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Pharmaceutical Substances Syntheses, Patents, Applications - Part 200 pptx

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2.5 mg, 5 mg Trade Names: D: Aerodur Astrdpharma- stern ARUBENDOL Isis Pharma Asthmo Krewel Meuselbach Asthmoprotect Azupharma Bricanyl pharma-stern; 1971 Bricanyl Astra-comb.. with the

Trang 1

Terbinafine T 1991

process for a polyrnorph:

C A 2 173 407 (Acic; appl 3.4.1993)

WO 9 721 705 (Uetikon; appl 12.12.1996; D-prior 13.12.1995)

US 5 587 377 (Invamed; USA-prior 24.10.1995)

capsules:

WO 9 805 308 (Novartis; appl 31.7.1997; USA-prior 1.8.1996)

pharmaceutical composition for treating glaucoma:

W09 531 200 (Senju Pharm.; appl 15.5.1995; J-prior 18.5.1994)

(R)-(+)-terazosin:

W09 200 073 (Abbott; appl 26.6.1991; USA-prior 29.6.1990)

Formulation(s): cps (USA) 1 mg, 2 mg, 5 mg, 10 mg; tabl 1 mg, 2 mg, 5 mg, 10 mg (as monohydrochloride

dihydrate)

Trade Nameis):

D: Flotrin Start (Abbott) Hytrine (Abbott) Vasomet (Mitsubishi) Heitrin (Abbott; 1985) GB: Hytrin (Abbott; 1987) USA: Hytrine (Abbott; 1987) F: Dysalfa (DEbat) J: Hytracin (Dainabot)

Terbinafine

(SF-86327)

ATC: DOlAEI5; DOIBA02; J02AX Use: orally and topically active antifungal

RN: 91 161-71-6 MF: C2,H2,N MW: 291.44

LD,,: 393 mglkg (M, i.v.); 4000 mglkg (M, p.0.); >2 glkg (M, s.c.);

213 m d k g (R, i.v.); 4000 rnglkg (R, p.0.); >2 g/kg (R, s.c.); >2 &kg (R, skin)

CN: (E)-N-(6,6-dimethyl-2-hepten-4-ynyl)-N-methyl-l-naphthalenemethanamine

hydrochloride

RN: 78628-80-5 MF: C2,H2,N HCl MW: 327.90

LD,o: >2 @kg (M, s.c.);

>2 glkg (R, s.c.); >2 g k g (R, skin)

CH3 CIHgLi

CH3 butyl-

lithium O H

acrolein tert-butyl-

acetylene

I Terbinofine

1 -bromo-6.6-dimethyl- (I -nophthyl-

hept-2-en-4-yne (I) rnethyl)methyl-

ornine

Reference(s):

EP 24 587 (Sandoz; appl 6.8.1980; CH-prior 22.8.1979)

Stiitz, A.; Petranyi, G.: J Med Chem (JMCMAR) 27, 1539 (1984)

Trang 2

1992 T Terbutaline

Formulation(s): cream 10 mglg; tabl 250 mg (as hydrochloride)

Trade Name(s):

D: Lamisil (Novartis; 1991) I: Daskil (LPB) J: Lamisil (Toko Yakuhin-

Use: bronchodilator, tocolytic RN: 23031-25-6 MF: C,,H,,NO, MW 225.29 EINECS: 245-385-8

CN: 5-[2-[(I, 1 -dimethylethyl)amino]- 1 -hydroxyethyl]- l,3-benzenediol

sulfate (2:l)

RN: 23031-32-5 MF: C12H19N03 1/2H2S04 MW: 548.65 EINECS: 245-386-3

LD,,,: 36mg/kg(M,i.v.);205mg/kg(M,p.o.);

69 mglkg (R, i.v.); 8700 mglkg (R, p.0.);

11 6 mglkg (dog, i.v.); 1520 mglkg (dog, p.0.)

butylarnine 3',5'-dibenzyloxy-

acetophenone

cHdm

? Y o Om

Terbutaline

Refer.ence(s):

DE 1 643 296 (Draco; prior 17.10.1967)

