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

CRA-0316

Chemical Name: 1-[7-[2,6-Dibromo-4-(trifluoromethyl)phenyl]-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-1,2,3,6-tetrahydropyridine-4-carboxamide
CAS No. 291538-79-9
项目整合开发状态: Preclinical 参考文献标题:Carbamoyl tetrahydropyridine derivs.
文献作者:Tomisawa,K.; Kumagai,T.; Nakazato,A.; Okubo,T.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 1176146

LY-344545

Chemical Name: 2(S)-Amino-2-[2(R)-carboxy-1(R)-cyclopropyl]-3-(9H-xanthen-9-yl)propionic acid
CAS No. 201851-20-9
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator)
合成路线:Partial hydro...
参考文献标题:Excitatory amino acid receptor antagonists
文献作者:Arnold,M.B.; Bleisch,T.J.; Helton,D.R.; Kallman,M.J.; Ornstein,P.L.; Schoepp,D.D.; Tizzano,J.P.(Eli Lilly and Company)
参考来源:EP 0771196; JP 1998505597; US 5717109; WO 9607405

ONO-8815

Chemical Name: 9-Chloro-9,15-dideoxy-16(S)-(1-ethylcyclobutyl)-16-hydroxy-17,18,19,20-tetranorprostaglandin F2beta
CAS No. 212311-08-5
项目整合开发状态: Preclinical
项目研究机构: Ono (Originator)
合成路线:P...
参考文献标题:Omega-cycloalkyl-prostaglandin E2 derivs.
文献作者:Ohuchida,S.; Tani,K.(Ono Pharmaceutical Co.,Ltd.)
参考来源:EP 0860430; JP 1999193268; JP 2000128858; US 6110969

TQX-173

Chemical Name: 7-Chloro-4-oxo-8-(4H-1,2,4-triazol-4-yl)-4,5-dihydro[1,2,4]triazolo[1,5-a]quinoxaline-2-carboxylic acid
CAS No. 308137-55-5
项目整合开发状态: Biological Testing
项目研究机构: Universit?degli...
参考文献标题:7-Chloro-4,5-dihydro-8-(1,2,4-triazol-4-yl)-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates as novel highly selective AMPA receptor antagonists
文献作者:Catarzi,D.; Colotta,V.; Varano,F.; Cecchi,L.; Filacchioni,G.; Galli,A.; Costagli,C.; Carl? V.
参考来源:J Med Chem 2000,43(21),3824

ORG-25435

Chemical Name: 2(R)-[N,N-Bis(2-methoxyethyl)amino]butyric acid 4-methyl-2,6-dimethoxyphenyl ester hydrobromide
CAS No. 256456-73-2 ((R)-isomer, free base), 256456-45-8 (free base)
项目整合开发状态: Phas...
参考文献标题:alpha-Amino acid phenyl ester derivs.
文献作者:Hamilton,N.M.(Akzo Nobel N.V.)
参考来源:EP 1098871; WO 0005196

ER-803022

Chemical Name: 1,3-Bis[2-[[3-[3(R)-(dodecanoyloxy)decyloxy]-2(R)-tetradecanamidopropoxy](hydroxy)phosphoryloxy]ethyl]urea disodium salt; Bis(dodecanoic acid) 1,27-diheptyl-9,19-dihydroxy-9,14,19-triox...
参考文献标题:Immunological adjuvant cpd.
文献作者:Rossignol,D.P.; Ishizaka,S.T.; Nault,A.; Lewis,M.; Rose,J.; McGuiness,P.; Hawkins,L.D.(Eisai Co.,Ltd.)
参考来源:EP 1147117; US 6290973; WO 0044758

VX-148

Chemical Name: N-[1(S)-[3-[3-(4-Cyano-3-methoxyphenyl)ureido]phenyl]ethyl]carbamic acid 1(R)-(cyanomethyl)propyl ester
CAS No. 297730-04-2
项目整合开发状态: Phase II
项目研究机构: Vertex (Originator)
合成...
参考文献标题:Inhibitors of IMPDH enzyme
文献作者:Saunders,J.; Bethiel,S.; Badia,M.; Stamos,D.; Trudeau,M.(Vertex Pharmaceuticals Inc.)
参考来源:WO 0056331

新产品编号:767779

Chemical Name: 1-[9-(3-Chloro-4-methoxybenzylamino)-3-ethyl-3H-pyrazolo[4',3':5,6]pyrido[3,4-d]pyridazin-6-yl]-N-methyl-1H-imidazole-4-carboxamide
CAS No. 296250-53-8, 296250-55-0 (hydrobromide), 2...
参考文献标题:Fused pyridopyridazine inhibitors of cGMP phosphodiesterase
文献作者:Kim,S.; Wang,Y.; Yu,G.; Macor,J.; Chung,H.-J.; Humora,M.; Katipally,K.(Bristol-Myers Squibb Co.)
参考来源:EP 1165521; JP 2002540102; US 6316438; WO 0056719

APCP-363, APO-363

Chemical Name: 3-Hydroxy-2-(1-methoxyethyl)-1,6-dimethyl-1,4-dihydropyridin-4-one
CAS No. 216581-37-2 (hydrochloride)
项目整合开发状态: Preclinical
项目研究机构: BTG (Originator), Apotex (Licensee)
合成路线...
参考文献标题:Novel orally active iron (III) chelators
文献作者:Tilbrook,G.S.; Hider,R.C.; Liu,Z.(BTG International Ltd.)
参考来源:WO 9854138

CJ-13610

Chemical Name: 4-[3-Fluoro-5-[4-(2-methyl-1H-imidazol-1-yl)phenylsulfanyl]phenyl]tetrahydro-2H-pyran-4-carboxamide hydrochloride
CAS No. 179420-35-0
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Orig...
参考文献标题:5-Lipoxygenase inhibitors
文献作者:Stevens,R.W.; Mano,T.; Nakao,K.; Okumura,Y.(Pfizer Inc.)
参考来源:EP 0787127; JP 1999507322; US 5883106; WO 9611911