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

Tecastemizole, Norastemizole, Soltara

诺阿斯米唑诺拉斯三唑氢溴化物 Chemical Name: 1-(4-Fluorobenzyl)-2-(piperidin-4-ylamino)-1H-benzimidazole
CAS No. 75970-99-9, 75970-64-8 (diHBr salt)
项目整合开发状态: Discontinued
项目研究机构: Sepracor (Originator)
...
参考文献标题:Methods for synthesizing 2-substd.imidazoles
文献作者:Hong,Y.; Senanayake,C.H.; Bakale,R.P.(Sepracor Inc.)
参考来源:EP 0977740; JP 2001520658; US 5817823; WO 9846571

Plaunotol, CS-684, Kelnac

谱劳诺托Chemical Name: (2Z,6E)-2-[(3E)-4,8-Dimethyl-3,7-nonanediyl]-6-methyl-2,6-octadiene-1,8-diol
CAS No. 64218-02-6
项目整合开发状态: Launched-1986
项目研究机构: Sankyo (Originator)
合成路线:By a Wittig cond...
参考文献标题:Polyprenyl derivatives
文献作者:Mishima,H.; Ogiso,A.; Kobayashi,S.(Sankyo Co.,Ltd.)
参考来源:DE 2652256; FR 2332009; GB 1533377; JP 52062213; US 4059641

Beraprost sodium, RU-55100, ML-1229(free acid), ML-1129, TRK-100, Beraprost, Dorner, Procylin

贝前列素钠贝前列素 Chemical Name: (?-(1R,2R,3aS,8bS)-2-Hydroxy-1-[(E)-(3S,4RS)-3-hydroxy-4-methyl-1-octen-6-ynyl]-2,3,3a,8b-tetrahydro-1H-cyclopenta[b]benzofuran-5-butyric acid sodium salt; (?-(1R,2R,3aS,8bS)...
参考文献标题:5,6,7-Trinor-4,8-inter-m-phenylene protaglandin I2 derivatives useful in anti-ulcer,hypotensive and platelet aggregation inhibiting compositions
文献作者:Ohno,K.; Nagase,H.; Matsumoto,K.; Nishio,S.(Toray Industries,Inc.)
参考来源:EP 0084856; JP 58124778; US 4474802

Becatecarin, NSC-D-640199, XL-119, DEAE-Rebeccamycin, NSC-655649, BMY-27557-14(tartrate), BMY-27557-01(HCl), BMS-181176

贝卡特林Chemical Name: 1,11-Dichloro-6-[2-(diethylamino)ethyl]-12-(4-O-methyl-beta-D-glucopyranosyl)-6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-dione phosphate
CAS No. 119673-08-4...
参考文献标题:Rebeccamycin analogs
文献作者:Kaneko,T.; Wong,H.S.; Utzig,J.J.(Bristol-Myers Squibb Co.)
参考来源:AU 8781148; EP 0269025; JP 1988198695; US 4808613

NSC-127755

贝氏抗叶酸物Chemical Name: 4,6-Diamino-2,2-dimethyl-1-[3-chloro-4-(4-fluorosulfonyl-2-chlorophenylbutyl)phenyl]-s-triazine ethanesulfonate; Ethanesulfonic acid,compound with 3-chloro-4-[4-[2-chloro-4-(4,6-d...
参考文献标题:NSC-127,755
文献作者:Blancafort,P.; Serradell,M.N.; Castar,J.; Hillier,K.
参考来源:Drugs Fut 1983,8(7),596

Befloxatone, MD-370503

贝氟沙通Chemical Name: 5(R)-(Methoxymethyl)-3-[4-[4,4,4-trifluoro-3(R)-hydroxybutoxy]phenyl]oxazolidin-2-one
CAS No. 134564-82-2
项目整合开发状态: Phase II
项目研究机构: Sanofi-Aventis (Originator)
合成路线:Bef...
参考文献标题:3-Aryl oxazolidinones,process for their preparation and their therapeutical use
文献作者:Koenig,J.-J.; Schoofs,A.; Jarreau,F.-X.; Rovei,V.(Laboratoires Delalande)
参考来源:EP 0424243; EP 0424244; EP 0428421; JP 1992502333; JP 1992502334; JP 1992502335; US 5036090; US 5036091; US 5171747; US 5196543; WO 9105775

Bemitradine, SC-33643

贝米曲啶Chemical Name: 8-(2-Ethoxyethyl)-7-phenyl-1,2,4-triazolo[1,5-c]pyrimidin-5-amine
CAS No. 88133-11-3
项目整合开发状态: Phase II
项目研究机构: Pfizer (Originator)
合成路线:The alkylation of ethyl benzoyla...
参考文献标题:SC-33643
文献作者:Rorig,K.L.; Heilman,R.D.
参考来源:Drugs Fut 1985,10(4),298

Lisinopril, ICI-209K, MK-521, Doneka, Prinzide, Zestril, Longes, Coric, Acerbon, Vivatec, Carace, Prinivil

赖诺普利Chemical Name: (S)-1-[N2-(1-Carboxy-3-phenylpropyl)-L-lysyl]-L-proline
CAS No. 76547-98-3
项目整合开发状态: Launched-1987
项目研究机构: Merck & Co. (Originator), Bristol-Myers Squibb (Marketer), AstraZ...
参考文献标题:Carboxyalkyl dipeptide derivs.,process for preparing them and pharmaceutical compsn.containing them
文献作者:Wyvratt,M.J.; Harris,E.E.; Patchett,A.A.; Tristram,E.W.(Merck & Co.,Inc.)
参考来源:EP 0012401

Synvinolin, Simvastatin, MK-733, Pantok, Colemin, Sinvacor, Lipex, Medipo, Zocor, Lipovas, Denan, Lodal鑣, Zocord

辛伐他汀,斯伐他汀Chemical Name: 2,2-Dimethylbutyric acid [1S-[1alpha,3alpha,7beta,8beta(2S*,4S*),8abeta]-3,7-dimethyl-8-[2-(4-hydroxy-6-oxotetrahydropyran-2-yl)ethyl]-1,2,3,7,8,8a-hexahydro-1-naphthyl ester; ...
参考文献标题:Antihypercholesterolemic cpds.
文献作者:Hoffman,W.F.; Smith,R.L.; Willard,A.K.(Merck & Co.,Inc.)
参考来源:US 4444784

Cinecromen, TVX-2656

辛克罗孟Chemical Name: 3-(3,4,5-Trimethoxyphenyl)propenoic acid 2-[4-methyl-7-(4-morpholinylcarboxamido)-2-oxo-2H-1-benzopyran-3-yl]-1-(4-morpholinylmethyl)ethyl ester
CAS No. 62380-23-8
项目整合开发状态: N...
参考文献标题:
文献作者:Boltze,K.; et al.
参考来源:BE 843810; DE 2530405; FR 2316939; JP 7725777; NL 7607494