GB 1 199 630 (Draco; Lund; appl 18.10.1967; S-prior 19.10.1966)

US 3 937 838 (Draco; 10.2.1976; prior 18.10.1967)

US 4 01 1 258 (Draco; 8.3.1977; prior 21.6.1973)

Formulation(s): amp 0.5 mglml, 1 mglml; powder inhaler 0.5 mglpuff; sol for inhalation 10 mglml (as

sulfate); s r cps 7.5 mg; s r tabl 7.5 mg; tabl 2.5 mg, 5 mg

Trade Name(s):

D: Aerodur (Astrdpharma-

stern)

ARUBENDOL (Isis

Pharma)

Asthmo (Krewel

Meuselbach)

Asthmoprotect

(Azupharma)

Bricanyl (pharma-stern;

1971) Bricanyl (Astra)-comb

with guaifenesin Butaliret (Fatol) Butalitab (Fato1)Contimit (Lindopharm)

Eudur (Astra)-comb with theophyllin

Terbul (Hexal) Terbutalin (Mundipharma; Stada; Aluid Pharma; ratiopharm)

Terbuturmant (Desitin) F: Bricanyl (Astra; 1973) Bricanyl Turbohaler (Astra) GB: Bricanyl (Astra; 1971) I: Bricanyl (Astra)

Trang 3

r'

Terconazole T 1993

J: Bricanyl (Astra-Fujisawa; Bristurin (Bristol) Brinacyl (Hoechst Marion

Terconazole

(Triconazole)

ATC: GOIAG02 Use: antifungal RN: 67915-31-5 MF: C2,H3,C12N503 MW: 532.47 EINECS: 267-751-6

LD,,: 1741 mgkg (Rm, p.0.); 849 mglkg (Rf, p.0.)

CN: cis-l-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-l-ylmethyl)-l,3-dioxolan-4-yl]methoxy]phenyl]-4-

(I -methylethyl)piperazine

CI

2'.4'-dichloro- glycerol

acetophenone

I (iN3 NOH

1 1H-1,2,4-triozole

1 -(4-methoxy- acetone

pheny1)piperozine

I Terconozole

Trang 4

1994 T Terfenadine

Reference(s):

DE 2 804 096 (Janssen; appl 3.8.1978; prior 31.1.1978)

US 4 358 449 (Janssen; 9.11.1982; prior 21.1 1.1977)

US 4 144 346 (Janssen; 13.3.l979; prior 21.1 1.1977, 31.1.1977)

US 4 223 036 (Janssen; 16.9.1980; prior 8.l.l979,2l.ll.l977,3l.l.l977)

Heeres, J et a].: J Med Chem (JMCMAR) 26, 61 1 (1983)

synthesis of 2-bromomethyl-2-(2,4-dichloropheny1)-4-(benzoyloxymethyl)-1,3-dioxolane:

Heeres, J et al.: J Med Chem (JMCMAR) 22, 1003 (1979)

Formulation(s): suppos 80 mg; vaginal cream 0.4 %, 0.8 %; vaginal tabl 80 mg

Trade Name(s):

D: Tercospor (Cilag; 1985); I: Terconal (Italchimici) USA: Terazol (Ortho-McNeil;

Use: antihistaminic, antiallergic RN: 50679-08-8 MF: C,,H,,NO, MW: 471.69 EINECS: 256-710-8

LD,,,: 5 glkg (M, p.0.);

5 glkg (R, p.0.)

CN: a-[4-(1,1-dimethylethyl)phenyl]-4-(hydroxydiphenylmethy1)-1-piperidinebutanol

KHC03, KI

toluene

+ c&cW3

/ \ / \

-

OH - W3C CH3

azacyclonol (1) 1-(4-tert-butylphenyl)-

( q v.1 4-chloro-1 -buton01

Terfenodine

KHCO, KI,

NoBH, sodium borohydride

Reference(s):

DOS 2 303 305 (Richardson-Merrell; appl 24.1.1973; USA-prior 28.1.1972)

DOS 2 503 362 (Richardson-Merrell; appl 28.1.1975; USA-prior 8.2.1974)

addition to DOS 2 303 306 (Richardson-Merrell; appl 28.1.1975; USA-prior 8.2.1974)

