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Bromocriptine B 271 ATC: G02CBO1; N04BCO1 Use: prolactin inhibitor RN: 25614-03-3 MF: C,,H,,,BrN,O, MW: 654.61 EINECS: 247-128-5 LD,: >800 mglkg (M, p.0.); 72 mglkg (R, i.v.) CN: (5'a)-2-bromo-l2'-hydroxy-2'-(l -methylethyl)-5'-(2-methylpropyl)ergotaman-3',6',18-trione monomesylate RN: 22260-51-1 MF: C3,H,oBrN,0, . CH,O,S MW: 750.71 EINECS: 244-881 - 1 LD,: 189 mg/kg (M, i.v.); 2502 mglkg (M, p.0.); 10.5 mg/kg (R, i.v.); >2 g/kg (R, p.0.) Reference(s): US 3 7.52 814 (Sandoz; 14.8.1973; CH-prior. 31.5.1968). DAS 1 926 045 (Sandoz; appl. 22.5.1969; CH-prior. 31.5.1968). ergocryptine medical use: US 3 7.52 888 (Sandoz; 14.8.1973; CH-prior. 3 1.5.1968). Bromocriptine nasal formulation: DOS 2 802 113 (Sandoz; appl. 19.1.1978). Formulation(s): cps. 5 mg, 10 mg; tabl. 2.5 mg (as mesylate) Trade Name(sJ: , . D: Kirim (Hormosan) Parlodel (Novartis; 1978) J: Parlodel (Novartis; 1979) Pravidel (Novartis Pharma; GB: Parlodel (Novartis; 1976) USA: Parlodel (Novartis; 1976) 1977) I: Parlodel (Sandoz; 1979) F: Bromo-Kin (Irex) Serocryptin (Serono) Bromopride ATC: A03FA04 Use: anti-emetic, gastric therapeutic RN: 4093-35-0 MF: C,,H,,BrN30, MW: 344.25 EINECS: 223-842-2 LD,,: 310 mg/kg (M, p.0.); 545 mg/kg (R, p.0.) CN: 4-amino-5-bromo-N-[2-(diethylamino)ethyl]-2-methoxybenzamide 272 B Bromopride 0 methyl 4-ocetamido- N,N-diethyl- 2-rnethoxybenzoate (I) ethylenediornine (11) Bromopride L"' 1. Br,, CH3COOH 2. HCI I11 -b @ COOH Br 1 NH2 acetic anhydride 4-amino- methanol methyl 4-amino- salicylic acid solicylate dimethyl sulfate I Br,. CH3COOH 2. HCI - Br k CH, K 0 methyl 4-ocetamido-5- broma-2-methaxybenzoate yH3 0 0 . W\I CH3 K 0 methyl 4-acetamido- solicylate (IV) Brornapride rn US 3 177 252 (Soc. &Etudes Scientifiques et Industrielles de 1'Ile-de-France; 6.4. 1965; F-prior. 25.7.1961). US 3 219 528 (Soc. &Etudes Scientifiques et Industrielles de I'Ile-de-France; 23.1 1.1965; F-prior. 5.8.1960, 4.11 .l96O, 25.7.1961). US 3 357 978 (Soc. &Etudes Scientifiques et Industrielles de 1'Ile-de-France; 12.12.1967; F-prior. 5.3.1963). DE 1 233 877 (Soc. dlEtudes Scientifiques et Industrielles de 1'Ile-de-France; appl. 14.7.1962; F-prior. 25.7.1961). Bromperidol B 273 alternative synthesis: DAS 2 102 848 (Delmar; appl. 21.1.1971; USA-prior. 21 .l. 1970). DAS 2 119 724 (Teikoku Hormone Mfg.; appl. 22.4.197 1 ; J-prior. 