HUP0303025A2 - Eljárás ariletanoldiaminok előállítására - Google Patents

Eljárás ariletanoldiaminok előállítására

Info

Publication number
HUP0303025A2
HUP0303025A2 HU0303025A HUP0303025A HUP0303025A2 HU P0303025 A2 HUP0303025 A2 HU P0303025A2 HU 0303025 A HU0303025 A HU 0303025A HU P0303025 A HUP0303025 A HU P0303025A HU P0303025 A2 HUP0303025 A2 HU P0303025A2
Authority
HU
Hungary
Prior art keywords
group
alkyl
atom
trifluoromethyl
alkoxy
Prior art date
Application number
HU0303025A
Other languages
English (en)
Inventor
Jason William Beames Cooke
Bobby Neal Glover
Ronnie Maxwell Lawrence
Matthew Jude Sharp
Maria Fumiko Tymoschenko
Original Assignee
Glaxo Group Limited
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 Glaxo Group Limited filed Critical Glaxo Group Limited
Publication of HUP0303025A2 publication Critical patent/HUP0303025A2/hu
Publication of HUP0303025A3 publication Critical patent/HUP0303025A3/hu

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/18Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79Acids; Esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/52Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/14Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-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 substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/26Radicals substituted by carbon atoms having three bonds to hetero atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/68Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Furan Compounds (AREA)
  • Glass Compositions (AREA)
  • Valve Device For Special Equipments (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Crystals, And After-Treatments Of Crystals (AREA)
  • Iron Core Of Rotating Electric Machines (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Cephalosporin Compounds (AREA)

Abstract

A találmány tárgya eljárás (IA) általános képletűariletanoldiaminszármazékok és gyógyászatilag elfogadható sóikelőállítására, ahol R1 jelentése aril-, fenoximetil- vagy 5- vagy 6-tagú heteroaromás csoport, amelyek mindegyike adott esetben azalábbiak közül választott egy vagy több szubsztituensselhelyettesített: halogénatom, 1-6 szénatomos alkoxi-, 1-6 szénatomosalkil-, nitro-, ciano-, trifluormetil- , -NR8R9- és -NHSO2R8 csoport;R2 jelentése hidrogénatom vagy 1-6 szénatomos alkilcsoport, R3 jelentése hidrogénatom vagy 1-6 szénatomos alkilcsoport, X1 ésX2 jelentése egymástól függetlenül (a) hidrogénatom, (b) 1-6szénatomos alkil-CO- vagy (c) adott esetben halogénatommal vagy 1-6szénatomos alkilcsoporttal helyettesített aril-CO-csoport, azzal amegkötéssel, hogy ha az egyik jelentése (b) vagy (c), akkor a másikhidrogénatom (a); R4 jelentése (a) az alábbiak közül választott egyvagy több szubsztituenssel helyettesített fenilcsoport: 1-6 szénatomosalkilcsoport, halogénatom, trifluormetil-, 1-6 szénatomos alkoxi-, -CO2H és -CO2R8; vagy (b), fenoximetil- vagy adott esetben az alábbiakközül választott egy vagy több szubsztituenssel helyettesített 5- vagy6-tagú heteroaromás csoport: 1-6 szénatomos alkilcsoport, halogénatom,trifluormetil-, 1-6 szénatomos alkoxi-, -CO2H, -CO2R8, CN, NO2,hidroximetilcsoport és -CONHR8; vagy (c) (W) általános képletűcsoport, ahol A jelentése arilcsoport vagy 5- vagy 6-tagú heteroaromáscsoport, R5 jelentése ciano-, tetrazol-5-il-, -CO2H vagy -CO2R8csoport; R6 és R7 jelentése egymástól függetlenül hidrogénatom, 1-6szénatomos alkil-, -CO2H, -CO2R8, ciano-, tetrazol-5-il-csoport,halogénatom, trifluormetil- vagy 1-6 szénatomos alkoxicsoport, vagy haR6 és R7 szomszédos szénatomokhoz kapcsolódik, akkor R6 és R7 azokkala szénatomokkal együtt, amelyekhez kapcsolódnak, 5- vagy 6-tagú adottesetben egy vagy két nitrogénatomot, oxigénatomot vagy kénatomottartalmazó kondenzált gyűrűt képez; valamennyi R12 jelentése egymástólfüggetlenül 1-6 szénatomos alkilcsoport, halogénatom, trifluormetil-vagy 1-6 szénatomos alkoxicsoport, és n értéke 0 és 4 közötti egészszám; és R8 és R9 jelentése egymástól függetlenül 1-6 szénatomosalkilcsoport. A találmány szerinti vegyületek az atípusos béta-adrenoreceptor agonistái, így többek között magas vércukorszintkezelésében alkalmazhatók. Ó
HU0303025A 2001-01-31 2001-12-17 Process for the preparation of arylethanoldiamines HUP0303025A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0102407.4A GB0102407D0 (en) 2001-01-31 2001-01-31 Process
PCT/US2001/049355 WO2002066418A2 (en) 2001-01-31 2001-12-17 Process for the preparation of arylethanoldiamines useful as agonists of the beta-3-adrenoceptor

