其它产品项目整合

项目整合的本质是一项集合成方法学、反应工程学与过程分析技术于一体的系统工程。其核心逻辑可以概括为以下几点：源头优选：利用如N-硝胺化学等底层方法学突破，从分子层面颠覆传统高成本、高污染路线。过程强化：依托连续流技术，攻克有机金属试剂应用、光化学反应放大等“不可能”任务，实现高危工艺的本质安全。系统集成：整合“反应-淬灭-分离”全流程，利用微流控与在线分析技术，消除批次间的差异，实现药品制造的连续化与智能化。当前，中间体工艺研发正在经历从“经验驱动”向“数据驱动”的转变。AI辅助路线设计、自动化高通量筛选与连续制造平台的结合，将使得“分子结构与最优工艺路径”之间的映射关系逐渐清晰。未来的竞争优势，将属于那些能够将底层化学创新与先进工程技术进行无缝整合的研发体系。
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其它产品项目整合

Mofezolac CAS Registry Number: 78967-07-4 莫非佐酸

CAS Name: 3,4-Bis(4-methoxyphenyl)-5-isoxazoleacetic acid
Additional Names: 3,4-di(p-methoxyphenyl)-5-isoxazoleacetic acidPercent Composition: C 67.25%, H 5.05%, N 4.13%, O 23.57%
Literature References: Prostaglandin biosynthetase inhibitor. Prepn: R. G. Micetich et al., EP 26928; eidem, US 4327222 (1981, 1982 both to CDC Life Sci.). Physico-chemical properties: T. Ushio et al., Iyakuhin Kenkyu 22, 892 (1991). HPLC determn in plasma and urine: T. Marunaka, M. Maniwa, J. Chromatogr. 422, 227 (1987). Pharmacology: K. Tanaka et al., Yakuri to Chiryo 18, 3347 (1990), C.A. 114, 135911 (1991). Acute toxicity: K. Satoh et al., J. Toxicol. Sci. 15, Suppl 2, 1 (1990).

Rioprostil CAS Registry Number: 77287-05-9 利奥前列素

CAS Name: (11a,13E)-1,11,16-Trihydroxy-16-methylprost-13-en-9-one
Additional Names: (2R,3R,4R)-4-hydroxy-2-(7-hydroxyheptyl)-3-[(E)-(4RS)-(4-hydroxy-4-methyl-1-octenyl)]cyclopentanone; 16-methy...
Literature References: Prostaglandin E1 analog with cytoprotective and gastric antisecretory activity. Prepn: H. C. Kluender et al., US 4132738 (1979 to Miles). Pharmacology: D. A. Shriver et al., Arzneim.-Forsch. 35, 839 (1985). Effect on human gastric secretion: P. Demol et al., ibid. 861; B. Vaona et al., Adv. Prostaglandin Thromboxane Leukotriene Res. 17, 328 (1987). Clinical evaluation in duodenal ulcer: H. G. Dammann et al., ibid. 303.

Enprostil CAS Registry Number: 73121-56-9 恩前列素

CAS Name: rel-7-[(1R,2R,3R)-3-Hydroxy-2-[(1E,3R)-3-hydroxy-4-phenoxy-1-butenyl]-5-oxocyclopentyl]-4,5-heptadienoic acid methyl ester
Additional Names: (dl)-9-keto-11a,15a-dihydroxy-16-phenoxy-1...
Literature References: Prostaglandin E2 derivative with antisecretory activity. Prepn: A. R. Van Horn et al., US 4178457 (1979 to Syntex). Pharmacokinetics: D. R. Stanski et al., Clin. Pharmacol. Ther. 31, 273 (1982). Cytoprotective effect against aspirin-induced gastromucosal injury in humans: M. M. Cohen et al., Gastroenterology 88, 382 (1985). Clinical comparison with cimetidine of antisecretory and antigastrin activity in duodenal ulcer: V. Mahachai et al., ibid. 89, 555 (1985); of efficacy in ulcer healing: L. Carling et al., Scand. J. Gastroenterol. 22, 325 (1987). Series of articles on pharmacology, clinical efficacy and safety: Am. J. Med. 81, Suppl. 2A, 1-88 (1986).

