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

Dofetilide, UK-68798, Tikosyn, Xelide

多非利特Chemical Name: N-[4-[2-[N-[2-[4-(Methanesulfonamido)phenyl]ethyl]-N-methylamino]ethoxy]phenyl]methanesulfonamide
CAS No. 115256-11-6
项目整合开发状态: Launched-2000
项目研究机构: Pfizer (Originator) 参考文献标题:N-Substituted p-aminoethylsulphonanilides as antiarrhythmic agents,and intermediates therefor
文献作者:Arrowsmith,J.E.; Cross,P.E.; Thomas,G.N.(Pfizer Inc.)
参考来源:EP 0245997; JP 1987267250; US 4959366; US 5079248

GFKI-258, CHIR-258LC, CHIR-258

多韦替尼Chemical Name: 4-Amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one
CAS No. 405169-16-6
项目整合开发状态: Phase I
项目研究机构: Chiron (Originator)
合成路线:The cycliza...
参考文献标题:Quinolinone derivs.
文献作者:Harris,A.; Renhowe,P.; Machajewski,T.; Shafer,C.; Wernette-Hammond,M.-E.; Pecchi,S.; Taylor,C.; McCrea,B.; McBride,C.; Jazan,E.(Chiron Corp.)
参考来源:WO 0222598

Allicin

大蒜素Chemical Name: 2-Propene-1-sulfinothioic acid S-2-propenyl ester; Diallyl disulfide-oxide; 2-Propenethiosulfinic acid S-2-propenyl ester; Allylthiosulfinic acid S-allyl ester
CAS No. 539-86-6 参考文献标题:Allicin
文献作者:Eilat,S.; Avramovitch,D.; Rabinkov,A.; Mirelman,A.; Battler,A.; Eldar,M.; Vered,Z.
参考来源:Drugs Fut 1996,21(11),1101

Nabilone, LY-109514, Cesamet

大麻隆Chemical Name: (?-trans-6,6-Dimethyl-3-(1,1-dimethylheptyl)-1-hydroxy-6,6a,7,8,10,10a-hexahydro-9H-dibenzo[b,d]pyran-9-one
CAS No. 51022-71-0
项目整合开发状态: Launched-1983
项目研究机构: Lilly (Origina...
参考文献标题:Nabilone
文献作者:Castar,J.; Weetman,D.F.
参考来源:Drugs Fut 1978,3(3),207

Alvocidib hydrochloride, Flavopiridol, HL-275, MDL-107826A, HMR-1275, NSC-649890, L86-8275

夫拉平度盐酸盐夫拉平度 Chemical Name: (-)-cis-2-(2-Chlorophenyl)-5,7-dihydroxy-8-(3-hydroxy-1-methylpiperidin-4-yl)-4H-1-benzopyran-4-one
CAS No. 131740-09-5, 146426-40-6 (free base), 131739-92-9 (racemic, H...
参考文献标题:Use of 4H-1-benzopyran-4-one derivs.,4H-1-benzopyran-4-one derivs.and medicines containing same
文献作者:Naik,R.G.; Lal,B.; Rupp,R.H.; Sedlacek,H.H.; Dickneite,G.; Czech,J.(Aventis SA)
参考来源:AU 8943841; DE 3836676; EP 0366061; JP 1990178225; US 5284856

Floctafenine, Ru-15750, R-4318, Idarac

夫洛非宁Chemical Name: 2-[8-(Trifluoromethyl)quinolin-4-ylamino]benzoic acid 2,3-dihydroxypropyl ester
CAS No. 23779-99-9
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:1) Condensation of 2-triflu...
参考文献标题:NMR structure of tissue inhibitor of metalloproteinases-1 implicates localized induced fit in recognition of matrix metalloproteinases
文献作者:Allais,A.; et al.
参考来源:Chim Ther 1973,8(2),154

Frovatriptan, SB-209509AX(succinate), VML-251, SB-209509, Auradol, Rilamig, Allegro, Frova, Frovelan(former Brand Name), Miguard, Migard

夫罗曲坦 S-夫罗曲坦 Chemical Name: (R)-(+)-3-(Methylamino)-1,2,3,4-tetrahydro-9H-carbazole-6-carboxamide
CAS No. 158747-02-5, 158930-18-8 ((S)-isomer), 158747-09-2 (racemate), 158930-17-7 (succinate), 1470...
参考文献标题:Use of tetrahydrocarbazole derivs.as 5HT1 receptor agonists
文献作者:King,F.D.; Gaster,L.M.; Kaumann,A.J.; Young,R.C.(SmithKline Beecham plc)
参考来源:EP 0591280; JP 1994508827; US 5464864; US 5827871; WO 9300086

Fradafiban, BIBU-52

夫雷非班Chemical Name: 5(S)-(4'-Amidinobiphenyl-4-yloxymethyl)-2-oxopyrrolidine-3(S)-acetic acid
CAS No. 148396-36-5
项目整合开发状态: Discontinued
项目研究机构: Boehringer Ingelheim (Originator)
合成路线:The c...
参考文献标题:Cyclic imino derivs.,process for their preparation and drugs containing them
文献作者:Himmelsbach,F.; Austel,V.; Pieper,H.; Eisert,W.; M黮ler,T.; Weisenberger,J.; Linz,G.; Kr黦er,G.(Dr.Karl Thomae GmbH)
参考来源:DE 4035961; EP 0483667; JP 1992264068; US 5591769

Fumagillin, SR-90144, Fugillin, Fumidil

夫马洁林Chemical Name: (2E,4E,6E,8E)-Decatetraenedioic acid (3R,4S,5S6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methyl-2-butenyl)oxiranyl]-1-oxaspiro[2.5]oct-6-yl monoester
CAS No. 23110-15-8
项目整合开发状态: ...
参考文献标题:A concise synthesis of fumagillol
文献作者:Vosburg,D.A.; et al.
参考来源:Angew Chem.Int Ed Engl 1999,38(7),971

Cefprozil, BMY-28100-03-800(monohydrate), BMY-28100, Cefzil, Procef

头孢丙烯头孢丙烯 Chemical Name: (6R,7R)-7-[(R)-2-Amino-2-(p-hydroxyphenyl)acetamido]-8-oxo-3-[(Z)-propenyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid; (6R,7R)-7-[(R)-2-Amino-2-(4-hydroxyphenyl)ac...
参考文献标题:Substd.vinyl cephalosporins
文献作者:Aburaki,S.; Okumura,J.; Naito,T.; Abe,Y.; Hoshi,H.(Bristol-Myers Squibb Co.)
参考来源:BE 0898778; CH 661731; DE 3402642; ES 8600310; GB 2135305; JP 1986171486; US 4520022