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PE20021067A1 - USE OF NK3 RECEIVER ANTAGONISTS - Google Patents

USE OF NK3 RECEIVER ANTAGONISTS

Info

Publication number
PE20021067A1
PE20021067A1 PE2002000415A PE2002000415A PE20021067A1 PE 20021067 A1 PE20021067 A1 PE 20021067A1 PE 2002000415 A PE2002000415 A PE 2002000415A PE 2002000415 A PE2002000415 A PE 2002000415A PE 20021067 A1 PE20021067 A1 PE 20021067A1
Authority
PE
Peru
Prior art keywords
alkyl
aryl
functional
candle7
cycloalkylalkyl
Prior art date
Application number
PE2002000415A
Other languages
Spanish (es)
Inventor
Douglas William Pierre Hay
Tadataka Yamada
Gareth John Sanger
Original Assignee
Smithkline Beecham Corp
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
Priority claimed from GB0112208A external-priority patent/GB0112208D0/en
Priority claimed from GB0129268A external-priority patent/GB0129268D0/en
Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of PE20021067A1 publication Critical patent/PE20021067A1/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Peptides Or Proteins (AREA)

Abstract

SE REFIERE A UN METODO PARA EL TRATAMIENTO DE SINDROME DEL INTESTINO IRRITABLE, DISTENSION ABDOMINAL FUNCIONAL, ESTRENIMIENTO FUNCIONAL, DIARREA FUNCIONAL QUE COMPRENDE LA ADMINISTRACION DE UN ANTAGONISTA DEL RECEPTOR NEUROQUININA B NK3 DE FORMULA I, DONDE Ar ES FENILO, NAFTILO, CICLOALCADIENILO C5-C7, HETEROCICLO; R ES ALQUILO C1-C8, CICLOALQUILO C3-C7, CICLOALQUILALQUILO C4-C7, FENILO, FENILALQUILO C1-C6, ENTRE OTROS; R1 Y R2 SON H, ALQUILO C1-C6 O JUNTOS FORMAN UN GRUPO (CH2)n; n ES 3-5 O R1 Y R FORMAN JUNTOS (CH2)q; q ES 2-5; R3 Y R4 SON H, ALQUILO C1-C6, ALQUENILO C1-C6, ARILO, ALCOXI C1-C6, HIDROXI, HALOGENO, O FORMAN UN GRUPO a, b, ENTRE OTROS; V Y V1 SON H, O; u ES 0-2; O(CH2)sOW; S ES 2-4; W ES H, ALQUILO C1-C6, HIDROXIALQUILO, ALQUILAMINO; O R4 ES (CH2)t CUANDO SE CICLA CON R5 COMO ARILO; t ES 1-3; R5 ES ALQUILO C1-C6, CICLOALQUILO C3-C7, CICLOALQUILALQUILO C4-C7, ARILO, HETEROCICLO; X ES O, S, N-CºN. SON COMPUESTOS PREFERIDOS (S)-N-(O-ETILBENCIL)-3-HIDROXI-2-FENILQUINOLINA-4-CARBOXAMIDA; [[(DICLOROFENIL)(TRIMETEOXIBENZOIL)MORFOLINIL]ETILESPIRO[BENZO(c)TIOFENOPIPERIDINA]REFERS TO A METHOD FOR THE TREATMENT OF IRRITABLE BOWEL SYNDROME, FUNCTIONAL ABDOMINAL DISTENSION, FUNCTIONAL STRENGTH, FUNCTIONAL DIARRHEA, INCLUDING THE ADMINISTRATION OF AN ANTAGONIST OF THE RECEPTOR NEUROQUININE B NK3 DE FORMILONIUS CANDYLUS 7, CANDYLONIUS CANDLE7, CANDYLONIC NAPHILUS I7, CANDYLONICLE I5 CANDYLENE CANDLE7 , HETEROCICLO; R IS C1-C8 ALKYL, C3-C7 CYCLOALKYL, C4-C7 CYCLOALKYLALKYL, PHENYL, C1-C6 PHENYLALKYL, AMONG OTHERS; R1 AND R2 ARE H, C1-C6 ALKYL OR TOGETHER FORM A (CH2) n GROUP; n IS 3-5 OR R1 AND R FORM TOGETHER (CH2) q; q IS 2-5; R3 AND R4 ARE H, C1-C6 ALKYL, C1-C6 ALKYL, ARYL, C1-C6 ALCOXY, HYDROXY, HALOGEN, OR FORM A GROUP a, b, AMONG OTHERS; V AND V1 ARE H, O; u ES 0-2; O (CH2) sOW; S IS 2-4; W IS H, C1-C6 ALKYL, HYDROXYALKYL, ALKYLAMINE; OR R4 IS (CH2) t WHEN CYCLING WITH R5 AS ARYL; t IS 1-3; R5 IS C1-C6 ALKYL, C3-C7 CYCLOALKYL, C4-C7 CYCLOALKYLALKYL, ARYL, HETEROCYCLE; X IS O, S, N-CºN. PREFERRED COMPOUNDS ARE (S) -N- (O-ETHYLBENZYL) -3-HYDROXY-2-PHENYLQUINOLINE-4-CARBOXAMIDE; [[(DICHLOROPHENIL) (TRIMETEOXIBENZOIL) MORFOLINYL] ETHYLSPIRO [BENZO (c) THIOPHENOPIPERIDINA]

