3 mg Trade Names: F: Apokinon Aguettant I: Apomor Tariff.. 20 mg, 40 mg, 80 mg Trade Names: D: Allional Hoffmann-La Nervisal Lappe-comb.; Vita-Dor Steigerwald... 500 mg, 1 g Trade Nam
Trang 1Apraclonidine A 131
Reference(s):
Small, L et a].: J Org Chem (JOCEAH) 5, 334 (1940)
Formulation(s): amp 10 mg; inj sol 10 mg/l ml, 5 mg/l ml; tabl 3 mg
Trade Name(s):
F: Apokinon (Aguettant) I: Apomor (Tariff
GB: Brilagel (Britannia; as Integrativo; as
Apraclonidine
(Aplonidine)
ATC: SOlEA03 Usc: selective q-agonist (for postsurgical control of intraocular pressure) RN: 6671 1-21-5 MF: CyHl,,Cl,N4 MW: 245.1 1
CN: 2,6-dichloro-N1-2-imidazolidinylidene-1,4-benzenediamine
monohydrochIoride
RN: 7321 8-79-8 MF: CYH,,C1,N4 HC1 MW: 281.57
LD,,: 6 mglkg (M, i.v.); 3 mglkg (M, p.0.);
9 mglkg (R, i.v.); 38 mglkg (R, p.0.)
dihydrochIoride
RN: 73217-88-6 MF: C9H,,Cl,N4 2HCI MW: 318.04
2.6-dichloro-4
nitroaniline
CI
S0Cl2 5O2CI2
thionyl chloride CC13 1.ethylenediomine
sulfuryl chloride H
N-[4-(dichlaromethylene- amino)-3.5-dichloro- phenyl]trichloroacet- omide
Trang 2Referencefs):
EP 81 924 (Alcon; appl 19.1 1.1982; USA-prior 20.1 1.1981)
EP 81 923 (Alcon; appl 19.11.1982; USA-prior 20.1 1.1981)
US 4 461 904 (Alcon; 24.7.1984; prior 20.11.198 1)
Ronot, B.; Leclerc, G.: Bull Soc Chim Fr (BSCFAS) Pt 2,520 (1979)
combination with P-receptor antagonist:
EP 365 662 (Alcon; 26.4.1989; USA-prior 26.4.1988)
preparation o f 2,6-dichloro-4-nitroaniline:
Goldschmidt; Strohmenger: Ber Dtsch Chem Ges (BDCGAS) 55,2455 (1922)
Pausadeer; Scroggie: Aust J Chem (AJCHAS) 12,430,432 (1959)
Fluerscheim: J Chem Soc (JCSOA9) 93 1774 (1908)
Datta; Miiller: J Am Chem Soc (JACSAT) 41, 2036 (1919)
Koerner: Gazz Chim Ital (GCITA9) 4,376 (1874)
Kohn; Pfeifer: Monatsh Chem (MOCMB7) 48,236 (1927)
Formulation(s): eye drops 0.5 %, 1 %; ophthalmic sol 10 mglml
Trade Name(s):
D: Iopidine (Alcon) GB: Iopidine (Alcon) USA: Iopidine (Alcon; 1988);
Use: antiarrhythmic RN: 37640-71-4 MF: CI2,H3,N, MW: 322.50
LD,,: 274 m g k g (M, p.0.)
monohydrochloride
RN: 33237-74-0 MF: CzZH3,N, HCI MW: 358.96 EINECS: 251-418-7
LD,,: 17.1 mglkg (M, i.v.); 262 mglkg (M, p.0.);
16.6 mglkg (R, i.v.); 525 mglkg (R, p.0.)
