AR101053A1 - Derivados de 1,5-diaril-4,5-dihidro-1h-pirazol-3-carboxamidina como antagonista del receptor cb1 de canabinoides, método para su preparación, y composición farmacéutica que comprende el mismo - Google Patents

Derivados de 1,5-diaril-4,5-dihidro-1h-pirazol-3-carboxamidina como antagonista del receptor cb1 de canabinoides, método para su preparación, y composición farmacéutica que comprende el mismo

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Publication number
AR101053A1
AR101053A1 ARP140102438A ARP140102438A AR101053A1 AR 101053 A1 AR101053 A1 AR 101053A1 AR P140102438 A ARP140102438 A AR P140102438A AR P140102438 A ARP140102438 A AR P140102438A AR 101053 A1 AR101053 A1 AR 101053A1
Authority
AR
Argentina
Prior art keywords
linear
branched
alkyl
nrr
nhr
Prior art date
Application number
ARP140102438A
Other languages
English (en)
Inventor
Hyun Suh Kwee
Hee Ha Tae
Du Kim Nam
Hee Jung Young
Ouk Baek Jong
Sook Oh Hee
Jin Hong Dong
Sub Lee Moon
Original Assignee
Hanmi Pharm Ind Co Ltd
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
Application filed by Hanmi Pharm Ind Co Ltd filed Critical Hanmi Pharm Ind Co Ltd
Publication of AR101053A1 publication Critical patent/AR101053A1/es

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Classifications

    • 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
    • A61K31/495—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D231/08—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with oxygen or sulfur atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Obesity (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

El compuesto de la presente muestra actividad como antagonista del receptor de canabinoides CB1 con una alta selectividad por los tejidos periféricos, exhibiendo de este modo efectos anti-obesidad, y de este modo es útil en la prevención o tratamiento de la obesidad o enfermedades metabólicas relacionadas con la obesidad. Reivindicación 1: Un compuesto representado por la fórmula (1) o una de sus sales aceptables desde el punto de vista farmacéutico, en donde A se selecciona del grupo que consiste en alquilo C₁₋₇, arilo C₆₋₁₀, heteroarilo C₄₋₁₀, cicloalquilo C₃₋₆, y heterocicloalquilo C₃₋₆, y en forma opcional, cada uno de los cuales está sustituido en forma independiente con por lo menos un sustituyente seleccionado del grupo que consiste en hidrógeno, alquilo C₁₋₆ lineal o ramificado, alcoxi C₁₋₆ lineal o ramificado, halo, dihalo, trihalo, CN, OH, NO₂, -(C=O)-R, SH, SR, SOR, SO₂R, NH₂, NHR, NRR, -(C=O)-NH₂, -(C=O)-NHR, y -(C=O)-NRR; B y C son cada uno en forma independiente arilo C₆₋₁₀ o heteroarilo C₄₋₁₀, y en forma opcional, cada uno de los cuales está sustituido en forma independiente con por lo menos un sustituyente seleccionado del grupo que consiste en hidrógeno, alquilo C₁₋₆ lineal o ramificado, alcoxi C₁₋₆ lineal o ramificado, halo, dihalo, trihalo, CN, OH, NO₂, -(C=O)-R, SH, SR, SOR, SO₂R, NH₂, NHR, NRR, -(C=O)-NH₂, -(C=O)-NHR, y -(C=O)-NRR; R y R son cada uno en forma independiente alquilo C₁₋₆ lineal o ramificado; y R¹ y R² son cada uno en forma independiente hidrógeno o alquilo C₁₋₆, y en forma opcional, cada uno de los cuales está sustituido en forma independiente con por lo menos un sustituyente seleccionado del grupo que consiste en hidrógeno, alquilo C₁₋₆ lineal o ramificado, alcoxi C₁₋₆ lineal o ramificado, halo, CN, OH, NO₂, y SH.
ARP140102438A 2013-06-28 2014-06-30 Derivados de 1,5-diaril-4,5-dihidro-1h-pirazol-3-carboxamidina como antagonista del receptor cb1 de canabinoides, método para su preparación, y composición farmacéutica que comprende el mismo AR101053A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR20130076063 2013-06-28

Publications (1)

Publication Number Publication Date
AR101053A1 true AR101053A1 (es) 2016-11-23

Family

ID=52142216

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140102438A AR101053A1 (es) 2013-06-28 2014-06-30 Derivados de 1,5-diaril-4,5-dihidro-1h-pirazol-3-carboxamidina como antagonista del receptor cb1 de canabinoides, método para su preparación, y composición farmacéutica que comprende el mismo

Country Status (4)

Country Link
KR (1) KR101650402B1 (es)
AR (1) AR101053A1 (es)
TW (1) TWI480266B (es)
WO (1) WO2014208939A1 (es)

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005074920A1 (en) * 2004-01-30 2005-08-18 Solvay Pharmaceuticals B.V. 1,3,5-trisubstituted 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity
CN101431998A (zh) * 2006-04-27 2009-05-13 索尔瓦药物有限公司 含有CBx大麻素受体调节剂和钾通道调节剂的药物组合物
AR071487A1 (es) * 2008-04-23 2010-06-23 Solvay Pharm Bv Derivados de (5r)-1,5-diaril-4,5-dihidro-1h-pirazol-3-carboxamidina que tienen actividad antagonista cb1
US8217038B2 (en) * 2009-10-07 2012-07-10 Jenrin Discovery, Inc. Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes

Also Published As

Publication number Publication date
WO2014208939A1 (en) 2014-12-31
TWI480266B (zh) 2015-04-11
KR20150002519A (ko) 2015-01-07
KR101650402B1 (ko) 2016-08-23
TW201506013A (zh) 2015-02-16

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