AR040253A1 - Fluorobenzamidas, procesos de preparacion y medicamento - Google Patents

Fluorobenzamidas, procesos de preparacion y medicamento

Info

Publication number
AR040253A1
AR040253A1 ARP030102056A ARP030102056A AR040253A1 AR 040253 A1 AR040253 A1 AR 040253A1 AR P030102056 A ARP030102056 A AR P030102056A AR P030102056 A ARP030102056 A AR P030102056A AR 040253 A1 AR040253 A1 AR 040253A1
Authority
AR
Argentina
Prior art keywords
formula
compound
alkyl
compounds
halogen
Prior art date
Application number
ARP030102056A
Other languages
English (en)
Inventor
Synese Jolidon
Sarmiento Rosa Maria Rodriguez
Andrew William Thomas
Rene Wyler
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 AR040253A1 publication Critical patent/AR040253A1/es

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Classifications

    • 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
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having 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
    • C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having 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 with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/52—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having 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 with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/67—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/68—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/69—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of an acyclic saturated carbon skeleton
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/66—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
    • 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
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having 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
    • C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having 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 with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/48—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having 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 with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • 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
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having 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
    • C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having 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 with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/50—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having 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 with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
    • C07C255/30—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the same unsaturated acyclic carbon skeleton

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Derivados de fluorobenzamida de la fórmula general (1) en donde: R1 es H, C1-6 alquilo o hidroxi-(C1-6)-alquilo; R2 es C1-6 alquilo, -CO-NR8R9; -(CH2)n-NR8R9; -(CH2)p-OR8, o -(CH2)n-CN; R3 se selecciona de H, halógeno, halógeno-(C1-6)-alquilo, ciano, C1-6 alcoxilo o halógeno-(C1-6)-alcoxilo; R4, R5, R6 y R7 son H o F, y al menos uno de R4, R5, R6 y R7 es F; R8 y R9 independientemente uno del otro son H o C1-6 alquilo; m es 1, 2 ó 3; n es 0, 1, 2 ó 3; y p es 1 ó 2; así como sus sales aceptables farmacéuticamente. Procesos de producción de los compuestos de fórmula (1), medicamento preparado en base a dichos compuestos y usos de estos para la producción de medicamentos. Los compuestos de fórmula general (1) son inhibidores selectivos monoamino oxidasa B y por lo tanto estos son adecuados para el tratamiento de la Enfermedad de Alzheimer o demencia senil. Reivindicación 27: Un proceso para la producción de un compuesto de fórmula (1) de acuerdo con cualquiera de las reivindicaciones 1 a 26, tales procesos comprenden: la reacción de un compuesto de fórmula (2) con un compuesto de fórmula (3) para obtener un compuesto de fórmula (4) que se transforma a un compuesto de fórmula (5) y se tratan con compuestos de fórmula (6) para obtener un compuesto de fórmula (1), y si se desea, la conversión de un compuesto de fórmula (1) en una sal farmacéuticamente aceptable.
ARP030102056A 2002-06-12 2003-06-10 Fluorobenzamidas, procesos de preparacion y medicamento AR040253A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP02012484 2002-06-12

Publications (1)

Publication Number Publication Date
AR040253A1 true AR040253A1 (es) 2005-03-23

Family

ID=29724375

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030102056A AR040253A1 (es) 2002-06-12 2003-06-10 Fluorobenzamidas, procesos de preparacion y medicamento

Country Status (20)