2-indonone aniline (I) N-(2-indanylidene) 2-anilinoindane (11)
aniline
+ 1 - 1 1
2 J-diethylomino- propyl chloride
methonesulfonote
Trang 3Aprobarbital A 133
Referenceis):
DE 2 060 721 (Christiaens S A.; appl 10.1 2.1970; GB-prior l9.l2.I968,26.ll.l970)
Formulation(s): cps 50 mg; inj sol 200 mg120 ml
Trade Name(s):
D: Amidonal (PCR F: Fiboran (Nycomed)
Arzneimittel) I: Aspenone (Mitsui)
Use: hypnotic, sedative RN: 77-02- 1 MF: CloH,,N,03 MW: 210.23 EINECS: 200-997-4
LD,,: 200 m g k g (M, i.p.); 350 m g k g (M, s.c.)
monosodium salt
RN: 125-88-2 MF: C,,H,,N,NaO, MW: 232.22 EINECS: 204-760-6
LD,,: 85 mgkg (R, i.p.)
5-isoprapyl- ollyl bromide
barbituric acid
I Aproborbitol /
Reference(s):
US 1 444 802 (Hoffmann-La Roche; 1923; appl 1921)
Formulation(s): elixir 40 mg; tabl 20 mg, 40 mg, 80 mg
Trade Name(s):
D: Allional (Hoffmann-La Nervisal (Lappe)-comb.; Vita-Dor (Steigerwald)
Mandotrilan-"Porte" Nervolitan (Kette1hack)- USA: Alurate (Roche); wfm
Nervinum Stada (Stada)- Resedorm (Lappe)-comb.;
Aprotinine
(Trasylol; Triazinin; Zymofren)
ATC: B02AB Use: proteinase inhibitor, kallikrein inhibitor
RN: 9087-70-1 MF: C2R4H432N8407YS7 MW: 6511.55 EINECS: 232-904-9
LD,,: >50 ml/kg (M, i.p.); >50 m l k g (M, s.c.);
>40 mllkg (R, i.p.); >40 m l k g (R, s.c.)
CN: trypsin inhibitor (ox pancreas basic)
antagosan
RN: 9050-74-2 MF: C284H432N8407YS7 MW: 651 1.55
iniprol
Trang 41 3 4 A Aranidipine
ox pancreas basic
RN: 12407-79-3 MF: C284H4,2N,407,S, MW: 65 1 1.55
ox pancreas basic reduced
RN: 11061-94-2 MF: C,,,H4,,N,407,S, MW: 6517.60
By extraction of animal lymph glands, parotid glands, pancreas, liver, milt and blood serum with dilutcd acetic acid-ethanol-mixtures upon removal of fat and proteins
Refererzce(s):
US 2 890 986 (Bayer; 16.6.1959; D-prior 29.5.1954)
Formulation(s): amp 200000 KIU; inj sol 100000 KIU/IO ml, 500000 KIU/SO ml
Trade Name(s):
D: Antagosan (Hoechst) Biscol (Lab Franpis du Trasylol (Bayer)
Beriplast (Centeon Fractionement ct dcs J: Trasylol (Bayer-Yoshitomi;
Tissucol (Immuno) Trasylol (Bayer-Pharma) USA: Trasylol Injection (Bayer) Trasylol (Bayer Vital) I: Antagosan (Behring)
F: Antagosan (Hoechst Fase (Astra-Simes)
Aranidipine
(MPC- 1304)
ATC: C04 Use: antihypertensive, calcium channel blocker
RN: 86780-90-7 MF: C,,H,,N207 MW: 388.38
LD,,: 143 mg/kg (M, p.0.);
1459 m g k g (R, p.0.);
3333 m g k g (dog, p.0.)
