Boake Roberts & Co.; appl... in numerous concentrations; powder 1 % Trade Names: D: numerous combination I: numerous combination Thera-Gesic Mission.. 100 mg Mepocrine Trade Natir~ls:
Trang 1Menadione sodium bisulfite M 1241
Trade Narne(s):
F: Bilkaby (Lehning) J: generic
-
(Menaphthone sodium bisulfite) Use: ant~hemorrhagic vitamin
RN: 130-37-0 MF: C,,H,Na05S MW: 276.24 EINECS: 204-987-0
CN: 1,2,3,4-tetrahydro-2-methyl-1,4-dioxo-2-naphthalenesulfonic acid sodium salt
0
Menadione sadium bisulfite
Reference(s):
Moore, M.B.: J Am Chem Soc (JACSAT) 63,2049 (1941)
Baker, B.R et al.: J Am Chem Soc (JACSAT) 64, 1096 (1942)
Menotti, A.R.: J Am Chem Soc (JACSAT) 65, 1209 (1943)
US 2 367 302 (Abbott; 1945; appl 1940)
Forrnulation(s): amp 1 mg, 2 mg, 3 mg, 10 mg, 50 mg
Trade Narne(s):
D: Chloramsaar (Chephasaar)- Poly-Vitamin-Saar F: ArhCmapectine vitaminCe
Geriatrie-Mulsin (Mucos)- Prenatal (Cyanamid)- CCpCvit K (UCB)-comb.;
Lentinorm (Kano1dt)- Tetracycletten (Voigt); wfm I: Vitamina K Salf (Salf)
Use: anesthetic (combination ingredient in antitussives and expectorants) RN: 2216-51-5 MF: C,,,H,,O MW: 156.27 EINECS: 218-690-9
LD,,: 3400 m g k g (M, p.0.);
3300 m g k g (R, p.0.)
CN: [1R-(la,2~,5)]-5-methyl-2-(l-methylethyl)cyclohexanol
Trang 2@ f r o m (+)-citronellol (contoining at 8 0 % in citronellol)
(+)-citronellol (I) (-)-isopulegol (II) (+)-neoiso- (+)-isoiso- (+)-neoisoiso-
pulegol (111) pulegol (IV) pulegol (V)
HZ, Raney-Ni
I1
pyrolysis
lhyrnal (+)-menthol (VI) (f)-neornenthol (f)-isamenthal
recycling! epimerization to the mtia (?)-menthol : (2)-neomenthol : (+)-isamentho1 =
6 : 3 : 1 under hydrogenation conditions:
separation of (?)-menthol by distillotion
1 fract crystallization
H ~ c / * ' c H ~
(+)-menthy1 benzoate
(+)-Menthol can be racemized under thymol hydrogenation conditions (also with Raney-Ni)
Referencefs):
review:
Ullmanns Encykl Tech Chem., 4 Aufl., Vol 20,220
b DAS 1 197 081 (A Boake Roberts & Co.; appl 31.10.1963)
c racemute resolution of (+_)-menthy1 benzoate:
DOS 2 109 456 (Haarmann & Reimer; appl 27.2.1971)
Trang 3Mepacrine M 1243
Formulation(s): cream 0.042-1 %; drg 1 mg; ointment, sol in numerous concentrations; powder 1 %
Trade Name(s):
D: numerous combination I: numerous combination Thera-Gesic (Mission)
F: numerous combination USA: Listerine (Warner- numerous combination
GB: numerous combination Panalgesic Gold (ECR)-
Mepacrine
(Quinacrine; Atebrin)
ATC: PO1 AX05 Use: antimalarial
RN: 83-89-6 MF: C2,H3,CIN30 MW: 399.97 EINECS: 201-508-7
LD,,: 5 0 m g k g (M,i.v.); 1320mgkg(M,p.o.)
CN: ~-(6-chloro-2-methoxy-9-acridinyl)-N1,NL-diethyl-l ,4-pentanediamine
dihydrochloride
RN: 69-05-6 MF: C,3H,oC1N,0~ 2HCI MW: 472.89 EINECS: 200-700-8
LD,,: 38 m g k g (M, i.v.); 557 mglkg (M, p.0.);
29 m g k g (R, i.v.); 660 m g k g (R, p.0.)
2.4-dichloro- 4-methoxy-
Reference (s):
DRP 553 072 (I G Farben; appl 1930)
Wingler, A.: Angew Chem (ANCEAD) 61,49 (1949)
Formulation(s): tabl 100 mg
Mepocrine
Trade Natir~ls):
F: Colla&nan (Sobio)-comb.; Tenicridine (Norgan); wfm
methoxyacridine (1) aminopentone
Trang 41244 M Mepartricin
Mepartricin
(Methylpartricin)
RN: 11 121-32-7 MF: C,,H,,N,O,, MW: 1141.36
LD,,: 11.1 mglkg (M, i.p.); 4300 pglkg (M, i.v.); >2 glkg (M, p.0.)
