NSC-267469(free base), IMI-58

依索比星 Chemical Name: 4'-Deoxydoxorubicin hydrochloride; [2S-[2alpha(8R*,10R*),4beta,6beta]]-10-[(4-Aminotetrahydro-6-methyl-2H-pyran-2-yl)oxy]-7,8,9,10-tetrahydro-6,8,11-trihydroxy-8-(hydroxyacetyl)-1...
参考文献标题:Novel antitumor glycosides of the anthracycline series and process for their preparation
文献作者:Penco,S.; Arcamone,F.; Di Marco,A.
参考来源:FR 2325659