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

T-440

Chemical Name: 4-[6,7-Diethoxy-2,3-bis(hydroxymethyl)naphthalen-1-yl]-1-(2-methoxyethyl)pyridin-2(1H)-one
CAS No. 155043-84-8
项目整合开发状态: Preclinical
项目研究机构: Tanabe Seiyaku (Originator)
合成路线...
参考文献标题:Naphthalene derivs.processes for preparing the same,and synthetic intermediates thereof
文献作者:Iwasaki,T.; Kondo,K.; Ikezawa,K.; Kikkawa,H.; Yamagata,S.(Tanabe Seiyaku Co.,Ltd.)
参考来源:EP 0557016; JP 1993229987; US 5342941

MF-8622

Chemical Name: N-[4-(4-Morpholinyl)butyl]carbamic acid 3-[2-(dimethylamino)-1,1-dimethylethyl]phenyl ester bitartrate
CAS No. 177338-89-5 (free base)
项目整合开发状态: Preclinical
项目研究机构: Mediolanum ...
参考文献标题:Phenylcarbamate derivs.suitable to the use as anticholinesterase substances
文献作者:Terni,P.; Mairani,L.; Mandelli,G.; Pagella,P.G.; Marchesini,D.; Maiorana,S.; Brufani,M.(Mediolanum Farmaceutici)
参考来源:EP 0772608; US 5869484; WO 9602524

ER-40121

Chemical Name: (3R,6S,9R,9aR)-9-Methyl-6-[3(S)-methyl-2(S)-sulfanylpentanamido]-5-oxooctahydrothiazolo[3,2-a]azepine-3-carboxylic acid
CAS No. 177566-01-7, 177359-23-8 (diastereomer)
项目整合开发状态: P...
参考文献标题:Substd.thiazolo[3,2-alpha]azepine deriv.
文献作者:Oinuma,H.; Suda,S.; Yoneda,N.; Kotake,M.; Mizuno,M.; Matsuhima,T.; Fukuda,Y.; Saito,M.; Matsuoka,T.; Adachi,H.; Namiki,M.; Sudo,T.; Miyake,K.; Okita,M.(Eisai Co.,Ltd.)
参考来源:EP 0719779; JP 1996027156; JP 1996059672; JP 1996165293; US 5789403; WO 9602549

FJ-776(formerly), SDZ-MKT-077, MKT-077

Chemical Name: 1-Ethyl-2-[3-ethyl-5-(3-methyl-2,3-dihydrobenzothiazolin-2-ylidene)-4-oxothiazolidin-2-ylidenemethyl]pyridinium chloride
CAS No. 147366-41-4
项目整合开发状态: Phase II
项目研究机构: Dana-Far...
参考文献标题:Compsn.and method for treating cancer
文献作者:Shishido,T.; Chen,L.B.(Dana-Farber Cancer Institute; Fuji Photo Film Co.,Ltd.)
参考来源:EP 0527494; US 5360803

L-NIL-TA, SC-51

Chemical Name: 2(S)-Amino-6-(1-iminoethylamino)-N-(1H-tetrazol-5-yl)hexanamide dihydrochloride; N6-(1-Iminoethyl)-N1-(1H-tetrazol-5-yl)-L-lysinamide dihydrochloride
CAS No. 179337-70-3, 179337-79-2...
参考文献标题:Aminotetrazole derivs.useful as nitric oxide synthase inhibitors
文献作者:Hallinan,E.A.; Hansen,D.W.Jr.; Tsymbalov,S.(Pharmacia Corp.)
参考来源:EP 0790987; EP 1113011; JP 1998508847; US 5684008; WO 9615120

NSC-716976, BNP-7787, Tavocept, Mesna disulfide, Dimesna

Chemical Name: 2,2'-Dithiobis(ethanesulfonic acid) disodium salt
CAS No. 16208-51-8
项目整合开发状态: Phase III
项目研究机构: BioNumerik (Originator), Takeda (Marketer), Baxter Oncology (Licensee), Grelan ...
参考文献标题:Compsn.of cisplatin in combination with 2,2'-dithio-bis(ethanesulfonate) (dimesna)
文献作者:Haridas,K.; Reddy,D.G.; Murali,D.; Hausheer,F.H.(BioNumerik Pharmaceuticals,Inc.)
参考来源:WO 9614852

RS-57067-000

Chemical Name: 6-[5-(4-Chlorobenzoyl)-1,4-dimethylpyrrol-2-ylmethyl]pyridazin-3(2H)-one
CAS No. 179382-91-3
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator)
合成路线:The methylation of zomepir...
参考文献标题:Pyrrole derivs.
文献作者:Barnett,J.W.; Dunn,J.P.; Kertesz,D.J.; Miller,A.B.; Morgans,D.J.Jr.; Ramesha,C.S.; Sigal,C.E.; Sjogren,E.B.; Smith,D.B.; Talamas,F.X.(F.Hoffmann-La Roche AG)
参考来源:CA 2163490; EP 0714895; JP 1996208639

新产品编号:165037

Chemical Name: 4-[5,5-Dimethyl-8(RS)-[2(RS)-tetrahydropyranyloxy]-5,6,7,8-tetrahydronaphth-2-ylethynyl]benzoic acid
CAS No. 180919-94-2
项目整合开发状态: Preclinical
项目研究机构: Allergan (Originator)
...
参考文献标题:A new class of RAR subtype selective retinoids: Co
文献作者:Vuligonda,V.; Lin,Y.; Thacher,S.M.; Standeven,A.M.; Kochar,D.M.; Chandraratna,R.A..
参考来源:Bioorg Med Chem 1999,7(2),263

Khafrefungin

Chemical Name: 2(S),3(S),5-Trihydroxy-4(R)-[11(R)-hydroxy-2,4(R),6,8,10(S),12(S)-hexamethyl-5-oxodocosa-2(E),6(E),8(E)-trienoyloxy]pentanoic acid
CAS No. 180992-28-3
项目整合开发状态: Biological Testing...
参考文献标题:Total synthesis and structural elucidation of khafrefungin
文献作者:Wakabayashi,T.; Mori,K.; Kobayashi,S.
参考来源:J Am Chem Soc 2001,123(7),1372

新产品编号:146053

Chemical Name: (2R,4R)-4-Amino-1-(1-napthylmethyl)pyrrolidine-2,4-dicarboxylic acid
CAS No. 178415-88-8
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator)
合成路线:The esterification of (...
参考文献标题:Synthesis of the four isomers of 4-aminopyrrolidine-2,4-dicarboxylate: Identification of a potent,highly selective,and systemically-active agonist for metabotropic glutamate receptors negatively coupled to adenylate cyclase
文献作者:Monn,J.A.; Valli,M.J.; Johnson,B.G.; Salhoff,C.R.; Wright,R.A.; Howe,T.J.; Bond,A.; Lodge,D.; Spangle,L.A.; Paschal,J.W.; Campbell,J.B.; Griffey,K.; Tizzano,J.P.; Schoepp,D.D.
参考来源:J Med Chem 1996,39(15),2990