Publications (2)

Publication Number Publication Date
HUP0303025A2 true HUP0303025A2 (hu) 2003-12-29
HUP0303025A3 HUP0303025A3 (en) 2012-01-30

Family

ID=9907833

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0303025A HUP0303025A3 (en) 2001-01-31 2001-12-17 Process for the preparation of arylethanoldiamines

Country Status (22)

Country Link
US (1) US7425639B2 (hu)
EP (1) EP1366016B1 (hu)
JP (2) JP4421818B2 (hu)
KR (1) KR100895159B1 (hu)
CN (3) CN100390160C (hu)
AT (1) ATE478838T1 (hu)
AU (1) AU2002253815B2 (hu)
BR (1) BR0116853B1 (hu)
CA (1) CA2435126C (hu)
CZ (1) CZ304887B6 (hu)
DE (1) DE60142931D1 (hu)
ES (1) ES2349455T3 (hu)
GB (1) GB0102407D0 (hu)
HK (1) HK1060873A1 (hu)
HU (1) HUP0303025A3 (hu)
IL (4) IL156640A0 (hu)
MX (1) MXPA03006845A (hu)
NO (1) NO20033400L (hu)
NZ (1) NZ526845A (hu)
PL (1) PL209540B1 (hu)
WO (1) WO2002066418A2 (hu)
ZA (1) ZA200305039B (hu)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010118291A2 (en) 2009-04-10 2010-10-14 Auspex Pharmaceuticals, Inc. Biphenyl-3-carboxylic acid modulators of beta-3-adrenoreceptor
US9522129B2 (en) 2010-08-03 2016-12-20 Velicept Therapeutics, Inc. Pharmaceutical Combination
US9907767B2 (en) 2010-08-03 2018-03-06 Velicept Therapeutics, Inc. Pharmaceutical compositions and the treatment of overactive bladder
KR20150020160A (ko) 2012-02-09 2015-02-25 앨씨알엑스, 인크. 과민성 방광의 치료를 위한 무스카린 수용체 길항제 및 베타―3 아드레날린 수용체 작용제의 조합물
KR20170086659A (ko) 2014-12-03 2017-07-26 벨리셉트 테라퓨틱스, 인크. 하부 요로 증상을 위한 변형 방출형 솔라베그론을 이용한 조성물 및 방법
CN114230477A (zh) * 2015-10-23 2022-03-25 B3Ar治疗股份有限公司 索拉贝隆两性离子及其应用

