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

MASTPROM, WHI-P154

2-溴-4-(6,7-二甲氧基喹唑啉-4-基氨基)苯酚Chemical Name: 4-(3-Bromo-4-hydroxyphenylamino)-6,7-dimethoxyquinazoline; 2-Bromo-4-(6,7-dimethoxyquinazolin-4-ylamino)phenol
CAS No. 211555-04-3
项目整合开发状态: Preclinical...
参考文献标题:Quinazolines for treating brain tumor
文献作者:Liu,X.-P.; Narla,R.K.; Uckun,F.M.(Parker Hughes Institute)
参考来源:WO 9961428

Dermofural, G1

2-溴-5-[(E)-2-溴-2-硝基乙烯基]呋喃Chemical Name: 2-Bromo-5-(2-bromo-2-nitrovinyl)furan
CAS No. 35950-55-1
项目整合开发状态: Phase II
项目研究机构: Universidad Central de Las Villas (Originator), YM BioSciences (Lic...
参考文献标题:Preparation of 2-bromo-5-(2-bromo-2-nitrovinyl)-furan and its use as microcide
文献作者:Lugo Farinas,E.; Goizueta Dominguez,R.D.; Gonz鄉ez Garcia,O.; Martinez del Pino,A.R.; Castanedo Cancio,N.R.; Delgado Lasval,M.S.; Zarraluqui,O.N.; Gonz鄉ez Feitot,J.; P鑢ez Donato,J.A.; et al.(Universidad Central de Las Villas)
参考来源:EP 0678516

D-43787

2-甲基-2-丙基2-({2-[(6-{[(苄氧基)羰基]氨基}-1-甲氧基-1-氧代-2-己烷基)氨基甲酰]-2,3-二氢-1H-吲哚-1-基}羰基)-1-吲哚啉羧酸酯Chemical Name: Nepsilon-(Benzyloxycarbonyl)-Nalpha-[1-[1-(tert-butoxycarbonyl)indolin-2(S)-ylcarbonyl]indolin-2(S)-...
参考文献标题:Specific immunophilin ligands as antiasthmatics and immunosuppressants
文献作者:Reichert,D.; Kutscher,B.; Bang,H.; Brune,K.; Quinkert,G.; Schaible,H.-G.(Asta Medica AG)
参考来源:DE 19616509; EP 0896580; JP 2000500776; WO 9741148

KC-764

2-甲基-3-(1,4,5,6-四氢烟酰)吡唑并[1,5-a]吡啶Chemical Name: 2-Methyl-3-(1,4,5,6-tetrahydronicotinoyl)pyrazolo[1,5-a]pyridine; (2-Methylpyrazolo[1,5-a]pyridin-3-yl)(1,4,5,6-tetrahydro-3-pyridyl)methanone; 2-Methyl...
参考文献标题:Indolalkylamines,pharmaceutical compsns.containing them and process for their preparation
文献作者:Hausberg,H.-H.; Koppe,V.; Poetsch,E.; Saiko,O.; Seyfried,C.(Merck Patent GmbH)
参考来源:EP 0007399

Lusaperidone, R-107474

2-甲基-3-[2-(1,2,3,4-四氢苯并呋喃并[3,2-c]吡啶-2-基)乙基]-4H-吡啶并[1,2-A]嘧啶-4-酮Chemical Name: 2-Methyl-3-[2-(1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridin-2-yl)ethyl]-4H-pyrido[1,2-a]pyrimidin-4-one
CAS No. 214548-46-...
参考文献标题:1,2,3,4-Tetrahydro-benzofuro[3,2-c]pyridine derivs.
文献作者:Bischoff,F.P.; Kennis,L.E.J.; Love,C.J.(Janssen Pharmaceutica NV)
参考来源:EP 1019408; JP 2000505115; WO 9845297

SIB-1893

2-甲基-6-(2-苯乙烯基)吡啶Chemical Name: 2-Methyl-6-[(E)-2-phenylethenyl]pyridine
CAS No. 6266-99-5
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Originator), Novartis (Originator)
合成路线:The title comp...
参考文献标题:Pyridine derivs.
文献作者:Endorn,R.; Veli鏴lebi,G.; Cosford,N.D.; Allgeier,H.; Kuhn,R.; Varney,M.A.; Biollaz,M.; Auberson,Y.; Gasparini,F.; Johnson,E.C.(Novartis AG; SIBIA Neurosciences,Inc.)
参考来源:WO 9902497

Sch-28080

2-甲基-8-(苯基甲氧基)咪唑并[1,2-a]吡啶-3-乙腈Chemical Name: 2-Methyl-8-benzyloxyimidazo[1,2-a]pyridine-3-acetonitrile; 2-Methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile
CAS No. 76081-98-6
项目整合开发...
参考文献标题:SCH-28,080
文献作者:Hillier,K.; Serradell,M.N.; Castar,J.; Blancafort,P.
参考来源:Drugs Fut 1982,7(10),755

NU-1025

2-甲基-8-羟基-4-喹唑啉酮Chemical Name: 8-Hydroxy-2-methylquinazolin-4(3H)-one
CAS No. 90417-38-2
项目整合开发状态: Preclinical
项目研究机构: Agouron (Originator), Cancer Research UK (Originator), University of New...
参考文献标题:Resistance-modifying agents.5.Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP)
文献作者:Griffin,R.J.; Srinivasan,S.; Bowman,K.; Calvert,A.H.; Curtin,N.J.; Newell,D.R.; Pemberton,L.C.; Golding,B.T.
参考来源:J Med Chem 1998,41(26),5247

Ibuprofen guaiacol ester, AF-2259, Benflogin

2-甲氧基-2-(4-异丁基苯基)丙酸苯酯Chemical Name: 2-Methoxyphenyl alpha-methyl-4-(isobutyl)phenylacetate; alpha-Methyl-4-(2-methylpropyl)benzeneacetic acid 2-methoxyphenyl ester
CAS No. 66332-77-2
项目整合开发状态: L...
参考文献标题:Guaiacol p-isobutyl hydratropate
文献作者:Baiochi,L.; Silvestrini,B.(ACRAF SpA)
参考来源:DE 2726435; FR 2357526; GB 1538636; JP 53025536; US 4134989

2-Methoxyestradiol, NSC-659853, 2-ME, 2ME2, Panzem

2-甲氧基雌二醇Chemical Name: 2-Methoxyestra-1,3,5(10)-triene-3,17beta-diol
CAS No. 362-07-2
项目整合开发状态: Phase II
项目研究机构: Tetrionics (Supplier), EntreMed (Orphan Drug), Children's Hospital of Boston (...
参考文献标题:Methods of obtaining 2-methoxyestradiol of high purity
文献作者:Shah,J.H.; Agoston,G.E.; Treston,A.M.(EntreMed,Inc.)
参考来源:WO 0114405