CN: 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylic acid methyl 2-oxopropyl ester
n NaH, benzene
0
diketene 2,2-(ethylene- 2,2-(ethy1enedioxy)-
dioxy)- 1 -propano1 propyl ocetoocetote (I)
n H3C
6 , cH,coou, benzene piperidine, acetic acid
2-nitro-
benzoldehyde
2,2-(ethy1enedioxy)- propyl 2-(2-nitro- benzy1idene)acetoacetate (11)
Trang 5H2N CH 2 1 C2H50H, A CH,COOH H 2 0
methyl 3-
aminocratonate
Arginine aspartate A 135
NH, CH,OH CZH50H A
Reference(s):
a Ohno, S eta].: Chem Pharm Bull (CPBTAL) 34(4), 1589-1606 (1986)
b FR 2 514761 (Maruko Seiyaku; appl 19.10.1982; J-prior 19.10.1981)
topical ophthalmic formulation:
WO 9 323 082 (Alcon Lab.; appl 12.5.1993; USA-prior 13.5.1992)
Formrrlution(s): gran 20 mg/g (2 %)
Trade Name(s):
J: Bec (Maruko; Bristol- Sapresta (Taiho)
Myers Squibb)
Use: liver dysfunction therapeutic, tonic RN: 7675-83-4 MF: C6H14N402 MW: 174.20 EINECS: 231-656-8
CN: L-aspartic acid compd with L-arginine (1:l)
H $2 H2N,,,, COOH
H 2 N -l' N d C O O H + [COOH H 2 HzN,,,
NH
Very pure preparations are obtained by treatment of L-aspartic acid loaded strong basic anion-exchange resins with an aqueous solution of L-arginine hydrochloride
L-arginine L-ospartic acid
Reference(s):
DAS 1 518 033 (Mundipharma; appl 17.9.1965; F-prior 14.1.1965)
Arginine asporiate
Formulation(s): tabl 1 g; sol 1 g/10 ml, 1 &/5 ml; tabl 500 mg, 1 g
Trade Name(s):
D: Argihepar (Chephasaar); F: Sargenor (ASTA Medica) I: Glutargin (Terapeutico
Trang 6136 A Arginine pidolate
Sargenor (ASTA Medica)
Arginine pidolate
(Arginine pyroglutamate)
ATC: A13A Use: tonic, cerebrostimulant
RN: 64855-91-0 MF: C6H,,N402 C5H,N03 MW: 303.32 EINECS: 265-253-3
CN: 5-0x0-proline compd with L-arginine (1: 1)
DL-pyroglutamic L-arginine
acid
Arginine pidolate
DAS 2 416 339 (Manetti Roberts; appl 4.4.1974; I-prior 4.4.1973)
GB 1 421 089 (Manetti Roberts; appl 27.3.1974; I-prior 4.4.1973)
Provenzano, P.M et al.: Arzneim.-Forsch (ARZNAD) 27, 1553 (1977)
use as sexual tonic:
DOS 3 125 512 (Manetti Roberts; appl 29.6.1981; I-prior 30.6.1980)
Formulation(s): lyo 500 mg, 1 g; tabl 500 mg
Trade Name(s):
I: Adiuvant (Manetti Roberts) Detoxergon Polvere
(Ba1dacci)-comb
Neoiodarsolo (Ba1dacci)- comb
Arotinolol
(S-596)
ATC: C07AA Use: P-adrenoceptor blocker, antihypertensive, antianginal RN: 52560-77-7 MF: C , ~ H , , N ; O ~ S ~ MW: 37 1.55
LD,,,: >360 mglkg (M, i.p.); 86 mglkg (M, i.v.); >5000 mglkg (M, p.0.)
hydrochloride
RN: 80416-73-5 MF: C15H2,N302S, xHC1 MW: unspecified
1 SOCI,
O O Br, CH,COOH
chloride
5-acetylthiophene-
2-carboxylic acid
Trang 7Ascorbic acid A 137
omrnoniurn 2-rnercopto-4-(5- butylornino-
dithiocorbomote corbornoyl-2-thienyl)- 2-proponol
(from tert-butyl- thiozole
ornine and epi- chlorohydrin)
Arotinolol
Reference(s):
DOS 2 341 753 (Sumitomo; appl 17.8.1973; J-prior 17.8.1972, 5.4.1973)
US 3 932 400 (Sumitomo; 13.1.1976; J-prior 17.8.1972, 5.4.1973)
Hara, Y et al.: J Pharm Sci (JPMSAE) 67, 1334 (1978)
Formulation(s): tabl 10 mg
Trade Narners):
J : Almarl (Surnitomo; 1986)
Ascorbic acid
(Acide ascorbique; Vitamin C)
ATC: AIlGAOl Use: antiscorbutical vitamin antioxidant
RN: 50-81-7 MF: C6H8O6 MW: 176.12 EINECS: 200-066-2
LDS,,: 518rnglkg (M,i.v.); 3367 mg/kg(M,p.o.);
>4 glkg (R, i.v.); 11.9 glkg (R, p.0.)
