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

CP-319340

Chemical Name: N-[2-(1H-Imidazol-2-ylmethyl)-1,2,3,4-tetrahydroisoquinolin-6-yl]-4'-(trifluoromethyl)biphenyl-2-carboxamide hydrochloride
CAS No. 186390-35-2 (free base)
项目整合开发状态: Preclinical 参考文献标题:Biphenyl-2-carboxylic acid-tetrahydro-isoquinolin-6-yl amide derivs.,their preparation and their use as inhibitors of microsomal triglyceride transfer protein and/or apolipoprotein B (Apo B) secretion
文献作者:Quallich,G.J.; Dorff,P.H.; Chang,G.(Pfizer Inc.)
参考来源:JP 1999514964; US 5919795; WO 9640640

K-777, CRA-3316, APC-3316, K-11777

Chemical Name: N-(4-Methylpiperazin-1-ylcarbonyl)-L-phenylalanine 1(S)-(2-phenylethyl)-3-(phenylsulfonyl) -2(E)-propenyl amide
CAS No. 233277-99-1
项目整合开发状态: Preclinical
项目研究机构: Celera (Origin...
参考文献标题:Irreversible cysteine protease inhibitors containing vinyl groups conjugated to electron withdrawing groups
文献作者:Palmer,J.T.; Rasnick,D.; Klaus,J.L.(Celera Genomics)
参考来源:US 6287840

ATI-2064

Chemical Name: 2-[3-[4-[2-(Diethylamino)ethoxy]-3,5-diiodobenzoyl]-1-benzofuran-2-yl]acetic acid isopropyl ester
CAS No. 270587-31-0
项目整合开发状态: Preclinical
项目研究机构: ARYx Therapeutics (Originato...
参考文献标题:Benzoylbenzofurane derivs.for treatment of cardiac arrhythmia
文献作者:Druzgala,P.(ARYx Therapeutics,Inc.)
参考来源:EP 0703910; JP 1996511546; US 5364880; WO 9429289

FR-227369

Chemical Name: N-(9-Methylsulfonyl-2,3-dihydro-1-benzoxepin-4-ylcarbonyl)guanidine methanesulfonate
CAS No. 248958-47-6, 248958-46-5 (free base), 248958-45-4 (hydrochloride)
项目整合开发状态: Preclinica...
参考文献标题:Guanidine derivs.
文献作者:Inoue,Y.; Akahane,A.; Takenaka,K.; Minagawa,M.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 1073650; US 6346527; WO 9955690

LY-402913

Chemical Name: 2-[3-(9-Chloro-3-methyl-4-oxo-4,5-dihydroisoxazolo[4,3-c]quinolin-5-yl)phenyl]-N-(3,4,5-trimethoxyphenyl)acetamide
CAS No. 246238-55-1
项目整合开发状态: Preclinical
项目研究机构: Lilly (Orig...
参考文献标题:Methods for inhibiting MRP1
文献作者:Kroin,J.S.; Norman,B.H.; Gruber,J.M.(Eli Lilly and Company)
参考来源:EP 1067928; JP 2002510625; US 6369070; WO 9951228

T-138026

Chemical Name: 2,3,4,5,6-Pentafluoro-N-(3-hydroxy-4-methoxyphenyl)benzenesulfonamide
CAS No. 195533-52-9, 195533-96-1 (potassium salt), 195533-95-0 (sodium salt)
项目整合开发状态: Preclinical
项目研究机构:...
参考文献标题:Pentafluorobenzenesulfonamides and analogs
文献作者:Flygare,J.; Medina,J.; Shan,B.; Clark,D.; Rosen,T.(Tularik Inc.)
参考来源:EP 0939627; WO 9805315

SR-16233(free base), TAS-108, SR-16234

Chemical Name: (7alpha,17beta)-17-[2-[4-(diethylaminomethyl)-2-methoxyphenoxy]ethyl]-7-methylestra-1,3,5(10)-trien-3-ol citrate
CAS No. 354808-46-1 (error), 354808-47-2 (error)
项目整合开发状态: Phase I...
参考文献标题:Synthesis of anti-estrogenic acid and other therapeutic steroids from 21-hydroxy-19-norpregna-4-en-3-one
文献作者:Peters,R.H.; Tanabe,M.; Chao,W.-R.; Johansson,J.G.; Ryan,K.J.; Liu,J.(SRI International)
参考来源:WO 0158919

Spisulosine 285, Spisulosine, ES-285

Chemical Name: 2(S)-Aminooctadecan-3(R)-ol
CAS No. 196497-48-0
项目整合开发状态: Phase I
项目研究机构: PharmaMar (Originator), University of Illinois (Originator)
合成路线:Alanine methyl ester (I) was prote...
参考文献标题:Spisulosine cpds.having antitumour activity
文献作者:Garcia Gravalos,D.; Warwick,R.A.; Avila,J.; Rinehart,K.L.; Fregeau,N.L.; Faircloth,G.T.(University of Illinois)
参考来源:WO 9952521

新产品编号:509913

Chemical Name: 4-(Aminomethyl)-2,6-difluorophenol
CAS No. 220353-10-6 (hydrochloride)
项目整合开发状态: Biological Testing
项目研究机构: AstraZeneca (Originator)
合成路线:Nitration of 2,6-difluorophenol (I)...
参考文献标题:2,6-Difluorophenol as a bioisostere of a carboxylic acid: Bioisosteric analogues of gamma-aminobutyric acid
文献作者:Qiu,J.; Stevenson,S.H.; O'Beirne,M.J.; Silverman,R.B.
参考来源:J Med Chem 1999,42(2),329

新产品编号:22657

Chemical Name: 4,4,4-Trifluoro-3-hydroxy-1-phenyl-2-butanone
CAS No. 121194-38-5, 120583-79-1 (R-isomer)
项目整合开发状态: Biological Testing
项目研究机构: Josai University (Originator), Meiji Pharmaceutic...
参考文献标题:alpha-Trifluoromethylated acyloins induce apoptosis in human oral tumor cell lines
文献作者:Kawase,M.; Sakagami,H.; Kusama,K.; Motohashi,N.; Saito,S.
参考来源:Bioorg Med Chem Lett 1999,9(21),3113