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

Triptolide, PG-490

雷公藤内酯醇Chemical Name: (-)-(3bS,4aS,5aS,6R,6aR,7aS,7bS,8aS,8bS)-3b,4,4a,6,6a,7a,7b,8b,9,10-Decahydro-6-hydroxy-6a-isopropyl-8b-methyltrisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1(3H)-one
CAS No....
参考文献标题:Triptolide
文献作者:Ruyun,J.
参考来源:Drugs Fut 1985,10(7),575

Ralitoline, CI-946, PD-117818, Goe-4942

雷利托林Chemical Name: (Z)-(3-Methyl-4-oxothiazolidin-2-yliden)-N-(2-chloro-6-methylphenyl)acetamide
CAS No. 93738-40-0
项目整合开发状态: Phase III
项目研究机构: G鰀ecke (Originator), Pfizer (Originator)
合成路...
参考文献标题:4-Oxothiazolidin-2-ylideneacetamide derivatives as CNS agents
文献作者:Bartoszyk,G.; Hartenstein,J.; Herrmann,M.; Fritschi,E.; Satzinger,G.(G鰀ecke AG)
参考来源:DE 3317000; EP 0124911; US 4563471

Razobazam, HR-175, Hoe-175

雷唑巴占Chemical Name: 4,8-Dihydro-3,8-dimethyl-4-phenylpyrazolo[3,4-b][1,4]diazepine-5,7(1H,6H)-dione
CAS No. 78466-98-5
项目整合开发状态: Biological Testing
项目研究机构: Aventis Pharma (Originator)
合成路线:...
参考文献标题:4-Aryl-5,6,7,8-tetrahydropyrazolo[3,4-b]-[1,5]diazepine-1H,4H-5,7-diones and medicaments containing same
文献作者:Rackur,G.; Hoffmann,I.(Aventis SA)
参考来源:DD 152936; DE 2932835; EP 0024038; EP 0050376; JP 5603977; US 4302468

Resequinil, AVE-3933, SX-3933, AC-3933

雷地奎尼Chemical Name: 5-(3-Methoxyphenyl)-3-(5-methyl-1,2,4-oxadiazol-3-yl)-1,6-naphthyridin-2(1H)-one
CAS No. 219846-31-8
项目整合开发状态: Phase II
项目研究机构: Dainippon Pharmaceutical (Originator), Avent...
参考文献标题:Structure-activity relationships and cognition-enhancing actions of novel 1,6-naphthyridine derivatives with benzodiazepine receptor inverse agonists activities
文献作者:Masumoto,K.; et al.
参考来源:Symp Med Chem 1998,Abst 2-P-10

Ranirestat, SX-3202((+)-(S)-isomer), SX-3030(racemate), AS-3201, SX-3201

雷尼司他Chemical Name: (-)-(R)-2-(4-Bromo-2-fluorobenzyl)spiro[1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-4,3'-pyrrolidine]-1,2',3,5'-tetraone
CAS No. 147254-64-6, 147254-65-7 ((+)-enantiomer), 147193-59...
参考文献标题:Novel,highly potent aldose reductase inhibitors: (R)-(-)-2-(4-Bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-4-spiro-3'-pyrrolidine-1,2',3,5'-tetrone (AS-3201) and its congeners
文献作者:Negoro,T.; Murata,M.; Ueda,S.; Fujitani,B.; Ono,Y.; Kuromiya,A.; Komiya,M.; Suzuki,M.; Matsumoto,J.
参考来源:J Med Chem 1998,41(21),4118-29

Sirolimus, Rapamycin, Wy-090217, AY-22989, Rapamune

雷帕霉素Chemical Name: [1R,9S,12S[1'R(1''S,3''R,4''R)],15R,18R,19R,21R,23S,30S,32S,35R]-1,18-Dihydroxy-12-[2-(4-hydroxy-3-methoxy-1-cyclohexyl)-1-methylethyl]-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-...
参考文献标题:Total synthesis of rapamycin
文献作者:Nicolaou,K.C.; Chakraborty,T.K.; Piscopio,A.D.; Minowa,N.; Bertinato,P.
参考来源:J Am Chem Soc 1993,115(10),4419

Retelliptine, NSC-D-626717-W, BD-84, SR-95325B(diHCl), SR-95325A(dimaleate), Peliptil

雷替尼卜定Chemical Name: 1-[[3-(Diethylamino)propyl]amino]-9-methoxy-5,11-dimethyl-6H-pyrido[4,3-b]carbazole
CAS No. 72238-02-9
项目整合开发状态: Phase II
项目研究机构: Sanofi-Aventis (Originator)
合成路线:The n...
参考文献标题:Substd.ellipticines in position 1 by a polyaminated chain,their synthesis and medicaments containing them
文献作者:Bisagni,E.; Ducrocq,C.; Rivalle,C.; Tambourin,P.; Wendling,F.; Civier,A.; Montagnier,L.; Chermann,J.-C.; Gruest,J.; Lidereau,R.(ANVAR (Agence Natl.Valor.Rech.))
参考来源:EP 0010029

Raltitrexed, NSC-639186, ZN-D1694, ZD-1694, ICI-D-1694, D-1694, Tomudex

雷替曲塞Chemical Name: N-[5-[N-Methyl-N-(2-methyl-4-oxo-3,4-dihydroquinazolin-6-ylmethyl)amino]-2-thenoyl]-L-glutamic acid
CAS No. 112887-68-0
项目整合开发状态: Launched-1996
项目研究机构: BTG (Originator), Na...
参考文献标题:Anti-tumor quinazolines
文献作者:Hughes,L.R.(AstraZeneca plc; National Research Development Corp.)
参考来源:EP 0239362; GB 2188319; JP 1989125373; US 4992550; US 5081124; US 5187167

Raclopride, A-40664(tartrate)

雷氯必利Chemical Name: (S)-3,5-Dichloro-N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-hydroxy-6-methoxybenzamide
CAS No. 84225-95-6
项目整合开发状态: Phase II
项目研究机构: AstraZeneca (Originator)
合成路线:The reaction...
参考文献标题:Benzamido-derivatives
文献作者:Florvall,G.L.; Lundstroem,J.O.G.; Raemsby,S.I.; Oegren,S.O.(AstraZeneca plc)
参考来源:DD 201886; EP 0060235; JP 57159762; US 4789683

Ramipril, Hoe-498, Carasel, Altace, Delix, Ramace, Unipril, Tritace, Triatec

雷米普利Chemical Name: (2S,3aS,6aS)-1-[N-[1(S)-(Ethoxycarbonyl)-3-phenylpropyl]-L-alanyl]octahydrocyclopenta[b]pyrrole-2-carboxylic acid; 1-[N-[1(S)-(Ethoxycarbonyl)-3-phenylpropyl]-L-alanyl]-(1S,5S)-2-az...
参考文献标题:Method for making 2-azabicyclo[3.3.0]octane-3-carboxylic acids
文献作者:Teetz,V.; et al.(Aventis Pharma AG)
参考来源:DE 3226768; EP 0079022; EP 0150263; JP 2104526; JP 2104573; JP 4217949; US 4727160; US 5053519