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

DB-51808

Chemical Name: N,N'-Bis[2-[2-[6-chloro-1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl]ethylamino]ethyl]-5-[1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl]isophthalamide
CAS No. 254452-58-9 (diHCl)
项目整合开...
参考文献标题:Naphthalimidobenzamide derivs.
文献作者:Suzuki,K.; Yamada,Y.; Asao,T.; Noguchi,K.; Wakida,M.(Taiho Pharmaceutical Co.,Ltd.)
参考来源:EP 1020446; US 6300331; WO 0001672

BILS-179 BS

Chemical Name: N-[N-[4-(2-Aminothiazol-4-yl)phenyl]carbamoylmethyl]-N-[1(S)-phenylethyl]pyridine-4-carboxamide
CAS No. 193346-73-5
项目整合开发状态: Preclinical
项目研究机构: Boehringer Ingelheim (Originat...
参考文献标题:Phenyl thiazole derivs.with anti-herpes virus properties
文献作者:Hargrave,K.D.; Simoneau,B.; Faucher,A.-M.; Thavonekham,B.; Grygon,C.A.; Crute,J.J.(Boehringer Ingelheim (Canada) Ltd.; Boehringer Ingelheim Pharmaceuticals Inc.)
参考来源:EP 0871619; JP 2000502702; US 6057451; WO 9724343

新产品编号:723483

Chemical Name: N2-[3-Methoxy-4-(5-oxazolyl)phenyl]-6-phenyl-N4-[2-(3-pyridyl)ethyl]-1,3,5-triazine-2,4-diamine
CAS No. 267646-31-1
项目整合开发状态: Biological Testing
项目研究机构: Bristol-Myers Squibb (O...
参考文献标题:Cpds.derived from an amine nucleus that are inhibitors of IMPDH enzyme
文献作者:Liu,C.; Leftheris,K.; Pitts,W.J.; Iwanowicz,E.J.; Dhar,T.G.M.; Gu,H.H.(Bristol-Myers Squibb Co.)
参考来源:EP 1126843; US 6399773; WO 0025780

新产品编号:869027

Chemical Name: 3-(3,5-Dichlorophenyl)-3-[5-oxo-1-[3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)phenyl]pyrrolidin-3-ylcarboxamido]propionic acid
CAS No. 345296-69-7, 345296-70-0 (trifluoroacetate)
项目...
参考文献标题:1-(Aminophenyl)-2-pyrrolidones as integrin inhibitors
文献作者:Dominguez,C.; Chen,G.; Liu,L.; Liu,Q.; Han,N.; Xi,N.; Xu,S.; Huang,Q.; Siegmund,A.; Handley,M.; Kiselyov,A.S.(Amgen Inc.)
参考来源:EP 1240158; US 2002019402; WO 0144230

新产品编号:873773

Chemical Name: 3-[6-(1H-Imidazol-1-yl)-1-methyl-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
CAS No. 346584-32-5
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator)
合成路线:Thi...
参考文献标题:Substd.pyrroles
文献作者:Lovey,A.J.; Fotouhi,N.; Kong,N.(F.Hoffmann-La Roche AG)
参考来源:WO 0146178

新产品编号:756705

Chemical Name: Phosphoric acid 2(R)-(3-methoxyphenyl)-1(S)-methyl-2-(octanamido)ethyl monoester disodium salt; N-[1(R)-(3-Methoxyphenyl)-2(S)-phosphonoxypropyl]octanamide disodium salt
CAS No. 2890...
参考文献标题:Drugs containing phosphoric acid derivs.as the active ingredient
文献作者:Matsui,T.; Ohmawari,N.(Ono Pharmaceutical Co.,Ltd.)
参考来源:EP 1156054; US 6495533; WO 0050429

新产品编号:888011

Chemical Name: 3,5-Dibenzoyl-4-(3-chlorophenyl)-2,6-dimethyl-1,4-dihydropyridine; [4-(3-Chlorophenyl)-2,6-dimethyl-1,4-dihydro-3,5-pyridinediyl]bis(phenylmethanone)
CAS No. 359764-00-4
项目整合开发状态:...
参考文献标题:3,5-Dibenzoyl-1,4-dihydropyridines: Synthesis and MDR reversal in tumor cells
文献作者:Kawase,M.; Shah,A.; Gaveriya,H.; Motohashi,N.; Sakagami,H.; Varga,A.; Molnar,J.
参考来源:Bioorg Med Chem 2002,10(4),1051

新产品编号:799419

Chemical Name: 3(R)-[1-(3,5-Dichlorophenylsulfonyl)azetidin-2(S)-ylcarboxamido]-3-(4-methoxyphenyl)propionic acid
CAS No. 309976-72-5
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Originator) 参考文献标题:Substd.beta-alanine derivs.as cell adhesion inhibitors
文献作者:Hagmann,W.K.; Durette,P.L.; Mumford,R.A.; Kopka,I.E.; Mills,S.G.; MacCoss,M.; Magriotis,P.A.(Merck & Co.,Inc.)
参考来源:WO 0071572

新产品编号:452961

Chemical Name: N-(3,5-Dichlorophenylsulfonyl)-2-methyl-L-prolyl-L-phenylalanine
CAS No. 217452-76-1
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Originator)
合成路线:N-Boc-L-Phenylalanine (I) is...
参考文献标题:Heterocyclic amide cpds.as cell adhesion inhibitors
文献作者:Hagmann,W.K.; Durette,P.L.; Mumford,R.A.; Mills,S.G.; Kevin,N.J.; Schmidt,J.A.; MacCoss,M.; Van Riper,G.M.(Merck & Co.,Inc.)
参考来源:EP 1001764; WO 9853814

新产品编号:364369

Chemical Name: (-)-1-[2(S)-[3-(2,3-Dihydro-1H-inden-2-yloxy)-4-methoxyphenyl]propyl]-2,3-dihydro-1H-imidazol-2-ylidenecyanamide
CAS No. 205699-43-0 (undefined stereochem.)
项目整合开发状态: Preclinical<...
参考文献标题:PDE IV inhibiting 2-cyanoiminoimidazole derivs.
文献作者:Freyne,E.J.E.; Fernandez-Gadea,F.J.; Andres-Gil,J.I.(Janssen Pharmaceutica NV)
参考来源:WO 9814432