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1. WO1997026240 - CONFORMATIONALLY RESTRICTED AROMATIC INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND METHOD

Publication Number WO/1997/026240
Publication Date 24.07.1997
International Application No. PCT/US1997/000587
International Filing Date 13.01.1997
Chapter 2 Demand Filed 05.08.1997
IPC
A61K 31/191 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
191Acyclic acids having two or more hydroxy groups, e.g. gluconic acid
A61K 31/366 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
365Lactones
366having six-membered rings, e.g. delta-lactones
A61K 31/404 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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
A61K 31/4468 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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
4468having a nitrogen atom directly attached in position 4, e.g. clebopride, fentanyl
C07C 17/093 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
17Preparation of halogenated hydrocarbons
093by replacement by halogens
C07C 47/453 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
47Compounds having -CHO groups
38Unsaturated compounds having -CHO groups bound to carbon atoms of rings other than six-membered aromatic rings
453containing six-membered aromatic rings
CPC
A61K 31/191
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
191having two or more hydroxy groups, e.g. gluconic acid
A61K 31/366
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
365Lactones
366having six-membered rings, e.g. delta-lactones
A61K 31/404
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
A61K 31/4468
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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
445Non condensed piperidines, e.g. piperocaine
4468having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
A61P 3/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
06Antihyperlipidemics
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Applicants
  • BRISTOL-MYERS SQUIBB COMPANY [US]/[US]
Inventors
  • BILLER, Scott, A.
  • DICKSON, John, K.
  • LAWRENCE, R., Michael
  • MAGNIN, David, R.
  • POSS, Michael, A.
  • ROBL, Jeffrey, A.
  • SLUSARCHYK, William, A.
  • SULSKY, Richard, B.
  • TINO, Joseph, A.
Agents
  • MALATESTINIC, Nicholas, P.
Priority Data
60/010,34616.01.1996US
60/017,22409.05.1996US
60/030,37005.11.1996US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) CONFORMATIONALLY RESTRICTED AROMATIC INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND METHOD
(FR) COMPOSES AROMATIQUES A CONFORMATION RESTREINTE SERVANT D'INHIBITEURS DE LA PROTEINE DE TRANSFERT DE TRIGLYCERIDE MICROSOMIQUE ET PROCEDE ASSOCIE
Abstract
(EN)
Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure (I) or (IA) or (IB) including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0,1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) -O-; or (3) (i); B is: (ii) or (iii) or (iv) or (v) (wherein (a = 2, 3 or 4)) or (vi) or (vii) or (viii); and wherein L2, L1, R1, R2, R3, R3', R3a, R3b, R4, R4', R5, X, (ix), (x) and (xi) are as defined herein.
(FR)
Cette invention se rapporte à de nouveaux composés qui sont des inhibiteurs de la protéine de transfert de triglycéride microsomique (MTP) et qui sont par conséquent utiles pour abaisser la teneur en lipides du sérum et pour traiter l'athérosclérose et les maladies apparentées, ces composés ayant la structure (I) ou (IA) ou (IB), ainsi qu'à des sels pharmaceutiquement acceptables de ces composés ou à des esters promédicaments de ces composés. Dans ces formules, q est égal à 0, à 1 ou à 2; Rx représente H, alkyle, aryle ou halogène; A représente (1) une liaison; (2) -O-; ou (3) (i); B représente (ii) ou (iii) ou (iv) ou (v) (où (a = 2, 3 ou 4)) ou (vi) ou (vii) ou (viii); et L2, L1, R1, R2, R3, R3', R3a, R3b, R4, R4', R5, X, (ix), (x) et (xi) sont tels que définis dans les pièces descriptives de l'invention.
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