Aztreonam
A
171
1.
CIS03H, 2-picoline. CH2C12
2.
V.
CH2CI2
b
iCH"'
XI
N1-sulfo-NZ-benzyloxycorbonyl-0-rnethylsulfonyl-
L-threoninornide tetrabutylornrnoniurn salt
(XII)
VIII.
K2C03, C2H4C12, H20 H2, Pd-C. CZH,OH N-hydroxybenzotriozole, DCC
w-VI
b
mr
b
IX
Reference(s):
US 4 386 034 (Squibb; 31.5.1983; prior. 10.2.1982).
US 4 529 698 (Squibb; 16.7.1985; prior. 5.11 ,1984).
US4 625 022 (Squibb; prior. 25.11.1986; 2.2.1981).
DOS
3
104 145 (Squibb; appl. 6.2.1981; USA-prior. 29.8.1980).
GB
2
071 650 (Squibb; appl. 6.2.1981; USA-prior. 7.2.1980,29.9.1980).

Formulation(s):
amp. 2 g;
inj.
powder 500 mg,
1
g,
2 g; lyo.
for
inf.
2 g;
vial
1 g13
ml
Trade Narnefs):
D:
Azactam (Bristol-Myers
GB:
Azactam (Bristol-Myers
J:
Azactam (Squibb; 1987)
Squibb; 1985) Squibb; 1986) USA: Azactam (Bristol-Myers
F:
Azactam (Sanofi Winthrop)
I:
Axactam (Squibb; 1984) Squibb; 1987)
172
B
Bacampicillin
Bacampicillin
ATC: JOlCA06

Use: antibiotic (broad spectrum penicillin)
RN: 50972-17-3 MF: CzIHz7N,07S MW: 465.53
CN:
[2S-[2a,5a,6~(S*)]]-6-[(aminophenylacetyl)a~no]-3,3-~methyl-7-oxo-4-thia-l-
azabicyclo[3.2.0]heptane-2-carboxylic
acid 1
-[(ethoxycarbonyl)oxy]ethyl
ester
monohydrochloride
RN: 37661-08-8 MF: CzIHz7N,07S
.
HCl MW: 501.99 EINECS: 253-580-4
LD,,: 184 mgkg (M, i.v.); 8529 mgkg (M, p.0.);
176 mgkg (R, i.v.); 10 gkg (R, p.0.)
azidocillin sodium salt
(9.
v.)
1
-chloroethyl
ethyl carbonote
Referencefs):
DAS 2 144 457 (Astra; appl. 4.9.1971; S-prior. 17.9.1970, 20.1 1.1970).
US 3 873 521 (Astra; 25.3.1975; S-prior. 17.9.1970; 20.11.1970).
US 3 939 270 (Astra; 17.2.1976; S-prior. 17.9.1970; 20.1
1.1970).
6-(D-a-azidaphenylacetamido)-
Formulation(s):
f.
c. tabl. 400 g, 800 mg; susp. 125 mg (as hydrochloride)
Bacampicillin

Trade Name(s):
D: Ambacamp (Pharmacia
&
Penglobe (Lematte et
Upjohn; 1981) Boinot)
Penglobe (Astra; 1977) GB: Ambaxin (Upjohn; 1980) J:
penicillanic acid
1
-ethoxycarbonyl-
oxyethyl ester
(1)
Bacacil (Pfizer)
Penglobe (Bracco)
Bacacil (Pfizer Taito)
F: Bacampicine (Pharmacia
&
I: Ambaxin (Upjohn) Penglobe (Yoshitomi)
Upjohn) Amplibac (Schwarz) USA: Spectrobid (Pfizer; 1981)
Bacitracin
ATC: D06AX05; R02AB04
Use: polypeptide antibiotic (mainly topical
application)
RN: 1405-87-4 MF: C66H,o,N17016S MW: 1422.72 EINECS: 215-786-2
LD,,,: 360 mglkg (M, i.v.); >3750 mglkg (M, p.0.)
CN: bacitracin
Bacitracin
B
173
bacitracin
A

