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

MX-68

Chemical Name: N-[4-(2,4-Diaminopteridin-6-ylmethyl)-3,4-dihydro-2H-1,4-benzothiazin-7-ylcarbonyl]-L-(3'-homo)glutamic acid; 2(S)-[4-(2,4-Diaminopteridin-6-ylmethyl)-3,4-dihydro-2H-1,4-benzothiazin-7-...
参考文献标题:Antirheumatic agents: Novel methotrexate derivatives bearing a benzoxazine or benzothiazine moiety
文献作者:Matsuoka,H.; Ohi,N.; Mihara,M.; Suzuki,H.; Miyamoto,K.; Maruyama,N.; Tsuji,K.; Kato,N.; Akimoto,T.; Takeda,Y.; Yano,K.; Kuroki,T.
参考来源:J Med Chem 1997,40(1),105

SIB-1663, S-1663

Chemical Name: 7-Methoxy-2,3,3a,4,5,9b-hexahydro-1H-pyrrolo[3,2-h]isoquinoline
CAS No. 179064-11-0
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Originator)
合成路线:Alkylation of isoquinolone (I...
参考文献标题:Conformationally restricted analogues of nicotine and anabasine
文献作者:Vernier,J.-M.; Holsenback,H.; Cosford,N.D.; Whitten,J.P.; Menzaghi,F.; Reid,R.; Rao,T.S.; Sacaan,A.I.; Lloyd,G.K.; Suto,C.M.; Chavez-Noriega,L.E.; Washburn,M.S.; Urrutia,A.; McDonald,I.A.
参考来源:Bioorg Med Chem Lett 1998,8(16),2173-2178

Involucratine, Saussureamine B

Chemical Name: 1-[(3R,3aS,9bS)-6,9-Bismethylene-2-oxoperhydroazulene[4,5-b]furan-3-ylmethyl]pyrrolidine-2(S)-carboxylic acid
CAS No. 126209-82-3
项目整合开发状态: Biological Testing
项目研究机构: Kuraray (...
参考文献标题:Absolute stereostructures and syntheses of saussureamines A,B,C,D and E,amino acid-sesquiterpene conjugates with gastroprotective effect,from the roots of Saussurea lappa
文献作者:Matsuda,H.; et al.
参考来源:Tetrahedron 2000,56(39),7763

Saussureamine C

Chemical Name: (-)-N2-[(3R,3aS,9bS)-6,9-Bismethylene-2-oxoperhydroazulene[4,5-b]furan-3-ylmethyl]-L-asparagine
CAS No. 148245-83-4
项目整合开发状态: Biological Testing
项目研究机构: Kuraray (Originator) 参考文献标题:Absolute stereostructures and syntheses of saussureamines A,B,C,D and E,amino acid-sesquiterpene conjugates with gastroprotective effect,from the roots of Saussurea lappa
文献作者:Matsuda,H.; et al.
参考来源:Tetrahedron 2000,56(39),7763

Saussureamine D

Chemical Name: (+)-1-[(3R,3aS,5aR,6R,9bS)-6-Hydroxy-5a,9-dimethyl-2-oxo-2,3,3a,4,5,5a,6,7,9a,9b-decahydronaphtho[1,2-b]furan-3-ylmethyl]pyrrolidine-2(S)-carboxylic acid
CAS No. 148225-51-8
项目整合开...
参考文献标题:Absolute stereostructures and syntheses of saussureamines A,B,C,D and E,amino acid-sesquiterpene conjugates with gastroprotective effect,from the roots of Saussurea lappa
文献作者:Matsuda,H.; et al.
参考来源:Tetrahedron 2000,56(39),7763

Saussureamine E

Chemical Name: 1-[(3R,3aS,5aR,6R,9bS)-6-Hydroxy-5a-methyl-9-methylene-2-oxoperhydronaphtho[1,2-b]furan-3-ylmethyl]pyrrolidine-2(S)-carboxylic acid
CAS No. 148225-52-9
项目整合开发状态: Biological Testin...
参考文献标题:Absolute stereostructures and syntheses of saussureamines A,B,C,D and E,amino acid-sesquiterpene conjugates with gastroprotective effect,from the roots of Saussurea lappa
文献作者:Matsuda,H.; et al.
参考来源:Tetrahedron 2000,56(39),7763

Sch-69956 [(-)-(S)-isomer], Sch-69955 [(+)-(R)-isomer], Sch-54429

Chemical Name: (?-8-Chloro-11-[4-[2-(4-pyridyl)acetyl]piperazin-1-yl]-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
CAS No. 169250-83-3
项目整合开发状态: Preclinical
项目研究机构: Schering-Plough (Or...
参考文献标题:Novel nojirimycin derivs.
文献作者:Lesur,B.; Ducep,J.-B.; Danzin,C.(Merrell Pharmaceuticals,Inc.)
参考来源:EP 0453692; EP 0454580; JP 1993086072; US 5252587; US 5536732

CGS-30440

Chemical Name: N-[1-[2(S)-(Acetylsulfanyl)-3-methylbutyramido]cyclopent-1-ylcarbonyl]-4-O-methyl-L-tyrosine ethyl ester
CAS No. 169319-62-4, 169320-23-4 ((R)-isomer)
项目整合开发状态: Preclinical
项目研...
参考文献标题:Mercaptoacyl dipeptides as orally active dual inhibitors of angiotensin-converting enzyme and neutral endopeptidase
文献作者:Fink,C.A.; Carlson,J.E.; McTaggart,P.A.; Qiao,Y.; Webb,R.; Chatelain,R.; Jeng,A.Y.; Trapani,A.J.
参考来源:J Med Chem 1996,39(16),3158

AGN-192093

Chemical Name: 1-Deoxoprostaglandin F2alpha 9,11-O-cyclic carbonate
CAS No. 159359-95-2
项目整合开发状态: Biological Testing
项目研究机构: Allergan (Originator)
合成路线:The esterification of prostaglandin ...
参考文献标题:7-[Carboxyalkyl or alkenyl]-6-[alkyl or alkenyl]3-oxo-2,4-dioxobicyclo[3.2.1]octane and derivs.thereof
文献作者:Burk,R.M.; Krauss,A.H.; Woodward,D.F.(Allergan,Inc.)
参考来源:EP 0737185; JP 1997507229; US 5416106; WO 9518103

E-1010, ER-35786

Chemical Name: (1R,5S,6S)-6-[1(R)-Hydroxymethyl]-2-[2(S)-[1(R)-hydroxy-1-[pyrrolidin-3(R)-yl]methyl]pyrrolidin-4(S)-ylsulfanyl]-1-methyl-1-carba-2-penem-3-carboxylic acid monohydrochloride
CAS No. ...
参考文献标题:2-(Substd.pyrrolidinylthio)carbapenem derivs
文献作者:Nakagawa,S.; Ohtake,N.; Nakano,F.; Yamada,K.; Ushijima,R.; Murase,S.; Fukatsu,H.(Banyu Pharmaceutical Co.,Ltd.)
参考来源:EP 0449191; JP 1992321688; US 5373002; US 5374720; US 5438054; WO 9114687