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

Fondaparinux Sodium CAS Registry Number: 114870-03-0 磺达肝癸钠

CAS Name: Methyl O-2-deoxy-6-O-sulfo-2-(sulfoamino)-a-D-glucopyranosyl-(1®4)-O-b-D-glucopyranuronosyl-(1®4)-O-2-deoxy-3,6-di-O-sulfo-2-(sulfoamino)-a-D-glucopyranosyl-(1®4)-O-2-O-sulfo-a-L-idopyra...
Literature References: Synthetic pentasaccharide corresponding to the antithrombin binding site of heparin, q.v. Prepn: M. Petitou et al., EP 84999; eidem, US 4818816 (1983, 1989 both to Choay); M. Petitou et al., Carbohydr. Res. 167, 67 (1987). Review of pharmacology: J. M. Herbert et al., Cardiovasc. Drug Rev. 15, 1-26 (1997). Clinical pharmacokinetics: B. Boneu et al., Thromb. Haemostasis 74, 1468 (1995). Clinical trial for prevention of post-operative deep-vein thrombosis: A. G. G. Turpie et al., N. Engl. J. Med. 344, 619 (2001). Clinical comparison with enoxaparin, q.v. in treatment of established deep-vein thrombosis: H. R. Büller et al., Ann. Intern. Med. 140, 867 (2004). Review of clinical safety and efficacy: A. G. G. Turpie, Expert Opin. Drug Saf. 4, 707-721 (2005).

Idraparinux Sodium CAS Registry Number: 149920-56-9; 162610-17-5 (Idraparinux) 艾屈肝素钠

CAS Name: Methyl O-2,3,4-tri-O-methyl-6-O-sulfo-a-D-glucopyranosyl-(1®4)-O-2,3-di-O-methyl-b-D-glucopyranuronosyl-(1®4)-O-2,3,6-tri-O-sulfo-a-D-glucopyranosyl-(1®4)-O-2,3-di-O-methyl-a-L-idopyranu...
Literature References: Synthetic pentasaccharide that inhibits factor Xa; analog of fondaparinux sodium, q.v. Prepn: M. Petitou, C. A. van Boeckel, EP 0529715; eidem, US 5378829 (1993, 1995 both to Akzo; Sanofi); P. Westerduin et al., Bioorg. Med. Chem. 2, 1267 (1994). Biochemical and pharmacological properties: J. M. Herbert et al., Blood 91, 4197 (1998). Comparative pharmacokinetics in rats: J. P. Hérault et al., Thromb. Haemostasis 87, 985 (2002). Clinical pharmacology and reversal by factor VIIa: N. R. Bijsterveld et al., Br. J. Haematol. 124, 653 (2004). Review of clinical development: Q. Ma, J. Fareed, IDrugs 7, 1028-1034 (2004).

Goserelin CAS Registry Number: 65807-02-5 戈舍瑞林

CAS Name: 6-[O-(1,1-Dimethylethyl)-D-serine]-10-deglycinamideluteinizing hormone-releasing factor (pig) 2-(aminocarbonyl)hydrazide
Additional Names: D-Ser(But)6Azgly10-gonadorelin; D-Ser(But)6A...
Literature References: Synthetic peptide agonist analog of LH-RH, q.v. Prepn: A. S. Dutta et al., DE 2720245; eidem, US 4100274 (1977, 1978 both to I.C.I.); eidem, J. Med. Chem. 21, 1018 (1978). Radioimmunoassay in serum: R. N. Clayton et al., Clin. Endocrinol. 22, 453 (1985). Endocrine effects in women: C. P. West, D. T. Baird, ibid. 26, 213 (1987). Review of pharmacokinetics and therapeutic efficacy in sex hormone related disorders: P. Chrisp, K. L. Goa, Drugs 41, 254-288 (1991). Clinical trial in treatment of uterine fibroids: J. Gerris et al., Horm. Res. 45, 279 (1996); in prostate cancer: M. Bolla et al., N. Engl. J. Med. 337, 295 (1997).

Triptorelin CAS Registry Number: 57773-63-4 曲普瑞林

CAS Name: 6-D-Tryptophanluteinizing hormone-releasing factor (pig)
Additional Names: 6-D-tryptophan-LH-RH; D-trp6-LHRH; D-Trp6LRH; D-trp6-gonadorelin; détryptorélinePercent Composition: C 58.61...
Literature References: Synthetic peptide agonist analog of LH-RH, q.v. Prepn: A. V. Schally, D. H. Coy, DE 2625843; eidem, US 4010125 (1976, 1977); D. H. Coy et al., J. Med. Chem. 19, 423 (1976). Comparison with LH-RH of in vitro activity: D. H. Coy et al., Biochem. Biophys. Res. Commun. 67, 576 (1975). Pharmacokinetics and metabolism in humans: J. L. Barron et al., J. Clin. Endocrinol. Metab. 54, 1169 (1982). HPLC analysis: D. C. Serti et al., J. Liq. Chromatogr. 4, 1135 (1981). RIA in human serum: M. Mason-Garcia et al., Proc. Natl. Acad. Sci. USA 82, 1547 (1985). Clinical trial for in vitro fertilization: A. Hazout et al., Fertil. Steril. 59, 596 (1993). Clinical trial in prostate cancer: C. F. Heyns et al., BJU Int. 92, 226 (2003); in severe endometriosis: A. Y. K. Wong, L. Tang, Fertil. Steril. 81, 1522 (2004).