GB 1 412 605 (Richardson-Merrell; valid from 15.12.1972; USA-prior 28.1.1972)

US 3 878 217 (Richardson-Merrell; lS.4.1975; appl 12.7.1973; prior 28.1.1972)

Formulation(s): susp 30 mg15 ml; s r tabl 60 mg in comb with pseudoephedrine.HC1; tabl 60 mg, 120 mg

Trang 5

Terodiline T 1995

Trade Narnefs):

D: Balkis (Dolorgiet) Terfium (Hexal) J: Triludan (Merrell Dow-

Histaterfen (Azupharma) F: Teldane (Merrell); wfm USA: Seldane (Hoechst Marion Teldane (Hoechst; 1982) Teldane (Richardson- Roussel; 1985)

Terfedura (durachemie) Merrell); wfm

Terfemundin GB: Triludan (Hoechst)

(Mundipharma) I: Teldane (Lepetit); wfm

Use: antianginal, calcium antagonist, anticholinergic, treatment of urinary frequency and incontinence RN: 15793-40-5 MF: C,H,N MW: 281.44

CN: N-(l,l-dimethylethyl)-a-methyl-y-phenylbenzenepropanamine

hydrochloride

RN: 7082-21-5 MF: C2,H,N HCI MW: 317.90

LD,,: 28 mglkg (M, i.v.); 330 mglkg (M, p.0.); 170 mglkg (M, s.c.)

27 mgkg (R, i.v.); 465 mg/kg (R, p.0.); 370 mglkg (R, s.c.)

63.3 g/kg (dog, p.0.)

!.p-diphenylethyl tert-butyl-

methyl ketone (I) amine (II)

Terodiline I

2 H2 Pd-C

1 aluminum trichloride

Referencefs):

a DE 1 170 417 (Aktiebolaget Recip.; appl 8.1 1.1961; GB-prior 8.11 l96O)

b HU T32 331 (Richter Gedeon Vegyeszeti Gyar; appl 30.7.1984; HU-prior 21.9.1982)

Formulation(s): f c tabl 12.5 mg, 25 mg (as hydrochloride)

Trade Narnefs):

D: Mictrol (Fresenius; 1990); GB: Micturin (Pharmacia & Midurin (Uabi; 1986); wfm

Trang 6

1996 T Tertatolol

Use: fhdrenoceptor antagonist, antihypertensive

RN: 34784-64-0 MF: C,6H2SN0,S MW: 295.45

CN: (f)-l-[(3,4-dihydro-2H-1-benzothiopyran-8-yl)wxy]-3-(l,l-dimethylethyl)amino]-2-propanol

hydrochloride

RN: 33580-30-2 MF: CI6H,,NO2S HC1 MW: 331.91 EINECS: 251-578-8

LD,,,: 120 mglkg (M, i.p.); 37 mg/kg (M, i.v.);

90 mglkg (R, i.p.); 40 mglkg (R, i.v.)

1 PPA

2 N p , , KOH

1 polyphosphoric' acid

2 hydrozine 2-methoxy- 8-chloro- 3-(2-methoxyphenyl

thiophenol propianic acid thio)propionic acid

B-hydroxy- thiochroman (I)

Reference(s):

DE 2 115 201 (Science Union et Cie.; appl 29.3.1971; GB-prior 6.4.1970)

US 3 960 891 (Science Union et Cie.; 1.6.1976; GB-prior 6.4.1970)

US 4 032 648 (Science Union et Cie.; 28.6.1977; GB-prior 6.4.1970)

alternative synthesis:

GB 1 561 153 (Science Union et Cie.; appl 23.8.1976)

Formulation(s): f c tabl 5 mg (as hydrochloride)

Trade Nnme(s):

D : Prenalex (Servier; 1990) F: Artex (Servier; Therval;

1990)

Use: antineoplastic (mamma carcinoma) RN: 968-93-4 MF: C1,H2,01 MW: 300.40 EINECS: 213-534-6

CN: D-homo-17a-oxaandrosta-l,4-diene-3,17-dione

Cylindracorpon rodicolo (ATCC 1101 1)

H H

0 '

Trang 7

Testosterone T 1997

Reference(s):

US 2 744 120 (Olin Mathieson; 1956; appl 1953)

Formulation(s): tabl 50 mg

Trade Name(s):

D: Fludestrin (Bristol-Myers I: Teslac (Squibb); wfm USA: Teslac (Bristol-Myers

Use: androgen RN: 58-22-0 MF: CI,H,802 MW: 288.43 EINECS: 200-370-5

LD,,: >5 g/kg (M, p.0.)

