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

Ampiroxicam, CP-65703, Nacyl, Flucam

安吡昔康Chemical Name: 4-(1-Hydroxyethoxy)-2-methyl-N-2-pyridyl-2H-1,2-benzothiazine-3-carboxamide ethyl carbonate (ester) 1,1-dioxide; Carbonic acid ethyl 1-[[2-methyl-3-[(2-pyridylamino)carbonyl]-2H-1,2...
参考文献标题:Ether prodrugs of anti-inflammatory oxicams
文献作者:Marfat,A.(Pfizer Inc.)
参考来源:EP 0147177; ES 8604215; JP 1985156688; US 4551452

Amperozide, FG-5606, Hogpax vet.

安哌齐持Chemical Name: 4-[4,4-Bis(4-fluorophenyl)butyl]-N-ethyl-1-piperazinecarboxamide
CAS No. 75558-90-6, 75529-73-6 (HCl)
项目整合开发状态: Phase III
项目研究机构: Ferrosan AB (Originator)
合成路线:The conde...
参考文献标题:Selective melanin concentrating hormone-1 (MCH1) receptor antagonists and uses thereof
文献作者:Gluchowski,C.; Chiu,G.; Marzabadi,M.R.; Nagarathnam,D.; Lagu,B.; Noble,S.; Wetzel,J.; Deleon,J.E.(Synaptic Pharmaceutical Corp.)
参考来源:EP 1299362; WO 0206245

SPD-420, BDP-12, CX-516, Ampalex

安帕来斯Chemical Name: 6-(Piperidin-1-ylcarbonyl)quinoxaline; 1-(Piperidin-1-yl)-1-(quinoxalin-6-yl)methanone
CAS No. 154235-83-3
项目整合开发状态: Phase II
项目研究机构: Cortex (Originator), University of Cal...
参考文献标题:Drugs that enhance synaptic responses mediated by AMPA receptors
文献作者:Lynch,G.S.; Rogers,G.A.(University of California,Oakland)
参考来源:EP 1156043; JP 1995509468; WO 9402475

Amprenavir, KVX-478, 141W94, VX-478, Prozei, Agenerase

安普那韦Chemical Name: 4-Amino-N-[2(R)-hydroxy-4-phenyl-3(S)-[tetrahydrofuran-3(S)-yloxycarbonylamino]butyl]-N-isobutylbenzenesulfonamide; (1S,2R)-3-[N-(4-Aminophenylsulfonyl)-N-ispropylamino]-1-benzyl-2-...
参考文献标题:Sulfonamide inhibitors of HIV-aspartyl protease
文献作者:Tung,R.D.; Murcko,M.A.; Bhisetti,G.R.(Vertex Pharmaceuticals Inc.)
参考来源:EP 0659181; EP 0885887; JP 1996501299; US 5585397; WO 9405639

Antrafenine

安曲非宁Chemical Name: 2-[7-(Trifluoromethyl)quinolin-4-ylamino]benzoic acid 2-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]ethyl ester
CAS No. 55300-29-3
项目整合开发状态: Not Determined
项目研究机构: Sanofi-...
参考文献标题:Esters of 2-[(4-quinolyl)amino]benzoic acids
文献作者:Giudicelli,P.R.L.; et al.(Sanofi-Synthabo)
参考来源:DE 2415982; DE 2462460; GB 1441184; JP 50030891; US 3935229

Amcinonide, CL-34699

安西奈德Chemical Name: 21-Acetoxy-9alpha-fluoro-11beta,16alpha,17-trihydroxypregna-1,4-diene-3,20-dione cyclic 16,17-acetal whith cyclopentanone; 11beta,16alpha-Acetoxy-16,17[cyclopentylidenebis(oxy)]-9-f...
参考文献标题:Administration of 16alpha,17alpha-cyclopentylidenedioxy-9alpha-fluoro-11beta,21-dihydroxy-1,4-pregnadiene-3,20-dione-21-acetate
文献作者:Sieger,G.M.; Krieger,C.(American Cyanamid Co.)
参考来源:DE 2437847; FR 2240738; GB 1442925; US 4158055

Ibutilide fumarate, U-70226E, Corvert

富马酸伊布利特伊布利特 Chemical Name: (?-4'-[4-(Ethylheptylamino)-1-hydroxybutyl]methanesulfoanilide fumarate (2:1) salt; (?-N-[4-[4-(Ethylheptylamino)-1-hydroxybutyl]phenyl]methanesulfonamide fumarate (2:1) sa...
参考文献标题:N-(Aminoalkylphenyl)sulfonamides their preparation and therapeutic use
文献作者:Hester,J.B.Jr.(Pharmacia Corp.)
参考来源:EP 0164865; JP 1985239458; US 5155268

Quetiapine fumarate, FK-949, ZD-5077, ZM-204636, ICI-204636, Seroquel

富马酸喹硫平喹硫平 Chemical Name: 11-[4-[2-(2-Hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine hemifumarate
CAS No. 111974-72-2, 111974-69-7 (free base)
项目整合开发状态: Launched-1997
项目研究机构: ...
参考文献标题:Thiazepine cpds
文献作者:Warawa,E.J.; Migler,B.M.(AstraZeneca LP)
参考来源:EP 0240228; JP 1988008378; US 4879288

Tenofovir disoproxil fumarate, GS-4331-05, Bis(POC)PMPA, Viread

富马酸替诺福韦酯替诺福韦酯 Chemical Name: (R)-[[2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phosphonic acid bis(isopropoxycarbonyloxymethyl) ester fumarate; 2-(Adenin-9-yl)-1(R)-methylethoxymethylphosphonic a...
参考文献标题:Nucleotide analogs
文献作者:Arimilli,M.N.; Cundy,K.C.; Dougherty,J.P.; Kim,C.U.; Oliyai,R.; Stella,V.J.(Gilead Sciences Inc.)
参考来源:US 5922695; WO 9804569

Eformoterol fumarate, Formoterol fumarate, CGP-25827A(free base), YM-08316, BD-40A(anhydrous), Foradil Aerolizer, Foradil Certihaler, Broncoral, Oxeze Turbuhaler, Oxis Turbuhaler, Foradil, Atock

富马酸福莫特罗福莫特罗 Chemical Name: (?-N-[2-Hydroxy-5-[1(R*)-hydroxy-2-[1(R*)-methyl-2-(4-methoxyphenyl)ethylamino]ethyl]phenyl]formamide fumarate (2:1) monohydrate
CAS No. 43229-80-7 (anhydrous), 73573-8...
参考文献标题:BD 40A
文献作者:Castar,J.; Weetman,D.F.
参考来源:Drugs Fut 1977,2(10),639