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

SP-057

Chemical Name: (8S,11R,12S)-N12-Hydroxy-11-isobutyl-N8-[2-(4-morpholinyl)-2-oxoethyl]-2,10-dioxo-1-oxa-3,9-diazacyclopentadecane-8,12-dicarboxamide
CAS No. 191408-36-3
项目整合开发状态: Preclinical
项...
参考文献标题:Novel macrocyclic cpds.as metalloprotease inhibitors
文献作者:Xue,C.-B.; Cherney,R.J.; DeCicco,C.P.; Degrado,W.F.; He,X.; Hodge,C.N.; Jacobson,I.C.; Magolda,R.L.; Arner,E.C.; Duan,J.; Nelson,D.J.(DuPont Pharmaceuticals Co.)
参考来源:EP 0863885; JP 2000502050; WO 9718207

LY-426410

Chemical Name: 2-Methylalanyl-N-[1-[1(R)-(4-methoxyphenyl)-2-(4-methyl-1-piperidinyl)-2-oxoethyl]-1H-imidazol-4-yl]-O-benzyl-D-serinamide; 2-Amino-N-[1(R)-(benzyloxymethyl)-2-[1-[1(R)-(4-methoxyphenyl...
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:579521

Chemical Name: 8-Methyl-N-[2-[1-(isopropoxyphenyl)methyl]-1,6-naphthyridine-2-carboxamide
CAS No. 227199-42-0
项目整合开发状态: Biological Testing
项目研究机构: Shire BioChem (Originator)
合成路线:The conde...
参考文献标题:Discovery of 1,6-naphthyridines as a novel class of potent and selective human cytomegalovirus inhibitors
文献作者:Chan,L.; Jin,H.; Stefanac,T.; Lavall閑,J.F.; Falardeau,G.; Wang,W.; B閐ard,J.; May,S.; Yuen,L.
参考来源:J Med Chem 1999,42(16),3023

新产品编号:628563

Chemical Name: 4-(Diphenylmethyl)-1-[3-phenylprop-2(E)-enyl]-1-(phosphonooxymethyl)piperazin-1-ium trifluoroacetate
CAS No. 243656-14-6, 243656-13-5 (free cation)
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Novel prodrug approach for tertiary amines: Synthesis and preliminary evaluation of N-phosphonooxymethyl prodrugs
文献作者:Krise,J.P.; Zygmunt,J.; Georg,G.I.; Stella,V.J.
参考来源:J Med Chem 1999,42(16),3094

新产品编号:626981

Chemical Name: 4-(2-Chlorodibenzo[b,f]-1,4-oxazepin-11-yl)-1-methyl-1-(phosphonooxymethyl)piperazin-1-ium trifluoroacetate
CAS No. 242816-65-5, 242816-64-4 (free cation)
项目整合开发状态: Preclinical 参考文献标题:Novel prodrug approach for tertiary amines: Synthesis and preliminary evaluation of N-phosphonooxymethyl prodrugs
文献作者:Krise,J.P.; Zygmunt,J.; Georg,G.I.; Stella,V.J.
参考来源:J Med Chem 1999,42(16),3094

RTI-112

Chemical Name: (-)-(1R,2S,3S,5S)-(4-Chloro-3-methylphenyl)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylic acid methyl ester
CAS No. 143982-09-6, 150653-92-2 (HCl)
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:Synthesis,ligand binding,and QSAR (CoMFA and classical) study of 3beta-(3'-substituted phenyl)-,3beta-(4'-substituted phenyl)-,and 3beta-(3',4'-disubstituted phenyl)tropane-2beta-carboxylic acid methyl esters
文献作者:Lewin,A.H.; Carroll,F.I.; Abraham,P.; Mascarella,S.W.; Gao,Y.; Boja,J.W.; Kuhar,M.J.; Kuzemko,M.A.
参考来源:J Med Chem 1994,37(18),2865

RPR-208707

Chemical Name: N-[2-Oxo-1-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)pyrrolidin-3(S)-yl]thieno[3,2-b]pyridine-2-sulfonamide
CAS No. 209285-84-7, 209285-85-8 (trifluoroacetate)
项目整合开发状态: Preclinical 参考文献标题:Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide cpds.
文献作者:Choi-Sledeski,Y.M.; Pauls,H.W.; Green,D.M.; Barton,J.N.; Becker,M.R.; Ewing,W.R.(Aventis Pharmaceuticals,Inc.)
参考来源:EP 0944386; WO 9825611

CP-4632

Chemical Name: 3-[3-Fluoro-4-[4-(1,4,5,6-tetrahydropyrimidin-2-ylamino)piperidin-1-yl]benzamido]-2(S)-(phenylsulfonamido)propionic acid
CAS No. 247034-18-0
项目整合开发状态: Preclinical
项目研究机构: Meiji...
参考文献标题:Aminopiperidine derivs.as integrin alphavbeta3 antagonists
文献作者:Ajito,K.; Katano,K.; Kubota,D.; Ishikawa,M.; Murakami,S.; Hachisu,M.; Yamamoto,M.(Meiji Seika Kaisha,Ltd.)
参考来源:EP 1074543; WO 9952872

J-112287

Chemical Name: 5(S)-(2,2-Difluoro-1,3-benzodioxol-5-yl)-7(R)-[2-(3-hydroxy-2-methylpropyl)-4-methoxyphenyl]-2-(isopropylamino)-6,7-dihydro-5H-cyclopenta[b]pyridine-6(R)-carboxylic acid
CAS No. 2329...
参考文献标题:Substd.5-(2,2-difluoro-1,3-benzodioxol-5-yl) cyclopentenopyridine deriv.
文献作者:Nishikibe,M.; Hayama,T.; Otake,N.(Banyu Pharmaceutical Co.,Ltd.)
参考来源:EP 1049691; WO 9937639

3-BAABU, MF-191

Chemical Name: N-[3-(Bromoacetamido)benzoyl]urea; N-(Aminocarbonyl)-3-(bromoacetamido)benzamide
CAS No. 209345-04-0
项目整合开发状态: Preclinical
项目研究机构: Cytoskeleton (Originator), Mount Sinai School...
参考文献标题:Synthesis,cancericidal and antimicrotubule activities of 3-(haloacetamido)-benzoylureas
文献作者:Bekesi,J.G.; Holland,J.F.; Jiang,J.-D.; Ma,L.; Roboz,J.; Deng,L.; Weisz,I.
参考来源:Anti-Cancer Drug Des 1998,13(7),735