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1. WO2003040126 - $g(v)-CYCLOALKYL 17-HETEROARYL PROSTAGLANDIN E2 ANALOGS AS EP2-RECEPTOR AGONISTS

Publication Number WO/2003/040126
Publication Date 15.05.2003
International Application No. PCT/US2002/034301
International Filing Date 25.10.2002
Chapter 2 Demand Filed 18.04.2003
IPC
C07D 333/16 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
333Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
02not condensed with other rings
04not substituted on the ring sulfur atom
06with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
14Radicals substituted by singly bound hetero atoms other than halogen
16by oxygen atoms
C07F 9/40 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
28with one or more P-C bonds
38Phosphonic acids ; Thiophosphonic acids
40Esters thereof
CPC
A61K 31/381
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
38having sulfur as a ring hetero atom
381having five-membered rings
A61K 31/41
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
A61K 31/557
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
557Eicosanoids, e.g. leukotrienes ; or prostaglandins
A61K 31/5575
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
557Eicosanoids, e.g. leukotrienes ; or prostaglandins
5575having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
A61P 27/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
02Ophthalmic agents
A61P 27/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
02Ophthalmic agents
06Antiglaucoma agents or miotics
Applicants
  • ALLERGAN, INC. [US]/[US]
Inventors
  • BURK, Robert, M.
  • HOLOBOSKI, Mark
  • POSNER, Mari, F.
Agents
  • BARAN, Robert, J.
Priority Data
60/338,83805.11.2001US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) $g(v)-CYCLOALKYL 17-HETEROARYL PROSTAGLANDIN E2 ANALOGS AS EP2-RECEPTOR AGONISTS
(FR) ANALOGUES DE $G(V)-CYCLOALKYL-7-HETEROARYL-PROSTAGLANDINE E¿2? UTILISES EN TANT QU'AGONISTES DU RECEPTEUR D'EP2
Abstract
(EN) The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the formula (I): wherein the hatched segment represents an $g(a) bonds, the solid triangle represents a $g(b) bond, the wavy segments represent $g(a) or $g(b) bond, dashed lines represent a double bond or a single bond, X is selected from the group consisting of hydrogen and halogen radicals, R3 is heteroaryl or a substituted heteroaryl radical, R1 and R2 are independently selected from the group consisting of hydrogen or a lower alkyl radical having up to six carbon atoms, or a lower acyl radical having up to six carbon atoms, R is selected from the group consisting of CO2R4, CONR42, CH2OR4, CONR4SO2R4, P(O)(OR4) and formula (II), wherein R4 is selected from the group consisting of H, phenyl and lower alkyl having from one to six carbon atoms and n is 0 or an integer of from 1 to 4.
(FR) L'invention concerne l'utilisation de dérivés de prostaglandines de type E en tant qu'agonistes d'EP2 en général, et, en particulier en tant qu'hypotenseurs oculaires. Les dérivés de PGE utilisés selon l'invention sont représentés par la formule (I), dans laquelle le segment hachuré représente une liaison &agr;, le triangle solide représente une liaison &bgr;, les segments ondulés représentent une liaison &agr; ou &bgr;, les lignes pointillées représentent une liaison double ou simple, X est choisi dans le groupe constitué d'halogène et de radicaux hydrogènes, R3 représente hétéroaryle ou un radical hétéroaryle substitué, R1 et R2 sont choisis séparément dans le groupe formé d'hydrogène ou d'un radical alkyle inférieur possédant jusqu'à six atomes de carbone, ou un radical acyle inférieur possédant jusqu'à six atomes de carbone, R est choisi dans le groupe formé de CO2R4, CONR42, CH2OR4, CONR4SO2R4, P(O)(OR4) et formule (II), R4 étant choisi dans le groupe formé de H, phényle et alkyle inférieur possédant un à six atomes de carbone et n vaut 0 ou un entier de 1 à 4.
Related patent documents
IN575/KOLNP/2004This application is not viewable in PATENTSCOPE because the national phase entry has not been published yet or the national entry is issued from a country that does not share data with WIPO or there is a formatting issue or an unavailability of the application.
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