RN:
22601-59-8 MF: Ch6H103Ni7016S MW:
Bacitracin
A
1422.72 EINECS: 245-1 15-9
"Bacitracin" is submitted as mixture of bacitracin A with other bacitracins.
From culture of
Bacillus subtilis
and purification on ion-exchangers.
Referencefs):
US 2498 165 (US-Secret. of War; 1950; appl. 1946).
US 2 828 246 (Commercial Solvents Corp.; 1958; appl. 1956).
purijication:
US 2 457 887 (Ben Venue Labs.; 1949; appl. 1947).
US 2
609
324 (Commercial Solvents Corp.; 1952; appl. 1949).
US 2 774 712 (S. B. Penick
&
Co.; 1956; appl. 1955).
US 2776 240 (Commercial Solvents Corp.; 1957; appl. 1954).
US 2 834 71
1 (Commercial Solvents Corp.; 1958; appl. 1956).
US 2 915 432 (Merck
&
Co.; 1959; appl. 1955).
US 2 960 437 (Pfizer; 1960; appl. 1955).
US 3 795 663 (Commercial Solvents Corp.; 5.3.1974; appl. 1.5.1972).
US4
101 539 (IMC Chemical; 18.7.1978; appl. 17.10.1977).

complexes with nickel salts:
US 2 903 357 (Grain Processing Corp.; 1959; appl. 1958).
Na-bacitracin methanesulfonate:
US 3 205 137 (Warner-Lambert; 7.9.1965; appl. 19.3.1963).
complexes with
zinc, cobalt
or
manganese sulfate
resp.
sulfonates:
US 3 384 631 (Spofa; 21.5.1968; appl. 23.6.1965; CSSR-prior. 26.6.1964).
complexes with metal methanesuljnates:
US 3 441 646 (Commercial Solvents; 29.4.1969; appl. 22.1.1965).
complex with calcium or magnesium alkylbenzenesulfonates:
US 3 891 615 (Commercial Solvents; 24.6.1975; appl. 25.10.1973).
Formulation(s):
amp. 50000 iu; vial 5000 iu; nasal ointment 300 iu; ointment 300 iu, 500 iu; powder 300 iu
Trade Namefs):
D:
Anginomycin (MIP Frubienzym (Boehringer Polyspectran (A1con)-
Pharma)
1ng.)-comb.
comb.
Batrax (Gewo)-comb. Nebacetin (Yamanouchi)-
Prednitracin (CIBA
Bivacyn (medphano)
comb.
Vision)-comb.
Cicatrex (Glaxo
Neobac (Dermapharm) Tonsilase (Media)-comb.

Wellcome)-comb.
Neotracin (CIBA Vision)
F:
Bacicoline (Merck Sharp
&
Dohme-Chibret)-comb.
T'
174
B
Baclofen
Collunovar (SynthC1abo)-
comb.
Lysopaine ORL
(Boehringer 1ng.)-comb.
Maxilase Bacitracine
(Sanofi
Winthrop)-comb.
Oropivalone (Jouveina1)-
comb.
Pimafucort (Beytout)-
comb.
generics
GB: Cicatrin (Glaxo
Wellcome)-comb.
Polyfax (Dominion)-comb.
I:
Bimixin (Lusofarmaco)-
comb.
Enterostop (Teafarma)-
comb.

Orobicin (Fu1ton)-comb.
J: Bacitracin (Ono)
USA:
Betadine (Purdue
Frederick)
Cortisporin (Burroughs
I
Wellcome)-comb.
Neosporin (Glaxo
Wellcome; Warner-
Lambert)
Polysporin (Warner-
,
Lambert)
generics
Baclofen
ATC: M03BXO1
t
Use: muscle relaxant (antispasmodic)
RN: 1134-47-0 MF: C,,H12ClN02 MW: 213.66 EINECS: 214-486-9
LD,,,: 3
1 mgkg (M,
i
.v.); 200 mglkg (M, p.0.);
78 mglkg (R, i.v.); 145 mglkg (R, p.0.)
CN:
P-(aminomethyl)-4-chlorobenzenepropanoic
acid
oldehyde
ethyl acetoacetole

