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:623817

Chemical Name: trans-6-Acetamido-5-guanidino-1-(2-ethylbutanoyl)-1,4,5,6-tetrahydropyridazine-3-carboxylic acid
CAS No. 240143-65-1
项目整合开发状态: Biological Testing
项目研究机构: Gilead (Originator), R...
参考文献标题:Synthesis and evaluation of 1,4,5,6-tetrahydropyridazine derivatives as influenza neuraminidase inhibitors
文献作者:Zhang,L.; Williams,M.A.; Mendel,D.B.; Escarpe,P.A.; Chen,X.; Wang,K.Y.; Graves,B.J.; Lawton,G.; Kim,C.U.
参考来源:Bioorg Med Chem Lett 1999,9(13),1751

L-165666

Chemical Name: 1-(2-Methylalanyl-D-tryptophyl)-3-(4-thiazolylmethyl)piperidine-3(S)-carboxylic acid ethyl ester
CAS No. 170842-63-4, 176525-44-3 (monoHCl)
项目整合开发状态: Preclinical
项目研究机构: Merck ...
参考文献标题:Piperidines,pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
文献作者:Morriello,G.J.; Patchett,A.A.; Yang,L.; Chen,M.H.; Nargund,R.(Merck & Co.,Inc.)
参考来源:EP 0739204; US 5492916; US 5492920; US 5494919; WO 9513069

新产品编号:134979

Chemical Name: 4-[2-(2-Cyclopentylethyl)-5-oxazolyl]-N-[4-[2-[2(R)-hydroxy-2-(3-pyridinyl)ethylamino]ethyl]phenyl]benzenesulfonamide
CAS No. 173902-04-0, 173900-95-3 (undefined isomer)
项目整合开发状态:...
参考文献标题:Substd.sulfonamides as selective beta3 agonists for the treatment of diabetes and obesity
文献作者:Fisher,M.H.; Naylor,E.M.; Ok,D.; Weber,A.E.; Shih,T.; Ok,H.(Merck & Co.,Inc.)
参考来源:EP 0757674; JP 1997512275; US 5541197; US 5561142; WO 9529159

新产品编号:365951

Chemical Name: 4(S)-(Cyclopropylethynyl)-6-methoxy-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one
CAS No. 205754-67-2 (undefined isomer)
项目整合开发状态: Biological Testing
项目研究机构: Bristol-...
参考文献标题:Synthesis and evaluation of analogs of efavirenz (Sustiva(TM)) as HIV-1 reverse transcriptase inhibitors
文献作者:Patel,M.; Ko,S.S.; McHugh,R.J.Jr.; Markwalder,J.A.; Srivastava,A.S.; Cordova,B.C.; Klabe,R.M.; Erickson-Vittanen,S.; Trainor,G.L.; Seitz,S.P.
参考来源:Bioorg Med Chem Lett 1999,9(19),2805

L-780945, SNAP-6991-(+), (+)-SNAP-6991

Chemical Name: (+)-3-[N-[2-[N-(cis-4-Cyano-4-phenylcyclohexyl)amino]ethyl]carbamoyl]-4-(3,4-difluorophenyl)-6-(methoxymethyl)-2-oxo-1,2,3,4-tetrahydro-5-pyrimidinecarboxylic acid methyl ester
CAS N...
参考文献标题:Dihydropyrimidines and uses thereof
文献作者:Nagarathnam,D.; Wong,W.C.; Miao,S.W.; Patane,M.A.; Gluchowski,C.(Merck & Co.,Inc.; Synaptic Pharmaceutical Corp.)
参考来源:EP 0866708; JP 2000500470; WO 9717969

新产品编号:971857

Chemical Name: 4-Chloro-N'-(4-methylphenyl)benzohydrazide
CAS No. 54812-59-8
项目整合开发状态: Biological Testing
项目研究机构: R.W. Johnson (Originator)
合成路线:The title hydrazide was prepared from 4-chl...
参考文献标题:1,3-Diarylcycloalkano-[1,2-d]-pyrazoles and diphenyl hydrazides as selective inhibitors of cyclooxygenase-2
文献作者:Sui,Z.; et al.
参考来源:217th ACS Natl Meet (March 21 1999,Anaheim) 1999,Abst MEDI 202

CP-199331

Chemical Name: N-[3-[6-(5,6-Difluoro-1,3-benzothiazol-2-ylmethoxy)-4(R)-hydroxy-3,4-dihydro-2H-1-benzopyran-3(R)-ylmethyl]-4-methoxyphenyl]trifluoromethanesulfonamide
CAS No. 158102-93-3
项目整合开发状...
参考文献标题:Discovery of CP-199,330 and CP-199,331: Two potent and orally efficacious cysteinyl LT1 receptor antagonists devoid of liver toxicity
文献作者:Chambers,R.J.; Marfat,A.; Antognoli,G.W.; Cheng,J.B.; Damon,D.B.; Kuperman,A.V.; Liston,T.C.; Mebus,C.; Pillar,J.S.; Shirley,J.T.; Watson,J.W.
参考来源:Bioorg Med Chem Lett 1999,9(18),2773

新产品编号:89101

Chemical Name: 1(R)-[3-(Cyclopentyloxy)-4-methoxyphenyl]-3(S)-(3-methyl-1,2,4-oxadiazol-5-yl)cyclohexanecarbonitrile
CAS No. 162101-90-8 (cis-isomer)
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithK...
参考文献标题:Use of glucokinase inhibitors for the manufacture of a medicament for treating tumours
文献作者:Board,M.; Newsholme,E.A.(Isis Pharmaceuticals,Inc.)
参考来源:WO 9503809

GPI-1234

Chemical Name: 1-(3,3-Dimethyl-2-oxopentanoyl)pyrrolidine-2(S)-carbothioic acid S-(3,3-diphenylpropyl) ester
CAS No. 205388-30-3
项目整合开发状态: Preclinical
项目研究机构: Guilford Pharmaceuticals (Origin...
参考文献标题:Heterocyclic thioesters and ketones
文献作者:Hamilton,G.S.; Li,J.-H.(Guilford Pharmaceuticals Inc.)
参考来源:EP 0934263; US 5786378; US 5990131; WO 9813343

新产品编号:397591

Chemical Name: 2-Oxo-N-[1(R)-Phenylethyl]-4-(2-pyridinylmethylsulfanyl)azetidine-1-carboxamide
CAS No. 210492-77-6
项目整合开发状态: Biological Testing
项目研究机构: Boehringer Ingelheim (Originator)
合成...
参考文献标题:Inhibition of human cytomegalovirus protease N(o) with monocyclic beta-lactams
文献作者:D閦iel,R.; Malenfant,E.
参考来源:Bioorg Med Chem Lett 1998,8(11),1437