CN: (17P)-17-hydroxyandrost-4-en-3-one

undecanoate

RN: 5949-44-0 MF: C3,H4,03 MW: 456.71

H2/Roney-Ni or NaBH4

sodium

38-acetoxy- 17-oxo-5-

ondroslene

(from 16-dehydropregne-

nolone ocetote)

1

-benzayl

chloride

& , NoC*(cH3)J3

KOH

11

cyclo- aluminum

hexanone triisopropylote

Testosterone

I

Reference(s):

US 2 308 833 (Ciba; 1943; CH-prior 1935)

US 2 308 834 (Ciba; 1943; CH-prior 1935)

US 2 379 832 (Schering Corp.; D-prior 1936)

US 2 387 469 (Ciba; 1945; CH-prior 1935)

starting material:

The Merck Index, 12th Ed., 1569 (1996)

Trang 8

1998 T Testosterone cvvionate

alternative syntheses:

US 2 236 574 (Schering Corp.; 1941, D-prior 1937)

US 2 341 110 (Schering Corp.; 1944, CS-prior 1939)

Formulation(s): cps 40 mg (as undecanoate); plaster 2.5 mgl37 cm2, 4 mgl40 cm2, 5 mgI44 cm2, 6 mg160 cm2

Trade Name(s):

D: Andriol (Organon) I: Mydrotest (Ayerst); wfm Testoviron Depot (Nihon F: Pantestone (Organon SA) Testosterone Tarrico &hering)-comb

Trotoseptine (Boehringer (Mitim); wfm USA: Androderm (SmithKline

Testoral (Organon); wfm Tes-Hol "Z" (Nippon Zoki)

Testosterone cypionate ATC: G O ~ E A O ~

(Testosterone cyclopentylpropionate) Use: depot androgen

RN: 58-20-8 MF: C2,H4,0, MW: 412.61 EINECS: 200-368-4

LD,,,: > I glkg (M, i.p.)

CN: (17~)-17-(3-cyclopentyl-l-oxopropoxy)androst-4-en-3-one

pyridine

Reference(s):

US 2 566 358 (Upjohn; 1951; prior 1949)

DE 896 805 (Upjohn; appl 1951)

Gould, D et al.: J Am Chem Soc (JACSAT) 79,4472 (1957)

testosterone 3-cyclopentyl-

alternative syntheses:

US 2 625 556 (Upjohn; 1953; prior 1949)

ES 241 206 (Alter; appl 1958)

US 2 742 485 (Francesco Vismara; 1956; prior 1954)

Testosterone cypionote

Formulation(s): vial 200 mglml (10 ml)

(4 v ) propionyl chloride

Trade Name(s):

D: Femovirin Amp (Albert-

Rousse1)-comb.; wfm

F: Ch P T ThCramex

(ThCramex): wfm

TestostCrone retard

ThCramex (Thtramex; as

cyclohexylpropionate);

w fm

Trioestrine-Retard ThCramex (ThCra.mex)- comb.; wfrn

Trioestrine-Retard ThCramex (ThCramex; as cyclohexylpropionate)- comb.; wfm

I: Ciclosterone (Farmigea)

Clym depositum (Po1i)- comb

Ginandrolo Depositum (Lusofarmaco)-comb Pertestis-Dep (Orma) Testorit-Dep (Gallo) Testosterone Depositum (Lusofarmaco)

Trang 9

Testosterone enanthate T 1999 J: Depo Testosteron LISA: Virilon (Star)

