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

Cariporide mesilate, Hoe-642

卡立泊来德甲磺酸盐卡立泊来德 Chemical Name: [4-Isopropyl-3-(methylsulfonyl)benzoyl]guanidine methanesulfonate; N-Amidino-4-isopropyl-3-(methylsulfonyl)benzamide methanesulfonate; N-(Diaminomethylene)-4-isopropyl-3...
参考文献标题:Benzoylguanidines,process for their preparation and their use as antiarrhythmic agents
文献作者:Lang,H.-J.; Weichert,A.; Kleemann,H.-W.; Englert,H.; Scholz,W.; Albus,U.(Aventis SA)
参考来源:EP 0589336; JP 1994228082; US 5591754

Canertinib dihydrochloride, CI-1033, PD-183805(free base)

卡纽替尼二盐酸盐卡奈替尼Chemical Name: N-[4-(3-Chloro-4-fluorophenylamino)-7-[3-(4-morpholinyl)propoxy]quinazolin-6-yl]-2-propenamide dihydrochloride
CAS No. 289499-45-2, 338796-35-3 (deleted CAS), 267243-28-7...
参考文献标题:N-[4-(3-Chloro-4-fluoro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide,an irreversible inhibitor of tyrosine kinases
文献作者:Bridges,A.J.; Klohs,W.D.; Driscoll,D.(Pfizer Inc.)
参考来源:EP 1131304; US 6344455; WO 0031048

Carvedilol, SK&F-105517, DQ-2466, BM-14190, Coreg CR, Querto, Dibloc, Coropress, Eucardic, Coreg, Artist, Dimitone, Dilatrend, Kredex

卡维地洛Chemical Name: 1-(9H-Carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]-2-propanol
CAS No. 72956-09-3
项目整合开发状态: Launched-1991
项目研究机构: Roche (Originator), Altana Pharma (Not Determined),...
参考文献标题:Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions
文献作者:Wiedemann,F.; Kampe,W.; Thiel,M.; Sponer,G.; Roesch,E.; Dietmann,H.(Roche Diagnostics GmbH)
参考来源:DE 2815926; EP 0004920; ES 479396; JP 54157558; US 4503067

Caracemide, NSC-253272

卡醋胺Chemical Name: N-[(Methylamino)carbonyl]-N-[[(methylamino)carbonyl]oxy]acetamide; N-Acetyl-N,O-bis(methylcarbamoyl)hydroxylamine
CAS No. 81424-67-1
项目整合开发状态: Phase II
项目研究机构: Aventis Pharm...
参考文献标题:N-[(Alkylamino)carbonyl]-N-[[(alkylamino)carbonyl]
文献作者:Reifschneider,W.(Marion Merrell Dow,Inc.)
参考来源:EP 0086492; US 4413009

Carboplatin, NSC-241240, JM-8, CBDCA, Ercar, Paraplatin

卡铂Chemical Name: cis-Diammine(1,1-cyclobutanedicarboxylato)platinum
CAS No. 41575-94-4
项目整合开发状态: Launched-1986
项目研究机构: Bristol-Myers Squibb (Originator), Johnson Matthey (Originator), America...
参考文献标题:Carboplatin
文献作者:Serradell,M.N.; Blancafort,P.; Castar,J.; Hopkins,S.J.
参考来源:Drugs Fut 1983,8(6),489

Cabergoline, CG-101, FCE-21336, Cabaseril, Sogilen, Cabaser, Dostinex

卡麦角林Chemical Name: 1-[(6-Allylergolin-8beta-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea; (6aR,9R,10aR)-7-Allyl-N-[3-(dimethylamino)propyl]-N-(N-ethylcarbamoyl)-4,6,6a,7,8,9,10,10a-octahydroin...
参考文献标题:Regiospecific process for the preparation of ergoline derivatives
文献作者:Temperilli,A.; Bernardi,L.; Brambilla,E.(Pharmacia Corp.)
参考来源:BE 0894060; JP 58038282

Luliconazole, PR-2699, NND-502

卢立康唑Chemical Name: (-)-(R)-(E)-2-[4-(2,4-Dichlorophenyl)-1,3-dithiolan-2-ylidene]-2-(1-imidazolyl)acetonitrile
CAS No. 187164-19-8
项目整合开发状态: Phase I
项目研究机构: Nihon Nohyaku (Originator), Bayer ...
参考文献标题:Antifungal agent,cpd.therefor,process for producing the same
文献作者:Kodama,H.; Niwano,Y.; Kanai,K.; Yoshida,M.(Nihon Nohyaku Co.,Ltd.)
参考来源:JP 1997100279; JP 1998158168; US 5900488; WO 9702821

Rufinamide, E-2080, RUF-331, CGP-33101, Xilep

卢非酰胺Chemical Name: 1-(2,6-Difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide
CAS No. 106308-44-5
项目整合开发状态: Phase III
项目研究机构: Novartis (Originator), Eisai (Licensee)
合成路线:Rufinamide has been o...
参考文献标题:Fluorinated benzyltriazole derivs.
文献作者:Meier,R.(Novartis AG)
参考来源:AU 8656319; EP 0199262; ES 8800176; ES 8802501; JP 1986243068

Ulobetasol propionate, Halobetasol propionate, CGP-14458, BMY-30056, Miracorten, Ultravate

卤倍他索丙酸酯卤贝他索 Chemical Name: 21-Chloro-6alpha,9-difluoro-11beta-hydroxy-16beta-methyl-17-(1-oxopropoxy)pregna-1,4-diene-3,20-dione; 21-Chloro-6alpha,9-difluoro-11beta,17-dihydroxy-16beta-methylpregna-1...
参考文献标题:Anner,G.(Ciba-Geigy AG).Polyhalogenated steroids
文献作者:Kalvoda,J.; Anner,G.(Novartis AG)
参考来源:CH 631185

Ertapenem sodium, MK-0826, MK-826, ZD-4433, L-749345, Invanz

厄他培南钠尔他培南钠厄他培南Chemical Name: (1R,5S,6S)-2-[2(S)-[N-(3-Carboxyphenyl)carbamoyl]pyrrolidin-4(S)-ylsulfanyl]-6-[1(R)-hydroxyethyl]-1-methyl-1-carba-2-penem-3-carboxylic acid monosodium salt; (4R,5S,6S...
参考文献标题:Carbapenems containing a carboxy substd.phenyl group,processes for their preparation,intermediates and use as antibiotics
文献作者:Betts,M.J.; Davies,G.M.; Swain,M.L.(AstraZeneca plc)
参考来源:EP 0579826; JP 1994506704; US 5478820; US 5652233; US 5856321; WO 9315078