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

SC-53228

(S)-5-(3-(2-羟基乙硫基)-5-甲氧基-4-丙氧基苯基)二氢呋喃-2(3H)-酮Chemical Name: (+)-(S)-3-[7-[3-[2-(Cyclopropylmethyl)-3-methoxy-4-(methylcarbamoyl)phenoxy]propoxy]-8-propyl-3,4-dihydro-2H-1-benzopyran-2-yl]propionic aci...
参考文献标题:Synthesis and pharmacological activity of SC-53228,a leukotriene B4 receptor antagonist with high intrinsic potency and selectivity
文献作者:Yu,S.; Docter,S.; Djuric,S.; et al.
参考来源:Bioorg Med Chem Lett 1994,4(6),811-6

Glaspimod, HP-5 dimer, SK&F-107647

(S)-5-氧代-L-脯氨酰-L-alpha-谷氨酰-L-alpha-天冬氨酰-N8-(5-氨基-1-羧基戊基)-8-氧代-N7-(N-(N-(5-氧代-L-脯氨酰)-L-alpha-谷氨酰)-L-alpha-天冬氨酰)-2,7,8-三氨基辛酰-L-赖氨酸Chemical Name: (2S,7S)-N2,N2'-[2,7-Bis(pyroglutamyl-glutamyl-aspartylami...
参考文献标题:Large-scale synthesis of hematoregulatory nonapeptide SK&F 107647 by fragment coupling
文献作者:Hiebl,J.; Alberts,D.P.; Banyard,A.F.; Baresch,K.; Baumgartner,H.; Bernwieser,I.; Bhatnagar,P.K.; Blanka,M.; Bodenteich,M.; Chen,T.; Esch,P.M.; Kollmann,H.; Lantos,I.; Leitner,K.; Mayrhofer,G.; Patel,R.; Rio,A.; Rovenszky,F.; et al.
参考来源:J Pept Res 1999,54(1),54

PA-824

(S)-6,7-二氢-2-硝基-6-[[4-(三氟甲氧基)苯基]甲氧基]-5H-咪唑并[2,1-B][1,3]恶嗪Chemical Name: 2-Nitro-6(S)-[4-(trifluoromethoxy)benzyloxy]-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine
CAS No. 187235-37-6
项目整合开发状态: Precl...
参考文献标题:Nitroimidazole antibacterial cpds.and methods of use thereof
文献作者:Baker,W.R.; Shaopei,C.; Keeler,E.L.(PathoGenesis Corp.)
参考来源:EP 0866793; JP 1999508270; WO 9701562

Fredericamycin A, NSC-305263, NSC-601617(sodium salt), KFM-A

(S)-6'',7''-二氢-4,9,9''-三羟基-6-甲氧基-3''-[1(E),3(E)-戊二烯基]spiro[2H-苯[f]茚-2,8''-[8H]环戊鼉[g]异喹啉-1,1'',3,5,8(2H)-戊酮Chemical Name: (S)-6',7'-Dihydro-4,9,9'-trihydroxy-6-methoxy-3'-[1(E),3(E)-pentadienyl]spiro[2...
参考文献标题:Asymmetric total synthesis of fredericamycin A
文献作者:Kitagaki,S.; Kita,Y.; Fujioka,H.; Iio,K.; Yoshida,Y.; Higuchi,K.; Akai,S.
参考来源:Angew Chem.Int Ed Engl 1999,38(5),683

Alaptide, VUFB-15754, CPA, c(Acp-Ala)

(S)-8-甲基-6,9-二氮杂螺环[4.5]癸烷-7,10-二酮Chemical Name: Cyclo(1-amino-1-cyclopentanecarbonyl-L-alanyl); 6'(S)-Methyl-2',5'-dioxospiro[cyclopentane-1,3'-piperazine]; 8(S)-Methyl-6,9-diazaspiro[4.5]decane-7,10-...
参考文献标题:2,5-Piperazinedione derivs
文献作者:Kasafirek,E.; Vanzura,J.; Krejci,I.; Krepelka,J.; Dlabac,A.; Valchar,M.(SPOFA - United Pharmaceutical Works)
参考来源:CS 231227; GB 2127807