(Upjohn); wfm

Use: androgen RN: 315-37-7 MF: C,,H,O, MW: 400.60 EINECS: 206-253-5

LD,: 4 mg/kg (M, i.p.):

2 glkg (R, i.p.1

CN: (l7P)- 17-[(I -oxoheptyl)oxy]androst-4-en-3-one

Reference(s):

U S 2 840 508 (Schering AG; 1958; D-prior 1951)

testosterone enanthic anhydride

Formulation(s): amp 250 mglml; vial 200 mglml, 1 g15 ml

Testosterone enanthate

Trade Name(s):

D: Testosteron-Depot F: Androtardyl (Schering) Primodian Depot (Nihon Jenapharm (Jenapharm) GB: Primoteston Depot Schering)-comb

Testosteron Depot- (Schering Chemicals); wfm Testoviron Depot (Nihon

(Rotexmedica) J: Enarmon Depot (Teikoku USA: Delatestryl (Bio-

(Schering)-comb

( q v.)

Testosterone propionate ATC: G03BA03

Use: androgen RN: 57-85-2 MF: C22H3203 MW: 344.50 EINECS: 200-351-1

LD,,: 1350 mgkg (M, p.0.);

1 g k g (R, p.0.)

CN: (17B)-17-(1-oxopropoxy)androst-4-en-3-one

0 0 pyridine

+

testosterone propionic anhydride

(4 v.)

Testosterane propionate

Trang 10

2000 T Tetracaine

rnlcrobiological dehydroganotion Acetabacter posteurionurn

ondrostenediol 17-propionote

Reference(s):

a CH 206 119 (Ciba; appl 1936) addition to CH 203 257

DRP 661 384 (Ciba; appl 1936; CH-prior 1935)

b US 2 236 574 (Schering Corp; 1941; D-prior 1937)

starting material:

The Merck Index, 12th Ed., 107 (1996)

allernarive ryntheses:

US 2 311 067 (Ciba; 1943; CH-prior 1939)

US 2 374 369 (Ciba; 1945; CH-prior 1939)

US 2 374 370 (Ciba; 1945; CH-prior 1939)

Formulotion(s): amp 10 mg, 25 mg, 5 0 mg, 100 mg; amp 5 0 mglml, 100 mglml (in comb.);

ointment 8 0 mg1100 mg (in comb.)

Trade Name(s):

D: Tachynerg (Eberth)-comb

Testosleron Propionat

"Eifclfango" (Eifelfango)

Testoviron (Schering)-

comb

F: Fadiamone (CS)-comb

GB; Sustanon (Organon)-comb

Virormone (Ferring)

I: Teslovis (SIT)

J: Enarmon Susp (Teikoku

Zoki)

Forton (Shionogi)

Primodian Inj (Nihon Schering)

Sonyhod M Inj (Sonybod- Torii)

Testinon (Mochida) USA: Androlan (Lannett); wfrn Androlin (Lincoln); wfrn Andrusol-P (Smith, Miller

& Patch); wfrn

Gy netone (Schering)- comb.; wfrn

Neo-Hombre01 (Organon);

wfrn

Neutron (Myers-Carter)- comb.; wfrn

Oreton Propionate (Schering), wfrn Synandrol (Pfizer); wfrn Synerone (Dow); wfrn Testex (Pasadena Res.); wfrn

Testodet (Merck Sharp & Dohme); wfrn

Testonate (Kay); wtm

Tetracaine

(Amethncaine)

ATC: CO5AD02; D04AB06; NOlBA03; SO1 HA03

Use: local anesthetic RN: 94-24-6 MF: C,,H2,N20, MW: 264.37 EINECS: 202-3 16-6

LD,,,: 6 mglkg (M, i.v.); 300 mglkg (M, p.o.1;

6 mglkg (R, i.v.)

CN: 4-(buty1amino)benzoic acid 2-(dimethy1amino)ethyl ester

no no hydrochloride

RN: 136-47-0 MF: C,511aN202 HC1 MW: 300.83 EINECS: 205-248-5

LD,,,: 6600 ~ g l k g (M, i.v.); 160 rnglkg (M, p.0.);

4500 pglkg (R, i.v.)

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