CN: I.-ascorbic acid
monopotassium salt
RN: 15421-15-5 MF: C6H7K06 MW: 214.21 EINECS: 239-432-1
monosodium salt
RN: 134-03-2 MF: C6H7Na0, MW: 198.11 EINECS: 205-126-1
calcium salt (2:l)
RN: 5743-27-1 MF: C,2Hl,Ca0,, MW: 390.31 EINECS: 227-261-5
magnesium salt (2:l)
RN: 1543 1-40-0 MF: C,,H,,MgOI2 MW: 374.54 EINECS: 239-442-6
Fe(I1) salt (2:l)
RN: 24808-52-4 MF: C,,H,,FeO,, MW: 406.08
Hz Roney-Ni
H , H:$-~ Acetobocter suboxydons
I
Trang 8138 A Ascorbic acid
CH,
acetone diacetone-L-sorbose
CH3
diocetone-2-0x0- L-gulonic acid (U)
COOH
ko
2-0x0-L-
gulonic ocid
HO 0 H
Ascorbic ocid
~eichstein, T.; Griissner, A.: Helv Chim Acta (HCACAV) 17, 31 1 (1934)
Ullmanns Encykl Tech Chem., 3 Aufl., Vol 18,223 ff
Kirk-Othmer Encycl Chem Technol., 2 Ed (15SWA8), Vol 2, (1963-1971), p 747 ff
Formul~ztion(s): amp 562 mg; eff tabl 1 g; powder 1 g; tabl 50 mg, 200 mg, 500 mg
Trade Name(s):
Ascorvit (Jenapharm)
Cebion (Merck)
Cetebe (SmithKline
Beecham)
Cevitt (Hermes)
Vitamin C Phytopharma
( O W )
numerous combination
preparations
Ascofer (Gerda; as iron-
salt)
Laroscorbine (Roche
Nicholas)
Midy Vitamine C
(SmithKline Beecham)
Vi tascorbol (ThCraplix)
generics (as salts) and
numerous combination
preparations
Ferfolic SV (Sinc1air)-
comb
Redoxon (Roche
Consumer)
Acidylina (1st Italiano
Ferm.)
Agrumina (Also) Agruvit (Lepetit) Ascomed (Ripari-Gero) Ascorgil (Biomedica Foscama)
Aster C (Corvi) Bio-Ci (Ceccarelli) C-Lisa (Lisapharma) C-Tard (Eurand-Mi) Cebion (Bracco) Cecon (Abbott) Cevit (Italfarmaco) Duo-C (Geymonat) Idro-C (Blue Cross) Lemonvit (Molteni) Rcdoxon (Roche) Vicifte (Iacopo Monico) Vicitina (CT)
Vitamina C Vca (Bergamon) Vitamina C Vita (Synthelabo) combination preparations J: Ascoyl (Shionogi); wfm Hicee (Takeda); wfm
Viscorin (Daiichi); wfm Vitacimin (Takeda); wfm numerous combination preparations
USA: ACES Antioxidant Soft Gels (Carlson)
Ce-Vi-Sol (Mead Johnson) Cevi-Bid (Geriatric Pharm.)
Chromagen (Savage) CitraDerm (Pedinol) Ferancee (Stuart) Fero-Folic-500 (Abbott) Fero-Grad-500 (Abbott) Fetrin (Lunsco) Irospam (Fielding) Materna (Lederle Labs.) Trinsicon (UCR) Vi-Daylin ADC (Ross) Vitron-C (Fisons) numerous combination
preparations
Trang 9Asparaginase A 139
Asparaginase
(L-Asparaginase)
ATC: LOIXX; LOlXXO2 Use: antineoplastic
RN: 9015-68-3 MF: unspecified MW: unspecified EINECS: 232-765-3
LD,,,: 136 glkg (M, iv.);
7568 mglkg (R, i.v.);
227 mglkg (dog, i.v.)