Nimesulide CAS Registry Number: 51803-78-2 尼美舒利

CAS Name: N-(4-Nitro-2-phenoxyphenyl)methanesulfonamide
Additional Names: 4-nitro-2-phenoxymethanesulfonanilideTrademarks: Aulin (Boehringer, Mann.); Fansidol (Brocchieri); Flogovital (Bago); M...
Literature References: Prostaglandin synthetase and platelet aggregation inhibitor. Prepn and anti-inflammatory activity: BE 801812; G. G. I. Moore, J. K. Harrington, US 3840597 (both 1974 to Riker). Activity, comparison with other non-steroidal anti-inflammatories: K. F. Swingle et al., Arch. Int. Pharmacodyn. Ther. 221, 132 (1976). Mechanism of action: R. L. Vigdahl, R. H. Tukey, Biochem. Pharmacol. 26, 307 (1977). Chromatographic determn in plasma: S. F. Chang et al., J. Pharm. Sci. 66, 1700 (1977). Pharmacology: K. F. Swingle, G. G. I. Moore, Drugs Exp. Clin. Res. 10, 587 (1984). Clinical trials in rheumatic disorders: R. Weissenbach, J. Int. Med. Res. 9, 349 (1981); in osteoarthritis: M. Reiner, ibid. 10, 92 (1982); in acute inflammation: J. M. Pais, F. M. Rosteiro, ibid. 11, 149 (1983); C. Milvio, ibid. 12, 327 (1984); M. E. Nouri, Clin. Ther. 6, 142 (1984).

Bermoprofen CAS Registry Number: 78499-27-1

CAS Name: 10,11-Dihydro-a,8-dimethyl-11-oxodibenz[b,f]oxepin-2-acetic acid
Additional Names: 2-(8-methyl-10,11-dihydro-11-oxodibenz[b,f]oxepin-2-yl)propionic acidTrademarks: Dibenon (Dainippon)...
Literature References: Prostaglandin synthetase inhibitor. Prepn: H. Uno et al., EP 3893; eidem, US 4238620 (1979, 1980 both to Dainippon); Y. Nagai et al., J. Med. Chem. 25, 1065 (1982). Pharmacology: H. Nakamura et al., Arzneim.-Forsch. 33, 1555 (1983). Mechanism of action: K. Ishii et al., Yakugaku Zasshi 108, 1001 (1988), C.A. 110, 33462v (1989).

Bromfenac CAS Registry Number: 91714-94-2 2-(2-氨基-3-(4-溴苯甲酰基)苯)乙酸

CAS Name: 2-Amino-3-(4-bromobenzoyl)benzeneacetic acidPercent Composition: C 53.91%, H 3.62%, Br 23.91%, N 4.19%, O 14.36%
Literature References: Prostaglandin synthetase inhibitor; analog of amfenac, q.v. Prepn: D. A. Walsh et al., J. Med. Chem. 27, 1379 (1984). See also: R. G. Poser, US 4683242 (1987 to A. H. Robins). HPLC determn in plasma: M. A. Osman et al., J. Chromatogr. 489, 452 (1989). Pharmacology: L. F. Sancilio et al., Arzneim.-Forsch. 37, 513 (1987). Clinical pharmacokinetics: P. Högger, P. Rohdewald, ibid. 43, 1114 (1993). Review: J. S. Wajdula et al. in Nonsteroidal Anti-inflammatory Drugs, A. J. Lewis, D. E. Furst, Eds. (Marcel Dekker, Inc., New York, 1994) 267-284. Evaluation of hepatotoxicity: R. J. Fontana et al., Liver Transpl. Surg. 5, 480 (1999). Clinical trial in allergic conjunctivitis: M. Miyake-Kashima et al., Jpn. J. Ophthalmol. 48, 587 (2004).

Staurosporine CAS Registry Number: 62996-74-1 星孢菌素

CAS Name: (9S,10R,11R,13R)- 2,3,10,11,12,13-Hexahydro-10-methoxy-9-methyl-11-(methylamino)-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-onePercent Composition:...
Literature References: Protein kinase C inhibitor; alkaloid isolated from Streptomyces staurosporeus. Isoln: S. Omura et al., J. Antibiot. 30, 275 (1977). Crystal and molecular structure: A. Furusaki et al., J. Chem. Soc. Chem. Commun. 1978, 800; eidem, Bull. Chem. Soc. Jpn. 55, 3681 (1982). Corrected stereochemistry: N. Funato et al., Tetrahedron Lett. 35, 1251 (1994). Total synthesis: J. T. Link et al., J. Am. Chem. Soc. 117, 552 (1995); idem et al., ibid. 118, 2825 (1996). Biosynthetic studies: D. Meksuriyen, G. A. Cordell, J. Nat. Prod. 51, 884, 893 (1988); S.-W. Yang et al., ibid. 62 1551 (1999). HPLC determn in blood and pharmacokinetics in rats: L. R. Gurley et al., J. Chromatogr. B 712, 211 (1998). Inhibition of protein kinase C: T. Tamaoki et al., Biochem. Biophys. Res. Commun. 135, 397 (1986); of other protein kinases: U. T. Rüegg, G. M. Burgess, Trends Pharmacol. Sci. 10, 218 (1989). Induction of apoptosis: E. Falcieri et al., Biochem. Biophys. Res. Commun. 193, 19 (1993); R. Bertrand et al., Exp. Cell Res. 211, 314 (1994); of tyrosine phosphorylation: D. Rasouly, P. Lazarovici, Eur. J. Pharmacol. 269, 255 (1994).

