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

NNC-53-0002

Chemical Name: 5'-O-Acetyl-2-chloro-N6-methoxyadenosine
CAS No. 202212-20-2
项目整合开发状态: Preclinical
项目研究机构: Novo Nordisk (Originator)
合成路线:The reaction of 2,6-dichloro-9-(2',3',5'-tri-O-acet...
参考文献标题:Novel N-alkoxyadenine derivs.acting as cytokine inhibitors
文献作者:Knutsen,L.; Olsen,U.B.; Roberts,S.M.; Varley,D.R.; Bowler,A.N.(Novo Nordisk A/S)
参考来源:WO 9801459

KCO-616, WAY-151616

Chemical Name: 3-(2,4-Dichloro-6-methylbenzylamino)-4-(1,1-dimethylpropylamino)-3-cyclobutene-1,2-dione
CAS No. 202520-55-6
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

DMAMI

Chemical Name: N-(3,5-Dimethyladamantan-1-yl)maleimide; 1-(3,5-Dimethyladamantan-1-yl)-2,5-dihydro-1H-pyrrole-2,5-dione
CAS No. 219135-20-3
项目整合开发状态: Preclinical
项目研究机构: National Taipei Colle...
参考文献标题:In vitro and in vivo growth inhibition of cancer cells by adamantylmaleimide derivatives
文献作者:Wang,J.J.; Chern,Y.-T.; Liu,T.-Y.; Chi,C.-W.
参考来源:Anti-Cancer Drug Des 1998,13(7),779

T-82

Chemical Name: 2-[2-(1-Benzylpiperidin-4-yl)ethyl]-9-methoxy-2,3-dihydro-1H-pyrrolo[3,4-b]quinolin-1-one hemifumarate
CAS No. 142471-56-5 (free base)
项目整合开发状态: Phase II
项目研究机构: SSP (Originato...
参考文献标题:Quinoline derivs.
文献作者:Hasegawa,H.; Isomae,K.; Kotsugai,T.; Shioiri,N.; Sekine,K.; Taido,N.; Sato,S.; Kuraishi,T.(SSP Co.,Ltd.)
参考来源:EP 0481429; JP 1993009188; JP 1993279355; US 5190951; US 5240934; US 5300517

SWR-0315Na(oxalate salt), SWR-0342SA

Chemical Name: 2-[4-[1-[2-[2(S)-Hydroxy-3-phenoxypropylamino]ethyl]-1(Z)-propenyl]phenoxy]acetic acid oxalate; (Z)-2-[4-[1-Ethylidene-3-[2(S)-hydroxy-3-phenoxypropylamino]propyl]phenoxy]acetic acid ox...
参考文献标题:Phenoxyacetic acid derivative
文献作者:Totani,H.; Masagaki,T.; Kakita,T.; Sawada,K.; Otsubo,Y.; Kiso,T.; Namikawa,T.(Sawai Pharmaceutical Co.,Ltd.)
参考来源:JP 11035534

KV-2920

Chemical Name: N-(1-Decyl-4,6-dimethyl-2,3-dihydro-1H-indol-7-yl)-2,2-dimethylpropionamide hydrochloride
CAS No. 288462-23-7 (free base)
项目整合开发状态: Preclinical
项目研究机构: Kyoto Pharmaceutical (Or...
参考文献标题:Bioavailable acyl-CoA: Cholesterol acyltransferase inhibitor with anti-peroxidative activity: Synthesis and biological activity of novel indolinyl amide and urea derivatives
文献作者:Kamiya,S.; Shirahase,H.; Yoshimi,A.; Nakamura,S.; Kanda,M.; Matsui,H.; Kasai,M.; Takahashi,K.; Kurahashi,K.
参考来源:Chem Pharm Bull 2000,48(6),817

XU-817

Chemical Name: 1-[2-(4-Benzylpiperidin-1-yl)-2-oxoethyl]-1H-indole-5-carboxamidine
CAS No. 202123-75-9
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:The alkylation o...
参考文献标题:Amidinoindoles,amidinoazoles,and analogs thereof as inhibitors of factor Xa and of thrombin
文献作者:Dominguez,C.; Han,Q.; Duffy,D.E.; Park,J.M.; Quan,M.L.; Rossi,K.A.; Wexler,R.R.(DuPont Pharmaceuticals Co.)
参考来源:EP 0960102; WO 9801428

G-20002, VN/87-1

Chemical Name: 3beta-Hydroxy-17-(1H-1,2,3-triazol-1-yl)androsta-5,16-diene
CAS No. 203503-62-2
项目整合开发状态: Preclinical
项目研究机构: University of Maryland (Originator), Genta (Codevelopment)
合成路线...
参考文献标题:17-Azolyl steroids useful as androgen synthesis inhibitors
文献作者:Brodie,A.; Njar,V.C.O.(University of Maryland)
参考来源:US 5994335

VN/108-1

Chemical Name: 17-(1H-Imidazol-1-yl)androsta-4,16-dien-3-one
CAS No. 203503-73-5
项目整合开发状态: Preclinical
项目研究机构: University of Maryland (Originator)
合成路线:The Vilsmeier-Haack reaction of 3-be...
参考文献标题:Novel 17-azolyl steroids,potent inhibitors of human cytochrome 17alpha-hydroxylase-C17,20-lyase (P45017alpha): Potential agents for the treatment of prostate cancer
文献作者:Njar,V.C.O.; Kato,K.; Nnane,I.P.; Grigoryev,D.N.; Long,B.J.; Brodie,A.M.H.
参考来源:J Med Chem 1998,41(6),902

G-20001, VN/85-1

Chemical Name: 17-(1H-1,2,3-triazol-1-yl)androsta-4,16-dien-3-one
CAS No. 203503-75-7
项目整合开发状态: Preclinical
项目研究机构: University of Maryland (Originator), Genta (Codevelopment)
合成路线:The Vils...
参考文献标题:Novel 17-azolyl steroids,potent inhibitors of human cytochrome 17alpha-hydroxylase-C17,20-lyase (P45017alpha): Potential agents for the treatment of prostate cancer
文献作者:Njar,V.C.O.; Kato,K.; Nnane,I.P.; Grigoryev,D.N.; Long,B.J.; Brodie,A.M.H.
参考来源:J Med Chem 1998,41(6),902