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Pharmaceutical Substances Syntheses, Patents, Applications - Part 54 doc

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CN: I -[2-chlorophenyldiphenylmethyl]- IH-imidazole 2-chloro- 2-chlorobenzo- 2-chlorotriphenyl- methyl chloride 11 2-chloro- phenylrnognesiurn 2-chlorotriphenyl- benzophenone In bromi

Trang 1

Clorprenaline C 531

: Reference(s):

! DOS 2 846 083 (Fidia; appl 23.10.1978; I-prior 17.11.1977)

US 4 296 039 (Fidia; 2O.lO.lY8 I; I-prior 17.1 1 l977)

, synthesis of ethyl 2-(2-diethy1aminoethyl)acetoacetate:

Weizmann, Ch.; Bergmann, E.; Sulzbacher, M.: J Org Chem (JOCEAH) 15, 918 (1950)

synthesis of 2-chlororesorcinol:

Schamp, N : Bull Soc Chim Belg (BSCBAG) 73,35 (1946)

Wauzlick, H.V.; Mohrmann, S.: Chem Ber (CHBEAM) 96, 2257 (1963)

Fonnulation(s): amp 30 mg15 ml; cps 100 mg; vial 30 mg

Trade Name(s):

I: Assogen (Metapharma) Proendotel (Fidia; 199 1)

Use: bronchodilator RN: 3811-25-4 MF: CIIHl,CINO MW: 213.71 EINECS: 223-291-8

CN: 2-~hloro-a-[[(l-methylethyl)amino]methyl]benzenemethanol

hydrochIoride monohydrate

RN: 5588-22-7 MF: C,lH16C1N0 HC1 H,O MW: 268.18

LD,: 54 mg/kg (M, i.v.); 298 mglkg (M, pa.);

68 mgkg (R, i.v.); 450 mglkg (R, p.0.);

>400 rn@g (dog, p.0.)

2'-chloro-

acetophenone

P-bromo- 2'-chloro- acetophenone

isopropylamine I ~lorprenoline 1

Reference(s):

US 2 816 059 (Lilly; 1957; appl 1956)

Formulation(s): sol 2 % (inhalation)

Trade Name(s):

Clopinerin (Nippon Shoji) Kalutein (Tatsumi) Propran (Kobayashi Kako) Clorprenalin HC1 (Kongo)

Trang 2

532 C Clortermine

Clortermine

RN: 10389-73-8 MF: Cl,HI4ClN MW: 183.68

CN: 2-chloro-a,a-dimethylbenzeneethanamine

hydrochloride

RN: 10389-72-7 MF: Cl,H14ClN HCI MW: 220.14

LD,,,: 332 m g k g (R, p.0.)

ATC: NO7 Use: appetite depressant

15; /

acetone

\

2-chlaro- 2-chlorobenzyl- 1 -(2-chloro-

Reference(s):

US 3 415 937 (Ciba; 10.12.1968; appl 1.12.1966; prior 31.8.1964)

Formulation(s): tabl 50 mg

Trade Namefs):

USA: Voranil (USV); wfm

Use: anabolic RN: 855-19-6 MF: C,,H&10, MW: 364.91 EINECS: 212-720-4

CN: (1 7P)- 17-(acetyloxy)-4-chloroandrost-4-en-3-one

clostebol

RN: 1093-58-9 MF: Cl,H,7C10, MW: 322.88 EINECS: 214-133-9

0 0

O H20Z, NaOH

HCI, CHC13

,

hydrogen peroxide

Clostebol acetote

Reference(s):

US 2 953 582 (Soc Farmaceutici Italia; 20.9.1960; appl 26.10.1M6; I-prior 23.4.1956)

US 2 933 510 (Julian Labs.; 19.4.1960, Prior 3.2.1955)

Formulation(s): cream 0.5 %; sugar coated tabl 15 mg; vial 10 mgl1.5 ml

Trade Name(s):

Trang 3

Clotiazepam C 533 I: Alfa-Trofodermine Trofodermin (Farmitalia)- J: Steranabol (Sumitomo)

Use: anxiolytlc, benzodiazepine analog RN: 33671-46-4 MF: C,,H,,ClN,OS MW: 318.83 EINECS: 251-627-3

LD,,: 440 mglkg (M, i.p.); 636 mglkg (M, p.0.)