ClW
O~CH~
3-(4-chlorapheny1)-
glutoric ocid
(1)
I
C
I
3-(4-chlorophenyl)- 3-(4-chloropheny1)- Baclofen
glutaric anhydride glutarimide
ethyl 4-chlorocinnamate nitromethone
(11)
Hz.
Raney-Ni
11
O~CH~
%
CI
Reference(s):
a
US 3 47
1
548 (Ciba; 7.10.1969; CH-prior. 9.6.1963; 22.5.1964).
lJS 3 634 428 (Ciba; 11.1.1972; CH-prior. 9.7.1963, 22.5.1964).
b
JP 45 016 692 (Uchimaru, F. et al.; Daiichi Seiyku; appl. 10.6.1970); C.A. (CHABAS)
73,
77617~ (1970).
Balsalazide sodium
B

175
conlbination with ncuroleptics:
US 3 947 579 (Nelson Research
&
Dev.; 30.3.1976; appl. 3.6.1974).
US 3 978 216 (Nelson Research
&
Dev.; 31.8.1976; prior. 3.6.1974, 16.7.1975).
US
4
138 484 (Nelson Research
&
Dev.; 6.2.1979; prior. 3.6.1974, 16.7.1975, 16.8.1976,25.7.1977).
Fonnulation(s):
inj. sol. 0.05 mgll ml, 10 mgl20 ml, 10 mg15 ml; intrathecal
inj.
50 pglml, 0.05 mglml,
10 mgl20 ml, 10 mg15
ml;
liquid 5 mgl5 ml; tabl. 5 mg, 10 mg, 25 mg
Trade Name(s):
D:
Lebic (Isis Puren)
GB:
Lioresal (Novartis)
Lioresal (Novartis Pharma)
I:
Lioresal (Ciba)
F:
LiorCsal (Novartis)

J:
Gabalon (Daiichi)
Lioresal (Novartis)
Balsalazide sodium
(BX-66
1
-A)
ATC:
DO8
Use: anti-inflammatory
RN: 82101-18-6 MF: C,,H,,N,Na,O,
MW:
401.29
CN:
5-[[4-[[(2-carboxyethyl)amino]carbonyl]phenyl]azo]-2-hydroxybenzoic
acid disodium salt
@)-free acid
RN: 80573-04-2 MF: C,,H,,N,O,
MW:
357.32
4-nitrobenzoyl ,L-alonine
chloride
N-(4-nitrobenzoyl)
p-olanine
(I)
1.
NoN02. HZO, HCI. 5
'C
COOH
H

,
Pd-C.
C
H
OH
L
a
H2N%gc"CooH
I,
sodium nitrite
+
11
""-0
0
2.
salicylic acid
N-(4-aminobenz0yl)-
palanine
COOH
I
OyONa
Refcrence(s):
DE
3 128 819 (Riorex Lab.; appl. 21.7.1981; GB-prior. 21.7.1980,7.7.1981).
(11)
Formulation(s):
cps. 750 mg (as disodium salt)
Balsalazide sodium
Trade Name(s):
GB:

Colazide (Astralmanuf. by
Salix)
176
B
Bambuterol
Bambuterol
(KWD-2183)
ATC: R03CC12
Use: P2-receptor agonist, orally active
lipophilic terbutaline ester
prodrug,
1
long lasting bronchodilator
RN: 81732-65-2 MF: C,,H,,N,OS MW: 367.45
CN: dimethylcarbamic acid
5-[2-[(1,1-dimethylethyl)amino]-l-hydroxyethyl]-l,3-phenylene
ester
monohy drochloride
RN: 81732-46-9 MF: CI,H2,N,0s
.
HCI
MW:
403.91
3',5'-dihydroxy- dimethyl-
acetophenone carbamoyl
chloride
3',5'-bis(dimethy1corb-
amoyloxy)acetophenone
(I)
I

