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

Altoqualine, 458-L(non-sterochem.)

阿托喹啉 7-氨基-4,5,6-三乙氧基-3-(6,7,8-三甲氧基-2-甲基-3,4-二氢-1H-异喹啉-1-基)-3H-2-苯并呋喃-1-酮 Chemical Name: (3S)-7-Amino-4,5,6-triethoxy-3-[(1R)-1,2,3,4-tetrahydro-6,7,8-trimethoxy-2-methyl-1-isoquinolinyl]-1(3H)-isobenz...
参考文献标题:458-L
文献作者:Castar,J.; Blancafort,P.; Serradell,M.N.
参考来源:Drugs Fut 1982,7(5),317

Azelnidipine, CS-905, RS-9054, Calblock

阿折地平Chemical Name: (?-2-Amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-[1-(diphenylmethyl)azetidin-3-yl] 5-isopropyl diester
CAS No. 123524-52-7, 116574-11-9 (diHCl sa...
参考文献标题:Dihydropyridine derivs.,their preparation and their use
文献作者:Koike,H.; Yoshimoto,M.; Nishino,H.(Sankyo Co.,Ltd.; Ube Industries,Ltd.)
参考来源:EP 0266922; EP 0529702; JP 1988253082; US 4772596

Araprofen, Camprofen

阿拉洛芬Chemical Name: (?-2-[4-(2-Carboxyphenylaminophenyl]propionic acid; (?-4-(2-Carboxyphenylamino)-alpha-methylbenzeneacetic acid; (?-p-(o-Carboxyanilino)hydratropic acid
CAS No. 15250-13-2
项目整合...
参考文献标题:Synthesis and structure activity relationships of anti-inflammatory 9,10-dihydro-9-oxo-2-acridine-alkanoic acids and 4-(2-carboxyphenyl)aminobenzenealkanoic acids
文献作者:Taraporewala,I.B.; Kauffman,J.M.
参考来源:J Pharm Sci 1990,79(2),173

Alafosfalin

阿拉磷Chemical Name: L-alanine N-[1(R)-phosphonoethyl]amide
CAS No. 60668-24-8
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:The reaction of ethyl alpha-bromopropionate (I) with triethyl phosphi...
参考文献标题:
文献作者:
参考来源:BE 844377

Alminoprofen, EB-382, Minalfene

阿明洛芬Chemical Name: p-[(2-Methylallyl)amino]hydratropic acid; 2-[4-(2-Methylallylamino)phenyl]propionic acid; alpha-Methyl-4-[(2-methyl-2-propenyl)amino]benzeneacetic acid
CAS No. 39718-89-3
项目整合...
参考文献标题:Nouveau procede de preparation de derives de l'acide phenylacetique
文献作者:Bouchara,E.(Laboratoires du Dr.E.Bouchara)
参考来源:FR 2289180

Acitemate, Chinoin-123

阿昔替酯3-乙氧羰基-6-甲基-9-羧甲基-4-氧代-6,7,8,9-四氢-4H-吡啶并(1,2-a)嘧啶Chemical Name: (?-cis-3-Ethoxycarbonyl-9-carboxymethyl-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine; (?-cis-3-Ethoxycarbonyl-6-meth...
参考文献标题:CHINOIN-123
文献作者:Paton,D.M.; Castar,J.
参考来源:Drugs Fut 1979,4(11),788

Laurocapram, N-0252, TraZone, Azone

阿昔洛韦Chemical Name: 1-Dodecylhexahydro-2H-azepin-2-one
CAS No. 59277-89-3
项目整合开发状态: Phase III
项目研究机构: UCB (Originator)
合成路线:By condensation of azacycloheptan-2-one (I) with 1-bromododecane ...
参考文献标题:Trisubstd.oxazole derivs.as serotonin ligands
文献作者:Kelly,M.G.; Greenblatt,L.P.; Nelson,F.C.(American Home Products Corp.)
参考来源:US 6242448

Acycloguanosine, Aciclovir, Acyclovir, W-248-U, BW-248-U, Maynar, Viropump(former Brand Name), Genvir, Zovirax

阿昔洛韦Chemical Name: 9-(2-Hydroxyethoxymethyl)guanine; 2-Amino-6-hydroxy-9-(2-hydroxyethoxymethyl)purine; 2-Amino-9-[(2-hydroxyethoxy)methyl]-1,9-dihydro-6H-purin-6-one
CAS No. 59277-89-3
项目整合开发状态...
参考文献标题:Preparation of acyclovir
文献作者:Han,Y.-K.; Harrington,P.J.; Schloemer,G.C.(F.Hoffmann-La Roche AG)
参考来源:EP 0709385; JP 1996053451

RP-49356, 49356RP

阿普卡林Chemical Name: (1RS,2RS)-N-Methyl-2-(3-pyridinyl)-2H-tetrahydrothiopyran-2-carbothioamide 1-oxide
CAS No. 89544-10-5, 92569-65-8 (trans-isomer)
项目整合开发状态: Phase II
项目研究机构: Aventis Pharma (...
参考文献标题:Novel thioformamide derivs.,their preparation and medicines containing them
文献作者:Aloup,J.-C.; Bouchaudon,J.; Farge,D.; James,C.(Aventis SA)
参考来源:EP 0097584

Aprikalim, RP-52891, Aprim

阿普卡林Chemical Name: (-)-(1R,2R)-N-Methyl-2-(3-pyridinyl)tetrahydro-2H-thiopyran-2-carbothioamide 1-oxide
CAS No. 89544-10-5 (non-specific stereoch.), 92569-65-8 (trans-isomer)
项目整合开发状态: Phase II<...
参考文献标题:2-(3-PYRIDYL)-TETRAHYDROTHIOPYRAN-2-CARBOTHIOAMIDE DERIVATIVES AND ANALOGUES: A NOVEL FAMILY OF POTENT POTASSIUM CHANNEL OPENERS
文献作者:Aloup,J.C.; Farge,D.; James,C.; Mondot,S.; Cavero,I.
参考来源:Drugs Fut 1990,15(11),1097