CN: 5-(2-chlorophenyl)-7-ethyl-1,3-dihydro-l-methyl-2H-thieno[2,3-e]-1,4-diazep~n-2-one

3-(2-chloro- ethyl glycinote

benzoyl)-5-ethyl- hydrochloride (11)

2-methylomino-

thiophene (I)

40;

CH3

-

Clotiazepom

N-benzyloxy-

corbonylglycyl

chloride

NH,

dimethyl zulfote

Trang 4

534 C Clotrimazole

Reference(s):

DOS 2 107 356 (Yoshitomi; appl 16.2.1971; J-prior 17.2.1970, 23.2.1970, 7.3.1970, 25.6.1970, 31.7.1970)

US 3 849 405 (Yoshitomi; 19.1 1.1974; J-prior 17.2.1970, 23.2.1970,7.3.1970, 25.6.1970, 31.7.1970)

Formulntion(s): drops 1 %; tabl 5 mg, 10 mg, 20 mg

Trade Name(s):

D: Trecalmo (Bayer Vital; Tienor (Farmaka)

F: VCratran (Murat; 1984) Isocline (Sawai)

I: Rizen (Puropharma; 1984) Lieze (Yoshitomi)

Reilyfter (Maruko) Rize (Yoshitomi)

Use: antifungal RN: 23593-75-1 MF: C,,H,,ClN, MW: 344.85 EINECS: 245-764-8

LD,,: 76 1 mg/kg (M, p.0.);

708 mglkg (R, p.0.);

>2 g/kg (dog, p.0.)

CN: I -[(2-chlorophenyl)diphenylmethyl]- IH-imidazole

2-chloro- 2-chlorobenzo-

2-chlorotriphenyl- methyl chloride (11)

2-chloro- phenylrnognesiurn 2-chlorotriphenyl-

benzophenone (In) bromide corbinol

Clotrimazole

Reference(s):

DE 1 617 481 (Bayer; appl 15.9.1967)

DAS 1 670 976 (Bayer; appl 29.1.1968)

DE 1 670 977 (Bayer; D-prior 29.1.1968)

US 3 660 577 (Bayer; 2.5.1972; D-prior 15.9.1967)

US 3 705 172 (Bayer; 5.12.1972; D-prior 15.9.1967)

Trang 5

mode of mechanism:

Berg, D et a].: Arzneim.-Forsch (ARZNAD) 34 (I), 139 (1984)

Cloxacillin C 535

! medical use at Herpes labialis:

$ US 4 438 129 (Pennwalt; 20.3.1984; appl 27.9.1982)

special formulations:

DOS 3 321 043 (Bayer; appl 10.6.1983)

EP 128 459 (Bayer; appl 30.5.1984; D-prior 10.6.1983)

EP 112 485 (Bayer; appl 17.1 1.1983; D-pr~or 25.1 1.1982)

combination wirh corticosteroids:

EP49 468 (Schering Corp.; appl 30.9.1981; USA-prior 6.10.1980)

&rmulation(s): pessaries 100 mg, 200 mg, powder 10 mglg (1 %); 500 mg; sol I %, 10 mg; spray 10 mglml

(1 %); topical cream 1 %, 10 mg; vaginal cream 10 mg, 20 mglml (2 %, 10 %); vaginal tabl

100 mg, 200 mg, 500 mg

Trade Name(s):

D: Antifungal (Hexal)

Apocanda (esparma)

ARU Spray (Chauvin

ankerpharm)

Azutrimazol (Azupharma)

