AR073928A1 - 4- butiratos de trimetilamonio como inhibidores de la cpt2, proceso para su preparacion, composiciones farmaceuticas y uso de los mismos - Google Patents

4- butiratos de trimetilamonio como inhibidores de la cpt2, proceso para su preparacion, composiciones farmaceuticas y uso de los mismos

Info

Publication number
AR073928A1
AR073928A1 ARP090101489A ARP090101489A AR073928A1 AR 073928 A1 AR073928 A1 AR 073928A1 AR P090101489 A ARP090101489 A AR P090101489A AR P090101489 A ARP090101489 A AR P090101489A AR 073928 A1 AR073928 A1 AR 073928A1
Authority
AR
Argentina
Prior art keywords
formula
chosen
halogen
lower alkyl
cpt2
Prior art date
Application number
ARP090101489A
Other languages
English (en)
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR073928A1 publication Critical patent/AR073928A1/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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/46—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/51—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—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
    • 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
    • C07C235/12—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 atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20—Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)

Abstract

Estos compuestos inhiben la actividad de la carnitina-palmitoil-transferasa (CPT), en particular la actividad de la CPT2, y pueden utilizarse como medicamentos. Reivindicacion 1: Compuestos de la formula (1) donde A es O o un enlace, m se elige entre los numeros 3, 4, 5, 6, 7, 8, 9 y 10, n se elige entre los numeros 1, 2, 3, 4 y 5, R1 es arilo elegido entre fenilo y naftilo, dicho arilo está sin sustituir o sustituido por uno, dos, tres, cuatro o cinco restos elegidos entre el grupo formado por alquilo inferior, halogeno, halogeno-alquilo inferior, alcoxi inferior y fenilo, o es heteroarilo elegido entre el grupo formado por piridilo, tienilo y tiazolilo, dicho heteroarilo está sin sustituir o sustituido por uno, dos o tres restos elegidos entre alquilo inferior, halogeno, halogeno-alquilo inferior, alcoxi inferior y fenilo, y sus sales farmacéuticamente aceptables. Reivindicacion 16: Un proceso para la obtencion de compuestos de la formula 1 definidos en una cualquiera de las reivindicaciones de 1 a 15, dicho proceso consiste en: hacer reaccionar una amina terciaria de la formula (2) en la que A1, m, n y R1 tienen los significados definidos anteriormente, con un agente metilante, en presencia de una base, en un disolvente polar, para obtener un compuesto de la formula (1). Reivindicacion 18: Composiciones farmacéuticas que contienen un compuesto de la formula (1) segun una cualquiera de las reivindicaciones de 1 a 15 y un vehiculo y/o adyuvante farmacéuticamente aceptable. Reivindicacion 21: El uso de los compuestos de la formula 1 segun una cualquiera de las reivindicaciones de 1 a 15 para la fabricacion de medicamentos destinados al tratamiento terapéutico o profiláctico de enfermedades que se modulan con inhibidores de la CPT2.
ARP090101489A 2008-04-29 2009-04-27 4- butiratos de trimetilamonio como inhibidores de la cpt2, proceso para su preparacion, composiciones farmaceuticas y uso de los mismos AR073928A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08155318 2008-04-29

Publications (1)

Publication Number Publication Date
AR073928A1 true AR073928A1 (es) 2010-12-15

Family

ID=40897574

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090101489A AR073928A1 (es) 2008-04-29 2009-04-27 4- butiratos de trimetilamonio como inhibidores de la cpt2, proceso para su preparacion, composiciones farmaceuticas y uso de los mismos

Country Status (18)

Country Link
US (2) US8349893B2 (es)
EP (1) EP2280935B1 (es)
JP (1) JP5373888B2 (es)
KR (1) KR101225320B1 (es)
CN (1) CN102015626B (es)
AR (1) AR073928A1 (es)
AU (1) AU2009242241B2 (es)
BR (1) BRPI0910591A2 (es)
CA (1) CA2722114A1 (es)
CL (1) CL2009001005A1 (es)
ES (1) ES2525340T3 (es)
IL (1) IL208062A0 (es)
MX (1) MX2010011458A (es)
PE (1) PE20091776A1 (es)
RU (1) RU2502727C2 (es)
TW (1) TWI369343B (es)
WO (1) WO2009132979A1 (es)
ZA (1) ZA201006567B (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5373888B2 (ja) * 2008-04-29 2013-12-18 エフ．ホフマン−ラ ロシュ アーゲー Ｃｐｔ２インヒビターとしての４−トリメチルアンモニオ−ブチラート類
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3476656D1 (en) * 1983-05-25 1989-03-16 Takeda Chemical Industries Ltd Derivatives of beta-amino-gamma-trimethylammonio-butyrate, their production and use
US4632925A (en) * 1985-10-07 1986-12-30 Hoffmann-La Roche Inc. N-substituted diphenylpiperidines and antiobesity use thereof
WO1999058120A1 (en) * 1998-05-08 1999-11-18 Rolf Berge USE OF NON-β-OXIDIZABLE FATTY ACID ANALOGUES FOR TREATMENT OF SYNDROME-X CONDITIONS
IT1299266B1 (it) * 1998-05-15 2000-02-29 Sigma Tau Ind Farmaceuti Inibitori reversibili della carnitina palmitoil trasferasi
ITRM20050090A1 (it) * 2005-03-02 2006-09-03 Sigma Tau Ind Farmaceutiche Riunite Spa Derivati dell'acido ammino-butanoico inibitore della cpt.
MX2009001104A (es) 2006-08-02 2009-02-10 Sigma Tau Ind Farmaceuti Derivados de 4-trimetilamonio-3-aminobutirato y 4-trimetilfosfonio-3-aminobutirato como inhibidores de carnitina palmitoil transferasa.
WO2008109991A1 (en) * 2007-03-09 2008-09-18 University Health Network Inhibitors of carnitine palmitoyltransferase and treating cancer
CN101952243B (zh) * 2008-04-29 2014-07-16 霍夫曼-拉罗奇有限公司 4-二甲氨基丁酸衍生物
JP5373888B2 (ja) * 2008-04-29 2013-12-18 エフ．ホフマン−ラ ロシュ アーゲー Ｃｐｔ２インヒビターとしての４−トリメチルアンモニオ−ブチラート類

Also Published As

Publication number Publication date
EP2280935A1 (en) 2011-02-09
CN102015626B (zh) 2013-12-11
JP2011518853A (ja) 2011-06-30
US8349893B2 (en) 2013-01-08
EP2280935B1 (en) 2014-10-15
KR101225320B1 (ko) 2013-01-22
TW200946107A (en) 2009-11-16
US20130030033A1 (en) 2013-01-31
IL208062A0 (en) 2010-12-30
US8673946B2 (en) 2014-03-18
JP5373888B2 (ja) 2013-12-18
AU2009242241B2 (en) 2014-01-16
CN102015626A (zh) 2011-04-13
ES2525340T3 (es) 2014-12-22
PE20091776A1 (es) 2009-11-13
CA2722114A1 (en) 2009-11-05
TWI369343B (en) 2012-08-01
ZA201006567B (en) 2011-06-29
US20090270500A1 (en) 2009-10-29
RU2010148530A (ru) 2012-06-10
CL2009001005A1 (es) 2010-06-04
WO2009132979A1 (en) 2009-11-05
AU2009242241A1 (en) 2009-11-05
BRPI0910591A2 (pt) 2015-09-22
KR20100127305A (ko) 2010-12-03
RU2502727C2 (ru) 2013-12-27
MX2010011458A (es) 2010-11-09

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