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

LY-444711

Chemical Name: 2(R)-(2-Amino-2-methylpropanamido)-N-[1-[1(R)-(4-methoxyphenyl)-1-methyl-2-oxo-2-(1-pyrrolidinyl)ethyl]-1H-imidazol-4-yl]-5-phenylpentanamide dihydrochloride
CAS No. 220540-02-3, 220...
参考文献标题:Growth hormone secretagogues
文献作者:Jungheim,L.N.; Palkowitz,A.D.; Trankle,W.G.; Lugar,C.W.III; Muehl,B.S.; Ratz,A.M.; Copp,J.D.; Jones,S.A.; Kennedy,J.H.; Shepherd,T.A.; Alt,C.A.; Fahey,K.J.; Thrasher,K.J.; Cohen,J.D.; Gritton,W.H.; et al.(Eli Lilly and Company)
参考来源:EP 0933365; WO 9908699

新产品编号:438723

Chemical Name: N2-[3(R)-(Decanoyloxy)tetradecanoyl]-O3-[2-[3(R)-(decanoyloxy)tetradecanamido]-3-O-[3(R)-(decanoyloxy)tetradecanoyl]-2-deoxy-4-O-phosphono-beta-D-glucopyranosyl]-L-serinamide triethylam...
参考文献标题:Aminoalkyl glucosamine phosphate cpds.and their use as adjuvants and immunoeffectors
文献作者:Johnson,D.A.; Sowell,C.G.(Corixa Corp.)
参考来源:EP 0983286; US 6113918; WO 9850399

新产品编号:557373

Chemical Name: 2(R)-(2-Benzothiazolylmethyl)-N-methyl-4-oxo-N-[4-(trifluoromethyl)benzyl]azetidine-1-carboxamide
CAS No. 223266-68-0
项目整合开发状态: Biological Testing
项目研究机构: Bio-Mega (Originator)...
参考文献标题:Azetidinone derivs.for the treatment of HCMV infections
文献作者:Ogilvie,W.W.; O'Meara,J.; Deziel,R.; Yoakim,C.(Boehringer Ingelheim (Canada) Ltd.)
参考来源:EP 1021405; WO 9918072

SK-1899

Chemical Name: Acetic acid 4-(2-amino-9H-purin-9-yl)-2-(isopropoxycarbonyloxymethyl)butyl ester; 9-[4-(Acetoxy)-3-(isopropoxycarbonyloxymethyl)butyl]-2-aminopurine
CAS No. 247081-81-8
项目整合开发状态: ...
参考文献标题:Synthesis and evaluation of 2-amino-9-(3-acyloxymethyl-4-alkoxycarbonyloxybut-1-yl)purines and 2-amino-9-(3-alkoxycarbonyloxymethyl-4-alkoxycarbonyloxybut-1-yl)purines as potential prodrugs of penciclovir
文献作者:Kim,D.K.; Lee,N.; Ryu,D.H.; Kim,Y.W.; Kim,J.S.; Chang,K.; Im,G.J.; Choi,W.S.; Cho,Y.B.; Kim,K.H.; Colledge,D.; Locarnini,S.
参考来源:Bioorg Med Chem 1999,7(8),1715

新产品编号:650711

Chemical Name: N2-[N-(Benzyloxycarbonyl)-L-histidyl]-N1-(2-methyl-2-phenylpropyl)-N2-[1(R)-phenylethyl]glycinamide
CAS No. 248603-60-3
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)...
参考文献标题:Functionalized alkyl and alkenyl side chain derivs.of glycinamides as farnesyl transferase inhibitors
文献作者:Doherty,A.M.; Quin,J.III; Kaltenbronn,J.S.; Leonard,D.M.; McNamara,D.J.(Pfizer Inc.)
参考来源:WO 9955725

新产品编号:476691

Chemical Name: N-[3(R)-Carboxy-2,2,3-trimethylcyclopent-1(S)-ylcarbonyl]-4-(2,4,6-trichlorobenzamido)-L-phenylalanine
CAS No. 219494-80-1
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originat...
参考文献标题:Inhibitors of alpha4beta1 mediated cell adhesion
文献作者:Rishton,G.; Chrusciel,R.A.; Yamagishi,M.; Polinsky,A.; Thomas,E.W.; Lobl,T.J.; Tanis,S.P.; Teegarden,B.; Fisher,J.F.(Pharmacia Corp.; Tanabe Seiyaku Co.,Ltd.)
参考来源:EP 0991619; WO 9858902

RWJ-69442

Chemical Name: 2-[4-(Dimethylamino)phenyl]-N-[2(S)-hydroxy-3-[4-(2-isopropoxyphenyl)piperazin-1-yl]propyl]-1,3-dioxo-2,3-dihydro-1H-isoindole-5-carboxamide
CAS No. 239807-61-5
项目整合开发状态: Preclini...
参考文献标题:Phthalimido arylpiperazines as alpha 1a receptor antagonists useful in the treatment of benign prostatic hyperplasia
文献作者:Murray,W.V.; Kuo,G.-H.; Prouty,C.P.(Ortho-McNeil Pharmaceutical,Inc.)
参考来源:US 6063785; WO 9942445

新产品编号:544717

Chemical Name: 1-(3,5-Diiodo-4-methoxybenzyl)-1,2,3,4-tetrahydroisoquinolin-6-ol hydrochloride
CAS No. 221659-13-8
项目整合开发状态: Biological Testing
项目研究机构: Molecular Design International (Origina...
参考文献标题:2-Amino-4-benzyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridines: Novel selective beta3-adrenoceptor agonists
文献作者:Zheng,W.; Nikulin,V.I.; Konkar,A.A.; Vansal,S.S.; Shams,G.; Feller,D,R.; Miller,D.D.
参考来源:J Med Chem 1999,42(12),2287

新产品编号:297925

Chemical Name: (Z)-5-[4-[1-(6-Benzyloxy-2,5,7,8-tetramethyl-3,4-dihydro-2H-1-benzopyran-2-ylmethyl)pyrrolidin-2(S)-ylmethoxy]benzylidene]thiazolidine-2,4-dione maleate
CAS No. 199108-11-7, 199108-1...
参考文献标题:Heterocyclic cpds.having antidiabetic,hypolipidaemic,antihypertensive properties,process for their preparation and pharmaceutical compsns.containing them
文献作者:Ramanujam,R.; Chakrabarti,R.; Lohray,B.B.; Bajji,A.C.; Lohray,V.B.; Alla,S.R.(Dr.Reddy's Research Foundation)
参考来源:US 5889032

新产品编号:214079

Chemical Name: N-(N-Phenylcarbamoyl)-L-seryl-L-leucyl-L-valine ethyl ester
CAS No. 189110-11-0
项目整合开发状态: Biological Testing
项目研究机构: Kirin Brewery (Originator)
合成路线:The title compound was o...
参考文献标题:Novel peptide cpds.and medicinal compsns.thereof
文献作者:Kataoka,S.; Nishitoba,T.; Takahashi,M.; Sawa,E.; Kamishohara,M.(Kirin Brewery Co.,Ltd.)
参考来源:JP 1999171896; WO 9711091