CN: partricin methyl ester
1 ferrnentotion of Streptornyces oureofociens
2 rnethylotion with excess of diozornethone
ATC: AOlAB16; DOlAA06; GOlAA09 Use: polyene antibiotic (for treatment of
Reference(s):
DE 2 154 436 (Spa; appl 2.1 1.1971; GB-prior 3.1 1.1970)
GB 1 359 473 (Spa; appl 3.1 1.1970)
GB 1 406 774 (Spa; appl 15.2.1973)
GB 1 462 442 (Spa; appl 29.8.1974)
DE 2 406 628 (Spa; appl 12.2.1974; GB-prior 15.2.1973)
US 3 773 925 (Spa; 20.11.1973; appl 3.1 1.1971; GB-prior 3.11.1970)
Bruzzese, T et al.: Experientia (EXPEAM) 28, 1515 (1972)
Pandey, R.C et al.: J Antibiot (JANTAJ) 30, 158 (1973)
Tweit, R.C et al.: J Antibiot (JANTAJ) 35, 997 (1982)
water soluble formulation:
GB 1 413 256 (Spa; appl 14.5.1973)
GB 1 463 348 (Spa; appl 3.9.1974)
medical use for treatment of benign prostatic hypertrophy:
US 4 237 117 (Spa; 2.12.1980; prior 6.1 l.l978,5.lO.l979)
candidal and trichomonal gynaecological infections, treatment
of benign prostatic hypertrophy)
liposomal formulation:
WO 89 103 677 (Board of Regents; Univ of Texas Syst.; appl 27.10.1988; USA-prior 27.10.1987)
structure of partricin:
Tweit, R.C et al.: J Antibiot (JANTAJ) 35, 997 (1982)
Formulation(s): tabl 50000 iulg, 40 mg; vaginal cream 5000 iulg; vaginal tabl 25000 iu
Trade Name(s):
1: Ipertrofan (SPA; 1986) Montricin (SPA; 1988 as Tricandil (SPA; 1975)
sodium lauryl sulfate)
Trang 5M e ~ e n z o l a t e bromide M 1245
Use: anticholinergic RN: 76-90-4 MF: C2,H2,BrN03 MW: 420.35 EINECS: 200-992-7
LD,,,: 9800 @kg (M, i.v.); 900 mglkg (M, p.0.);
22 m g k g (R, i.v.); 742 mg/kg (R, p.0.)
CN: 3-[(hydroxydiphenylacetyl)oxy]-1,1-dimethylpiperidinium bromide
Reference(s):
US 2 918 408 (Lakeside Labs.; 1959; prior 1950)
Formulation(s): tabl 7.5 mg, 15 mg, 25 mg
Mepenzolate bromide
Trade Name(s):
piperidine
F: Cantil (Roger Bellon); wfm Colum (Jamco) J: Eftoron (Maruko Seiyaku)
I: Cantril Lakeside (Roger Enterocantril (Roger Trancolon (Fujisawa)
Colibantil (Tosi-Novara) Gastropidil (Fabo) Roussel)
Use: muscle relaxant RN: 59-47-2 MF: c,,H,,o~ MW: 182.22 EINECS: 200-427-4
LD,,: 175 mg/kg (M, i.v.); 720 mgkg (M, p.0.);
133 mglkg (R, i.v.); 625 mgkg (R, p.0.)
CN: 3-(2-methy1phenoxy)- 1,2-propanediol
o-cresol (1) 3-chloro-1,2-
Trang 61246 M Mephenytoin
Mephenesin
0
glycide
Reference(s):
a Marie, E.R.: J Chem Soc (JCSOA9) 101, 310 (1912)
b GB 628 497 (British Drug Houses; appl 1948)
Formulation(s): drg 250 mg; tabl 500 mg
Trade Nnrne(s):
F: Algipan Baume (Darcy)- (Pharmad6veloppement)- Relaxar Linimento
DCcontractyl (Synthe1abo)- GB: Myanesin (Duncan, J: Curaresin (Kyoto)
1: Mefenesina (Tariff Myoserol (Sankyo) Integrativo) USA: Tolserol (Squibb); wfm
Mephenytoin
(Methoin)
ATC: N03AB04 Use: antiepileptic, anticonvulsant
RN: 50-12-4 MF: CI2Hl4N2O2 MW: 218.26 EINECS: 200-012-8
LD,,,: 440 mglkg (M, p.0.);
850 mgkg (R, p.0.)
