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

GW-7845

2(S)-[2-(甲氧基羰基)苯胺基]-3-[4-[2-(5-甲基-2-苯氯佐尔-4-基)乙氧基]苯基]丙酸Chemical Name: 2(S)-[2-(Methoxycarbonyl)phenylamino]-3-[4-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]phenyl]propionic acid
CAS No. 196809-22-0
...
参考文献标题:N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists.3.Structure-activity relationship and optimization of the N-aryl substituent
文献作者:Cobb,J.E.; Blanchard,S.G.; Boswell,E.G.; Brown,K.K.; Charifson,P.S.; Cooper,J.P.; Collins,J.L.; Dezube,M.; Henke,B.R.; Hull-Ryde,E.A.; Lake,D.H.; Lenhard,J.M.; Oliver,W.Jr.; Oplinger,J.; Pentti,M.; Parks,D.J.; Plunket,K.D.; Tong,W.Q.
参考来源:J Med Chem 1998,41(25),5055

L-Dopa ethyl ester, Etilevodopa, Levodopa ethyl ester, TV-1203

2(S)-氨基-3-(3,4-二羟基苯基)丙酸乙酯Chemical Name: 2(S)-Amino-3-(3,4-dihydroxyphenyl)propionic acid ethyl ester; 3-Hydroxy-L-tyrosine ethyl ester
CAS No. 37178-37-3
项目整合开发状态: Phase III
项目研究机构: Teva (Pro...
参考文献标题:Process for preparing ethyl ester of L-DOPA
文献作者:Atlas,D.; Veinberg,A.; Melamed,E.; Milman,I.(Teva Pharmaceutical Industries Ltd.; Yissum Research Development Co.)
参考来源:EP 0610595; US 5354885

Carbisocaine hydrochloride, Carbizocaine hydrochloride, BK 95

2-(庚氧基)苯胺基甲酸 2-(二乙基氨基)-1-甲基乙基酯盐酸盐 1-二乙基氨基丙-2-基N-(2-庚氧基苯基)氨基甲酸酯 Chemical Name: N-(2-Heptyloxyphenyl)carbamic acid 2-(diethylamino)-1-methylethyl ester hydrochloride
CAS No. 68931-03-3, 76629-87-3 (f...
参考文献标题:Carbizocaine hydrochloride
文献作者:R醖i,S.
参考来源:Drugs Fut 1986,11(7),555

Belotecan hydrochloride, CKD-602, Camtobell

2-(氨甲基)苯乙酸盐酸盐贝洛替康 Chemical Name: 4(S)-Ethyl-4-hydroxy-11-[2-(isopropylamino)ethyl]-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-dione hydrochloride; (20S)-7-[2-(Isopropyla...
参考文献标题:Chemical modification of an antitumor alkaloid camptothecin: Synthesis and antitumor activity of 7-C-substituted camptothecins
文献作者:Sawada,S.; Nokata,K.; Furuta,T.; Yokokura,T.; Miyasaka,T.
参考来源:Chem Pharm Bull 1991,39(10),2574

BM-567

2-(环己基氨基)-5-硝基-N-(戊基氨基甲酰)苯磺酰胺Chemical Name: 2-(Cyclohexylamino)-5-nitro-N-(pentylcarbamoyl)benzenesulfonamide
CAS No. 284464-77-3
项目整合开发状态: Preclinical
项目研究机构: University of Li鑗e (Originator)...
参考文献标题:Benzenic sulphonamide derivs.and their uses
文献作者:Delarge,J.; Masereel,B.; Dogne,J.-M.(University of Li鑗e)
参考来源:WO 0042004

BR-227

2-(甲基氨基)丙-2-烯酸Chemical Name: N-[2,4-Dibromo-6-(N-cyclohexyl-N-methylaminomethyl)phenyl]-4-hydroxy-3-methoxybenzamide; 2',4'-Dibromo-alpha-(cyclohexylmethylamino)-o-vanillotoluidide
CAS No. 84461-99...
参考文献标题:2-Benzoylamino substituted benzylamine derivative and a process for preparation thereof
文献作者:Koshinaka,E.; Ogawa,N.; Kurata,S.; Yamagashi,K.; Kato,I.(Hokuriku Seiyaku Co.,Ltd.)
参考来源:DE 3209970; EP 0061157; ES 510608

NND, CD-349

2-(硝基氧基)丙基3-(硝基氧基)丙基2,6-二甲基-4-(3-硝基苯基)-1,4-二氢-3,5-吡啶二羧酸酯Chemical Name: 3-(2-Nitrooxypropyl) 5-(3-nitrooxypropyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
CAS No. 88594-0...
参考文献标题:1,4-Dihydropyridine derivs.
文献作者:Hatayama,K.; Sawada,J.; Nakazato,A.; Ogawa,T.; Ito,S.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 0092936; US 4472411

Fosfosal, UR-1521, Aydolid, Disdolen

2-(膦酸氧基)苯甲酸Chemical Name: Salicylic acid dihydrogen phosphate
CAS No. 6064-83-1
项目整合开发状态: Launched-1984
项目研究机构: Uriach (Originator)
合成路线:It is prepared by treatment of 2-hydroxybenzoic aci...
参考文献标题:Fosfosal
文献作者:Francia,E.; Garc韆-Rafanell,J.; Mar韓,A.
参考来源:Drugs Fut 1980,5(6),290

DuP-654

2-(苯基甲基)萘-1-醇Chemical Name: 2-Benzyl-1-naphthol; 2-(Phenylmethyl)-1-naphthalenol; 2-Benzyl-1-hydroxynaphthalene
CAS No. 36441-32-4
项目整合开发状态: Phase II
项目研究机构: Bristol-Myers Squibb (Originator)...
参考文献标题:2-Substituted-1-naphthols as 5-lipoxygenase inhibitors
文献作者:Batt,D.G.(E.I.Du Pont de Nemours & Co.)
参考来源:AU 8657186; EP 0201071; ES 8801780; US 4833164

GT-3381, CHF-3381

2-(茚基氨基)乙酰胺,盐酸盐印丹他多 Chemical Name: N-(2-Indanyl)glycinamide hydrochloride; 2-(2,3-Dihydro-1H-inden-2-ylamino)acetamide hydrochloride
CAS No. 202914-18-9, 202844-10-8 (free base)
项目整合开发状态: Phase...
参考文献标题:alpha-Amino acid amides,preparation thereof and the therapeutical use thereof
文献作者:Chiesi,P.; Ventura,P.; Delcanale,M.; De Fanti,R.; Armani,E.; Villetti,G.; Pietra,C.(Chiesi Farmaceutici SpA)
参考来源:EP 0951465; JP 2001506577; US 6114391; WO 9803472