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

Dazoxiben hydrochloride, UK-37248-01

4-(2-咪唑-1-基乙氧基)苯甲酸盐酸盐达唑氧苯 Chemical Name: 4-[2-(1H-Imidazol-1-yl)ethoxy]benzoic acid monohydrochloride; 1-[2-(4-Carboxyphenoxy)ethyl]imidazole monohydrochloride
CAS No. 74226-22-5, 78218-09-4 (free...
参考文献标题:UK-37,248-01
文献作者:Sneddon,J.; Castar,J.
参考来源:Drugs Fut 1981,6(11),693

AA-10026, AA-10025, DDP-225, AA-10021, MCI-225

4-(2-氟苯基)-6-甲基-2-哌嗪-1-基噻吩并[2,3-d]嘧啶Chemical Name: 4-(2-Fluorophenyl)-6-methyl-2-piperazinothieno[2,3-d]pyrimidine hydrochloride hydrate
CAS No. 135991-48-9, 109348-38-1 (anhydrous), 99487-25-9 (anh...
参考文献标题:Thieno[2,3-d]pyrimidine derivs.And salts thereof
文献作者:Ninomiya,K.; Nitta,I.; Tobe,A.; Egawa,M.; Kikumoto,R.(Mitsubishi Chemical Corp.)
参考来源:EP 0150469; JP 1985146891

SSR-125543A

4-(2-氯-4-甲氧基-5-甲基苯基)-N-[2-环丙基-1(S)-(3-氟-4-甲基苯基)乙基]-5-甲基-N-(2-丙烯基)噻唑-2-盐酸胺Chemical Name: 4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[2-cyclopropyl-1(S)-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-(2-propyn...
参考文献标题:Aminothiazole derivs.and their use as CRF receptor ligands
文献作者:Roger,P.; Gully,D.; Pradines,A.; Fontaine,E.; Geslin,M.(Sanofi-Synthabo)
参考来源:EP 1200419; FR 2796380; JP 2003505380; WO 0105776

BAY-R-3401

4-(2-氯苯基)-1-乙基-2-甲基-5-羰基-1,4,5,7-四氢呋喃并[3,4-B]吡啶-3-羧酸异丙基酯Chemical Name: (?-4-(2-Chlorophenyl)-1-ethyl-2-methyl-5-oxo-1,4,5,7-tetrahydrofuro[3,4-b]pyridine-3-carboxylic acid isopropyl ester
CAS No. 1...
参考文献标题:1-Alkyl-substd.1,4-dihydropyridine lactones,process for their preparation and their use in pharmaceuticals
文献作者:Puls,W.; Bossert,F.; Petzinna,D.; Schlossmann,K.; Goldmann,S.; Bischoff,H.(Bayer AG)
参考来源:DE 3410645; EP 0158138; ES 8607309; ES 8702413; ES 8702414; ES 8702415; ES 8702416; ES 8702417; ES 8702418; ES 8704173; ES 8704174; US 5026714

SC-299

4-(2-甲基-4-苯基-1,3-恶唑-5-基)苯磺酰胺Chemical Name: 4-(2-Methyl-4-phenyloxazol-5-yl)benzenesulfonamide
CAS No. 93014-16-5
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:Chlorosulfonation of...
参考文献标题:Substd.oxazoles for the treatment of inflammation
文献作者:Talley,J.J.; Bertenshaw,S.; Rogier,D.J.Jr.; Graneto,M.; Brown,D.L.; Devadas,B.; Hwang-Fun,L.; Sikorski,J.A.(Pharmacia Corp.)
参考来源:EP 0825989; JP 1999509835; WO 9636617

CP-93318

4-(2-甲氧基苯基)-2-[(5-甲基-1H-咪唑-4-基)甲基]-1,3-噻唑Chemical Name: 4-(2-Methoxyphenyl)-2-[4(5)-methyl-5(4)-imidazolylmethyl]thiazole
CAS No. 129486-32-4, 130096-16-1 (tritiated analog)
项目整合开发状态: Preclinica...
参考文献标题:Synthesis,in vitro binding profile,and central nervous system penetrability of the highly potent 5-HT3 receptor antagonist [3H]-4-(2-methoxyphenyl)-2-[4(5)-methyl-5(4)-imidazolylmethyl]thiazole
文献作者:Guarino,K.J.; Furman,J.; Rosen,T.; Chalabi,P.M.; Ives,J.L.; Windels,J.H.; McLean,S.; Nagel,A.A.; Bryce,D.; Seeger,T.F.; Roth,R.W.
参考来源:J Med Chem 1990,33(11),3020-3

Actiketal, RK-441S

4-(2-羟基-5,7-二甲基-3-氧代-1-苯并呋喃-2-基)哌啶-2,6-二酮Chemical Name: 4-(2-Hydroxy-5,7-dimethyl-3-oxo-2,3-dihydrobenzofuran-2-yl)piperidine-2,6-dione
CAS No. 133658-47-6
项目整合开发状态: Biological Testing
项目研究机构...
参考文献标题:Synthesis of actiketal,a glutarimide antibiotic
文献作者:Kiyota,H.; et al.
参考来源:Tetrahedron Lett 2000,41(31),5887

CB-10-277(free acid), DM-COOK

4-(3,3-二甲基三氮烯-1-基)苯甲酸钾盐Chemical Name: 4-(3,3-Dimethyl-1-triazenyl)benzoic acid potassium salt; p-(3,3-Dimethyl-1-triazeno)benzoic acid potassium salt
CAS No. 70055-49-1
项目整合开发状态: Phase II
项目研...
参考文献标题:DM-COOK
文献作者:Giraldi,T.
参考来源:Drugs Fut 1984,9(7),503

CL-329167

4(3H)-喽喴唑酮,2-丁基-6-(1-甲氧基-1-甲基乙基)-3-[[2'-(2H-四唑-5-基)[1,1'-双苯基]-4-基]甲基]-Chemical Name: 2-Butyl-6-(1-methoxy-1-methylethyl)-3-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]quinazolin-4(3H)-one
CAS No. 143...
参考文献标题:2,3,6-Substituted quinazolinones as angiotensin II receptor antagonists
文献作者:Levin,J.I.; Chen,P.S.; Porter,R.S.
参考来源:Drugs Fut 1995,20(1),55

L-757793

4-(3-己基脲基)-N-[4-[2-[2(R)-羟基-2-(3-吡啶基)乙胺基]乙基]苯基]苯磺酰胺Chemical Name: 4-(3-Hexylureido)-N-[4-[2-[2(R)-hydroxy-2-(3-pyridinyl)ethylamino]ethyl]phenyl]benzenesulfonamide
CAS No. 173901-42-3, 173900-70-4 ...
参考文献标题:Substd.sulfonamides as selective beta3 agonists for the treatment of diabetes and obesity
文献作者:Fisher,M.H.; Naylor,E.M.; Ok,D.; Weber,A.E.; Shih,T.; Ok,H.(Merck & Co.,Inc.)
参考来源:EP 0757674; JP 1997512275; US 5541197; US 5561142; WO 9529159