24.4.1970). DAS 2 162 917 (Soc. d'Etudes Scientifiques et Industrielles de l'lle-de-France; appl. 17.12.197 1 ; J-prior. 21.12.1970). DAS 2 166 118 (Teikoku Hormone Mfg.; appl. 22.4.1971; J-prior. 24.4.1970). DOS 2 435 222 (Soc. dlEtudes Scientifiques et Industrielles de l'Ile-de-France; appl. 22.7.1974; J-prior. 24.7.1973). Formulation(s): amp. 10 mg; cps. 10 mg; drops 13.3 mg Trade Narne(s): D: Cascapride (Merck) I: Opridan (Locatelli; as Valopride (Synthelabo) di hydrochloride monohydrate) Bromperidol ATC: N05AD06 Use: antipsychotic, neuroleptic RN: 10457-90-6 MF: C,,H,,BrFNO, MW: 420.32 EINECS: 233-943-3 LD,,: 18.9 mgkg (M, i.v.); 174 mglkg (M, p.0.); 10 mgkg (R, i.v.); 359 mgkg (R, p.0.) CN: 4-[4-(4-bromophenyl)-4-hydroxy-l-piperidinyl]-l-(4-fluorophenyl)-l-butanone monohydrochloride RN: 59453-24-6 MF: CzIHZ3BrFNO2 . HCI MW: 456.78 LD,,: 18.9mgkg(R,i.v.); 174mgkg(R, p.0.) fluorobenzene 4-chlorobutyryl 4-chloro-4'-fluoro- chloride butyrophenone (I) (cf. holoperidol) 4-bromo-a-methyl- form- styrene aldehyde pyridine (11) 1. HBr . HOAc HO 2. NoOH D - EWWNH + I 4-(4-bromapheny1)- 4-hydraxypiperidine Br&N+ 'F Bromperidol 274 B Brompheniramine Reference(s): US 3 438 991 (Janssen; appl. 15.4.1969; GB-prior. 18.1 1.1959). DE 1 289 845 (Janssen; appl. 18.4.1959; GB-prior. 22.4.1958). Niemegeers, C.J.E.; Janssen, P.A.J.: Arzneirn Forsch. (ARZNAD) 24,45 (1974). Formulation(s): amp. 5 mglml; drops 2 mglrnl; tabl. 1 mg, 5 mg, 10 mg Trade Name(s): D: Impromen (~ansseh; 1983) I: lmpromen (Formenti; J: Impromen (Yoshitomi; Tesoprel (Organon; 1984) 1989) 1986) Brompheniramine ATC: RO~ABO~ Use: antihistaminic RN: 86-22-6 MF: C,,H1,BrN, MW: 319.25 EINECS: 201-657-8 CN: y-(4-bromophenyl)-N,N-dimethyl-2-pyridinepropanamine maleate (1:l) RN: 980-71-2 MF: C1,H,,BrN,. C4H404 MW: 435.32 EINECS: 213-562-9 LD,,: 3 18 mgkg (R, p.0.) + OC' q sod~um amide 4-bromo- 2-chloro- (4-bromopheny1)- benzyl pyridine (2-pyridyl). cyanide ocetonitrile 1. NaNH2 2. CI- CH3 Y' CH3 1. sodium omide 2. 2-(dimethylomi- no)ethyl chloride CN CH, 2-(4-bromopheny1)-4- dimethylamino-2-(2- pyridy1)butyronitrile (I) Reference(s): US 2 567 245 (Schering Corp.; 1951; prior. 1948). US 2 676 964 (Schering Corp.; 1954; prior. 