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

PNU-177496

Chemical Name: 2-[4-[2(S)-[3-[1(S)-Carboxy-2-phenylethyl]ureido]-2-(N-pentylcarbamoyl)ethyl]phenoxy]malonic acid
CAS No. 221076-63-7
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator) 参考文献标题:Inhibitors of protein tyrosine phosphatase
文献作者:Bleasdale,J.; May,P.D.; Schostarez,H.J.; Barf,T.; Larsen,S.D.; Liljebris,C.(Pharmacia Corp.)
参考来源:WO 9911606

SUN-C8257

Chemical Name: 2-Amino-4-(7-chloro-2,4-dioxo-1,2,3,4-tetrahydroquinazolin-3-ylsulfonyl)benzoic acid
CAS No. 259536-74-8, 259536-75-9 (Na salt)
项目整合开发状态: Preclinical
项目研究机构: Daiichi Suntory Ph...
参考文献标题:Quinazoline derivs.and pharmaceutical application thereof
文献作者:Ito,A.; Fukami,H.; Imajo,S.(Suntory Ltd.)
参考来源:EP 1114035; JP 2002523404; WO 0010982

SM-130686

Chemical Name: (+)-3(S)-(2-Chlorophenyl)-1-[2-(diethylamino)ethyl]-3-hydroxy-2-oxo-4-(trifluoromethyl)-2,3-dihydro-1H-indole-6-carboxamide hydrochloride
CAS No. 259666-71-2 (free base), 259667-25-9...
参考文献标题:Oxindole derivs.as growth hormone releasers
文献作者:Okazaki,K.; Kumagai,K.; Tokunaga,T.; Ueki,Y.; Nagata,R.; Umezome,T.; Hume,W.E.(Sumitomo Pharmaceuticals Co.,Ltd.)
参考来源:EP 1105376; JP 2002523400; WO 0010975

RPR-208566

Chemical Name: 2(R)-(3-Amidinobenzyl)-3(R)-(3',4'-dimethoxybiphenyl-4-ylcarboxamido)butyric acid methyl ester trifluoroacetate
CAS No. 219672-61-4, 219672-60-3 (free base)
项目整合开发状态: Preclinical<...
参考文献标题:Substd.N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides
文献作者:Gong,Y.; Guertin,K.R.; McGarry,D.G.; Pauls,H.W.; Klein,S.I.; Spada,A.P.(Aventis Pharmaceuticals,Inc.)
参考来源:CA 2264556; EP 0931060; WO 9900356

YJA-20379-2

Chemical Name: N-[4,5-Dihydropyrido[3',2':4,5]imidazo[1,2-a][1,3]thiazolo[4,5-c]pyridin-2-yl]-N,N-dimethylamine hydrobromide
CAS No. 188954-24-7, 187743-25-5 (free base)
项目整合开发状态: Preclinical 参考文献标题:Benz- or pyrido-imidazole derivs.
文献作者:Chang,M.S.; Chung,K.J.; Park,S.H.; Kim,Y.H.; Kim,K.B.; Choi,W.S.; Kim,S.G.; Lee,J.M.; Seo,K.H.; Yoo,H.Y.; Paek,J.H.; Kang,D.P.(Yung-Jin Pharmaceutical Co.,Ltd.)
参考来源:WO 9703077

CNS-5655(racemate), CNS-5788

Chemical Name: (+)-N1-[2-Chloro-5-(methylsulfanyl)phenyl]-N3-methyl-N3-[3-[(R)-methylsulfinyl]phenyl]guanidine
CAS No. 222734-66-9, 222734-67-0 (acetate), 222734-64-7 (enantiomer), 222734-69-2 (rac...
参考文献标题:Pharmaceutically active cpd.and methods of use
文献作者:Durant,G.J.; Fischer,J.B.; Perlman,M.; Padmanabhan,S.(Cambridge NeuroScience,Inc.)
参考来源:WO 9918962

SQ-311

Chemical Name: 1-(1-Aminoisoquinolin-7-yl)-N-(2'-sulfamoylbiphenyl-4-yl)-3-methyl-1H-pyrazole-5-carboxamide
CAS No. 218297-83-7, 218299-31-1 (methanesulfonate), 218300-55-1 (trifluoroacetate)
项目...
参考文献标题:Novel guanidine mimics as factor Xa inhibitors
文献作者:Quan,M.L.; Clark,C.G.; Lam,P.Y.; Pinto,D.J.-P.; Han,Q.; Fevig,J.M.; Li,R.; Pruitt,J.R.; Dominguez,C.(DuPont Pharmaceuticals Co.)
参考来源:EP 0991638; WO 9857951

SQ-315

Chemical Name: 1-(1-Aminoisoquinolin-7-yl)-3-methyl-N-(2'-methylsulfonylbiphenyl-4-yl)-1H-pyrazole-5-carboxamide
CAS No. 218297-85-9, 218299-32-2 (methanesulfonate)
项目整合开发状态: Preclinical
项目研究...
参考文献标题:Novel guanidine mimics as factor Xa inhibitors
文献作者:Quan,M.L.; Clark,C.G.; Lam,P.Y.; Pinto,D.J.-P.; Han,Q.; Fevig,J.M.; Li,R.; Pruitt,J.R.; Dominguez,C.(DuPont Pharmaceuticals Co.)
参考来源:EP 0991638; WO 9857951

RWJ-314313

Chemical Name: 4-[2-Chloro-5-[3(R)-pyrrolidinyloxy]pyridin-3-yl]benzonitrile
CAS No. 259262-24-3
项目整合开发状态: Biological Testing
项目研究机构: R.W. Johnson (Originator)
合成路线:Mitsunobu coupling of N...
参考文献标题:Pyridyl ethers and thioethers as ligands for nicotinic acetylcholine receptor and its therapeutic application
文献作者:Jung,S.L.(Ortho-McNeil Pharmaceutical,Inc.)
参考来源:WO 0010997

FR-177995

Chemical Name: 2,6-Dichloro-N-[1-[2-(4-morpholinyl)-2-oxoethyl]-2-(trifluoromethyl)-1H-benzimidazol-4-yl]benzamide
CAS No. 189043-21-8
项目整合开发状态: Preclinical
项目研究机构: Fujisawa (Originator)
合...
参考文献标题:Benzimidazole derivs.and their use in the prevention and/or the treatment of bone diseases
文献作者:Oku,T.; Kawai,Y.; Yatabe,T.; Sato,S.; Yamazaki,H.; Kayakiri,N.; Yoshihara,K.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0863881; JP 1999513364; WO 9710219