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

T-3782

Chemical Name: [2aR-[2aalpha,4beta,4abeta,6beta,9alpha(2R,3S),11beta,12alpha,12aalpha,12balpha]]-12b-Acetoxy-9-[2(R)-[2-[3(S)-amino-3-carbamoylpropionyloxy)acetoxy]-3(S)-(tert-butoxycarbonylamino)-3-c...
参考文献标题:Baccatin derivs.and processes for preparing the same
文献作者:Tsujihari,K.; Hashiyama,T.; Ohashi,M.; Nakanishi,N.(Tanabe Seiyaku Co.,Ltd.)
参考来源:CA 2162759; EP 0712854; JP 1997151181; US 5589502

NIP-142

Chemical Name: N-[4(S)-(Cyclopropylamino)-3(R)-hydroxy-2,2-dimethyl-7-nitro-3,4-dihydro-2H-1-benzopyran-6-yl]-2-(4-methoxyphenyl)acetamide
CAS No. 203002-75-9, 203002-58-8 (trans-isomer)
项目整合开发状...
参考文献标题:Chroman derivs.
文献作者:Tanikawa,K.; Ohrai,K.; Sato,M.; Yamashita,T.; Yanagihara,K.(Nissan Chemical Industry,Ltd.)
参考来源:EP 0934296; JP 1998087650; US 6066631; WO 9804542

APC-2848, K02

Chemical Name: N-(4-Morpholinylcarbonyl)-L-phenylalanine 1(S)-(2-phenylethyl)-3-(phenylsulfonyl)-2(E)-propenyl amide
CAS No. 170111-23-6
项目整合开发状态: Preclinical
项目研究机构: Celera (Originator), Khe...
参考文献标题:Irreversible cysteine protease inhibitors containi
文献作者:Rasnick,D.; Klaus,J.L.; Palmer,J.T.(Khepri Pharmaceuticals Inc.)
参考来源:WO 9523222

新产品编号:441887

Chemical Name: 6-[N-(3,4-Dimethoxyphenyl)-N-methylamino]pyrido[3,2-d]pyrimidine-2,4-diamine
CAS No. 216167-24-7
项目整合开发状态: Biological Testing
项目研究机构: Duquesne University (Originator), Indiana ...
参考文献标题:6-Substituted 2,4-diaminopyrido[3,2-d]pyrimidine analogues of piritrexim as inhibitors of dihydrofolate reductase from rat liver,Pneumocystis carinii,and Toxoplasma gondii and as antitumor agents
文献作者:Gangjee,A.; Zhu,Y.; Queener,S.F.
参考来源:J Med Chem 1998,41(23),4533

新产品编号:451379

Chemical Name: (+)-cis-6-Oxo-4-sulfanyl-1,4-azaphosphorinane-2-carboxylic acid P-oxide
CAS No. 217199-44-5 (cis-racemic)
项目整合开发状态: Biological Testing
项目研究机构: University of Sydney (Originator)...
参考文献标题:Synthesis and enzymic evaluation of 4-mercapto-6-oxo-1,4-azaphosphinane-2-carboxylic acid 4-oxide as an inhibitor of mammalian dihydroorotase
文献作者:Manthey,M.K.; Huang,D.T.C.; Bubb,W.A.; Christopherson,R.I.
参考来源:J Med Chem 1998,41(23),4550

FR-119680

Chemical Name: 4-[1-(6,6-Dimethyl-6H-dibenzo[b,d]pyran-3-ylmethyl)-1H-indol-3-yl]butyric acid
CAS No. 219566-51-5
项目整合开发状态: Preclinical
项目研究机构: Fujisawa (Originator)
合成路线:Cyclization of m-...
参考文献标题:(1-Benzylindole-3-yl)-alkanoic acids; novel nonsteroidal inhibitors of steroid 5alpha-reductase (I)
文献作者:Sawada,K.; Hirai,H.; Golden,P.; Okada,S.; Sawada,Y.; Hashimoto,M.; Tanaka,H.
参考来源:Chem Pharm Bull 1998,46(11),1683

新产品编号:82773

Chemical Name: 4-[3,5-Bis(trifluoromethyl)benzyloxymethyl]-1-(2-methyl-5-thiazolylmethyl)-4-phenylpiperidine dihydrochloride
CAS No. 160377-16-2, 160376-22-7 (free base)
项目整合开发状态: Preclinical 参考文献标题:4-Arylmethyloxymethyl piperidines as tachykinin antagonists
文献作者:Harrison,T.; Mcleod,A.M.; Stevenson,G.I.; Williams,B.J.(Merck Sharp & Dohme Ltd.)
参考来源:EP 0666856; JP 1996502510; US 5620989; WO 9410165

新产品编号:392845

Chemical Name: Bis(3,3-dimethylglutaric acid) 3beta,28-dihydroxylup-20(29)-en-3,28-diyl diester ; [1R(1alpha,3aalpha,5aalpha,5bbeta,7aalpha,9beta,11aalpha,11balpha,13abeta,13balpha)]-3a-(Hydroxymethyl...
参考文献标题:Acylated betulin and dihydrobetulin derivs.,preparation thereof and use thereof
文献作者:Sun,I.-C.; Cosentino,L.M.; Lee,K.-H.; Wang,H.-K.(BBI Biotech Research Laboratories,Inc.; University of North Carolina)
参考来源:US 6172110

新产品编号:435559

Chemical Name: 2-(1-Acetoxyethyl)-4,8-dihydrobenzo[1,2-b:4,5-b']dithiophene-4,8-dione
CAS No. 215371-58-7
项目整合开发状态: Biological Testing
项目研究机构: China Medical College (Originator), National Ins...
参考文献标题:Synthesis and cytotoxicity of 2-acetyl-4,8-dihydrobenzodithiophene-4,8-dione derivatives
文献作者:Chao,Y.-H.; Kuo,S.-C.; Wu,C.-H.; Lee,C.-Y.; Mauger,A.; Sun,I.-C.; Morris-Natschke,S.L.; Lee,K.-H.
参考来源:J Med Chem 1998,41(23),4658

KW-7158

Chemical Name: 3,3,3-Trifluoro-2-hydroxy-2-methyl-N-(10-oxo-4,10-dihydrothieno[3,2-c][1]benzothiepin-9-yl)propanamide 5,5-dioxide
CAS No. 214763-95-8
项目整合开发状态: Phase II
项目研究机构: Kyowa Hakko (O...
参考文献标题:Preparation method of tricyclic cpds.
文献作者:Mimura,T.; Ogasa,T.; Mori,S.; Matsushita,T.; Imai,E.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:JP 2002053580