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

A-420983

N-[4-[4-氨基-1-[转-4-(4-甲基哌嗪-1-基)环己基]-1H-吡喰唑[3,4-d]嘧啶-3-基]-2-甲氧基苯基]-1-甲基-1H-吲哚-2-羧酰胺Chemical Name: N-[4-[4-Amino-1-[trans-4-(4-methylpiperazin-1-yl)cyclohexyl]-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-2-methoxy...
参考文献标题:Pyrazolopyrimidines as therapeutic agents
文献作者:Hirst,G.C.; Rafferty,P.; Ritter,K.; Arnold,L.D.; Wishart,N.; Calderwood,D.; Friedman,M.M.(BASF AG)
参考来源:EP 1212327; WO 0119829

LY-329146

N-[4-[6-羟基-3-[4-[2-(4-吗酚醛)乙氧基]苯甲酰]-1-苯并哧-2-基]苯基]-N-(甲基磺酰)甲烷磺酰胺Chemical Name: N-[4-[6-Hydroxy-3-[4-[2-(4-morpholinyl)ethoxy]benzoyl]-1-benzothien-2-yl]phenyl]-N-(methylsulfonyl)methanesulfonamide
CA...
参考文献标题:Methods for treating resistant tumors
文献作者:Dantzig,A.H.; Grese,T.A.; Normal,B.H.; Palkowitz,A.D.; Sluka,J.P.; Starling,J.J.II; Winter,M.A.(Eli Lilly and Company)
参考来源:EP 0773217; JP 2000500138; WO 9717069

FK-3311

N-[4-乙酰基-2-(2,4-二氟苯氧基)苯基]-甲烷磺酰胺Chemical Name: 4-Acetyl-2-(2,4-difluorophenoxy)methanesulfonanilide; 3-(2,4-Difluorophenoxy)-4-(methanesulfonamido)acetophenone; N-[4-Acetyl-2-(2,4-difluorophenoxy)pheny...
参考文献标题:Studies on antiinflammatory agents.I.Synthesis and pharmacological properties of 2'-phenoxymethanesulfonanilide derivatives
文献作者:Tsuji,K.; Nakamura,K.; Konishi,N.; Okumura,H.; Matsuo,M.
参考来源:Chem Pharm Bull 1992,40(9),2399

UC-781

N-[4-氯-3-(3-甲基丁-2-烯氧基)苯基]-2-甲基呋喃-3-硫代甲酰胺Chemical Name: N-[4-Chloro-3-(3-methyl-2-butenyloxy)phenyl]-2-methylfuran-3-carbothioamide
CAS No. 178870-32-1
项目整合开发状态: Phase I
项目研究机构: Cellegy (Propr...
参考文献标题:Furan- and thiophenecarbothioamide derivs.,their preparation and their use as inhibitors of the replication of HIV-1 and HIV-1 mutants
文献作者:Brouwer,W.G.; Osika,E.M.; Pierce,B.J.(Uniroyal Chemical Company,Inc.)
参考来源:EP 0874839; JP 1999504657; US 5696151; WO 9719940

FTI-2148

N-[5-(1H-吡唑-4-甲基氨基甲基)-2'-甲基苯基-2-酰羰基]-L-甲硫氨酸Chemical Name: N-[5-(1H-Imidazol-4-ylmethylaminomethyl)-2'-methylbiphenyl-2-ylcarbonyl]-L-methionine
CAS No. 251577-09-0
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: Combination therapy with the cytotoxic agents cisplatin,Taxol,and gemcitabine
文献作者:Sun,J.; Blaskovich,M.A.; Knowles,D.; Qian,Y.; Ohkanda,J.; Bailey,R.D.; Hamilton,A.D.; Sebti,S.M.
参考来源:Cancer Res 1999,59(19),4919