PE2002000415A 2001-05-18 2002-05-17 USE OF NK3 RECEIVER ANTAGONISTS PE20021067A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0112208A GB0112208D0 (en) 2001-05-18 2001-05-18 New use
GB0129268A GB0129268D0 (en) 2001-12-06 2001-12-06 Novel use

Publications (1)

Publication Number Publication Date
PE20021067A1 true PE20021067A1 (en) 2003-02-02

Family

ID=26246093

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002000415A PE20021067A1 (en) 2001-05-18 2002-05-17 USE OF NK3 RECEIVER ANTAGONISTS

Country Status (19)

Country Link
EP (1) EP1387687A4 (en)
JP (1) JP2004534761A (en)
KR (1) KR20040016865A (en)
CN (1) CN1269483C (en)
AR (1) AR045879A1 (en)
AU (1) AU2002303811B2 (en)
BR (1) BR0209662A (en)
CA (1) CA2447063A1 (en)
CZ (1) CZ20033115A3 (en)
HU (1) HUP0400966A2 (en)
IL (1) IL158701A0 (en)
MX (1) MXPA03010509A (en)
MY (1) MY134211A (en)
NO (1) NO20035121L (en)
NZ (1) NZ529462A (en)
PE (1) PE20021067A1 (en)
PL (1) PL367308A1 (en)
TW (1) TWI243678B (en)
WO (1) WO2002094187A2 (en)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
BR122018074353B8 (en) 2003-01-28 2023-05-02 Ironwood Pharmaceuticals Inc pharmaceutical composition, polypeptide and methods for producing them
ATE387189T1 (en) * 2004-03-30 2008-03-15 Smithkline Beecham Corp SPRAY DRIED PHARMACEUTICAL COMPOSITIONS
WO2005100997A2 (en) * 2004-04-16 2005-10-27 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with tachykinin receptor 3 (tacr3)
WO2007041479A2 (en) * 2005-09-30 2007-04-12 Smithkline Beecham Corporation Pharmaceutical compositions
TW201018662A (en) 2005-12-12 2010-05-16 Astrazeneca Ab Alkylsulphonamide quinolines
ES2559319T3 (en) 2007-06-04 2016-02-11 Synergy Pharmaceuticals Inc. Guanylate cliclas agonists useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
CA2726917C (en) 2008-06-04 2018-06-26 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
EP3241839B1 (en) 2008-07-16 2019-09-04 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
EP2384318B1 (en) 2008-12-31 2017-11-15 Ardelyx, Inc. Compounds and methods for inhibiting nhe-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders
WO2018129556A1 (en) 2017-01-09 2018-07-12 Ardelyx, Inc. Compounds and methods for inhibiting nhe-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders
KR200452372Y1 (en) * 2010-05-14 2011-02-22 서일수 Communication line support device of construction lift
KR101034774B1 (en) * 2010-07-30 2011-05-17 (주)챔피온코리아 Lift device using wire rope
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
US10376481B2 (en) 2012-08-21 2019-08-13 Ardelyx, Inc. Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders
HK1211469A1 (en) 2012-08-21 2016-05-27 Ardelyx, Inc. Compounds and methods for inhibiting nhe-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders
CA2905438A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
EP2968439A2 (en) 2013-03-15 2016-01-20 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
AU2014250956B2 (en) 2013-04-12 2019-04-04 Ardelyx, Inc. NHE3-binding compounds and methods for inhibiting phosphate transport
EP2986293A1 (en) 2013-04-19 2016-02-24 Astrazeneca AB A nk3 receptor antagonist compound (nk3ra) for use in a method for the treatment of polycystic ovary syndrome (pcos)
EA201592263A1 (en) 2013-06-05 2016-05-31 Синерджи Фармасьютикалз, Инк. ULTRASCULAR AGONISTS OF GUANYLACYCLASE C, METHOD OF THEIR RECEIVING AND USING
WO2018129557A1 (en) 2017-01-09 2018-07-12 Ardelyx, Inc. Inhibitors of nhe-mediated antiport
WO2018129552A1 (en) 2017-01-09 2018-07-12 Ardelyx, Inc. Compounds useful for treating gastrointestinal tract disorders