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DE200619C (hu)
DE2965655D1 (en) 1978-06-28 1983-07-21 Beecham Group Plc Secondary amines, their preparation, pharmaceutical compositions containing them and their use
DD200619A1 (de) * 1981-08-21 1983-05-25 Heinz Paul Verfahren zur herstellung von 1,2-disubstituierten deltaquadrat-imidazolinen und deren salzen
EP0103830A3 (de) 1982-09-22 1985-07-31 Bayer Ag Wachstumsfördernde Phenylethylamin-Derivate
GB8519154D0 (en) 1985-07-30 1985-09-04 Ici Plc Aromatic ethers
DE3718638A1 (de) 1987-06-04 1988-12-22 Thomae Gmbh Dr K Neue phenylethanolamine, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
DE3934436A1 (de) 1989-06-01 1991-04-18 Thomae Gmbh Dr K 2-hydroxy-n-propylamine, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
US5061727A (en) 1990-05-04 1991-10-29 American Cyanamid Company Substituted 5-(2-((2-aryl-2-hydroxyethyl)amino)propyl)-1,3-benzodioxoles
GB9111426D0 (en) 1991-05-28 1991-07-17 Ici Plc Chemical compounds
GB9111425D0 (en) 1991-05-28 1991-07-17 Ici Plc Chemical compounds
NO179246C (no) 1991-11-20 1996-09-04 Sankyo Co Aromatiske amino-alkoholderivater og mellomprodukter til fremstilling derav
GB9207964D0 (en) 1992-04-10 1992-05-27 Ici Plc Chemical compounds
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AU2737295A (en) 1994-06-09 1996-01-04 Glaxo Group Limited Phenethanolamine derivatives and their use as atypical beta-adrenoceptor agonists
GB9525177D0 (en) * 1995-12-08 1996-02-07 Glaxo Group Ltd Chemical compounds
GB9525121D0 (en) * 1995-12-08 1996-02-07 Glaxo Group Ltd Chemical compounds
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GB9812709D0 (en) * 1998-06-13 1998-08-12 Glaxo Group Ltd Chemical compounds
GB0102408D0 (en) * 2001-01-31 2001-03-14 Glaxo Group Ltd Chemical compounds

Also Published As

Publication number Publication date
NO20033400L (no) 2003-09-30
CA2435126C (en) 2012-03-13
PL209540B1 (pl) 2011-09-30
ATE478838T1 (de) 2010-09-15
KR100895159B1 (ko) 2009-05-04
EP1366016A2 (en) 2003-12-03
NO20033400D0 (no) 2003-07-30
AU2002253815B2 (en) 2005-07-14
DE60142931D1 (de) 2010-10-07
CZ20032086A3 (en) 2004-03-17
CN1487916A (zh) 2004-04-07
CN1765886A (zh) 2006-05-03
ZA200305039B (en) 2004-08-31
IL195384A0 (en) 2009-08-03
JP2009137946A (ja) 2009-06-25
MXPA03006845A (es) 2003-11-13
IL156640A (en) 2010-12-30
IL195385A0 (en) 2009-08-03
NZ526845A (en) 2005-09-30
JP5049946B2 (ja) 2012-10-17
US20040077868A1 (en) 2004-04-22
ES2349455T3 (es) 2011-01-03
IL156640A0 (en) 2004-01-04
JP2004524307A (ja) 2004-08-12
CN1765893A (zh) 2006-05-03
EP1366016B1 (en) 2010-08-25
BR0116853B1 (pt) 2014-04-08
GB0102407D0 (en) 2001-03-14
CZ304887B6 (cs) 2015-01-07
BR0116853A (pt) 2004-02-25
WO2002066418A2 (en) 2002-08-29
CA2435126A1 (en) 2002-08-29
HUP0303025A3 (en) 2012-01-30
KR20030087183A (ko) 2003-11-13
US7425639B2 (en) 2008-09-16
HK1060873A1 (en) 2004-08-27
PL363360A1 (en) 2004-11-15
CN100390160C (zh) 2008-05-28
JP4421818B2 (ja) 2010-02-24
WO2002066418A3 (en) 2003-02-06

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