Benzoderm (Athenstaedt)

Candazol (Apogepha)

Canesten (Bayer; 1973)

Canifug (Wolff)

Cloderm (Dermapharm)

Cutistad (Stada)

Durafungol (durachemie)

Gilt (Solvay Arzneimittel)

Gyno Canesten (Bayer

Vital)

Holfungin (Holborn)

Jenamazol (Jenapharm)

Lobalacid (Kade)

Mono Baycuten (Bayropharm)

M ycofug (Hermal) Myko Cordes (Ichthyol) Mykofungin (Wyeth) Mykohaug (betapharm) Ovis (Warner-Lambert) Pedisafe (BASF Generics) Radical (Maurer) Uromycol (Hayer) F: Trimysten (Roger Bellon;

1978); wfm GB: Canesten (Bayer; 1973) Canesten HC (Bayer)- comb

Lotriderm (Dominion)- comb

Masnoderm (Dominion)

I: Antimicotico Same (Savoma)

Canesten (Bayropharm;

1973) Desamix Effe (Savoma)- comb

Gy no-Canesten (Bayropharm) Meclon (Farmigea) J: Empecid (Bayer-Takeda;

1976) Tao (Toko-Fujisawa) USA: Fungoid (Pedinol) Lotrimin (Schering; 1976) Lotrisone (Schering) Mycelex (Bayer)

Use: antibiotic RN: 61-72-3 MF: C,yH18ClN30SS MW: 435.89 EINECS: 200-5 14-7

CN: [2S-(2a,5a,6~)~-6-[[[3-(2-chlorophenyl)-5-methyl-4-isoxazolyl]carbonyl]amino]-3,3-dimethyl-7-oxo-4- thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid

monosodium salt

RN: 642-78-4 MF: Cl,H,7ClN,NaOSS MW: 457.87 EINECS: 21 1-390-9

LDS,: 916 mglkg (M, i.v.); 5 glkg (M, p.0.);

1660 mgkg (R, i.v.); 5 glkg (R, p.0.)

monosodium salt monohydrate

RN: 7081-44-9 MF: ClyH,7C1N3NaOSS H,O MW: 475.89

LD,,: ll00mg/kg(M,i.v.);5g/kg(M,p.o.);

1660 mgkg (R, i.v.); 5 glkg (R, p.0.)

Trang 6

536 C Cloxazolam

CHO hydroxyl- - \=N-OH )=N-OH ethyl acetoacetate

2-chloro- Z-chlorobenz-

benzaldehyde aldehyde oxirne

3-(2-chlorapheny1)- 5-methylisaxazale- 4-carboxylic acid

C O O H

C H 3

US 2 996 501 (Beecham; 15.8.1961; GB-prior 3 1.3.1960)

GB 905 778 (Beecham; appl 31.3.1960; valid from 14.3.1961)

GB 958 478 (Beecham; appl 28.2.1963; USA-prior 13.3.1962)

Formulation(s): amp 250 mg, 500 mg; cps 250 mg, 500 mg; tabl 250 mg, 500 mg (as sodium salt)

Trade Name(s):

D: Ampiclox (Beecham)-

comb with ampicillin; wfm

Pyoclox (Beecham)-comb

with carbenicillin; wfm

Pyolox (Beecham)-comb

with carbenicillin; wfm

F: Orbenine (SmithKline

Beecham)

GB: Ampiclox (SmithKline Beecham)-comb with ampicillin

Orbenin (Beecham); wfm I: Amplium (Sigma-Tau)- comb

Cloxac (Formulario Naz.) J: Acucillin (Fuji)-comb

Methocillin-S (Meiji Seik Orbenin (Beecham- Fujisawa) Prostaphlin (Bristre-Bany Solcillin C (Takeda)-coml Totaclox (Beecham)-com USA: Cloxapen (Beecham); wfi Tegopen (Bristol); wfm

Use: tranquilizer RN: 24166-13-0 MF: C1,H,,C12N202 MW: 349.22

LD,,,: 2630 mglkg (M, p.0.);

1780 mglkg (R, p.0.)

