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

新产品编号:460871

Chemical Name: 5-[1-[4-[6-(2-Chlorophenyl)-1,4-dimethyl-7,8,9,10-tetrahydro-4H-pyrido[4',3':4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-9-ylcarbonylphenyl]-1-(3-pyridyl)methylideneaminooxy]pe...
参考文献标题:Triazolo-1,4-diazepine cpds.and medicinal compsn.containing the same
文献作者:Sano,T.; Seki,T.; Fujita,M.; Inada,H.(Nikken Chemicals Co.,Ltd.)
参考来源:EP 0995752; JP 1999071378; US 6433167; WO 9858930

新产品编号:919651

Chemical Name: 1-[4-(Allyloxycarbonylamino)-5-fluoro-2-oxo-1,2-dihydropyrimidin-1-yl]-1-deoxy-beta-D-ribofuranuronic acid
CAS No. 396684-66-5
项目整合开发状态: Preclinical
项目研究机构: Kolon Industries (O...
参考文献标题:5'-Deoxy-N-(substd.oxycarbonyl)-5-fluorocytosine and derivs.thereof,method of preparing same,and anticancer compsn.comprising same as active ingredients
文献作者:Lee,K.-H.; Kim,J.-Y.; Kim,Y.-C.; Kim,K.-H.; Park,H.-J.; Noh,M.-J.; Park,Y.-S.; Cho,S.-M.(Kolon Industries,Inc.)
参考来源:WO 0211668

新产品编号:881683

Chemical Name: N-[2(R)-[1(R)-indanyl]-3-sulfanylpropionyl]-L-tryptophan
CAS No. 355016-72-7 (diastereomeric mixture)
项目整合开发状态: Biological Testing
项目研究机构: INSERM (Originator), Servier (Origina...
参考文献标题:Amino acid derivs.and use thereof as NEP,ACE and ECE inhibitors
文献作者:Roques,B.P.; Renard,P.; Scalbert,E.; Bennejean,C.; Fournie-Lazuski,M.-C.; Inguimbert,N.; Poras,H.(ADIR et Cie.; INSERM (Institut National de la Sante et de la Recherche Medicale))
参考来源:FR 2805259; WO 0160822

新产品编号:989259

Chemical Name: 2-Hydroxy-N-(2-hydroxyethyl)-N,N-dimethyl-1-hexadecanaminium bromide
CAS No. 86579-60-4, 126150-49-0 (acetate), 85006-12-8 (cation), 84643-53-8 (chloride), 124591-63-5 (iodide), 8500...
参考文献标题:Process for preparing quaternary ammonium cpds.
文献作者:Rutzen,H.(Henkel KgA)
参考来源:DE 3136628; EP 0075066; JP 1983046043; US 4480126

CT-53608

Chemical Name: N-(4-Isopropoxyphenyl)-4-[6-methoxy-7-[3-(4-morpholinyl)propoxy]quinazolin-4-yl]piperazine-1-carboxamide
CAS No. 401903-53-5
项目整合开发状态: Clinical
项目研究机构: Kyowa Hakko (Originator)...
参考文献标题:Quinazoline derivs.as kinase inhibitors
文献作者:Nomoto,Y.; Scarborough,R.M.; Ichimura,M.; Fujiwara,S.; Ide,S.; Oda,S.; Pandey,A.; Tsukuda,E.; Matsuno,K.; Irie,J.(Kyowa Hakko Kogyo Co.,Ltd.; Millennium Pharmaceuticals,Inc.)
参考来源:WO 0216351

NNC-52-0956

Chemical Name: 2-(Oxaloamino)-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylic acid; N-(3-Carboxy-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl)oxamic acid
CAS No. 243967-42-2, 243966-09-8 (hydro...
参考文献标题:Modulators of protein tyrosine phosphatases
文献作者:Jones,T.K.; Jeppesen,L.; Ripka,W.C.; Andersen,H.S.; Olsen,O.H.; Bakir,F.; Branner,S.; Moller,N.P.H.; Jeppesen,C.B.; Richter,L.S.; Vagner,J.; Iversen,L.F.; Holsworth,D.D.; Axe,F.U.; Ge,Y.; et al.(Novo Nordisk A/S; Ontogen Corp.)
参考来源:WO 9946237

NNC-52-1246

Chemical Name: 7(S)-(5-Hydroxy-1H-indol-2-ylcarboxamidomethyl)-2-(oxaloamino)-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylic acid; N-[3-Carboxy-7(S)-(5-hydroxy-1H-indol-2-ylcarboxamidomethyl)-4,...
参考文献标题:Modulators of protein tyrosine phosphatases (PTPases)
文献作者:Lau,J.; Andersen,H.S.; Newman,M.J.; Hansen,T.K.; Olsen,O.H.; Bakir,F.; Holsworth,D.D.; Axe,F.U.; Ge,Y.; Uyeda,R.T.; Judge,L.M.; Moeller,N.P.H.; Shapira,B.Z.(Novo Nordisk A/S; Ontogen Corp.)
参考来源:WO 0204459

A-318315

Chemical Name: N-[2-(Dimethylamino)acetyl]-1-methyl-N-(3,4,5-trimethoxyphenyl)-1H-indole-5-sulfonamide hydrochloride; N2,N2-Dimethyl-N1-(1-methyl-1H-indol-5-ylsulfonyl)-N1-(3,4,5-trimethoxyphenyl)glyc...
参考文献标题:Cell proliferation inhibitors
文献作者:Barr,K.J.; Steiner,B.A.; Qun,L.; Rosenberg,S.; Sham,H.; Gwaltney,S.L.II; Imade,H.M.; Woods,K.W.(Abbott Laboratories Inc.)
参考来源:WO 0073264

新产品编号:487765

Chemical Name: 3(S)-[5(S)-[2(S)-Amino-4-pentenamido]-2(S),3(R),4(R),6-tetrahydroxyhexanamido]-3-phenylpropionic acid hydrochloride
CAS No. 219813-22-6 (free base)
项目整合开发状态: Biological Testing 参考文献标题:Polyol-amino acid cpds.having anti-Helicobacter pylori activity
文献作者:Akiyama,Y.; Nakano,Y.; Tsubotani,S.; Izawa,M.; Nakao,M.; Miyagawa,K.; Kamiyama,K.; Nishikimi,Y.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0998488; JP 1999080109; WO 9902549

LG-101506

Chemical Name: 7-[3,5-Di-tert-butyl-2-(2,2-difluoroethoxy)phenyl]-3-methyl-2(E),4(E),6(Z)-octatrienoic acid
CAS No. 331248-11-4
项目整合开发状态: Preclinical
项目研究机构: Ligand (Originator)
合成路线:Addit...
参考文献标题:RXR modulators with improved pharmacologic profile
文献作者:Jones,T.K.; Ardecky,R.J.; Boehm,M.F.; Hamann,L.G.; Thompson,A.J.; Michellys,P.-Y.; Tyhonas,J.S.; Faulkner,A.L.; Mapes,C.M.; Chen,J.-H.(Ligand Pharmaceuticals,Inc.)
参考来源:EP 1216221; WO 0119770