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

新产品编号:951291

Chemical Name: 6-(5-Chloro-3-methyl-1-benzofuran-2-ylsulfonyl)pyridazin-3(2H)-one
CAS No. 463976-07-0, 463976-85-4 (sodium salt)
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:The ...
参考文献标题:Combinations of aldose reductase inhibitors and cyclooxygenase-2 inhibitors
文献作者:Mylari,B.L.(Pfizer Products Inc.)
参考来源:WO 0287584

新产品编号:622235

Chemical Name: 1-Benzyl-4-[4-(4-chlorophenoxy)phenylsulfonyl]piperidine-4-carbohydroxamic acid
CAS No. 239796-97-5, 239796-78-2 (hydrochloride)
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharmaceuti...
参考文献标题:N-Hydroxy-2-(alkyl,aryl,or heteroaryl sulfanyl,sulfinyl or sulfonyl)-3-substd.-alkyl,aryl or heteroarylamides as matrix metalloproteinase inhibitors
文献作者:Venkatesan,A.M.(Wyeth)
参考来源:EP 1054858; JP 2002503717; US 6197791; WO 9942436

新产品编号:973439

Chemical Name: 5-[4-Methoxy-9(R)-methyl-6,7,8,9-tetrahydro[1,3]dioxolo[4,5-h]isoquinolin-8-ylmethyl]pyrimidine-2,4-diamine
CAS No. 562856-94-4
项目整合开发状态: Biological Testing
项目研究机构: Roche (Orig...
参考文献标题:Novel dihydrofolate reductase inhibitors.Structure-based versus diversity-based library design and high-throughput synthesis and screening
文献作者:Wyss,P.C.; Gerber,P.; Hartman,P.G.; Hubschwerlen,C.; Locher,H.; Marty,H.-P.; Stahl,M.
参考来源:J Med Chem 2003,46(12),2304

AP-2238

Chemical Name: 3-[4-(N-Benzyl-N-methylaminomethyl)phenyl]-6,7-dimethoxy-2H-1-benzopyran-2-one
CAS No. 553681-56-4
项目整合开发状态: Biological Testing
项目研究机构: Universit?degli Studi di Bologna (Origin...
参考文献标题:3-(4-{[Benzyl(methyl)amino]methyl}phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: A dual function lead for Alzheimer's disease therapy
文献作者:Piazzi,L.; Rampa,A.; Bisi,A.; Gobbi,S.; Belluti,F.; Cavalli,A.; Bartolini,M..; Andrisano,V.; Valenti,P.; Recanatini,M.
参考来源:J Med Chem 2003,46(12),2279

新产品编号:903831

Chemical Name: 3(R)-(3,4-Difluorophenyl)-2(S)-(4-fluorophenyl)-4-hydroxy-N-[2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3(S)-yl]butyramide
CAS No. 376582-48-8 (stereoisomer)
项目整合开发状态: Biolog...
参考文献标题:Benzodiazepine derivs.as APP modulators
文献作者:Teall,M.R.; Castro Pineiro,J.L.; Harrison,T.; Owens,A.P.; Guiblin,A.R.; Madin,A.; Williams,S.; Sparey,T.J.; Nadin,A.J.; Churcher,I.; Kerrad,S.(Merck Sharp & Dohme Ltd.)
参考来源:EP 1294702; JP 2003534333; WO 0190084

Campestanol ascorbyl phosphate

Chemical Name: Phosphoric acid [(3beta,5alpha,24R)-ergostan-3-yl] L-ascorbic acid-2-O-yl diester disodium salt; 2-O-[[(3beta,5alpha,24R)-Ergostan-3-O-yl](hydroxy)phosphoryl]-L-ascorbic acid disodium s...
参考文献标题:Conjugates of phytosterol or phytostanol with ascorbic acid and use thereof in treating or preventing cardiovascular disease
文献作者:Chen,H.; Milanova,R.K.; Kutney,J.P.; Hou,D.; Ding,Y.(Forbes Medi-Tech Inc.)
参考来源:JP 2003522124; WO 0100653

Sitostanol ascorbyl phosphate

Chemical Name: Phosphoric acid [(3beta,5alpha,24R)-stigmastan-3-yl] L-ascorbic acid-2-O-yl diester disodium salt; 2-O-[Hydroxy[(3beta,5alpha,24R)-stigmastan-3-O-yl]phosphoryl]-L-ascorbic acid disodium...
参考文献标题:Conjugates of phytosterol or phytostanol with ascorbic acid and use thereof in treating or preventing cardiovascular disease
文献作者:Chen,H.; Milanova,R.K.; Kutney,J.P.; Hou,D.; Ding,Y.(Forbes Medi-Tech Inc.)
参考来源:JP 2003522124; WO 0100653

新产品编号:965529

Chemical Name: 1-O-[2-[N-[4-[(5R,5aR,8aR,9S)-9-[4,6-O-[(1R)-Ethylidene]-beta-D-glucopyranosyloxy]-6-oxo-5,5a,6,8,8a,9-hexahydrofuro[3',4':6,7]naphtho[2,3-d][1,3]dioxol-5-yl]-2,6-dimethoxyphenoxycarbon...
参考文献标题:Derivs.of etoposide and analogs,and pharmaceutical compsns.containing them
文献作者:Monneret,C.; Schmidt,F.(CNRS (Centre National de la Recherche Scientifique); Institut Curie)
参考来源:WO 0335661

Dysinosin A

Chemical Name: Sulfuric acid 2(R)-[N-[1(R)-[(2S,3aR,5S,6S,7aS)-[N-[2-[2-[1-(diaminomethylene)-2,5-dihydro-1H-pyrrol-3-yl]ethyl]carbamoyl]-5,6-dihydroxyperhydroindol-1-ylcarbonyl]-3-methylbutyl]carbamo...
参考文献标题:Total synthesis and structural confirmation of the marine natural product Dysinosin A: A novel inhibitor of thrombin and Factor VIIa
文献作者:Hanessian,S.; Margarita,R.; Hall,A.; Johnstone,S.; Tremblay,M.; Parlanti,L.
参考来源:J Am Chem Soc 2002,124(45),13342

新产品编号:666531

Chemical Name: 2(R),4-Dihydroxy-3,3-dimethyl-N-[2-(N-nonylcarbamoyl)ethyl]butyramide
CAS No. 25303-16-6 (undefined stereoch.)
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKline (Originator)...
参考文献标题:N1-(Substituted) pantothenamides,antimetabolites of pantothenic acid
文献作者:Clifton,G.; Bryant,S.R.; Skinner,C.G.
参考来源:Arch Biochem Biophys 1970,137(2),523