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

PTR-3046

Chemical Name: [3S-(3alpha,6alpha,9beta,12alpha,15alpha)]-2(S)-[6-(4-Aminobutyl)-15-benzyl-12-(4-hydroxybenzyl)-9-(1H-indol-3-ylmethyl)-3-isopropyl-2,5,8,11,14,20-hexaoxo-1,4,7,10,13,16,19-heptaazacyc...
参考文献标题:Conformationally constrained backbone cyclized somatostatin analogs
文献作者:Hornik,V.; Seri-Levy,A.; Gellerman,G.; Gilon,C.(Yissum Research Development Co.)
参考来源:WO 9804583

L-757464

Chemical Name: 5-Chloro-2-[4-[4-(2-oxo-2,3-dihydrobenzoxazol-3-yl)piperidin-1-yl]butyl]-1,2-benzisothiazol-3(2H)-one 1,1-dioxide
CAS No. 173842-04-1
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. ...
参考文献标题:Design and synthesis of N-alkylated saccharins as selective alpha1-a adrenergic receptor antagonists
文献作者:Nerenberg,J.B.; Erb,J.M.; Thompson,W.J.; Lee,H.Y.; Guare,J.P.; Munson,P.M.; Bergman,J.M.; Huff,J.R.; Broten,T.P.; Chang,R.S.; Chen,T.B..; O'Malley,S.; Schorn,T.W.; Scott,A.L.
参考来源:Bioorg Med Chem Lett 1998,8(18),2467

L-163540

Chemical Name: 1-[2(R)-(2-Amino-2-methylpropionamido)-3-(3-indolyl)propionyl]-3(S)-benzylpiperidine-3-carboxylic acid ethyl ester
CAS No. 170842-48-5
项目整合开发状态: Preclinical
项目研究机构: Merck & Co....
参考文献标题:Preparation of (S)-3-carbethoxy-3-benzylpiperidine and the growth hormone secretagogue L-163,540
文献作者:Maligres,P.E.; et al.
参考来源:J Org Chem 1998,63(25),9548

CZ-48

Chemical Name: 4(S)-Ethyl-4-(propionyloxy)-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-dione; 20(S)-(Propionyloxy)camptothecin
CAS No. 194414-69-2
项目整合开发状态: Preclini...
参考文献标题:Derivs.of camptothecin for use in treating cancer
文献作者:Ciovanella,B.C.; Zhisong,C.(The Stehlin Foundation for Cancer Research)
参考来源:EP 0879236; WO 9728165

SM-084

Chemical Name: 2-[6-[3-(3-Amidinophenyl)-5-(1-tetrazolylmethyl)-4,5-dihydroisoxazol-5-ylcarboxamido]pyridin-3-yl]benzenesulfonamide trifluoroacetate
CAS No. 193005-21-9 ((-)-enantiomer, free base),...
参考文献标题:Design and synthesis of isoxazoline derivatives as factor Xa inhibitors.2(1)
文献作者:Quan,M.L.; Ellis,C.D.; Liauw,A.Y.; Alexander,R.S.; Knabb,R.M.; Lam,G.; Wright,M.R.; Wong,P.C.; Wexler,R.R.
参考来源:J Med Chem 1999,42(15),2760

SK-549

Chemical Name: 4'-[3-(3-Amidinophenyl)-5-(1-tetrazolylmethyl)-4,5-dihydroisoxazol-5-ylcarboxamido]biphenyl-2-sulfonamide trifluoroacetate
CAS No. 193004-07-8, 193005-13-9 ((-)-enantiomer), 193005-1...
参考文献标题:Design and synthesis of isoxazoline derivatives as factor Xa inhibitors.2(1)
文献作者:Quan,M.L.; Ellis,C.D.; Liauw,A.Y.; Alexander,R.S.; Knabb,R.M.; Lam,G.; Wright,M.R.; Wong,P.C.; Wexler,R.R.
参考来源:J Med Chem 1999,42(15),2760

RPR-130737

Chemical Name: 4-Hydroxy-3-[2-oxo-3(S)-[5-(3-pyridyl)thiophen-2-ylsulfonamido]pyrrolidin-1-ylmethyl]benzamidine
CAS No. 205054-36-0
项目整合开发状态: Preclinical
项目研究机构: Aventis Pharma (Originator) 参考文献标题:Sulfonamidopyrrolidinone factor Xa inhibitors: Potency and selectivity enhancements via P-1 and P-2 optimization
文献作者:Choi-Sledeski,Y.M.; McGarry,D.G.; Green,D.M.; Mason,H.J.; Becker,M.R.; Davis,R.S.; Ewing,W.R.; Dankulich,W.P.; Manetta,V.E.; Morris,R.L.; Spada,A.P.; Cheney,D.L.; Brown,K,D.; Colussi,D.J.; Chu,V.; Heran,C.L.; Morgan,S.R.; et al.
参考来源:J Med Chem 1999,42(18),3572

RPR-120844

Chemical Name: 4-[3(S)-(7-Methoxy-N-methylnaphthalen-2-ylsulfonamido)-2-oxopyrrolidin-1-ylmethyl]thiophene-2-carboxamidine
CAS No. 186549-27-9
项目整合开发状态: Preclinical
项目研究机构: Aventis Pharma (Or...
参考文献标题:Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa
文献作者:Ewing,W.R.; Becker,M.R.; Manetta,V.E.; Davis,R.S.; Pauls,H.W.; Mason,H.; Choi-Sledeski,Y.M.; Green,D.; Cha,D.; Spada,A.P.; Cheney,D.L.; Mason,J.S.; Maignan,S.; Guilloteau,J.P.; Brown,K.; Colussi,D.; Bentley,R.; Bostwick,J.; et al.
参考来源:J Med Chem 1999,42(18),3557

WAY-138351

Chemical Name: 4-[2-(tert-Butylamino)-3,4-dioxo-1-cyclobutenylaminomethyl]-3-chlorobenzonitrile
CAS No. 202520-72-7
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:A ...
参考文献标题:Substd.N-arylmethylamino derivs.of cyclobutene-3,4-diones
文献作者:Antane,M.M.; Herbst,D.R.; McFarlane,G.R.; Gundersen,E.G.; Hirth,B.H.; Quagliato,D.A.; Graceffa,R.F.; Butera,J.A.; Gilbert,A.M.(American Home Products Corp.)
参考来源:US 5763474; US 5780505; WO 9802413

WAY-139799

Chemical Name: 3-Chloro-4-[2-(1,1-dimethylpropylamino)-3,4-dioxo-1-cyclobutenylaminomethyl]benzonitrile
CAS No. 202521-43-5
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharmaceuticals (Originator) 参考文献标题:Substd.N-arylmethylamino derivs.of cyclobutene-3,4-diones
文献作者:Antane,M.M.; Herbst,D.R.; McFarlane,G.R.; Gundersen,E.G.; Hirth,B.H.; Quagliato,D.A.; Graceffa,R.F.; Butera,J.A.; Gilbert,A.M.(American Home Products Corp.)
参考来源:US 5763474; US 5780505; WO 9802413