Processing

Please wait...

Settings

Settings

1. WO2000042999 - PHENYLPROPIONIC ACIDS AND ESTER COMPOUNDS AND METHODS FOR INDUCING BETA-BLOCKADE

Publication Number WO/2000/042999
Publication Date 27.07.2000
International Application No. PCT/US2000/001285
International Filing Date 20.01.2000
Chapter 2 Demand Filed 18.08.2000
IPC
A61K 31/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
A61K 31/195 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
A61K 31/216 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
21Esters, e.g. nitroglycerine, selenocyanates
215of carboxylic acids
216of acids having aromatic rings, e.g. benactizyne, clofibrate
A61K 31/351 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
35having six-membered rings with one oxygen as the only ring hetero atom
351not condensed with another ring
A61K 31/357 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
357having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A61K 31/5375 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
CPC
A61K 31/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
A61K 31/195
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic, hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
A61K 31/216
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
21Esters, e.g. nitroglycerine, selenocyanates
215of carboxylic acids
216of acids having aromatic rings, e.g. benactizyne, clofibrate
A61K 31/351
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
35having six-membered rings with one oxygen as the only ring hetero atom
351not condensed with another ring
A61K 31/357
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
357having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A61K 31/5375
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
Applicants
  • SELECTUS PHARMACEUTICALS, INC. [US/US]; Suite 11 110 East State Street Kennett Square, PA 19348-3100, US
Inventors
  • MATIER, William, L.; US
  • PATIL, Ghanshyam; US
Agents
  • REED, Janet, E. ; Saul, Ewing, Remick & Saul LLP Centre Square West 38th Floor 1500 Market Street Philadelphia, PA 19102-2186, US
Priority Data
09/235,84422.01.1999US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PHENYLPROPIONIC ACIDS AND ESTER COMPOUNDS AND METHODS FOR INDUCING BETA-BLOCKADE
(FR) COMPOSES A BASE D'ACIDES ET D'ESTERS PHENYLPROPIONIQUES ET METHODES PERMETTANT DE PROVOQUER DES BETA-BLOCKAGES
Abstract
(EN)
Disclosed are compounds of formula (I) wherein R represents hydrogen or is a C-3 to C-6 cycloalkyl or C-4 to C-10 straight or branched carbon chain alkyl-cycloalkyl or a group -B-D, where B is C-2 to C-10 straight or branched carbon chain alkyl and D is hydroxy or alkyloxy or 2,3-dihydroxypropyl or 2,3-dialkyloxypropyl or 2,2-dialkyl-1,3-dioxolane-5-methyl, where alkyl is C-1 to C-10 straight or branched carbon chain; W represents CH(CH3)CH2-, C(CH3)2CH2-; Z represents hydrogen, -NHCOR2, -NHCONR2R3 or -NHSO2R2 or -NHSO2NR2R3 or -NHCOOR4 wherein R4 is alkyl of from 1 to about 6 carbon atoms, alkoxyalkyl wherein the alkyl groups may be the same or different and contain from 1 to about 6 carbon atoms, alkoxyaryl, cycloalkyl of from 3 to about 8 carbon atoms. R2 and R3 may be the same or different and represent hydrogen, alkyl of from 1 to about 6 carbon atoms, alkoxyalkyl wherein the alkyl groups may be the same or different and contain from 1 to about 6 carbon atoms, alkoxyaryl, cycloalkyl of from 3 to about 8 carbon atoms, a phenyl group substituted or unsubstituted, heteroaryl, furanyl, thiophenyl, imidazolyl, oxazolyl or indolyl or tetrahydrofuranyl, tetrahydropyranyl, dioxanyl, 2,2-dimethyl dioxolane-5-methyl, pyrrolidinyl, piperazinyl and tetrahydrooxazolyl, aralkyl except that R2 and R3 are not hydrogen when Z is -NHSO2R2, or R2 and R3 may together with N form a 5 to 7 membered heterocyclic group; and pharmaceutically acceptable salts thereof; and all stereoisomeric forms, as well as racemic mixtures. The compounds in the present invention relates to compounds, methods, formulation and pharmaceutical compositions for the general treatment or prophylaxis of diseases states which are responsive to attenuation of sympathetic nervous system activity or beta adrenergic blockade namely: coronary artery disease including myocardial ischemic disorders, angina and myocardial infarction; arrhythmia; hypertension; anxiety including panic attack; migraine or glaucoma by the intravenous or sublingual or oral or topical ocular administration.
(FR)
Cette invention a trait à des composés correspondant à la formule (I) dans laquelle R représente un hydrogène ou cycloalkyle en C3-C6 ou un alkyle-cycloalkyle en C 3-C10 à chaîne carbone droite ou ramifiée ou un groupe -B-D, B représentant un alkyle en C 2-C10 à chaîne carbone droite ou ramifiée et D représentant un hydroxy ou un alkyloxy ou un 2,3-dihydroxypropyle ou 2,3-dialkyloxypropyle ou 2,2- dialkyl-1,3-dioxolane-5-méthyle, l'alkyle étant une chaîne carbone C1-C10 droite ou ramifiée, W représente CH(CH3)CH2-, C(CH3)2CH2-; Z représente un hydrogène, -NHCOR2, -NHCONR2R3 ou -NHSO2R2 ou -NHSO2NR2R3 ou -NHCOOR4, R4 représente un alkyle porteur de 1 à 6 atomes de carbone environ, un alcoxyalkyle dans lequel les groupes alkyles peuvent être identiques ou différents et contenir de 1 à 6 atomes de carbone, un alcoxyaryle, un cycloalkyle porteur de 3 à 8 atomes de carbone environ. R2 et R3 peuvent être identiques ou différents et représenter un hydrogène, un alkyle porteur de 1 à 6 atomes de carbone, un alcoxyalkyle, dans lequel es groupes alkyles peuvent être identiques ou différents et contenir de 1 à 6 atomes de carbone environ, un alcoxyaryle, un cycloalkyle porteur de 3 à 8 atomes de carbone environ, un groupe phényle substitué ou non substituée, un hétéroaryle, un furanyle, un thiophényle, un imidazolyle, un oxazolyle ou un indolyle ou un indolyle ou un tétrahydrofuranyle, un tétrahydropyranyle, un dioxanyle, un 2,2-diméthyl dioxolane-5-méthyle, un pyrrolidinyle, un pipérazinyle et un tétrahydrooxazolyle, un aralkyle, sauf si R2 et R3 ne représentent pas un hydrogène lorsque Z représente -NHSO2R2, ou que R2 et R3 peuvent ensemble former avec N un groupe hétérocyclique comprenant de 5 à 7 maillons. Cette invention a trait également aux sels pharmaceutiquement acceptables de ces composés ainsi qu'à toutes leurs formes stéréoisomères ainsi qu'à leurs mélanges racémiques. Cette invention concerne, de surcroît, des composés, des méthodes, des formulations et des compositions pharmaceutiques destinés au traitement général ou à la prévention de maladies réagissant à l'affaiblissement de l'activité du système nerveux sympathique ou à un blocage bêta adrénergique, à savoir, des troubles des artères coronaires, notamment des troubles ischémiques du myocarde, l'angine et l'infarctus du myocarde, l'arythmie, l'hypertension, l'anxiété, y compris, la crise de panique, la migraine ou le glaucome et ce, par administration intraveineuse ou sublinguale ou orale ou oculaire topique.
Also published as
Latest bibliographic data on file with the International Bureau