Nibentan, HE-11

N-[5-(二乙胺)-1-苯基戊基]-4-硝基苯甲酰盐酸盐Chemical Name: (?-N-[5-(Diethylamino)-1-phenylpentyl]-4-nitrobenzamide hydrochloride
CAS No. 150491-98-8, 150492-05-0 ((-)-enantiomer), 150492-02-7 ((-)-enantiomer, fre...
参考文献标题:The method of preparation of hydrochloride 1-phenyl-1-p-nitrobenzoylamino-5-N,N-diethylaminopentane and 1-phenyl-1-amino-5-N,N-diethylaminopentane
文献作者:Glushkov,R.G.; Lvov,A.I.; Davidova,N.K.; Sizova,O.S.; Sanzarova,G.M.; Polakova,M.J.; Skachilova,S.J.; Zeltuchin,N.K.; Cherkasova,E.M.
参考来源:SU 2059612

BMS-196085

N-[5-[2-[1(R)-[4-(二氟甲氧基)苯基]-2-苯乙基氨基]-1(R)-羟基]-2-羟基苯基]-2-羟基苯基]甲烷磺酰胺Chemical Name: N-[5-[2-[1(R)-[4-(Difluoromethoxy)phenyl]-2-phenylethylamino]-1(R)-hydroxyethyl]-2-hydroxyphenyl]methanesulfonamide
...
参考文献标题:Catecholamine surrogates useful as B3 agonists
文献作者:Washburn,W.N.; Girotra,R.N.; Sher,P.M.; Mikkilineni,A.B.; Poss,K.M.; Mathur,A.; Gavai,A.; Bisacchi,G.S.(Bristol-Myers Squibb Co.)
参考来源:CA 2138675; EP 0659737; JP 1995206806; US 5776983

Tezosentan disodium, Ro-61-0612, Veletri

N-[6-(2-羟基乙氧基)-5-(2-甲氧基苯氧基)-2-[2-[(1H-四唑-5-基)吡啶-4-基]嘧啶-4-基]-5-异丙基吡啶-2-磺酰胺二钠盐替唑生坦 Chemical Name: N-[6-(2-Hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(1H-tetrazol-5-yl)pyridin-4-yl]pyrimidin-4-yl]-5-isopr...
参考文献标题:Novel sulfonamides
文献作者:Breu,V.; Burri,K.; Cassal,J.-M.; Clozel,M.; Hirth,G.; L鰂fler,B.-M.; M黮ler,M.; Neidhart,W.; Ramuz,H.(F.Hoffmann-La Roche AG)
参考来源:EP 0799209; JP 1998509182; WO 9619459

L-377202

N-[N-(4-羧丁基)-4(R)-羟基-L-脯氨基-L-丙烯酰-L-丝基-环己基甘基-L-谷氨酰-L-丝基-L-白乙酰]多柔比星Chemical Name: N-[N-(4-Carboxybutyryl)-4(R)-hydroxy-L-prolyl-L-alanyl-L-seryl-L-cyclohexylglycyl-L-glutaminyl-L-seryl-L-leucyl]doxorubi...
参考文献标题:Conjugates useful in the treatment of prostate cancer
文献作者:Garsky,V.M.; Feng,D.-M.; DeFeo-Jones,D.(Merck & Co.,Inc.)
参考来源:JP 2000509407; WO 9818493

PD-176252

N-{[1-(5-甲氧基-2-吡啶基)环己基]甲基}-alpha-甲基-Nalpha-[(4-硝基苯基)氨基甲酰]-L-色氨酰胺Chemical Name: 3-(1H-Indol-3-yl)-N-[1-(5-methoxy-2-pyridinyl)cyclohexylmethyl]-2(S)-methyl-2-[3-(4-nitrophenyl)ureido]propionamide
CA...
参考文献标题:Non-peptide bombesin receptor antagonists
文献作者:Horwell,D.C.; Pritchard,M.C.(Pfizer Inc.)
参考来源:EP 0920424; WO 9807718