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2719311B1 (en) * 1994-03-18 1998-06-26 Sanofi Sa Compounds that are selective antagonists of the human NK3 receptor and their use as drugs and diagnostic tools.
US5434158A (en) * 1994-04-26 1995-07-18 Merck & Co., Inc. Spiro-substituted azacycles as neurokinin-3 antagonists
AR004735A1 (en) * 1995-11-24 1999-03-10 Smithkline Beecham Spa CHINOLEIN 4-AMIDO SUBSTITUTED, A PROCEDURE FOR ITS PREPARATION, A PHARMACEUTICAL COMPOSITION THAT CONTAINS THEM AND THE USE OF THE SAME FOR THE PREPARATION OF A MEDICINAL PRODUCT.
JP2002500645A (en) * 1997-05-23 2002-01-08 スミスクライン・ビーチャム・ソシエタ・ペル・アチオニ Quinoline-4-carboxamide derivatives as NK-2 and NK-3 receptor antagonists
AR021355A1 (en) * 1998-11-20 2002-07-17 Smithkline Beecham Spa DERIVATIVES OF QUINOLINA. PROCEDURE FOR THE PREPARATION, PHARMACEUTICAL COMPOSITION THAT INCLUDES THEM, AND THE USE OF THEM FOR THE MANUFACTURE OF A MEDICINE

Also Published As

Publication number Publication date
CZ20033115A3 (en) 2004-09-15
PL367308A1 (en) 2005-02-21
MXPA03010509A (en) 2004-03-02
TWI243678B (en) 2005-11-21
EP1387687A2 (en) 2004-02-11
AR045879A1 (en) 2005-11-16
IL158701A0 (en) 2004-05-12
HUP0400966A2 (en) 2004-08-30
JP2004534761A (en) 2004-11-18
EP1387687A4 (en) 2006-07-05
CN1509175A (en) 2004-06-30
WO2002094187A2 (en) 2002-11-28
BR0209662A (en) 2004-04-20
MY134211A (en) 2007-11-30
AU2002303811B2 (en) 2005-07-07
WO2002094187A3 (en) 2003-05-30
KR20040016865A (en) 2004-02-25
NO20035121D0 (en) 2003-11-17
CN1269483C (en) 2006-08-16
NZ529462A (en) 2005-07-29
CA2447063A1 (en) 2002-11-28
NO20035121L (en) 2003-11-17

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