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1. WO2000040558 - ASPARTIC PROTEASE INHIBITORS

Publication Number WO/2000/040558
Publication Date 13.07.2000
International Application No. PCT/US2000/000265
International Filing Date 06.01.2000
Chapter 2 Demand Filed 04.08.2000
IPC
C07C 235/20 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
02having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
04the carbon skeleton being acyclic and saturated
18having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides
20having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 235/50 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
42having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
44with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
50having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
C07C 237/34 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
28having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
34having the nitrogen atom of the carboxamide group bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
C07C 271/20 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
271Derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
06Esters of carbamic acids
08having oxygen atoms of carbamate groups bound to acyclic carbon atoms
10with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
20to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
C07C 271/22 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
271Derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
06Esters of carbamic acids
08having oxygen atoms of carbamate groups bound to acyclic carbon atoms
10with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
22to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07C 311/29 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
311Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
22Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
29having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
CPC
C07C 235/20
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
02having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
04the carbon skeleton being acyclic and saturated
18having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides
20having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 235/50
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
42having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
44with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
50having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
C07C 237/34
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
28having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
34having the nitrogen atom of the carboxamide group bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
C07C 271/20
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
271Derivatives of carbamic acids, i.e. compounds containing any of the groups , the nitrogen atom not being part of nitro or nitroso groups
06Esters of carbamic acids
08having oxygen atoms of carbamate groups bound to acyclic carbon atoms
10with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
20to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
C07C 271/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
271Derivatives of carbamic acids, i.e. compounds containing any of the groups , the nitrogen atom not being part of nitro or nitroso groups
06Esters of carbamic acids
08having oxygen atoms of carbamate groups bound to acyclic carbon atoms
10with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
22to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07C 311/29
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
311Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
22Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
29having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
Applicants
  • THE GOVERNMENT OF THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES [US/US]; National Institutes of Health Office of Technology Transfer Suite 325 6011 Executive Boulevard Rockville, MD 20852, US (AllExceptUS)
  • RANDAD, Ramnarayan, S. [IN/US]; US (UsOnly)
  • ERICKSON, John, W. [US/US]; US (UsOnly)
  • EISSENSTAT, Michael, A. [US/US]; US (UsOnly)
  • LUBKOWSKA, Lucyna [PL/US]; US (UsOnly)
Inventors
  • RANDAD, Ramnarayan, S.; US
  • ERICKSON, John, W.; US
  • EISSENSTAT, Michael, A.; US
  • LUBKOWSKA, Lucyna; US
Agents
  • GAGALA, Bruce, M. ; Leydig, Voit & Mayer, Ltd. Two Prudential Plaza Suite 4900 180 North Stetson Chicago, IL 60601-6780, US
Priority Data
60/114,86806.01.1999US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ASPARTIC PROTEASE INHIBITORS
(FR) INHIBITEURS DE PROTEASE ASPARTIQUE
Abstract
(EN)
The present invention provides a compound of formula (I) wherein a, b, c, d, and e, are R7, OR7, SR7, NR7R8, NHCOR7, CO2R7, CN, NO2, NH2, N3, or a halogen. R7 and R8 are H or alkyl, R1 and R2 are H or alkyl, and R3 is a non-aromatic substituent. Substituent A is OH, NH2, or SH. Substituents B and B1 include amide and sulfonamide groups, which can be cyclic, acyclic, or amino acid derivatives. Alternatively, B and R' together with the nitrogen to which they are bonded, and/or B' and R2 together with the nitrogen to which they are bonded, define a heterocycle. The present invention further provides a pharmaceutical composition that includes a carrier and a therapeutically effective amount of at least one compound of the present invention. The present invention further provides therapeutic methods that include administering a therapeutically effective amount of at least one compound of the present invention.
(FR)
La présente invention concerne un composé représenté par la formule (I) dans laquelle a, b, c, d, et e sont R7, OR7, SR7, NR7R8, NHCOR7, CO2R7, CN, NO2, NH2, N3, ou un halogène. R7 et R8 sont H ou un alkyle, R1 et R2 sont H ou un alkyle, et R3 est un substituant non aromatique. Le substituant A est OH, NH2, ou SH. Les substituants B et B1 comprennent les groupes amide et sulfonamide, qui peuvent être des dérivés cycliques, acycliques, ou amino-acides. Dans une variante, B et R' ainsi que l'azote auquel ils sont liés, et/ou B' et R2 ainsi que l'azote auquel ils sont liés, définissent un hétérocycle. L'invention concerne également une composition pharmaceutique comprenant un excipient et une quantité efficace du point de vue thérapeutique d'au moins un desdits composés. Elle concerne en outre des méthodes thérapeutiques qui consistent, entre autres, à administrer une quantité efficace du point de vue thérapeutique d'au moins un desdits composés.
Also published as
Latest bibliographic data on file with the International Bureau