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PE20020602A1 - Derivados de fenilcetona sustituidos como antagonistas del receptor de prostaglandina i2 (ip) - Google Patents

Derivados de fenilcetona sustituidos como antagonistas del receptor de prostaglandina i2 (ip)

Info

Publication number
PE20020602A1
PE20020602A1 PE2001001118A PE2001001118A PE20020602A1 PE 20020602 A1 PE20020602 A1 PE 20020602A1 PE 2001001118 A PE2001001118 A PE 2001001118A PE 2001001118 A PE2001001118 A PE 2001001118A PE 20020602 A1 PE20020602 A1 PE 20020602A1
Authority
PE
Peru
Prior art keywords
phenyl
antagonists
prostaglandin
receptor
ona
Prior art date
Application number
PE2001001118A
Other languages
English (en)
Inventor
Alam Jahangir
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 PE20020602A1 publication Critical patent/PE20020602A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D233/28Heterocyclic 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 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
    • C07D233/44Nitrogen atoms not forming part of a nitro radical
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41681,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • C07D233/28Heterocyclic 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 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
    • C07D233/44Nitrogen atoms not forming part of a nitro radical
    • C07D233/50Nitrogen atoms not forming part of a nitro radical with carbocyclic radicals directly attached to said nitrogen atoms
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A DERIVADOS DE FENILCETONA SUSTITUIDOS DE FORMULA I DONDE R1 ES ARILO CON ALQUILO C1-C6, ALCOXILO, ARILO, ARILOXI, ENTRE OTROS; R2 ES H, ALQUILO C1-C6, HALOGENO; A ES -C(O)-(CH2)n-, -C(O)-CH2-O- DONDE n ES 2-6. SON COMPUESTOS PREFERIDOS 4-[4-(4,5-DIHIDRO-1H-IMIDAZOL-2-ILAMINO)FENIL]-1-(4-FLUORO-FENIL)-PROPAN-1-ONA, 1-(2,4-DIFLUOROFENIL)-4-[4-(4,5-DIHIDRO-1H-IMIDAZOL-2-IL-AMINO)FENIL]PROPAN-1-ONA, 1-(4-CLOROFENIL)-4-[4-(4,5-DIHIDRO-1H-IMIDAZOL-2-IL-AMINO)FENIL]PROPAN-1-ONA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA, UN PROCEDIMIENTO PARA LA PREPARACION Y COMPUESTOS INTERMEDIOS. LOS COMPUESTOS MENCIONADOS SON ANTAGONISTAS DEL RECEPTOR DE PROSTAGLANDINAS I2 (IP) Y SON UTILES PARA EL TRATAMIENTO DE ENFERMEDADES ASOCIADAS AL DOLOR E INFLAMACION
PE2001001118A 2000-11-14 2001-11-09 Derivados de fenilcetona sustituidos como antagonistas del receptor de prostaglandina i2 (ip) PE20020602A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US24888800P 2000-11-14 2000-11-14

Publications (1)

Publication Number Publication Date
PE20020602A1 true PE20020602A1 (es) 2002-07-08

Family

ID=22941114

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2001001118A PE20020602A1 (es) 2000-11-14 2001-11-09 Derivados de fenilcetona sustituidos como antagonistas del receptor de prostaglandina i2 (ip)

Country Status (29)

