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1. WO2004110379 - A1 ADENOSINE RECEPTOR ANTAGONISTS

Publication Number WO/2004/110379
Publication Date 23.12.2004
International Application No. PCT/US2004/018171
International Filing Date 07.06.2004
IPC
A61K 31/522 2006.1
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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
52Purines, e.g. adenine
522having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61P 3/04 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
04Anorexiants; Antiobesity agents
A61P 3/10 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
A61P 9/04 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
A61P 11/06 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
A61P 13/12 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
CPC
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
A61P 13/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
A61P 19/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
04for non-specific disorders of the connective tissue
A61P 25/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
04Centrally acting analgesics, e.g. opioids
A61P 25/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
14for treating abnormal movements, e.g. chorea, dyskinesia
16Anti-Parkinson drugs
Applicants
  • ENDACEA, INC. [US]/[US] (AllExceptUS)
  • WILSON, Constance, N. [US]/[US] (UsOnly)
  • PARTRIDGE, John, J. [US]/[US] (UsOnly)
Inventors
  • WILSON, Constance, N.
  • PARTRIDGE, John, J.
Agents
  • SPRUILL, W. Murray,
Priority Data
60/476,96709.06.2003US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) A1 ADENOSINE RECEPTOR ANTAGONISTS
(FR) ANTAGONISTES DE RECEPTEUR D'ADENOSINE A1
Abstract
(EN) This invention relates to compounds of formula (I): wherein R1 is a branched or straight chain C1-C8 alkyl; R2 is of the formula (II), wherein n is an integer ranging from 1 to 8; R5 is H or (CH2)pCH3, and R6 is H or (CH2)mOH, wherein p is an integer ranging from 1 to 7 and m is an integer ranging from 1 to 8; R3 is of the formula (III), wherein q is an integer ranging from 1 to 8; and R7 is selected from the group consisting of H, OH, NH2, (CH2)tOH, and R9COOH; wherein R9 is a straight or branched chain alkylene or alkenylene group having 1 to 8 carbon atoms, and t is an integer ranging from 1 to 8; R4 is of the formula (IV), wherein r is an integer ranging from 1 to 8 and R8 is selected from the group consisting of H, OH, (CH2)fNH2, (CH2)sOH, and R10COOH; wherein f is 0 or f and s are independently integers ranging from 1 to 8; and, R10 is a C1-C8 straight or branched chain alkylene or alkenylene; and; salts, solvates, and hydrates thereof. The present invention further provides methods of preparing the compounds of formula (I) and their use as therapeutic agents and diagnostic agents.
(FR) L'invention concerne des composés de formule (I), dans laquelle R1 est alkyle C1-C8 à chaîne droite ou ramifiée; R2 est de formule (II), dans laquelle n est un entier compris entre 1 et 8; R5 est H ou (CH2)pCH3, et R6 est H ou (CH2)mOH, sachant que p est un entier compris entre 1 et 7 et que m est un entier compris entre 1 et 8; R3 est de formule (III), dans laquelle q est un entier compris entre 1 et 8; et R7 peut être H, OH, NH2, (CH2)tOH, et R9COOH; en l'occurrence, R9 est un groupe alkylène ou alcénylène à chaîne droite ou ramifiée ayant entre 1 et 8 atomes de carbone, et t est un entier compris entre 1 et 8; R4 est de formule (IV), dans laquelle r est un entier compris entre 1 et 8 et R8 peut être un groupe comprenant H, OH, (CH2)fNH2, (CH2)sOH, et R10COOH; en l'occurrence, f vaut 0 ou f et s sont des entiers indépendants compris entre 1 et 8; et, R10 est alkylène or alcénylène C1-C8 à chaîne droite ou ramifiée ; y compris les sels, solvates et hydrates correspondants. L'invention concerne également des procédés relatifs à l'élaboration des composés de formule (I), et leur utilisation comme agents thérapeutiques et agents diagnostiques.
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