1950). Formulntion(s): elixir 4 mg, 2 mgl5 ml; cps. 12 mg Trade Name(s): D: Dimegan (Kreussler) F: Chronotrophir (Sanofi Winthrop) DimCgan (Dexo) Dimetane Expectorant (Whitehall) Martigbne (CIBA Vision 0phthalmics)-comb. Rupton Chronules (Dexo)- USA: Bromfed (Muro; as comb. maleate) GB: Dimotane (Wyeth) Dallergy (Laser; as Dirnotane Plus (Wyeth)- maleate) comb. Dimetane (Robins) I: Ilvin (Bracco; as maleate) Ladrame (ECR; as maleate) J: Bromrun (Hokuriku) Poly-Histine (Sanofi; as maleate) Broparestrol B 275 Respahist (Respa; as maleate) Rondec (Dura; as maleate) Ultrabrom (We; as maleate) Broparestrol ATC: GO3 Use: estrogen (synthetic) RN: 479-68-5 MF: CzzHI,Br MW: 363.30 EINECS: 207-537-1 CN: 1-(2-bromo-l,2-diphenylethenyl)-4-ethylbenzene I-ethyl-4-phenyl- phenylmognesium 1.2-diphenyl-1-(4- Broporestrol ocetylbenzene bromide ethylpheny1)ethene Reference(s): Dvolaitzky, M.; Jacques, J.: Bull. Soc. Chim. Biol. (BSCIA3) 40,939 (1958). Formulation(s): cream 10 %; emulsion 5 % Trade Narne(s1: F: Acnestrol (Devimy)-comb.; Longestrol (Laroche I: Acnestrol (Scharper); wfm wfm Navarron); wfm Brotizolam ATC: N05CD09 Use: tranquilizer, hypnotic RN: 57801-81-7 MF: C,,H,,BrCIN,S MW: 393.70 EINECS: 260-964-5 LD,: 920 mglkg (M, i.p.1; >10000 mgkg (M, p.0.); 1000 mgkg (R, i.p.); >10000 mglkg (R, p.0.) CN: 2-bromo-4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-[1,2,4]triazolo[4,3-a][1,4]diazepine 1. "J~~~~~~~ CI 2. H+ 0 WZH,), NCa + - H2N -1 1. glycine ethyl OH 2-chlorobenzoyl- 2.5-dihydroxy- acetonitrile 1 -3-dithiane ester 2-omino-3-(2- chlorobenzoyl)- thiophene 1. Br2, pyridine 1. bromine HN 2. phosphorus 5-(2-chl0rophenyl)- pentosulfide 7-brom0-5-(2- 1,3-dihydro-2H-thieno- chloropheny1)- 1.3- [2,3-el-1.4-diozepin- 2-one (I) 276 B Broxvauinoline 1. N2H4 CH. H oJ- 2. ;OXOhcti3 H3C I1 - 1. hydrazine 2. triethyl orthoacetate I Brotizolam Reference(s): DOS 2 410 030 (Boehringer Ing.; appl. 2.3.1974). Weber, K.H. et al.: Arzneim Forsch. (ARZNAD) 36, 518 (1986). alternative synthesis: DOS 2 503 235 (Boehringer Ing.; appl. 27.1.1975). DOS 2 533 924 (Boehringer Ing.; appl. 30.7.1975). synthesis of 5-(2-chloropheny 1)-1,3-dihydro-2H-thieno[2,3-e]-1,4-diazepin-2-one: DOS 2 221 623 (Hoffmann-La Roche; appl. 3.5.1972; CH-prior. 14.5.1971). Gewald, K.: Chem. Ber. (CHBEAM) 98; 3571 (1965). Formularion(s): tabl. 0.25 mg Trade Name(s): D: Lendormin (Boehringer I: Lendormin (Boehringer J: Lendormin (Nippon Ing.) Ing.1 Boehringer) Broxyquinoline ATC: A07AX01; GOlAC06; POI AAOl Use: intestinal antiseptic RN: 521-74-4 MF: C,H,Br,NO MW: 302.95 EINECS: 208-317-8 LDso: 7420 mgkg (M, p.0.) CN: 5,6-dibromo-8-quinolinol oxyquinoline (q. v.) Broxyquinoline Reference(s): Bedall, K; Fischer, 