Country Link
EP (1) EP1339694B1 (es)
JP (1) JP4108474B2 (es)
KR (1) KR100562605B1 (es)
CN (1) CN1267423C (es)
AR (1) AR035502A1 (es)
AT (1) ATE305002T1 (es)
AU (1) AU2180802A (es)
BG (1) BG107814A (es)
BR (1) BR0115291A (es)
CA (1) CA2427900A1 (es)
CZ (1) CZ20031596A3 (es)
DE (1) DE60113563T2 (es)
EC (1) ECSP034602A (es)
ES (1) ES2248413T3 (es)
HU (1) HUP0303156A3 (es)
IL (1) IL155436A0 (es)
MA (1) MA26958A1 (es)
MX (1) MXPA03004073A (es)
NO (1) NO20032142L (es)
NZ (1) NZ525330A (es)
PA (1) PA8532201A1 (es)
PE (1) PE20020602A1 (es)
PL (1) PL362549A1 (es)
RU (1) RU2284995C2 (es)
SK (1) SK7222003A3 (es)
UY (1) UY27023A1 (es)
WO (1) WO2002040453A1 (es)
YU (1) YU37203A (es)
ZA (1) ZA200303413B (es)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1596858A1 (en) * 2003-02-14 2005-11-23 Medical Research Council Ip receptor antagonists for the treatment of pathological uterine conditions
MXPA05011476A (es) 2003-05-01 2005-12-12 Hoffmann La Roche Imidazolin-2-il-aminofenil-amidas como antagonistas de prostaglandina i2.
EP1635834A4 (en) * 2003-06-25 2009-12-02 Smithkline Beecham Corp NEW CONNECTIONS
KR100768609B1 (ko) * 2003-07-09 2007-10-18 에프. 호프만-라 로슈 아게 티오페닐아미노이미다졸린
BRPI0707308A2 (pt) * 2006-01-27 2011-05-03 Hoffmann La Roche uso de 2-imidazóis para o tratamento de distúrbios do snc
CA2666762C (en) 2006-10-19 2014-12-30 F. Hoffmann-La Roche Ag Aminomethyl-4-imidazoles
AU2007316257A1 (en) 2006-11-02 2008-05-08 F. Hoffmann-La Roche Ag Substituted 2-imidazoles as modulators of the trace amine associated receptors
WO2008058867A2 (en) 2006-11-16 2008-05-22 F. Hoffmann-La Roche Ag Substituted 4-imidazoles
CA2672617A1 (en) 2006-12-13 2008-06-19 F. Hoffmann-La Roche Ag Novel 2-imidazoles as ligands for trace amine associated receptors (taar)
US20080146523A1 (en) 2006-12-18 2008-06-19 Guido Galley Imidazole derivatives
WO2008092785A1 (en) 2007-02-02 2008-08-07 F. Hoffmann-La Roche Ag Novel 2-aminooxazolines as taar1 ligands for cns disorders
KR101222412B1 (ko) 2007-02-15 2013-01-15 에프. 호프만-라 로슈 아게 Taar1 리간드로서의 2-아미노옥사졸린
WO2009003868A2 (en) 2007-07-02 2009-01-08 F. Hoffmann-La Roche Ag 2 -imidazolines having a good affinity to the trace amine associated receptors (taars)
JP2010531836A (ja) 2007-07-03 2010-09-30 エフ.ホフマン−ラ ロシュ アーゲー 4−イミダゾリン及びそれらの抗うつ剤としての使用
CA2694362A1 (en) 2007-07-27 2009-02-05 F. Hoffmann-La Roche Ag 2-azetidinemethaneamines and 2-pyrrolidinemethaneamines as taar-ligands
KR101167773B1 (ko) 2007-08-03 2012-07-24 에프. 호프만-라 로슈 아게 Taar1 리간드로서의 피리딘카복스아마이드 및 벤즈아마이드 유도체
US8242153B2 (en) 2008-07-24 2012-08-14 Hoffmann-La Roche Inc. 4,5-dihydro-oxazol-2YL derivatives
US8354441B2 (en) 2009-11-11 2013-01-15 Hoffmann-La Roche Inc. Oxazoline derivatives
WO2011080132A2 (en) 2009-12-17 2011-07-07 Katholieke Universiteit Leuven, K.U. Leuven R&D Compounds, compositions and methods for controlling biofilms
US9452980B2 (en) 2009-12-22 2016-09-27 Hoffmann-La Roche Inc. Substituted benzamides
WO2014143591A1 (en) 2013-03-12 2014-09-18 Allergan, Inc. Inhibition of neovascularization by simultaneous inhibition of prostanoid ip and ep4 receptors
WO2014143592A1 (en) 2013-03-12 2014-09-18 Allergan, Inc. Inhibition of neovascularization by inhibition of prostanoid ip receptors
US9827225B2 (en) * 2016-01-25 2017-11-28 Jenivision Inc. Use of prostacyclin antagonists for treating ocular surface nociception
RS60825B1 (sr) 2016-03-17 2020-10-30 Hoffmann La Roche Aktivnost derivata 5-etiol-4-metil-pirazol-3-karboksamida kao agonista taar-a
US20240002369A1 (en) * 2020-11-12 2024-01-04 3Z Ehf Novel treatments of attention deficit/hyperactivity disorder

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US4889868A (en) * 1984-12-20 1989-12-26 Rorer Pharmaceutical Corporation Bis-imidazolinoamino derivatives as antiallergy compounds
GB9506188D0 (en) * 1995-03-27 1995-05-17 Fujisawa Pharmaceutical Co Amidine derivatives
NZ331480A (en) * 1997-09-04 2000-02-28 F 2-(Arylphenyl)amino-imidazoline derivatives and pharmaceutical compositions

Also Published As

Publication number Publication date
RU2284995C2 (ru) 2006-10-10
CN1474813A (zh) 2004-02-11
PL362549A1 (en) 2004-11-02
CZ20031596A3 (cs) 2004-01-14
ES2248413T3 (es) 2006-03-16
BR0115291A (pt) 2003-08-19
BG107814A (bg) 2004-02-27
NO20032142D0 (no) 2003-05-13
ECSP034602A (es) 2003-06-25
JP2004513940A (ja) 2004-05-13
EP1339694B1 (en) 2005-09-21
SK7222003A3 (en) 2004-05-04
IL155436A0 (en) 2003-11-23
AR035502A1 (es) 2004-06-02
WO2002040453A1 (en) 2002-05-23
JP4108474B2 (ja) 2008-06-25
DE60113563D1 (de) 2006-02-02
CN1267423C (zh) 2006-08-02
MXPA03004073A (es) 2003-09-04
PA8532201A1 (es) 2002-08-26
MA26958A1 (fr) 2004-12-20
CA2427900A1 (en) 2002-05-23
KR100562605B1 (ko) 2006-03-17
KR20030065512A (ko) 2003-08-06
NO20032142L (no) 2003-05-13
ZA200303413B (en) 2004-08-02
YU37203A (sh) 2006-05-25
NZ525330A (en) 2004-10-29
AU2180802A (en) 2002-05-27
DE60113563T2 (de) 2006-07-13
HUP0303156A2 (hu) 2004-01-28
UY27023A1 (es) 2002-06-20
EP1339694A1 (en) 2003-09-03
ATE305002T1 (de) 2005-10-15
HUP0303156A3 (en) 2004-03-29

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