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

SRI-8228

6-[2-甲氧基-5-(三氟甲基)苯氨甲基]-5-甲基吡啶[2,3-d]嘧啶-2,4-二胺Chemical Name: 6-[2-Methoxy-5-(trifluoromethyl)phenylaminomethyl]-5-methylpyrido[2,3-d]pyrimidine-2,4-diamine
CAS No. 174654-98-9
项目整合开发状态: Preclinic...
参考文献标题:Lipophilic antifolates as agents against opportunistic infections.1.Agents superior to trimetrexate and piritrexim against Toxoplasma gondii and Pneumocystis carinii in in vitro evaluations
文献作者:Piper,J.R.; Johnson,C.A.; Krauth,C.A.; Carter,R.L.; Hosmer,C.A.; Queener,S.F.; Borotz,S.E.; Pfefferkorn,E.R.
参考来源:J Med Chem 1996,39(6),1271

CI-930

6-[4-(1H-咪唑-1-基)苯基]-5-甲基-4,5-二氢-3(2H)-哒嗪酮Chemical Name: 4,5-Dihydro-6-[4-(1-imidazolyl)phenyl]-5-methyl-3(2H)-pyridazinone
CAS No. 86798-59-6, 90791-23-4 (diHCl)
项目整合开发状态: Phase I
项目研究机构: Pfi...
参考文献标题:Substituted 4,5-dihydro-6-(substituted)phenyl-3(2H)-pyridazinones and 6-(substituted)phenyl-3(2H)-pyridazinones
文献作者:Sircar,I.; Bristol,J.A.(Pfizer Inc.)
参考来源:CA 1190548; DD 208615; EP 0075436

Metesind glucuronate, AG-265(free base), AG-331

6-[N-甲基-N-[4-(吗啉基磺酰基)苄基]氨基苯[cd]吲吲-2(1H)-亚胺葡萄糖醛酸盐Chemical Name: 6-[N-Methyl-N-[4-(morpholinosulfonyl)benzyl]amino]benz[cd]indol-2(1H)-imine glucuronate
CAS No. 157182-23-5, 138384-68-6 (free base) 参考文献标题:Crystal-structure-based design and synthesis of benz[cd]indole-containing inhibitors of thymidylate synthase
文献作者:Varney,M.D.; Marzoni,G.P.; Palmer,C.L.; Deal,J.G.; Webber,S.E.; Welsh,K.M.; Bacquet,R.J.; Bartlett,C.A.; Morse,C.A.; Booth,C.L.; et al.
参考来源:J Med Chem 1992,35(4),663

MRS-1476

6-乙基-5-(乙基磺酰羰基)-2-苯基-4-丙基吡啶-3-羧酸乙酯Chemical Name: 6-Ethyl-5-(ethylsulfanylcarbonyl)-2-phenyl-4-propylpyridine-3-carboxylic acid ethyl ester
CAS No. 212329-36-7
项目整合开发状态: Biological Testing
项目研...
参考文献标题:Structure-activity relationships and molecular mod
文献作者:Li,A.-H.; Moro,S.; Melman,N.; Ji,X.D.; Jacobson,K.A.
参考来源:J Med Chem 1998,41(17),3186

FS-205-397

6-乙氧基-3,3-二甲基-1,2-二氢吲哚甲烷磺酸盐 6-乙氧基-3,3-二甲基-1,2-二氢吲哚 Chemical Name: 6-Ethoxy-3,3-dimethyl-2,3-dihydro-1H-indole methanesulfonate; 6-Ethoxy-3,3-dimethylindoline methanesulfonate
CAS No. 116861-51-9, 8...
参考文献标题:3,3-Dialkyl and 3,3-alkylene-indoline derivs.,process for their preparation and pharmaceutical compsns.Containing them
文献作者:Achini,R.(Novartis Deutschland GmbH)
参考来源:DE 3300522

BW-683C

6-氯-2-(4-氯苯基)色满Chemical Name: 6-Chloro-2-(4-chlorophenyl)-3,4-dihydro-2H-1-benzopyran; 4',6-Dichloroflavan
CAS No. 73110-56-2
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKline (Originator)...
参考文献标题:Flavans,process for their preparation and pharmaceutical compsns.containing them
文献作者:Batchelor,J.F.; Bauer,D.J.; Hodson,H.F.; Selway,J.W.T.; Young,D.A.B.(Glaxo Wellcome plc)
参考来源:EP 0004579

Fenoldopam mesilate, SK&F-82526J, Corlopam

6-氯-2,3,4,5-四氢-1-(4-羟苯基)-1H-3-苯并氮杂卓-7,8-二醇甲磺酸盐非诺多泮单氢溴酸盐芬洛多潘Chemical Name: 6-Chloro-7,8-dihydroxy-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine methanesulfonate; 6-Chloro-1-(4-hydroxyphenyl...
参考文献标题:Benz-tetrasubstituted 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines
文献作者:Weinstock,J.(SmithKline Beecham plc)
参考来源:EP 0004794; JP 54135787; JP 63065663B; US 4171359

SB-215505

6-氯-2,3-二氢-5-甲基-N-5-喹啉基-1H-吲哚-1-甲酰胺Chemical Name: 6-Chloro-5-methyl-N-(5-quinolinyl)-2,3-dihydro-1H-indole-1-carboxamide
CAS No. 162100-15-4
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Ori...
参考文献标题:Indoline derivs.as 5HT2C antagonists
文献作者:Ham,P.; Jones,G.E.; Forbes,I.T.(SmithKline Beecham plc)
参考来源:EP 0707581; JP 1996512299; US 5834494; WO 9501976

FK-803, FR-46171

6-氯-2-吡啶基甲基硝酸酯Chemical Name: 6-Chloro-2-pyridylmethyl nitrate; 6-Chloro-2-pyridinemethanol nitrate ester
CAS No. 90500-72-4
项目整合开发状态: Phase II
项目研究机构: Fujisawa (Originator)
合成路线:By esterif...
参考文献标题:2-Nitroxymethyl and 2,6-bis-nitroxymethyl-pyridine cpds.having vasodilating activity
文献作者:Ueda,I.; Morino,D.; Takimoto,K.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:US 4540701; US 4613608

Tifenazoxide, NN-414

6-氯-3-((1-甲基环丙基)氨基)-4H-噻吩并(3,2-e)-1,2,4-噻二嗪 1,1-二氧化物Chemical Name: 6-Chloro-3-(1-methylcyclopropylamino)-4H-thieno[3,2-e][1,2,4]thiadiazine-1,1-dioxide
CAS No. 279215-43-9
项目整合开发状态: Discontinued...
参考文献标题:Fused 1,2,4-thiadiazine derivs.,their preparation and use
文献作者:Hansen,J.B.; Nielsen,F.E.(Novo Nordisk A/S)
参考来源:EP 1140945; US 6329367; WO 0037474