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

新产品编号:538389

Chemical Name: 2(S)-[3-(4-Methylsulfonylphenyl)-5-(trifluoromethyl)pyridin-2-ylsulfanyl]propan-1-ol
CAS No. 221383-28-4 (non-specified steroch.)
项目整合开发状态: Preclinical
项目研究机构: Merck Frosst (Or...
参考文献标题:2-Heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors
文献作者:Dube,D.; Brideau,C.; Deschenes,D.; Fortin,R.; Friesen,R.W.; Gordon,R.; Girard,Y.; Riendeau,D.; Savoie,C.; Chan,C.C.
参考来源:Bioorg Med Chem Lett 1999,9(12),1715

ML-3176

Chemical Name: 1-[2-[4-(Carboxymethyl)phenoxy]ethyl]-3-(1-dodecanoyl)-1H-indole-2-carboxylic acid
CAS No. 192182-47-1
项目整合开发状态: Preclinical
项目研究机构: Merckle (Originator)
合成路线:The condensati...
参考文献标题:Acylpyrroldicarboxylic acids and acylindoldicarboxylic acids and their derivs.and inhibitors of the cytosolic phospholipase A2
文献作者:Lehr,M.(Merckle GmbH)
参考来源:EP 0923546; WO 9805637

NCS-706

Chemical Name: 2-Iodo-9-(2-methoxybenzyl)-N6-methyladenine hydrochloride
CAS No. 396653-34-2
项目整合开发状态: Biological Testing
项目研究机构: CNRS (Originator)
合成路线:Alkylation of 2-amino-6-chloropurin...
参考文献标题:Design,synthesis and structure-activity relationships of a series of 9-substituted adenine derivatives as selective phosphodiesterase type-4 inhibitors
文献作者:Raboisson,P.; Lugnier,C.; Muller,C.; Reimund,J.-M.; Schultz,D.; Pinna,G.; Le Bec,A.; Basaran,H.; Desaubry,L.; Gaudiot,F.; Seloum,M.; Bourguignon,J.-J.
参考来源:Eur J Med Chem 2003,38(2),199

新产品编号:220407

Chemical Name: 4-[1-Methyl-2-(4-piperidinyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-N-[1(S)-phenylethyl]pyridine-2-amine
CAS No. 189442-43-1
项目整合开发状态: Preclinical
项目研究机构: Merck & Co....
参考文献标题:Substd.imidazoles having anti-cancer and cytokine inhibitory activity
文献作者:Selnick,H.G.; Claremon,D.A.; Liverton,N.J.(Merck & Co.,Inc.)
参考来源:JP 1999514353; US 5717100; WO 9712876

新产品编号:513077

Chemical Name: N-[2-(Dimethylamino)ethyl]-9-hydroxy-5,6,11-trimethyl-6H-pyrido[4,3-b]carbazole-1-carboxamide dihydrochloride
CAS No. 220443-16-3 (free base)
项目整合开发状态: Preclinical
项目研究机构: Serv...
参考文献标题:Synthesis of 9-O-substituted derivatives of 9-hydroxy-5,6-dimethyl-6H-pyrido[4,3-b]carbazole-1-carboxylic acid (2-(dimethylamino)ethyl)amide and their 10- and 11-methyl analogues with improved antitumor activity
文献作者:Guillonneau,C.; Pierre,A.; Charton,Y.; Guilbaud,N.; Kraus-Berthier,L.; Leonce,S.; Michel,A.; Bisagni,E.; Atassi,G.
参考来源:J Med Chem 1999,42(12),2191

A-85380-[18F]-F, [18F]-F-A-85380

Chemical Name: 3-[Azetidin-2(S)-ylmethoxy]-2-(18-fluoro)pyridine
CAS No. 205594-65-6
项目整合开发状态: Phase I
项目研究机构: Commissariat a l'Energie Atomique (Originator)
合成路线:In a related procedure,2-...
参考文献标题:Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2azetidinylmethoxylpyridine: A new positron emission tomography ligand for nicotinic receptors
文献作者:Doll,F.; Dolci,L.; Valette,H.; Hinnen,F.; Vaufrey,F.; Guenther,I.; Fuseau,C.; Coulon,C.; Bottlaender,M.; Crouzel,C.
参考来源:J Med Chem 1999,42(12),2251

新产品编号:541553

Chemical Name: 4-(3,4,5-Trimethoxybenzyl)-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-amine dihydrochloride
CAS No. 221658-92-0, 221659-12-7 (monohydrochloride)
项目整合开发状态: Biological Testing
项目...
参考文献标题:beta3-Adrenoreceptor agonists,agonist compsns.and methods of using
文献作者:Miller,D.D.; Feller,D.R.(Molecular Design International,Inc.)
参考来源:EP 1023269; WO 9916752

新产品编号:543135

Chemical Name: 4-(3,5-Diiodo-4-methoxybenzyl)-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-amine dihydrochloride
CAS No. 221658-94-2, 221659-10-5 (free base), 221659-45-6 (HCl), 221659-44-5 (monoHBr)...
参考文献标题:beta3-Adrenoreceptor agonists,agonist compsns.and methods of using
文献作者:Miller,D.D.; Feller,D.R.(Molecular Design International,Inc.)
参考来源:EP 1023269; WO 9916752

EGIS-8332

Chemical Name: (+)-7-Acetyl-5-(4-aminophenyl)-8-methyl-8,9-dihydro-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine-8-carbonitrile
CAS No. 220725-87-1 (undefined isomer), 220725-88-2 (undefined isomer, HCl...
参考文献标题:5H-2,3-Benzodiazepine derivs.,process for their preparation and pharmaceutical compsns.which contain them
文献作者:Andr醩i,F.; Balogh,T.; Botka,P.; Elekes,I.; Goldschmidt,K.; H醡ori,T.; Korosi,J.; L醤g,T.; Moravcsik,I.; Sineger,E.; Somogyi,G.; Zolyomi,G.(Egis Pharmaceuticals Ltd.)
参考来源:FR 2566774; HU 191702

R-137696

Chemical Name: (-)-1-[3-[3,4-Dihydro-2H-1-benzopyran-2(R)-ylmethylamino]propyl]perhydropyrimidin-2-one
CAS No. 227296-56-2, 227296-61-9 ((S)-isomer), 227296-62-0 ((S)-isomer, oxalate (1:1)), 227296...
参考文献标题:(Benzodioxan,benzofuran or benzopyran) derivs.having fundic relaxation properties
文献作者:De Bruyn,M.F.L.; Schroven,M.F.J.; Wigerinck,P.T.B.P.; Verschueren,W.G.(Janssen Pharmaceutica NV)
参考来源:WO 9929687