0. et al.: Ber. Dtsch. Chem. Ges. (BDCGAS) 14, 1367 (1881). Zinnei; Fiedler: Arch. Pharm. Ber. Dtsch. Pharm. Ges. (APBDAJ) 291,493 (1958). DOS 2 515 476 (Chem. Fabrik Kak; appl. 9.4.1975). Formulation(s): ointment 1.5 % Trade Name(s): D: Dysentrocym (Sano1)- comb.; wfrn Fenilor Lutschtabletten (UCB); wfrn Intestopan (Sandoz)-comb.; F: Colipar (UcCpha); wfrn wfm Entercine (Robapharm); Sandoinl-C (Sandoz)- wfm comb.; wfrn B Bucillamine B 277 Intestopan (Sandoz)-comb.; Norquinol (Norgan)-comb.; wfm wfm Bucillamine (DE-019; SA-96; Tiobutarit) RN: 65002-17-7 MF: C7H13N03S2 MW: 223.32 LD50: 2285 mgkg (M, i.p.); 989 mglkg (M, i.v.) CN: N-(2-mercapto-2-methyl-1-oxopropyl)-~-cysteine 3.3-dimethyl- benzyl a-benzylthio- ocryllc acid rnercoptan isobutyric acid (I) a-benzylthio- isobutyryl chloride ATC: MOICC02 Use: immunomodulator. treatment of Referencefs): US 4 137 420 (Santen; 30.1.1979; J-prior. 8.3.1976). DE 2 709 820 (Santen; appl. 7.3.1977; J-prior. 8.3.1976). medical use as mucolytic: , US 4305 958 (Santen; 15.12.1981; J-prior. 8.3.1976). Formulation(s): tabl. 100 mg (sugar coated) Trade Name(s): 1: Rimatil (Santen) rheumatoid arthritis Bucladesine sodium ATC: COICE04 Use: cardiotonic, phosphodiesterase inhibitor, positive inotropic acting drug RN: 16980-89-5 MF: Cl,H23N,Na0,P MW: 49 1.37 EINECS: 241-059-4 LD,,: 543 mglkg (M, i.v.); >5 glkg (M, p.0.); 448 mgkg (R, i.v.); >5 gkg (R, p.0.) CN: N-(1-oxybuty1)adenosine cyclic 3',5'-(hydrogen phosphate) 2'-butanoate monosodium salt 278 B Buclizine bucladesine RN: 362-74-3 MF: C,xH,N,OxP MW: 469.39 EINECS: 206-649-8 OH adenosine cyclic 3',5'-(hydrogen phosphate) butyric anhydride buclodesine (I) H N o=p-0 0 I pCH3 0 ONa I Budodesine sodium Reference (s): JP~ 195 096 (Daiichi Seiyaku; appl. 14.2.1975). JP 51 113 896 (Daiichi Seiyaku; appl. 31.3.1975). JP 5 239 699 (Daiichi Seiyaku; appl. 26.9.1975). Formulation(s): amp. 0.05 mg, 0.2 mg; tabl. 200 mg, 400 mg Trade Name(s): J: Actocin (Daiichi) Buclizine (Histabutizine) ATC: R06AEO1 Use: antiallergic, antihistaminic RN: 82-95-1 MF: C2,H3,ClN2 MW: 433.04 EINECS: 201-448-1 CN: 1-[(4-chlorophenyl)phenylmethyl]-4-[[4-(l,1-dimethylethyl)phenyl]methyl]piperazine dihydrochloride RN: 129-74-8 MF: C2,H3,C1N,. 2HC1 MW: 505.96 EINECS: 204-962-4 LD,,,: 21 00 mgkg (M, p.0.) 1 Buclosamide B 279 1 4-chiorobenz- ethyl piperozine- ethyl 4-(4-chlorobenz- hydryl chloride N-carboxylate hydry1)piperazine-1 -carboxylote (I) H&' 'CH, ' + - 4-tert-butyl- benzyl chloride Reference(s): DE 964 048 (H. Morren; appl. 1952; B-prior. 