Nafarelin CAS Registry Number: 76932-56-4 那法瑞林

CAS Name: 6-[3-(2-Naphthalenyl)-D-alanine]luteinizing hormone-releasing factor(pig)
Additional Names: 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-3-(2-naphthyl)-D-alanyl-L-leucyl-L...
Literature References: Synthetic peptide agonist analog of LH-RH, q.v. Prepn: J. J. Nestor et al., US 4234571 (1980 to Syntex); eidem, J. Med. Chem. 25, 795 (1982). Suppression of luteal and placental function in baboons: B. H. Vickery et al., Fertil. Steril. 36, 664 (1981). Inhibition of ovulation in humans: J. A. Gudmundsson et al., Contraception 30, 107 (1984). Radioimmunoassay in plasma and serum: C. Nerenberg et al., Anal. Biochem. 141, 10 (1984). Kinetics and tissue disposition in animals: N. I. Chu et al., Drug Metab. Dispos. 13, 560 (1985). Clinical evaluation in benign prostatic hyperplasia: C. A. Peters, P. C. Walsh, N. Engl. J. Med. 317, 599 (1987); in endometriosis: M. R. Henzl et al., ibid. 318, 485 (1988). Review of clinical studies: P. G. Hoffman et al., J. Androl. 8, Suppl., S17-S22 (1987).

Miltefosine CAS Registry Number: 58066-85-6 米替福新

CAS Name: 2-[[(Hexadecyloxy)hydroxyphosphinyl]oxy]-N,N,N-trimethylethanaminium inner salt
Additional Names: choline phosphate hexadecyl ester, hydroxide, inner salt; hexadecyl 2-(N,N,N-trimethy...
Literature References: Synthetic phospholipid; affects cell-signaling pathways and membrane synthesis. Synthesis: U. Kaatze et al., Chem. Phys. Lipids 27, 263 (1980); W. J. Hansen et al., Lipids 17, 453 (1982). See also: H. Eibl, EP 225608; idem, US 4837023 (1987, 1989 both to Max-Planck Ges. Wissensch.). Toxicity and anticancer properties: C. Muschiol et al., Lipids 22, 930 (1987). Structure-activity study: M. R. Berger et al., Cancer Treat. Rev. 17, 143 (1990). HPTLC determn in plasma: I. Rustenbeck, S. Lenzen, J. Chromatogr. 525, 85 (1990). Clinical evaluation in topical treatment of cutaneous breast cancer metastases: C. Unger et al., Cancer Treat. Rev. 17, 243 (1990). Clinical trial in visceral leishmaniasis: S. Sundar et al., N. Engl. J. Med. 347, 1739 (2002). Review: H. Eibl, C. Unger, Cancer Treat. Rev. 17, 233-242 (1990).

Cosyntropin CAS Registry Number: 16960-16-0 替可克肽

CAS Name: a1-24-Corticotropin
Additional Names: b1-24-corticotropin; tetracosactide
Trademarks: Cortrosyn (Amphastar)
Percent Composition: C 55.68%, H 7.22%, N 19.10%, O 16.91%, S 1.09%
Literature References: Synthetic polypeptide corresponding to the first 24 amino acids of ACTH, q.v. Identification of activity: R. G. Shepherd et al., J. Am. Chem. Soc. 78, 5067 (1956). Synthesis: H. Kappeler, R. Schwyzer, Helv. Chim. Acta 44, 1136 (1961); eidem, ibid. 46, 1550 (1963); solid-state synthesis: R. Matsueda et al., J. Am. Chem. Soc. 97, 2573 (1975). Assessment of hormone levels for adrenal function in cats: M. E. Peterson et al., Res. Vet. Sci. 37, 331 (1984); in dogs: L. A. Frank et al., Domest. Anim. Endocrinol. 24, 43 (2003). Review as diagnostic aid in assessment of secondary adrenal insufficiency: T. A. M. Abdu, R. N. Clayton, Curr. Opin. Endocrinol. Diabetes 7, 116-121 (2000); in primary or secondary adrenal insufficiency: R. I. Dorin et al., Ann. Intern. Med. 139, 194-204, E205-E206 (2003).