CN: 1 0-chloro- 1 1 b-(2-chloropheny1)-2,3,7,11 b-tetrahydrooxazolo[3,2-d][l,4]benzodiazepin-6(5H)-one

Trang 7

Clozapine C 537

H

2-amino-2'3- bromoocetyl

dlchlorobenzo- chloride

heno one

Referencefs):

DOS 1 812 252 (Sankyo; appl 26.11.1968; J-prior 27.1 1.1967)

DOS 1 817 923 (Sankyo; appl 26.1 1.1968; J-prior 27.1 1.1967)

alternative synthesis:

DOS 1 954 065 (Sankyo; appl 23.10.1969; J-prior 24.10.1968, 17.4.1969)

US 3 696 094 (Sankyo; 3.10.1972; J-prior 24.10.1968,25.10.1968)

US 3 772 371 (Sankyo; 13.1 1.1973; J-prior 27.1 1.1967)

review:

Schulte, E.: Dtsch Apoth Ztg (DAZEA2) 115, 1253, 1828 (1975)

Formulation(s): tabl 1 mg, 2 mg

Trade Namefs):

J: Enadel (Taito Pfizer) Sepazon (Sankyo)

cl%

H 0

Cloxozolorn

Use: neuroleptic RN: 5786-21-0 MF: Cl,H19C1N, MW: 326.83 EINECS: 227-313-7

LD,,: 36.5 mglkg (M, i.v.); 150 m g k g (M, p.0.);

41.6 m a g (R, i.v.); 251 m g k g (R, p.0.);

145 m a g (dog, p.0.)

CN: 8-chloro-1144-methyl- 1 -piperazinyl)-5H-dibenzo[b,cJ[ 1,4]diazepine

4-chloro-2-

nitrooniline

H3C\

methyl 2-chloro- benzoate

F H 3

8

b

I -methyl- piperozine (1)

b

Trang 8

538 C Cobamamide

1 KO-C(CH3)3

Ciozopine

1 potossium tert-butylote

2 4-nitrobenzyl chloride

8 - c h l o r o - l l -thioxo

10.1 1 -dihydro-5H-

dibenzo[b.e][l.4]-

diozepine

Reference(s):

CH 404 677 (Dr A Wander; appl 2.12.1960)

CH 398 620 (Dr A Wander; appl 16.8.1960)

GB 980 853 (Dr A Wander; appl 16.8.1961; CH-prior 16.8.1960,2.12.1960)

NL 147 426 (Dr A Wander; appl 24.5.1963; CH-prior 25.5.1962, 8.6.1962, 5.12.1962, 15.2.1963)

DE 1 280 879 (Wander; appl 7.8.1961; CH-prior 16.8.1960,2.12.1960)

US 3 539 573 (Wander; 10.11.1970; CH-prior 16.8.1060,2.12.1960,20.7.1961,25.5.1962,5.12.1962,15.2.1963,

22.3.1967, 11.7.1967, 3.11.1967)

Hunziker, F et al.: Helv Chim Acta (HCACAV) 50, 1588 (1967)

Formulation(s): inj sol 50 mgl2 ml; tabl 25 mg, 100 mg

Trade Name(s):

D: Clozaril (Novartis) F: Leponex (Novartis)

Leponex (Novartis Pharma) USA: Clozaril (Novartis)

(Adenosylcobalamin; Coenzym B,,; Djbencozide) Use: anabolic

RN: 13870-90-1 MF: C7,Hl,C~N,RO17P MW: 1579.61 EINECS: 237-627-6

LDSo: 1 g/kg (M, i.v.)