Midostaurin CAS Registry Number: 120685-11-2 米哚妥林

CAS Name: N-[(9S,10R,11R,13R)-2,3,10,11,12,13-Hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl]-N-methylbenzamide
Additi...
Literature References: Protein kinase C inhibitor; derivative of the naturally occurring alkaloid, staurosporine, q.v. Prepn: G. Caravatti, A. Fredenhagen, EP 296110; eidem, US 5093330 (1988, 1992 both to Ciba-Geigy); G. Caravatti et al., Bioorg. Med. Chem. Lett. 4, 399 (1994). HPLC determn in plasma: R. van Gijn et al., J. Chromatogr. B 667, 269 (1995). Review of pharmacology: D. Fabbro et al., Pharmacol. Ther. 82, 293-301 (1999); of mechanism of action and therapeutic potential: A. Gescher, Crit. Rev. Oncol. Hematol. 34, 127-135 (2000). Clinical pharmacokinetics and tolerability: D. J. Propper et al., J. Clin. Oncol. 19, 1485 (2001). Clinical evaluation in diabetic macular edema: P. A. Campochiaro et al., Invest. Ophthalmol. Visual Sci. 45, 922 (2004); in acute myeloid leukemia: R. M. Stone et al., Blood 105, 54 (2005).

Ruboxistaurin CAS Registry Number: 169939-94-0 鲁伯斯塔

CAS Name: (9S)-9-[(Dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione
Additional Names: (S)-3,4-[(N,...
Literature References: Protein kinase Cb (PKCb) inhibitor; macrocyclic bisindolylmaleimide. Prepn: W. F. Heath, Jr. et al., EP 657458; eidem, US 5552396 (1995, 1996 both to Eli Lilly); M. R. Jirousek et al., J. Med. Chem. 39, 2664 (1996); M. M. Faul et al., J. Org. Chem. 63, 1961 (1998). Characterization of salt forms: G. L. Engel et al., Int. J. Pharm. 198, 239 (2000). Enantioselective synthesis: B. M. Trost, W. Tang, Org. Lett. 3, 3409 (2001). Antiangiogenic activity: R. P. Danis et al., Invest. Ophthalmol. Visual Sci. 39, 171 (1998). Clinical trial in diabetic retinopathy: PKC-DRS Study Group, Diabetes 54, 2188 (2005); in diabetic neuropathy: A. I. Vinik et al., Clin. Ther. 27, 1164 (2005); in diabetic nephropathy: K. R. Tuttle et al., Diabetes Care 28, 2686 (2005). Review of pharmacology and therapeutic potential: S. V. Joy et al., Ann. Pharmacother. 39, 1693-1699 (2005); A. Vinik, Expert Opin. Invest. Drugs 14, 1547-1559 (2005).

Harpin CAS Registry Number: 151438-54-9

Trademarks: Messenger (Eden Bioscience)
Literature References: Protein product of the hrpN gene of Erwinia amylovora, a phytopathogenic bacterium that causes fire blight disease. Composed of 403 amino acid residues; mol wt ~44 kDa. Member of a class of glycine-rich, acidic, heat stable proteins that elicit the hypersensitive response as part of the plant's defense mechanism vs pathogenic bacteria. Induces systemic acquired resistance to fire blight and many other plant pathogens, enhances plant growth, and promotes insect repellency. Isoln: Z.-M. Wei et al., Science 257, 85 (1992). Prepn: S. V. Beer et al., WO 9401546; eidem, US 5849868 (1994, 1998 both to Cornell Research Foundation). Elicitation of hypersensitive response: S. V. Beer et al. in Curr. Plant Sci. Biotechnol. Agric. vol. 14, E. W. Nester, D. P. S. Verma, Eds. (Kluwer, Dordrecht, 1993) pp 281-286. Induction of plant resistance: Z.-M. Wei, S. V. Beer, Acta Hortic. 411, 223 (1996); and mode of action of disease resistance: H. Dong et al., Plant J. 20, 207 (1999). Effects on tobacco leaf cell membranes: S. M. Pike et al., Physiol. Mol. Plant Pathol. 53, 39 (1998). Blue mold resistance study in apples: G. de Capdeville et al., Plant Dis. 87, 39 (2003). Review of hrp genes and harpin proteins: J. F. Kim, S. V. Beer in Fire Blight, J. Vanneste, Ed. (CABI Publishing, Wallingford, 2000) pp. 141-161; of commercial product: Biopesticide Regulatory Action Document: Harpin Protein (U.S. EPA, 2002) 32 pp.