CN: asparaginase
L-Asparagine-amidohydrolase
Relative mol mass 133000 + 5000
By separation from bacterial culture such as Escherichia coli, Serratia rnarcescens, Erwinia aroideae, Erwinia atrosepfica, Erwinia carotovora
Reference(s):
Ho et al.: J Riol Chem (JBCHA3) 245,3708 (1970)
DAS 1 642 615 (Bayer; appl 27.12.1967)
DAS 1 942 833 (Secret of Statc for Social Services, London; appl 22.8.1969; GB-prior 23.8.1968)
DAS 1 942 900 (Secret of State for Social Services, London; appl 22.8.1969; GB-prior 23.8.1968)
Formulation(s): inj powder 10000 iul2.5 ml
Trade Name(s):
D: Erwinase (Ipsen Pharma) 1: Crasnitin (Bayer); wfm USA: Elspar (Merck)
F: Kidrolase (Bellon) J: Leunasc (Kyowa Hakko)
RN: 22839-47-0 MF: C,,H,,N,O, MW: 294.31 EINECS: 245-261-3
CN: N-L-a-aspartyl-L-phenylalanine 1-methyl ester
L-osportic L-aspartic anhydride
acid hydrochlaride I Aspartame
(olong with aspartame ore formed
up to 20% p-isomer
seporoted by crystallization)
Refuence(s):
DE 1 692 768 (Searle & Co.; prior 16.2.1968)
Mazur, R.H et al.: J Am Chem Soc (JACSA'I') 91, 264 (1969)
Ariyoshi, Y et al.: Bull Chem Soc Jpn (BCSJA8) 46, 1893 (1973)
DE 2 104 620 (Ajinomoto; appl 1.2.1971; J-prior 31.1.1970.23.2.1970, 26.6.1970)
DAS 2 152 11 1 (Ajinomoto; appl 19.10.1971; J-prior 26.10.1970)
DAS 2 233 535 (Ajinomoto; appl 7.7.1972; J-prior 9.7.1972)
US 3 492 131 (Searle; 27.1.1970; appl 18.4.1966)
Trang 10140 A L -Aspartic acid
alternative synthesis:
US 4 238 392 (Pfizer; 9.12.1980; appl 29.10.1979)
US 4 173 562 (Monsanto; 6.1 1.1979; prior 27.12.1976, 3 1.3.1978)
EP 143 881 (Gema; appl 6.7.1984; CH-prior 7.9.1983)
,fermentative preparation from L-aspartic acid and L-phenylalanine methyl ester:
US 4 506 011 (Toyo Soda; 19.3.1985; J-prior 5.9.1981; 14.10.1981, 18.1.1982)
purijication:
US 3 798 207 (Ajinomoto; 19.3.1 974; J-prior 26.10.1970)
Formulation(s): eff tabl 20 mg; tabl 18 mg
Trade Name(s):
D: Canderel (Wander)
F: Candtrel (Monsanto; 1980)
1: Aspardolce Dolafic
(Ganassini)
Asparel Dietason
(Formenti)
Aspartina (Ilex)
Bil Aspatame dolaf Hermesetas Gold
Dietoman aspartame Snel Miel (Fea) (Sterling Midy) Suaviter (Boehringer
Futura aspartame J: Pal-Sweet (Ajinomoto) (Farmacologico Milanese)
L-Aspartic acid
(L-2-Aminosuccinic acid; Acide aspartique)
Use: non-essential proteinogenic amino acid (for infusion solutions and as salt former)
RN: 56-84-8 MF: C,H,NO, MW: 133.10 EINECS: 200-291-6
LD,,: 6 glkg (M, i.p.1
CN: L-aspartic acid
monopotassium salt
RN: 11 15-63-5 MF: C4H6KN0, MW: 171.19 EINECS: 214-226-4
monosodium salt
RN: 3792-50-5 MF: C,H,NNaO, MW: 155.09 EINECS: 223-264-0
magnesium salt (2:l)
KN: 2068-80-6 MF: C,HI,MgN,O, MW: 288.50 EINECS: 218-191-6
magnesium salt (2:l) tetrahydrate
RN: 7018-07-7 MF: C8HL2MgN2O8 4H20 MW: 360.56
Rcference(s):
with immovable aspartase:
Tosa, T et al.: Biotechnol Bioeng (BIBIAU) 15.69 (1973)