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

RS-1653

Chemical Name: 2-(4-Fluoro-7-methyl-1,2-benzisoxazol-3-yloxy)ethanamine hydrochloride
CAS No. 178746-70-8, 178746-69-5 (free base)
项目整合开发状态: Preclinical
项目研究机构: Sankyo (Originator)
合成路线:Me...
参考文献标题:Isoxazoles
文献作者:Kojima,K.; Aizawa,Y.; Kaneko,I.; Sakai,J.; Kozuka,M.; Koyama,K.; Samata,N.; Yoshimi,K.(Sankyo Co.,Ltd.)
参考来源:EP 0779281; JP 1997059264; US 5965591; US 6096771; WO 9606837

新产品编号:207751

Chemical Name: N6-Cyclopropyl-2',3'-didehydro-2',3'-dideoxyadenosine
CAS No. 188525-24-8
项目整合开发状态: Biological Testing
项目研究机构: University of Georgia (Originator), Yale University (Originator)<...
参考文献标题:Novel use of a guanosine prodrug approach to convert 2',3'-didehydro-2',3'-dideoxyguanosine into a viable antiviral agent
文献作者:Ray,A.S.; Yang,Z.; Chu,C.K.; Anderson,K.S.
参考来源:Antimicrob Agents Chemother 2002,46(3),887

新产品编号:108085

Chemical Name: N-[2-[1-[2-(4-Chlorophenoxy)-2-methylpropyl]piperidin-4-yl]-2-methylpropyl]-N,N-dimethylamine difumarate
CAS No. 167710-61-4 (free base), 167710-62-5 (monofumarate)
项目整合开发状态: Biol...
参考文献标题:Derivs.of beta,beta-dimethyl-4-piperidineethanamine as inhibitors of the cholesterol biosynthesis
文献作者:Binet,J.; Samreth,S.; De Fornel,D.(Laboratoires Fournier SA)
参考来源:EP 0699187; FR 2705343; JP 1996510726; US 5614534; WO 9426713

新产品编号:215661

Chemical Name: (6aR,7S,9aS,13aS)-5-Hydroxy-6a,7,10,10-tetramethyl-2,3,6,6a,7,8,9,9a,10,11,12,13-dodecahydro-1H-naphtho[1',8'a:5,6]pyrano[2,3-e]isoindol-3,11-dione
CAS No. 189185-70-4
项目整合开发状态: B...
参考文献标题:Sesquiterpene derivs.having antiviral activity
文献作者:Kamigauchi,T.; Fujiwara,T.; Tani,H.; Kawamura,Y.; Horibe,I.(Shionogi & Co.Ltd.)
参考来源:EP 0855398; WO 9711947

新产品编号:819985

Chemical Name: 2,6-(Methanoxy[1,4]benzenomethano[1,4]benzenoxymethano[2,6]naphthalenomethanoxy[1,4]benzenomethano[1,4]benzenoxymethano)naphthalene-12,20,37,45-tetracarboxylic acid
CAS No. 327028-14...
参考文献标题:Use of chemical chelators as reversal agents for drug-induced neuromuscular block
文献作者:Muir,A.W.; Rees,D.; Bom,A.H.A.(Akzo Nobel N.V.)
参考来源:WO 0112202

新产品编号:794673

Chemical Name: 4-(2,4,4-Trimethyl-1,4-dihydro-2H-3,1-benzoxazin-6-yl)thiophene-2-carbonitrile
CAS No. 304857-74-7
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:Addi...
参考文献标题:Quinazolinone and benzoxazine derivs.as progesterone receptor modulators
文献作者:Jones,T.K.; Zhi,L.; Tegley,C.M.; Fensome,A.; Zhang,P.; Terefenko,E.A.; Marschke,K.B.(Ligand Pharmaceuticals,Inc.; Wyeth)
参考来源:EP 1175404; WO 0066560

新产品编号:680769

Chemical Name: N-[2(S)-[5-[2-(2-Azabicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxoethyl]-2-(3,5-dimethylphenyl)-1H-indol-3-yl]propyl]-N-[2-(1H-1,2,3-benzotriazol-5-yl)ethyl]amine
CAS No. 255864-13-2
...
参考文献标题:Antagonists of gonadotropin releasing hormone
文献作者:Chu,L.; Wyvratt,M.J.; Ponpipom,M.M.; Lin,P.; Ashton,W.T.; Goulet,M.; Young,J.; Girotra,N.N.; Fisher,M.H.(Merck & Co.,Inc.)
参考来源:EP 1095038; WO 0004013

新产品编号:573193

Chemical Name: N-[2(E)-[2-Amino-2(E)-(hydroxyimino)ethoxyimino]-3(R)-(3,4-dichlorophenyl)-5-(2-oxo-1,4'-bipiperidin-1'-yl)pentyl]-3,5-dichloro-N-methylbenzamide
CAS No. 226915-84-0 (undefined isome...
参考文献标题:Substd.oximes as neurokinin antagonists
文献作者:Carruthers,N.I.; Alaimo,C.A.; Shih,N.-Y.; Lavey,B.J.; Ting,P.C.; Reichard,G.A.(Schering Corp.)
参考来源:EP 1032561; WO 9926924

新产品编号:886429

Chemical Name: N-(1,3-Benzodioxol-5-ylmethyl)-3-(3,5-difluorophenyl)-N-[3-(perhydroazepin-1-yl)propyl]isoxazol-5-amine
CAS No. 359418-53-4, 359418-52-3 (hydrochloride), 359418-54-5 (trifluoroacetat...
参考文献标题:Isoxazole thrombin receptor antagonists
文献作者:Freidinger,R.M.; Selnick,H.G.; Connolly,T.; Barrow,J.C.; Nantermet,P.G.(Merck & Co.,Inc.)
参考来源:GB 2356198

KCL-1999000269

Chemical Name: (+)-2(S)-[4-Methoxy-3-[N-[4-(trifluoromethyl)benzyl]carbamoyl]benzyl]butyric acid; alpha(S)-Ethyl-4-methoxy-3-[N-[4-(trifluoromethyl)benzyll]carbamoyl]benzenepropanoic acid
CAS No. 3...
参考文献标题:Enantio-dependent binding and transactivation of optically active phenylpropanoic acid derivatives at human peroxisome proliferator-activated receptor alpha
文献作者:Miyachi,H.; Nomura,M.; Tanase,T.; Suzuki,M.; Murakami,K.; Awano,K.
参考来源:Bioorg Med Chem Lett 2002,12(3),333