CN: 5-ethyl-3-methyl-5-phenyl-2,4-imidazolidinedione
ethyl
bromide
2-cyono-2-phenyl- butyromide
dimethyl sulfote (In) I Mephenytoin
5-ethyl-5- phenylhydontoin (U)
Trang 7Mepindolol M 1247
+ N o C N + ( N H 4 ) 2 C 0 3
propiophenone
Reference(s):
Ehrhart-Ruschig, Vol 1, 196
DRP 309 508 (Chem Fabrik von Heyden; appl 1914)
FR 769 667 (Sandoz; 1934)
Formulation(s): tabl 100 mg
Trade Name(s):
D: Mesantoin (Sandoz); wfm GB: Mesantoin (Sandoz); wfm USA: Mesantoin (Sandoz); wfrn F: SCdantoinal (Sandoz); wfm I: Mesantoina (Sandoz); wfm
Use: beta blocking agent, antianginal RN: 23694-81-7 MF: C,,H22N20, MW: 262.35 EINECS: 245-831-1
CN: l-[(l-methylethyl)amino]-3-[(2-methyl-1H-indol-4-yl)oxy~-2-propanol
sulfate
RN: 56396-94-2 MF: C3,H,N404 H2S04 MW: 622.78
4-benzyloxyindole-2-
corboxylic acid
4-benzyloxy-2-di- methylaminornethyl- indole (I)
methyl
iodide
Trang 81248 M Mepitiostane
CH3
isopropyl-
o n e V I
epichloro-
8'
0+ , benzoyl peroxide
NoHCO,, OMSO
C H O
2-methyl-3-
nitroonisole
2-methoxy-6- nitrobenzyl bromide
2-rnethoxy-6- nitrobenz- oldehyde (W)
nitro-
ethane
1 -(2-methoxy-6- 4-methoxy-2-
nitroprop-1 -ene
NoOH
Reference(s):
a GB 1 260 907 (Sandoz; appl 23.5.1969; BR-prior 7.6.1968)
Seemann, F et al.: Helv Chim Acta (HCACAV) 54, 241 1 (1971)
b DOS 2 905 054 (Schering AG; appl 8.2.1979)
combination with hydrochlorothiazide:
DOS 3 027 392 (Schering AG; appl 17.7.1980)
Formulation(s): f c tabl 2.5 mg, 5- mg (as sulfate)
Trade Namefs):
D: Corindocomb (Schering) Corindolan (Schering; as I: Betagon (Schering; as
Use: antiestrogen, antineoplastic RN: 21362-69-6 MF: C,,H,,O,S MW: 404.66
CN: (2a,3a,5a,17~)-2,3-epithio-17-[(l-methoxycyclopentyl)oxy]androstane
Trang 9Mepivacaine M 1249
p-toluenesulfonic ocid
epithiostonol 1 -methoxy-
( q v.) cyclopentene
Reference(s):
DE 1 668 659 (Shionogi; appl 27.1.1968; J-prior 28.1.1967)
US 3 567 713 (Shionogi; 2.3.1971; appl 26.1.1968; J-prior 28.1.1967)
Trade Name(s):
J: Thioderon (Shionogi;
1979)
Use: local anesthetic RN: 22801-44-1 MF: C,5H22N20 MW: 246.35
CN: (+)-N-(2,6-dimethylphenyl)-l-methyl-2-piperidinecarboxamide
monohydrochloride
RN: 1722-62-9 MF: C,,HZ2N2O HC1 MW: 282.82 EINECS: 217-023-9
LD,: 32 m g k g (M, i.v.)
' ethyl 1-methyl
/ CH3 I piperidine- 2.6-dimethyl- ethyl-
bromide
picolinic acid
2.6-xylidide
(cf bupivocaine
Mepivocoine
aldehyde
pipecalinic acid 2,6-xylidide
Trang 101250 M Meprednisone
Reference(s):
a US 2 799 679 (AB Bofors; 1957; S-prior 1955)
Ekenstam, 9 af et al.: Acta Chem Scand (ACHSE7) 11, 1183 (1957)
Rinderknecht, H.: Helv Chim Acta (HCACAV) 42, 1324 (1959)
b DOS 2 726 200 (Bofors; appl 10.6.1977; S-prior 22.6.1976)
US 4 110 33 1 (Bofors; 29.8.1978; S-prior 22.6.1976)
analogous method with methylation before hydrogenation ofpyridine nucleus:
GB 826 668 (Crookes Labs.; appl 1955)
D-(-)-mepivacaine:
DOS 2 259 517 (Bofors; appl 5.12.1972; USA-prior 6.12.1971)
Formulation(s): amp 0.5 %, 1 %, 2 96, 3 %, 4 % (as hydrochloride)
Trade Name(s):
D: Meaverin (RhGne-Poulenc F: Carbocaine (Astra; as Mepident (Parke Davis)
Mecain (curasan) GB: Estradurin (Lundbeck)- - Mepimynol (Molteni)
Scandicain (Astra) I: Carbocaina (Astra-Simes) J: Carbocain (Yoshitomi) numerous combination Carbocaina adrenalina USA: Polocaine (Astra; as
Use: glucocorticoid RN: 1247-42-3 MF: CzzH,,O, MW: 372.46 EINECS: 214-996-1
CN: (16P)-17,21 -dihydroxy-16-methylpregna-l,4-diene-3,11,20-trione
_,
1 diazo-
methane
4 OH-
perchlaric acid
1 bromine
3 N-brama-