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1. WO2000043372 - ACYL DERIVATIVES WHICH TREAT VLA-4 RELATED DISORDERS

Publication Number WO/2000/043372
Publication Date 27.07.2000
International Application No. PCT/US2000/001686
International Filing Date 21.01.2000
Chapter 2 Demand Filed 10.08.2000
IPC
A61K 31/41 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61K 31/495 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/505 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
C07D 211/58 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
56Nitrogen atoms
58attached in position 4
C07D 213/74 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 213/76 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
76to which a second hetero atom is attached
CPC
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 31/495
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 ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
A61K 31/505
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 ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
C07D 211/58
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
56Nitrogen atoms
58attached in position 4
C07D 213/74
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 213/76
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
76to which a second hetero atom is attached
Applicants
  • ELAN PHARMACEUTICALS, INC. [US/US]; 800 Gateway Boulevard South San Francisco, CA 94080, US (AllExceptUS)
  • AMERICAN HOME PRODUCTS [US/US]; 5 Giraldi Farms Madison, NJ 07940, US (AllExceptUS)
  • KONRADI, Andrei [US/US]; US (UsOnly)
  • PLEISS, Michael, A. [US/US]; US (UsOnly)
  • THORSETT, Eugene, D. [US/US]; US (UsOnly)
  • ASHWELL, Susan [GB/US]; US (UsOnly)
  • WELMAKER, Gregory, S. [US/US]; US (UsOnly)
  • KREFT, Anthony [US/US]; US (UsOnly)
  • SARANTAKIS, Dimitrios [US/US]; US (UsOnly)
  • DRESSEN, Darren, B. [US/US]; US (UsOnly)
  • GRANT, Francine, S. [FR/US]; US (UsOnly)
  • SEMKO, Christopher [CA/US]; US (UsOnly)
  • XU, Ying-Zi [CN/US]; US (UsOnly)
Inventors
  • KONRADI, Andrei; US
  • PLEISS, Michael, A.; US
  • THORSETT, Eugene, D.; US
  • ASHWELL, Susan; US
  • WELMAKER, Gregory, S.; US
  • KREFT, Anthony; US
  • SARANTAKIS, Dimitrios; US
  • DRESSEN, Darren, B.; US
  • GRANT, Francine, S.; US
  • SEMKO, Christopher; US
  • XU, Ying-Zi; US
Agents
  • HAGENAH, Jeffrey, A. ; Burns, Doane Swecker & Mathis, LLP P.O. Box 1404 Alexandria, VA 22313-1404, US
Priority Data
60/116,92322.01.1999US
60/160,99921.10.1999US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ACYL DERIVATIVES WHICH TREAT VLA-4 RELATED DISORDERS
(FR) DERIVES D'ACYLE UTILES POUR TRAITER DES AFFECTIONS ASSOCIEES A VLA-4
Abstract
(EN)
Disclosed are compounds such as Ia and Ib which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiples sclerosis.
(FR)
L'invention concerne des composés représentés par les formules Ia et Ib, qui se lient à VLA-4. Certains de ces composés inhibent également l'adhérence leucocytaire et, en particulier, l'adhérence leucocytaire dépendant de VLA-4. Ces composés sont utiles pour traiter des maladies inflammatoires chez un patient mammifère, p. ex. l'être humain, telles que l'asthme, la maladie d'Alzheimer, l'athérosclérose, le syndrome démentiel lié au SIDA, le diabète, l'affection intestinale inflammatoire, la polyarthrite rhumatoïde, la greffe de tissus, les métastases de tumeur et l'ischémie myocardique. Les composés peuvent également être administrés pour traiter des affections cérébrales inflammatoires telles que la sclérose en plaques.
Also published as
CZPV2001-2361
ININ/PCT/2001/984/CHE
NO20013600
NZ512563
ZA200105314
Latest bibliographic data on file with the International Bureau