GYKI-14166, RGH-2958

(S)-D-苯丙氨酰-N-(4-((氨基亚胺甲基)氨基)-1-甲酰基丁基)-L-脯氨酰胺硫酸盐 (1:1)Chemical Name: D-Phenylalanyl-L-prolyl-L-argininal sulfate (1:1); D-Phenylalanyl-N-[4-guanidino-1(S)-formylbutyl]-L-prolinamide sulfate (1:1)
CA...
参考文献标题:RGH-2958
文献作者:Rabloczky,Gy.; Bagdy,D.; Bajusz,S.
参考来源:Drugs Fut 1985,10(10),829

Anatibant mesilate, LF-16-0687MS, LF-16-0687(free base)

(S)-N-(3-(4-氨酰胺基苯甲胺基苯甲胺)丙基)-1-((2,4-二氯-3-(((2,4-二甲基喹啉-8-基)氧)甲基)苯基)磺酰)吡咯氨酸-2-羧酰胺二盐酸盐 (2S)-N-(3-(4-甲脒基苯甲酰胺基)丙基)-1-(2,4-二氯-3-((2,4-二甲基-8-喹啉基氧基)甲基)苯磺酰基)吡咯烷-2-甲酰胺 Chemical Name: N-[3-(4-Amidinobenzamido)p...
参考文献标题:Novel N-benzenesulphonyl-L-proline derivs.,method for preparing and therapeutic use
文献作者:Dodey,P.; Bondoux,M.; Ou,K.; Barth,M.; Houziaux,P.(Fournier Industrie et Sant?
参考来源:EP 0944618; US 6063791; WO 9824783

AR-R17779, AR-R13489(racemate)

(S)-螺[1-氮杂双环[2.2.2]辛烷-3,5'-恶唑啉]-2'-酮 4-氨基甲酰吡啶-3-羧酸酯 (9CI)-螺[1-氮杂双环[2.2.2]辛烷-3,5-噁唑啉]-2-酮Chemical Name: (S)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin]-2'-one
CAS No. 178419-47-1 ((-)-enantiom...
参考文献标题:Spiro-azabicyclic cpds.useful in therapy
文献作者:Murray,R.J.; Gordon,J.C.; Griffith,R.C.; Balestra,M.(AstraZeneca plc)
参考来源:WO 9606098

XA12

(Z)-7-[(1R,2R,3R,5S)-3,5-二羟基-2-[(E)-3-氧代-5-苯基戊-1-烯基]环戊基]庚-5-烯酸丙-2-基酯Chemical Name: 15-Oxo-17-phenyl-18,19,20-trinor-PGF2alpha isopropyl ester; [1R-[1alpha(Z),2beta(E),3alpha,5alpha]]-7-[3,5-Dihydroxy-...
参考文献标题:Phenyl substituted prostaglandin analogs for glaucoma treatment
文献作者:Stjernschantz,J.; Resul,B.
参考来源:Drugs Fut 1992,17(8),691

BGP-15

(Z)-N-(2-羟基-3-(哌啶-1-基)丙氧基)烟酰胺双盐酸盐Chemical Name: N'-[2-Hydroxy-3-(1-piperidinyl)propoxy]pyridine-3-carboxamidine dihydrochloride
CAS No. 66611-37-8 (tautomer)
项目整合开发状态: Discontinued
项目研究机构: N-...
参考文献标题:Improved process for the preparation of amidoxime derivs.
文献作者:Somfai,?; Bert髃,B.; Sz閗ely,I.; Tak醕s,K.; Thurner,A.; Gaj醨y,A.; Bot醨,S.; Nagy,L.(Chinoin Pharmaceutical and Chemical Works Co.,Ltd.)
参考来源:WO 9008131