Bombuterol
EP
43 807 (Draco; appl. 30.6.1981; GB-prior. 9.7.1980,29.5.1981).
DOS 3 163 871 (Draco; appl. 23.1.1981; GB-prior. 9.7.1980,29.5.1981).
(alternative synthes~s given).
Formulation(s):
tabl. 10 mg, 20 mg; sol. 0.1%
Trade Namefs):
D: Bambec (Astra)
Bamethan
(Butylnorsynephrine; Butyloctopamine)
ATC: C04AA31
Use: sympathomimetic, vasodilator
RN: 3703-79-5 MF: C,,Hl,N02 MW: 209.29 EINECS: 223-043-9
LD,,,: 72 mgkg (M, i.v.); 562 mglkg (M, p.0.);
80 mgkg (R, i.v.)
CN:
a-[(butylamino)methyl]-4-hydroxybenzenemethanol
sulfate
(2:l)
RN: 5716-20-1 MF: CI2Hl9NO2. 1/2H2S04 MW: 516.66 EINECS: 227-214-9
LD,,: 72 mgkg (M, i.v.); 1600 mglkg (M, p.0.);
>I500 mgkg (R, p.0.)
Bamifylline
B
177
benzoyl 4'- hydroxy- 4'-benzoyloxy-
chloride ocetophenone acetophenone
butylornine N-(4-benzoyloxy-
phenocyl)butylomine

4-benzoyloxy-
phenocyl bromide
(1)
Corrigan,
J.R.
et al.:
J.
Am. Chem. Soc. (JACSAT)
67,
1894 (1945).
D:
Emasex (Eurim Pharma)-
comb.
Heweven (Hevert)
Medigel (Medice)-comb.
Theo-Hexanicit (Astral
Promed)
Vasoforte N
Kapseln
(Krugmann)
F:
Escinogel (Doms-Adrian)-
comb.
GB: Vasculit (Boehringer Ing.);
wfm
I:
Vasculat (Boehringer Ing.;
as sulfate)
J: Bloodbin (Nakataki)
Butibatol (Hishiyama)

Butosin (Kobayashi)
Cyclate (Hokuriku)
Garmin (Fuso)
.
Pan Line (Maruishi)
Pericardin (Santen-
Yamanouchi)
Simpelate (Seiko Eiyo)
Valtolmin (Sanwa)
Vasculat (Tanabe; as
sulfate)
Vasolat (Kanto)
Vasolen (Toho)
Vasstol (Nichiiko)
Yonomol A (Sawai)
Bamifylline
ATC: R03BA; R03DA08
Use: bronchodilator, coronary vasodilator
RN:
2016-63-9
MF: C,,H,,N,O,
MW:
385.47
CN:
7-[2-[ethyl(2-hydroxyethyl)aminolethyl]-3,7-dihydro-1,3-dimethyl-8-(phenylmethyl)-1H-purine-2,6~
dione
monohydrochloride
RN:
20684-06-4 MF: C,,H,N,O,
.

HCl
MW:
421.93 EINECS: 243-967-6
178
B
Bamipine
Reference(s):
BE
602 888
(A.
Christiaens S.A.; appl. 21.4.1961; GB-prior. 22.4.1960).
ethanol
Fonnulation(s):
inj. sol. 300 mgf5 ml; suppos. 250 mg, 750
mg;
tabl. 300
mg
Barnifylline
Trade Name(s):
D: Trentadil (Fresenius); wfm Trentadil injectable (Evans I: Bamifix (Chiesi)
F:
Trentadil (Evans Medical) Medical) Briafil (Alfa Wassermann)
Trentadil (Scdaph);
wfm
GB:
Trentadil (Armour); wfm
Bamipine
ATC: D04AA 15; R06AXO
I
Use: antihistaminic

RN: 4945-47-5
MF:
C,,H2,N2
MW:
280.42 EINECS: 225-587-2
LD,,: 250 mglkg (M, p.0.)
CN:
l-methyl-N-phenyl-N-(phenylmethyl)-4-piperidinamine
monohydrochloride
RN: 1229-69-2 MF: C,,H,N,. HCI MW: 316.88
LD,,: 60
mgkg
(M,
i.v.); 750 mglkg (M, p.0.);
460 mgkg (R, p.0.);
189 mglkg (dog, p.0.)
lactate
(1:l)
RN: 61670-09-5 MF: C,,H2,N,.
C,H,O,
MW: 370.49
aniline
1
-methyl- 1-methyl-4-
4-piperidone phenylimino-
piperidine
CH3
I
+
1.

