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PE20040599A1 - Amidas sustituidas como moduladores del receptor cannabinoide-1 (cb1) - Google Patents

Amidas sustituidas como moduladores del receptor cannabinoide-1 (cb1)

Info

Publication number
PE20040599A1
PE20040599A1 PE2003000230A PE2003000230A PE20040599A1 PE 20040599 A1 PE20040599 A1 PE 20040599A1 PE 2003000230 A PE2003000230 A PE 2003000230A PE 2003000230 A PE2003000230 A PE 2003000230A PE 20040599 A1 PE20040599 A1 PE 20040599A1
Authority
PE
Peru
Prior art keywords
alkyl
methyl
arilo
heteroarilo
methylpropanamide
Prior art date
Application number
PE2003000230A
Other languages
English (en)
Inventor
Helen M Armstrong
Linda L Chang
William K Hagmann
Lanza
Ping Liu
Shrenik K Shah
Hongbo Qi
Linus S Lin
James P Jewell
Ravindra N Guthikonda
Original Assignee
Merck & Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=32393400&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20040599(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of PE20040599A1 publication Critical patent/PE20040599A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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 having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic 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 having three double bonds between ring members or between ring members and non-ring members having 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
    • C07D213/60—Heterocyclic 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 having three double bonds between ring members or between ring members and non-ring members having 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 with 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61P25/16—Anti-Parkinson drugs
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    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
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    • C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C235/06—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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    • C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C235/18—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides
    • C07C235/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/06—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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    • C07D213/02—Heterocyclic 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 having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic 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 having three double bonds between ring members or between ring members and non-ring members having 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
    • C07D213/24—Heterocyclic 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 having three double bonds between ring members or between ring members and non-ring members having 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 with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
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    • C07D213/02—Heterocyclic 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 having three double bonds between ring members or between ring members and non-ring members
    • C07D213/89—Heterocyclic 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 having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
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    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • C07C2601/14—The ring being saturated

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pulmonology (AREA)
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  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hematology (AREA)
  • Addiction (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyrane Compounds (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I O UNA SAL FARMACEUTICAMENTE ACEPTABLE, EN LA QUE R1 ES CICLOHETEROARILO, ARILO, HETEROARILO O NRaRc, EN DONDE ARILO Y HETEROARILO SON OPCIONALMENTE SUSTITUIDOS POR 1 A 3 SUSTITUYENTES TIPO Rb; R2 ES ALQUILO C1-C10, CICLOALQUILO C3-C10 ALQUILO C1-C4; ARILO C1-C4 ALQUILO, HETEROARILO C1-C4 ALQUILO, EN DONDE CICLOALQUILO, ARILO Y HETEROARILO ES OPCIONALMENTE SUSTITUIDO POR 1 A 3 SUSTITUYENTES TIPO Rb; Ra ES H, METILO Y CF3; Rb ES HALOGENO, CIANO, TRIFLUOROMETILO, TRIFLUOROMETOXI; Rc ES H, ALQUILO C1-C6, ARILO, HETEROARILO, ARILO-METILO; Rd ES CICLOALQUILO, ARILO, HETEROARILO, SUSTITUIDOS O NO CON 1 A 3 SUSTITUYENTES TIPO Rh; Rh PUEDE SER HALOGENO, ALQUILO C1-C3, CN O CF3. CUANDO LOS GRUPOS PIRIDILO NO SON SUSTITUIDOS EN N, PUEDE ENCONTRARSE OPCIONALMENTE PRESENTE COMO N-OXIDO. SON COMPUESTOS PREFERIDOS: N-[3-(4-CLOROFENIL)-1-METILO-2-FENILPROPILO]-2-(4-CLOROFENILOX)-2-METILPROPANAMIDA; N-[3-(4-CLOROFENIL)-1-METILO-2-FENILPROPILO]-2-(2-PIRIDILOXI)-2-METILPROPANAMIDA; N-[3-(4-CLOROFENIL)-1-METILO-2-(3-PIRIDILO)PROPILO]-2-(4-CLOROFENILOXI)-2-METILPROPANAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION Y UN PORTADOR FARMACEUTICAMENTE ACEPTABLES. DICHOS COMPUESTOS SON UTILES PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR EL RECEPTOR CANNABINOIDE-1 COMO LA OBESIDAD ASOCIADA CON LA INGESTA EXCESIVA DE COMIDA
PE2003000230A 2002-11-22 2003-03-07 Amidas sustituidas como moduladores del receptor cannabinoide-1 (cb1) PE20040599A1 (es)

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US42841502P 2002-11-22 2002-11-22

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KR (1) KR100748380B1 (es)
CN (1) CN1639112A (es)
AR (1) AR038948A1 (es)
AU (1) AU2003218005A1 (es)
BR (1) BR0308349A (es)
CR (1) CR7432A (es)
DO (1) DOP2003000609A (es)
EA (1) EA007747B1 (es)
EC (1) ECSP045289A (es)
GE (1) GEP20074208B (es)
HR (1) HRP20040823A2 (es)
IL (1) IL163824A0 (es)
IS (1) IS7411A (es)
JO (1) JO2482B1 (es)
MA (1) MA27185A1 (es)
MX (1) MXPA04008748A (es)
MY (1) MY134457A (es)
NO (1) NO20043803L (es)
PE (1) PE20040599A1 (es)
PL (1) PL200328B1 (es)
RS (1) RS79104A (es)
TN (1) TNSN04176A1 (es)
TW (1) TW200408620A (es)
UA (1) UA76590C2 (es)
WO (1) WO2004048317A1 (es)

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