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

Atamestane, Biomed-777, SH-489

阿他美坦Chemical Name: 1-Methylandrosta-1,4-dien-3,17-dione
CAS No. 96301-34-7
项目整合开发状态: Phase III
项目研究机构: Schering AG (Originator), Intarcia (Licensee)
合成路线:This compound can be obtained by t...
参考文献标题:Process for the production of 1-methyl-1,4-androstadien-3,17-dione
文献作者:Petzoldt,K.(Schering AG)
参考来源:WO 8605813

Avasimibe, CI-1011

阿伐麦布Chemical Name: N-[2-(2,4,6-Triisopropylphenyl)acetyl]sulfamic acid 2,6-diisopropylphenyl ester
CAS No. 166518-60-1, 166518-61-2 (sodium salt)
项目整合开发状态: Phase III
项目研究机构: Pfizer (Originato...
参考文献标题:N-Acyl sulfamic acid esters (or thioesters),N-acyl sulfonamides,and N-sulfonyl carbamic acid esters (or thioesters) as hypercholesterolemic agents
文献作者:Lee,H.T.; Picad,J.A.; Sliskovic,D.R.; Wierenga,W.(Pfizer Inc.)
参考来源:EP 0698010; JP 1996510256; US 5491172; WO 9426702

Arzoxifene hydrochloride, SERM 3, LY-353381.HCl

阿佐昔芬盐酸盐阿佐昔芬 Chemical Name: 2-(4-Methoxyphenyl)-3-[4-[2-(piperidin-1-yl)ethoxy]phenoxy]benzo[b]thiophen-6-ol hydrochloride
CAS No. 182133-27-3, 182133-25-1 (free base)
项目整合开发状态: Phase III
项目研...
参考文献标题:Benzothiophene cpds.,intermediates,compsns.,and methods
文献作者:Palkowitz,A.D.(Eli Lilly and Company)
参考来源:EP 0729956; JP 1997183776; US 5488058; US 5492922; US 5510357; US 5856339

Actarit, MS-932, Mover, Orcl

阿克他利Chemical Name: 2-(4-Acetamidophenyl)acetic acid; 4-(Acetylamino)benzeneacetic acid
CAS No. 18699-02-0
项目整合开发状态: Launched-1994
项目研究机构: Mitsubishi Chemical (Originator), Nippon Shinyaku (Li...
参考文献标题:Immunomodulating agents
文献作者:Sato,S.; Tsurufuji,M.; Enomoto,H.; Sugiyama,M.; Shibata,Y.; Morita,I.; Munakata,H.; Kobayashi,M.; Wagatsuma,K.(Mitsubishi Chem.Inds.Co.; Ltd.)
参考来源:DE 3317107; US 4720506

Acrihellin, D-12316

阿克海林Chemical Name: 3beta,5,14-Trihydroxy-19-oxo-5-beta-vufa-20,22-dienolide 3-(3-methylcrotonate); 5beta,14beta-Dihydroxy-3beta-(3-methylbut-2-enoyloxy)-19-oxovufa-20,22-dienolide; (3beta,5beta)-5,14-...
参考文献标题:Acrihellin
文献作者:Thiemer,K.; Isaac,O.; Schlichtegroll,A.v.; Engel,J.
参考来源:Drugs Fut 1981,6(8),459

Alemcinal, ABT-229, A-81229

阿兰西那Chemical Name: 8,9-Didehydro-3'N-demethyl-9-deoxo-4'',6,12-trideoxy-6,9-epoxy-3'N-ethylerythromycin
CAS No. 150785-53-8
项目整合开发状态: Phase II
项目研究机构: Abbott (Originator)
合成路线:The selectiv...
参考文献标题:4''-Deoxyerythromycin derivs.
文献作者:Lartey,P.A.; Nellans,H.N.; Klein,L.L.; Faghih,R.(Abbott Laboratories Inc.)
参考来源:EP 0623021; JP 1994511257; US 5578579; WO 9313780

Aliskiren fumarate, CGP-60536(free base), SPP-100B, SPP-100(free base), CGP-60536B

阿利克仑半富马酸盐阿利吉仑 (2S,4S,5S,7S)-7-(3-(3-甲氧基丙氧基)-4-甲氧基苄基)-5-氨基-N-(2-氨基甲酰基-2-甲基丙基)-4-羟基-2-异丙基-8-甲基壬酰胺盐酸盐Chemical Name: (2S,4S,5S,7S)-5-Amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-[4-metho...
参考文献标题:Delta-amino-gamma-hydroxy-omega-aryl alkanoic acid amides with enzyme especially renin inhibiting activities
文献作者:Gchke,R.; Maibaum,J.K.; Schilling,W.; Stutz,S.; Rigollier,P.; Yamaguchi,Y.; Cohen,N.C.; Herold,P.(Novartis AG)
参考来源:EP 0678500; EP 0678503; JP 1996053434; JP 1996081430; US 5559111; US 5627182; US 5646143

Ataprost, OP-41483, Ono-41483

阿前列素Chemical Name: [3aS-[2E,3aalpha,4alpha(1E,3R*),5beta,6aalpha]]-5-[4-(3-Cyclopentyl-3-hydroxy-1-propenyl)hexahydro-5-hydroxy-2(1H)-pentalenylidene]pentanoic acid; (9alpha,11alpha,15alpha)-6,9-Metha...
参考文献标题:ONO-41483
文献作者:Kottegoda,S.R.; Serradell,M.N.; Adaikan,P.G.; Castar,J.
参考来源:Drugs Fut 1984,9(11),833

Argipidine, Argatroban monohydrate, GN1600, DK-7419, MDI-805, OM-805, MCI-9038, MD-805, Argatroban Injection, Acova, Slonnon, Novastan

阿加曲班阿加曲班(MCI-9038) Chemical Name: (2R,4R)-4-Methyl-1-[N2-(3-methyl-1,2,3,4-tetrahydroquinolin-8-ylsulfonyl)-L-arginyl]piperidine-2-carboxylic acid monohydrate; (2R,4R)-1-[5-Guanidino-1-oxo-2(S)-(1,2,...
参考文献标题:N2-Arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
文献作者:Kikumoto,R.; Tamao,Y.; Onkubo,K.; Tezuka,T.; Tonomura,S.; Hihikata,A.; Okamoto,S.(Mitsubishi Chemical Corp.)
参考来源:EP 0008746; US 4258192

Acarbose, Bay-g-5421, Prandase, Glucor, Precose, Glucobay

阿卡波糖Chemical Name: O-4,6-Dideoxy-4-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-2-cyclohexen-1-yl]amino]-alpha-D-glucopyranosyl-(1--4)-O-alpha-D-glucopyranosyl-(1--4)-D-glucose; O-4,6-Dideoxy-4-...
参考文献标题:Valiolone,a method of preparing it,and its use to prepare acarbose and voglibose
文献作者:Lee,S.; Tornus,I.; Floss,H.G.(Bayer AG)
参考来源:WO 9950217