sodium amide
2.
benzyl chloride
EINECS: 262-887-2
1 -methyl-4-anilino-
piperidine
(I)
Reference(s):
US
2 683 714 (Knoll AG; 1954; D-prior. 1949).
Barbexaclone
B
179
Formulation(s):
cream 20 mg; drg. 20 mg; f.
c.
tabl. 50 mg; gel 20 mg
Trade Nameis):
D:
Bamipin (ratiopharm)
F:
Taumidrine (Knoll); wfm
Soventol (Knoll) I: Soventol (Knoll); wfm
Barbexaclone
ATC: N03AA04
Use: antiepileptic
RN: 4388-82-3 MF: C,2H,2N203 MW: 232.24 EINECS: 224-504-7
LD,,: 334 mg/kg (M, p.0.);
306 mg/kg
(R,

pa)
CN:
5-ethyl-5-phenyl-2,4,6(1H,3H,SH)-pyrimidinetrione,
compd. with
(9-N,a-
dimethylcyclohexaneethanamine (1: I)
Reference (s):
DE 1 120 452 (Knoll; appl. 16.4.1960)
phenaborbitol (-)-propylhexedrine
Formulation(s):
drg. 100 mg, 25 mg
Barbexaclone
Trade Nurne(s):
D:
Maliasin (Knoll) I: Maliasin (Ravizza)
(4.
v.)
(9.
v.1
Barbital
ATC: N05CA04
Use: hypnotic
RN:
57-44-3 MF: C8HI2N2O3
MW:
184.20 EINECS: 200-331-2
LD,,:
600
mg/kg
(M,

pa)
CN:
5,5-diethyl-2,4,6(1H,3H,5H)-pyrimidinetrione
monosodium salt
RN: 144-02-5
MF:
C,H,,N,Na03 MW: 206.18 EINECS: 205-613-9
LD,,:
830 mglkg
(M,
i.v.); 800 mglkg (M, p.0.);
280 mglkg (R, i.v.1; 600 mglkg
(R,
p.0.)
diethyl
diethylrnolonate
urea
1
Barbitol
I
Reference(s):
Fischer; Dilthey: Justus Liebigs Ann. Chem. (JLACBF) 335,338 (1904).
180
B
Barnidipine
Formulation(s):
tabl. 250 mg, 500 mg
Trade Name(s):
D:
Barbimetten (Hormosan);

F:
combination preparations;
1:
Barbitt (Tariff.
Integrative)
wfm wfm Veronidia (Vaillant);
wfm
Barnidipine
(Mepirodipine hydrochloride)
ATC: C08CA12
Use: antihypertensive agent, long active
calcium antagonist
RN: 104757-53-1 MF:
C2,H2,N,0,
.
HC1
MW:
528.01
CN:
[S-(R*
,R*)]-l,4-Dihydro-2,6-dimethyl-4-(3-nitropheny~boxyic
acid methyl 1
-
(phenylmethy1)-3-pyrrolidinyl
ester hydrochloride
free base
RN: 104713-75-9 MF: C2,H2,N,0, MW: 491.54
racemate
RN: 71863-55-3
MF:

C2,H2,N,0,
MW:
491.54
HO*,,, COOH
CCOOH
L-molic acid
OvCH3
I
.H2N
9
2.
LiAlH THF
a
1.
benzylamine
2.
lithium oluminum
hydride
o7
9
CH,COONo, 80°C
+
U
diketene
(3s)-1
-benzyl-3-
hydroxypyrrolidine
(I)
2.
methyl 3-aminocrotonote

(IV)
2.
N
3. hydrolysis
_____+
1,
tert-butyl
acetoocetote
m-nitro-
benzoldehyde
(111)
Bornidipine