Country Link
US (1) US6951884B2 (es)
EP (1) EP1515926B1 (es)
JP (1) JP4181540B2 (es)
KR (1) KR100641963B1 (es)
CN (1) CN1274669C (es)
AR (1) AR040253A1 (es)
AT (1) ATE427928T1 (es)
AU (1) AU2003236719B2 (es)
BR (1) BR0311719A (es)
CA (1) CA2489247A1 (es)
DE (1) DE60327074D1 (es)
ES (1) ES2322254T3 (es)
MX (1) MXPA04012511A (es)
PA (1) PA8575001A1 (es)
PE (1) PE20040558A1 (es)
PL (1) PL374545A1 (es)
RU (1) RU2314289C2 (es)
TW (1) TW200406201A (es)
UY (1) UY27842A1 (es)
WO (1) WO2003106380A2 (es)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7321065B2 (en) 2003-04-18 2008-01-22 The Regents Of The University Of California Thyronamine derivatives and analogs and methods of use thereof
US6979750B1 (en) 2003-04-18 2005-12-27 The Regents Of The University Of California Thyronamine derivatives and analogs and methods of use thereof
BRPI0507670A (pt) * 2004-02-13 2007-07-17 Warner Lambert Co moduladores do receptor de androgênio
JP4874965B2 (ja) * 2004-07-08 2012-02-15 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー アンドロゲン調節剤
CA2598762A1 (en) 2005-02-25 2006-08-31 F. Hoffmann-La Roche Ag Tablets with improved drug substance dispersibility
CA2602854C (en) 2005-04-01 2013-05-14 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
TW200724139A (en) * 2005-05-05 2007-07-01 Warner Lambert Co Androgen modulators
WO2007008963A1 (en) * 2005-07-13 2007-01-18 Jenrin Discovery Mao-b inhibitors useful for treating obesity
US20090170886A1 (en) * 2005-08-08 2009-07-02 Pfizer Inc Androgen modulators
US8372885B2 (en) * 2008-09-17 2013-02-12 Novartis Ag Organic compounds and their uses
CN102816082B (zh) * 2010-01-29 2015-03-11 浙江大学 苯甲酰胺类衍生物及制备方法和应用
TWI518062B (zh) 2011-12-26 2016-01-21 迪愛生股份有限公司 具有２－氟苯基氧基甲烷構造之化合物
CN105308028B (zh) 2013-07-25 2017-04-05 Dic株式会社 具有2,6‑二氟苯醚结构的液晶性化合物及其液晶组合物
US10544365B2 (en) 2013-08-30 2020-01-28 Dic Corporation Nematic liquid crystal composition
JP5741986B1 (ja) 2013-10-03 2015-07-01 Dic株式会社 ２，６−ジフルオロフェニルエーテル構造を持つ液晶性化合物及びその液晶組成物
JP5910800B1 (ja) 2014-07-31 2016-04-27 Dic株式会社 ネマチック液晶組成物
US10253258B2 (en) 2014-07-31 2019-04-09 Dic Corporation Nematic liquid crystal composition
CN108912029B (zh) * 2017-08-25 2021-10-01 广东东阳光药业有限公司 含氮杂环酰胺衍生物及其用途
CN110483324A (zh) * 2019-09-10 2019-11-22 深圳振强生物技术有限公司 沙芬酰胺杂质的制备方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1332151C (en) * 1988-01-28 1994-09-27 Roman Amrein Use of a benzamide to treat cognitive disorder
TW498067B (en) * 1996-07-19 2002-08-11 Hoffmann La Roche 4-hydroxy-piperidine derivatives

Also Published As

Publication number Publication date
JP4181540B2 (ja) 2008-11-19
EP1515926A2 (en) 2005-03-23
RU2005100755A (ru) 2005-08-10
WO2003106380A3 (en) 2004-03-11
AU2003236719B2 (en) 2008-06-05
UY27842A1 (es) 2003-12-31
ES2322254T3 (es) 2009-06-18
CA2489247A1 (en) 2003-12-24
EP1515926B1 (en) 2009-04-08
ATE427928T1 (de) 2009-04-15
US20030236304A1 (en) 2003-12-25
BR0311719A (pt) 2005-03-15
WO2003106380A2 (en) 2003-12-24
US6951884B2 (en) 2005-10-04
KR100641963B1 (ko) 2006-11-06
PE20040558A1 (es) 2004-09-09
PA8575001A1 (es) 2003-12-30
AU2003236719A1 (en) 2003-12-31
MXPA04012511A (es) 2005-02-17
RU2314289C2 (ru) 2008-01-10
PL374545A1 (en) 2005-10-31
DE60327074D1 (de) 2009-05-20
TW200406201A (en) 2004-05-01
CN1274669C (zh) 2006-09-13
JP2005529176A (ja) 2005-09-29
CN1659135A (zh) 2005-08-24
KR20050009743A (ko) 2005-01-25

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