Promegestone CAS Registry Number: 34184-77-5 普美孕酮

CAS Name: (17b)-17-Methyl-17-(1-oxopropyl)estra-4,9-dien-3-one
Additional Names: 17a-methyl-17-propionylestra-4,9-dien-3-one; 17a-methyl-17b-propionyl-19-nor-4,9-androstadien-3-one; 17a,21-dime...
Literature References: Synthetic progestin with no androgenic activity and with high affinity for the progesterone receptor. Prepn: J. Warnant, A. Farcilli, BE 763099; eidem, US 3679714, US 3761591 (1971, 1972, 1973 all to Roussel-UCLAF). Inhibition of gonadotropin secretion and lack of androgenic activity: F. Labrie et al., Fertil. Steril. 28, 1104 (1977). Binding studies in mouse uterus: D. Philibert, J.-P. Raynaud, Steroids 22, 89 (1973); eidem, Endocrinology 94, 627 (1974). Binding to human endometrium: eidem, Contraception 10, 457 (1974); M. Haukkamaa, T. Luukkainen, J. Steroid Biochem. 5, 447 (1974). Review and possible use in treatment of hormone-dependent breast cancer: J.-P. Raynaud, T. Ojasoo, J. Gynecol. Obstet. Biol. Reprod. 12, 697 (1983).

Trimoprostil CAS Registry Number: 69900-72-7 曲莫前列素

CAS Name: (5Z,11a,13E,15R)-15-Hydroxy-11,16,16-trimethyl-9-oxoprosta-5,13-dien-1-oic acid
Additional Names: (Z)-7-[(1R,2R,3R)-2-[(E)-(3R)-3-hydroxy-4,4-dimethyl-1-octenyl]-3-methyl-5-oxocyclope...
Literature References: Synthetic prostaglandin E2 analog with antisecretory activity. Prepn: G. W. Holland et al., DE 2437622; eidem, US 4052446; US 4190587 (1975, 1977, 1980 all to Hoffmann-La Roche). Pharmacology: D. E. Wilson, S. L. Winter, Prostaglandins 16, 127 (1978); S. P. Lee et al., Eur. J. Clin. Invest. 17, 1 (1987). Effect on bicarbonate secretion: M. Feldman, J. Clin. Invest. 72, 295 (1983); on inhibition of gastric acid secretion: R. J. Wills et al., Clin. Pharmacol. Ther. 37, 113 (1985). Metabolism: S. J. Kolis et al., Drug Metab. Dispos. 14, 465 (1986). Clinical pharmacokinetics: R. J. Wills et al., J. Clin. Pharmacol. 26, 48 (1986). Clinical evaluation: H. G. Dammann et al., Arzneim.-Forsch. 36, 500 (1986). Multicenter clinical comparison with cimetidine, q.v.: K. D. Bardhan et al., Scand. J. Gastroenterol. 23, 134 (1988); with aldioxa, q.v.: A. Ishimori et al., Acta Ther. 15, 27 (1989). Toxicity study: M. Shimizu et al., Shin'yaku to Rinsho 35, 2199 (1986), C.A. 106, 150180e (1987).

Bimatoprost CAS Registry Number: 155206-00-1 比马前列素

CAS Name: (5Z)-7-[(1R,2R,3R,5S)-3,5-Dihydroxy-2-[(1E,3S)-3-hydroxy-5-phenyl-1-pentenyl]cyclopentyl]-N-ethyl-5-heptenamide
Additional Names: (5Z,9a,11a,13E,15S)-9,11,15-trihydroxy-17-phenyl-18,1...
Literature References: Synthetic prostamide; structurally related to prostaglandin F2a, q.v. Prepn: D. F. Woodward et al., WO 9406433; eidem, US 6403649 (1994, 2002 both to Allergan). Series of articles on pharmacology and clinical experience: Surv. Ophthalmol. 45, Suppl. 4, S335-S368 (2001). Pharmacology: D. F. Woodward et al., J. Pharmacol. Exp. Ther. 305, 772 (2003). Clinical comparison with timolol in glaucoma and ocular hypertension: J. D. Brandt et al., Ophthalmology 108, 1023 (2001). Clinical trial in glaucoma and ocular hypertension: R. Quinones et al., J. Ocul. Pharmacol. Ther. 20, 115 (2004). Review of pharmacology and clinical efficacy: L. B. Cantor, Expert Opin. Invest. Drugs 10, 721-731 (2001); of mechanism of action: A. H.-P. Krauss, D. F. Woodward, Surv. Ophthalmol. 49, Suppl. 1, S5-S11 (2004): of pharmacoeconomics of use: G. L. Plosker, S. J. Keam, Pharmacoeconomics 24, 297-314 (2006).