CN: cobinamide Co-(5'-deoxyadenosine-5') deriv hydroxide dihydrogen phosphate (ester) inner salt 3'-ester

with 5,6-dimethyl-l-a-~-ribofuranosyl-1H-benzimidazole

Zn/HCI or Zn/CH3COOH or NoBH4 [under exclusion of 02]

b I1 hydroxocobolomin (I)

Trang 9

Cobamamide C 539

hydridocobolornin (11)

aq HCI

II f

3 K2C03 or NoOH

1

2 5'-deoxy-5'-iodoodenosin

Reference(s):

a Bemhauer, K et al.: Angew Chem (ANCEAD) 75, 1145 (1963)

US 3 213 082 (Glaxo; 19.10.1965; GB-prior 11.12.1961)

b US 3 461 114 (Yamanouchi; 12.8.1969; J-prior 1.10.1966)

Formulation(s): cps 0.25 mg, 1 mg; drops 30 mg; tabl 0.25 mg, I mg, 2.5 mg

Trade Name(s):

D: Xobaline (Albert-Roussel); wfm

Trang 10

540 C Cocarboxvlase

F: Vibalgan (Doms-Adrian)-

comb

I: Amico (SIT)-comb

Aminozim (Pierrel)-comb J:

Anabasi (Zilliken)

Calciozim (Pierrel)-comb

Calisvit (Menarini)-comb

Cobaforte (Roussel)

Cocametina B 12 (Sigma-

Tau)-comb

Glutacomplex (Chemi1)-

comb

Hepafactor Complex (Sigma-Tau)-comb

Indusil (Recordati) Actavix (Nippon Kayaku) Actimide (Tobishi) Ademide (Toyo Jozo) Cabarol (Daiko) Calomide (Yamanouchi) Cobaforte (Roussel- Chugai)

Cobalan (Daiichi) Cobaltamin-S (Wakamoto)

Cobamyde (Shiu Nihon Jitsugyo)

Funacomide (Funai) Hokurarnide (Hokuriku) Hycobal (Eisai) Hyrasedon (Sawai) Lasedmeide (Choseido) Metamide (Nakataki) Sabalamin (Sato-Santen) Satomid (Shinshin) generics and combination preparations

Use: enzyme against metabolic disturbance

RN: 154-87-0 MF: CI,H,,CIN,O,P,S MW: 460.77 EINECS: 205-836-1

LD,,,: > I g/kg (M, i.m.);

>500 mglkg (R, i.m.)

CN: 3-[(4-amino-2-methyl-5-pyrimidinyl)methy1]-4-methyl-5-(4,6,6-trihydroxy-4,6-dioxido-3,5-dioxa-4,6- diphosphahex-1-y1)thiazolium chloride

H2N

Cacarboxylase

Work up of the reaction mixtures on ion-exchangers

Reference(s):

US 2 991 284 (E Merck AG; 4.7.1961; D-prior 28.9.1957)

Formulation(s): vial 5.8 mgIlO mg, 20 mg, 50 mg, 100 mg

Trade Name(s):

D: Cernevit (Baxter)-comb

F: CernCnit (Baxter)-comb

Plenyl (0berlin)-comb

generics and combination

preparations

I: Adenobeta (Salus

Research)-comb

Adenoplex (Lepetit)-comb

Adenovit (Nuovo Cons

Sanit Naz.)-comb

Benexol (Roche)-comb

Bivitasi (ISI)

Firmavit (Firma)-comb

Fosforilasi (Po1ifarma)- comb

Neogeynevral (Geymonat)- comb

Piruvasi (Delalande 1snardi)-comb

salts and combination preparations

J: Bicholase (Fuso) Cocalbose (Fuji Zoki) Cocalox (Maruko) Co-Carten (Sanken) Coxylase (Funai)

Carboxin (Toa Eiyo- Yamanouchi) Hiactose (Ohno) Metabolase (Takeda) Neo Alinachiol (Kanto) Nutrase (Kyorin) Paraboramin (Hoei) Proffit (Isei) Pyrolase (Chugai) Reborase (Kanto) Thiamilase (Hokuriku)

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