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

Tosifen, Sch-11973

Chemical Name: 4-Methyl-N-[N-[1(S)-methyl-2-phenylethyl]carbamoyl]benzenesulfonamide
CAS No. 32295-48-0
项目整合开发状态: Not Determined
项目研究机构:
合成路线:It can be prepared in several different ways:...
参考文献标题:
文献作者:Zitowitz,L.; et al.
参考来源:AU 321930; CA 976188; CH 580579; DE 2042230; FR 2068521; GB 1308210; ZA 7005866

S-34730-1

Chemical Name: (7-Chloro-2-oxo-6-sulfamoyl-1,2-dihydroquinolin-3-yl)phosphonic acid
CAS No. 355408-08-1
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator)
合成路线:Acylation of 2-amino-4-chlor...
参考文献标题:Derivs.of 6-sulfamoyl-3-quinolyl phosphonic acids,process for their preparation and pharmaceutical compsns.containing them
文献作者:Lestage,P.; Cordi,A.; Desos,P.(ADIR et Cie.)
参考来源:EP 1125941; FR 2805260; JP 2001253892; US 6518258

新产品编号:739303

Chemical Name: 2,3-Dimethoxy-6-[4-[4-(trifluoromethyl)phenoxy]piperidin-1-ylsulfonyl]benzohydroxamic acid
CAS No. 279221-23-7
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:Couplin...
参考文献标题:Hydroxamic acid derivs.as matrix metalloprotease inhibitors
文献作者:Villamil,C.I.; Becker,D.P.; Bedell,L.J.; Freskos,J.N.; Rao,S.N.; Getman,D.P.; Decrescenzo,G.A.; Mischke,B.V.; Barta,T.E.; McDonald,J.J.(Pharmacia Corp.)
参考来源:EP 1177173; WO 0069819

Calebin A

Chemical Name: 3-(4-Hydroxy-3-methoxyphenyl)-2-propenoic acid 4-(4-hydroxy-3-methoxyphenyl)-2-oxo-3-butenyl ester
CAS No. 336784-82-8 (E-isomer)
项目整合开发状态: Biological Testing
项目研究机构: Universit...
参考文献标题:Pharmaceutical compsns.useful in the prevention and treatment of beta-amyloid protein-induced disease
文献作者:Kim,D.S.H.L.(University of Illinois)
参考来源:WO 0130335

ER-129517

Chemical Name: 3-[4-[2-[3-(Methylsulfonyl)thien-2-yl]ethyl]piperidin-1-ylmethyl]pyridin-2(1H)-one
CAS No. 351407-14-2
项目整合开发状态: Preclinical
项目研究机构: Eisai (Originator)
合成路线:The reaction of ...
参考文献标题:Novel piperidine cpds.and drugs containing the same
文献作者:Kaneko,T.; Sawada,K.; Takahashi,Y.; Kato,K.; Ohkubo,M.; Ozaki,F.; Miyazaki,K.; Kobayashi,K.; Matsukura,M.; Suzuki,H.; Ishihara,H.; Yoshida,I.; Kamata,J.; Yoshinaga,T.; Tabata,M.; Onogi,T.(Eisai Co.,Ltd.)
参考来源:EP 1254904; JP 2001270883; WO 0153288

KR-31378

Chemical Name: N-[6-Amino-2-(dimethoxymethyl)-3(S)-hydroxy-2(S)-methyl-3,4-dihydro-2H-1-benzopyran-4(R)-yl]-N'-benzyl-N''-cyanoguanidine
CAS No. 335381-99-2, 335381-85-6 (diastereomer), 335381-86-7...
参考文献标题:Benzopyranyl guanidine derivs.,process for preparation thereof,and pharmaceutical compsns.containing them
文献作者:Jang,D.S.; Kim,S.-O.; Hwang,S.K.; Suh,J.H.; Park,Y.S.; Lee,B.H.; Lee,S.K.; Seo,H.W.; Yi,K.-Y.; Lim,H.; Namkoog,M.A.; Cho,I.S.; Kim,N.-J.; et al.(Dongbu Hannong Chemical Co.Ltd.; Korea Research Institute of Chemical Technology)
参考来源:US 6323238; WO 0129023

新产品编号:772525

Chemical Name: (+)-(22E,24E)-25-(tert-Butylsulfonyl)-1alpha-hydroxy-22,23,24,25-tetradehydro-26,27-dinorvitamin D3
CAS No. 300344-76-7, 300344-75-6 (diastereomer)
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Non-calcemic,antiproliferative,transcriptionally active sulfur-containing analogs of 1alpha,25-dihydroxyvitamin D3
文献作者:Lee,J.K.; Crawford,K.R.; Wang,Q.; Posner,G.H.; Han,G.(Johns Hopkins University)
参考来源:US 6380408; WO 0059513

XR-11211

Chemical Name: (Z,Z)-8-[4-[3,6-Dioxo-5-[4-(thien-2-ylcarboxamido)benzylidene]piperazin-2-ylidenemethyl]phenoxy]octanoic acid
CAS No. 386212-69-7
项目整合开发状态: Biological Testing
项目研究机构: Xenova (O...
参考文献标题:Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1
文献作者:Folkes,A.; Roe,M.B.; Sohal,S.; Golec,J.; Faint,R.; Brooks,T.; Charlton,P.
参考来源:Bioorg Med Chem Lett 2001,11(19),2589

CP-664511

Chemical Name: 3-[3-[1(S)-[2-[3-Methoxy-4-[3-(2-methylphenyl)ureido]phenyl]acetamido]-3-methylbutyl]isoxazol-5-yl]propionic acid
CAS No. 379692-00-9, 253347-08-9 (racemate)
项目整合开发状态: Preclinical...
参考文献标题:Isoxazolyl,oxazolyl,and thiazolylpropionic acid derivatives as potent alpha4beta1 integrin antagonists
文献作者:Duplantier,A.J.; Beckius,G.E.; Chambers,R.J.; Chupak,L.S.; Jenkinson,T.H.; Klein,A.S.; Kraus,K.G.; Kudlacz,E.M.; McKechney,M.W.; Pettersson,M.P.; Whitney,C.A.; Milici,A.J.
参考来源:Bioorg Med Chem Lett 2001,11(19),2593

新产品编号:679187

Chemical Name: 2(S)-[5-[2-(2-Azabicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxoethyl]-2-(3,5-dimethylphenyl)-1H-indol-3-yl]-N-[2-(4-pyridyl)ethyl]propan-1-amine
CAS No. 255863-81-1
项目整合开发状态: Preclini...
参考文献标题:Antagonists of gonadotropin releasing hormone
文献作者:Chu,L.; Wyvratt,M.J.; Ponpipom,M.M.; Lin,P.; Ashton,W.T.; Goulet,M.; Young,J.; Girotra,N.N.; Fisher,M.H.(Merck & Co.,Inc.)
参考来源:EP 1095038; WO 0004013