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

新产品编号:614325

Chemical Name: N-Allyl-N-[1-[4-(1H-benzimidazol-1-yl)-3-phenylbutyl]piperidin-4-yl]carbamic acid 4-nitrobenzyl ester
CAS No. 235420-00-5
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Originator)...
参考文献标题:Cyclic amine modulators of chemokine receptor activity
文献作者:Finke,P.E.; Mills,S.G.; Caldwell,C.G.; MacCoss,M.; Wang,L.; Kothandaraman,S.; Kim,D.; Oates,B.(Merck & Co.,Inc.)
参考来源:EP 1052992; US 6140349; WO 9938514

新产品编号:633309

Chemical Name: 2,5-Dihydroxy-3-(1-methylindol-3-yl)-6-phenyl-2,5-cyclohexadiene-1,4-dione
CAS No. 245737-50-2
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Originator)
合成路线:Treatment of pheny...
参考文献标题:Antidiabetic agents
文献作者:Wood,H.B.; Jones,A.B.; Zhang,B.; Liu,K.(Merck & Co.,Inc.)
参考来源:EP 1067925; US 6077849; WO 9951225

新产品编号:740885

Chemical Name: N-[4-Chloro-2-[N-(5-chloropyridin-2-yl)carbamoyl]phenyl]-1-isopropylpiperidine-4-carboxamide
CAS No. 280771-57-5, 280769-08-6 (HCl)
项目整合开发状态: Preclinical
项目研究机构: Lilly (Origina...
参考文献标题:Aromatic amides
文献作者:Wikel,J.H.; Yee,Y.K.; Weir,L.C.; Joseph,S.P.; Tebbe,A.L.; Sawyer,J.S.; Goodson,T.J.; Franciscovich,J.B.; Tinsley,J.M.; Wiley,M.R.; Milot,G.; Pineiro-Nunez,M.M.; Masters,J.J.; Hall,S.E.; (Eli Lilly and Company)
参考来源:WO 0039118

新产品编号:696589

Chemical Name: 3-Oxoolean-1,12(13)-dien-2,28-dioic acid
CAS No. 259526-05-1
项目整合开发状态: Biological Testing
项目研究机构: Dartmouth College (Originator)
合成路线:Hydrolysis of the acetate ester from ol...
参考文献标题:Novel synthetic oleanate triterpenoids: A series of highly active inhibitors of nitric production in mouse macrophages
文献作者:Honda,T.; Rounds,B.V.; Bore,L.; Favaloro,F.G.Jr.; Gribble,G.W.; Suh,N.; Wang,Y.; Sporn,M.B.
参考来源:Bioorg Med Chem Lett 1999,9(24),3429

新产品编号:345385

Chemical Name: 3(S)-[2-[5(R)-Methyl-2-oxo-3(S)-(5,6,7,8-tetrahydro[1,8]naphthyridin-2-ylmethylamino)pyrrolidin-1-yl]acetamido]-4-pentynoic acid ethyl ester
CAS No. 204452-88-0
项目整合开发状态: Preclini...
参考文献标题:Integrin antagonists
文献作者:Duggan,M.E.; Hartman,G.D.; Hoffman,W.F.; Meissner,R.S.; Perkins,J.J.; Askew,B.C.; Coleman,P.J.; Hutchinson,J.H.; Naylor-Olsen,A.M.(Merck & Co.,Inc.)
参考来源:EP 0934305; US 5981546; WO 9808840

新产品编号:612743

Chemical Name: 1-[3(S)-Methyl-4-[N-methyl-N-(phenylsulfonyl)amino]-3-phenylbutyl]piperidin-4-yl-N-(2-propenyl)carbamic acid 4-nitrobenzyl ester
CAS No. 235418-89-0 (undefined isomer), 235418-88-9 (...
参考文献标题:Cyclic amine modulators of chemokine receptor activity
文献作者:Finke,P.E.; Mills,S.G.; Caldwell,C.G.; MacCoss,M.; Wang,L.; Kothandaraman,S.; Kim,D.; Oates,B.(Merck & Co.,Inc.)
参考来源:EP 1052992; US 6140349; WO 9938514

Dendroamide A

Chemical Name: (4R,11R,18R)-11-Isopropyl-4,7,18-trimethyl-6-oxa-13,20-dithia-3,10,17,22,23,24-hexaazatetracyclo[17.2.1.1(5,8).1(12,15)]tetracosa-1(21),5(24),7,12(23),14,19(22)-hexaene-2,9,16-trione 参考文献标题:Total synthesis of dendroamide A,a novel cyclic peptide that reverses multiple drug resistance
文献作者:Xia,Z.; Smith,C.D.
参考来源:J Org Chem 2001,66(10),3459

新产品编号:52715

Chemical Name: 1-Ethyl-7-[3-[4-(4-fluorophenyl)-1-piperazinyl]propyl]-6,7-dihydropyrrolo[2,3-c]azepine-4,8(1H,5H)-dione 4-oxime
CAS No. 150159-63-0
项目整合开发状态: Preclinical
项目研究机构: Daiichi Sunto...
参考文献标题:Pyrroloazepine cpd.
文献作者:Mizuno,A.; Miya,M.; Inomata,N.; Tatsuoka,T.; Ishihara,T.(Suntory Ltd.)
参考来源:EP 0557526; JP 1993503481; US 5399557; WO 9303032

新产品编号:484601

Chemical Name: 3-Chloro-4-hydroxy-N2-(4-hydroxynaphthalen-1-ylmethylidene)benzohydrazide
CAS No. 219680-33-8
项目整合开发状态: Preclinical
项目研究机构: Novo Nordisk (Originator), Pfizer (Originator)
合成...
参考文献标题:Glucagon antagonists/inverse agonists
文献作者:Gonzales,J.; Sams,C.; Teng,M.(Alanex Corp.; Novo Nordisk A/S)
参考来源:EP 0994848; WO 9901423

新产品编号:744049

Chemical Name: 2-(4-Fluorophenyl)-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one
CAS No. 283172-76-9
项目整合开发状态: Preclinical
项目研究机构: Agouron (Originator), Cancer Research UK (Originator) 参考文献标题:Tricyclic inhibitors of poly(ADP-ribose) polymerases
文献作者:Thoresen,L.H.; Webber,S.E.; Tikhe,J.; Canan-Koch,S.S.(Agouron Pharmaceuticals,Inc.; Cancer Research Campaign Technology Ltd.)
参考来源:EP 1140936; WO 0042040