195 1). Formulation(s): tabl. 25 mg Trade Name(s): D: Migralave (Temm1er)- F: Aphilan (Darcy) GB: Migraleve (Pfizer comb. with paracetamol Consumer)-comb. Buclosamide ATC: DOlAE12 Usc: fungicide RN: 575-74-6 MF: CI,H,,CINO2 MW: 227.69 EINECS: 209-390-9 CN: N-butyl-4-chloro-2-hydroxybenzamide methyl 4-chloro- butylamine salicylate US 2 923 737 (Hoechst; 2.2.1960; D-prior. 26.1.1956). Formulation(s): ointment 10 g1100 g; sol. 10 dl00 ml Buclosarnide I Trade Narne(s): D: Jadit (Hoechst)-comb.; Jadit-Hydrocortisone I: Jadit (Hoechst)-comb.; wfm (Hoechst)-comb.; wfm wfm F: Jadit (Hoechst); wfm 280 B Bucloxic acid Bucloxic acid (Acide bucloxique) ATC: NO2 Use: anti-inflammatory RN: 32808-51-8 MF: Cl6HI,ClO, MW: 294.78 EINECS: 251-231-0 LD,,: 852 mglkg (M, p.0.); 120 mglkg (R, p.0.) CN: 3-chloro-4-cyclohexyl-y-oxobenzenebutanoic acid calcium salt RN: 32808-53-0 MF: C,,H,,CaCl,O,, MW: 627.62 EINECS: 251-232-6 LD,,: 1700 mgkg (M, p.0.); 175 mglkg (R, p.0.) cyclohexyl- succinic 4-0x0-4-(4-cyclohexyl- benzene anhydride pheny1)butyric acid Reference(s): DE 2 021 445 (Clin-Byla; appl. 2.5.1970; F-prior. 12.5.1969). GB 1 315 542 (Clin-Byla; appl. 7.5.1970; F-prior. 12.5.1969). Trade Nnrnefs): F: Esfar (Midy); wfm Bucloxic acid ATC: C07A Use: P-adrenoceptor blocker RN: 58409-59-9 MF: C1,H2,NO4 MW: 305.37 LD,,: 31 mglkg (M, i.v.); 680 mgkg (M, p.0.) CN: 8-[3-[(1,1-dimethylethy1)amino]-2-hydroxypropoxy]-5-methyl-2H-1-benzopyran-2-one hydrochloride RN: 30073-40-6 MF: C,,H2,N04 . HCI MW: 341.84 H C H C 1. HBr '0 '0 HOOC~~OO~ + @OH H".04b OH CH3 '3'3 rnolic acid 2-methoxy- 5-rnethyl-8- 5-methyl- rnethoxycournorin phenol . phosphorus 5-( 2-chl0rophenyl )- pentosulfide 7-brom 0-5 -( 2- 1,3-dihydro-2H-thieno- chloropheny1 )- 1. 3- [2,3-el-1.4-diozepin- 2-one (I) 276 B Broxvauinoline 1. N2H4 CH. H oJ- 2. ;OXOhcti3. (synthetic) RN: 47 9-6 8-5 MF: CzzHI,Br MW: 363.30 EINECS: 20 7-5 3 7-1 CN: 1-( 2-bromo-l,2-diphenylethenyl )-4 -ethylbenzene I-ethyl-4-phenyl- phenylmognesium 1.2-diphenyl- 1-( 4- Broporestrol ocetylbenzene. 2561 4-0 3-3 MF: C,,H,,,BrN,O, MW: 654.61 EINECS: 24 7-1 2 8-5 LD,: >800 mglkg (M, p.0.); 72 mglkg (R, i.v.) CN: (5'a )-2 -bromo-l2'-hydroxy-2&apos ;-( l -methylethyl )-5 &apos ;-( 2-methylpropyl)ergotaman-3',6',18-trione
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