ES2183567T3 - Inhibidores de fkbp. - Google Patents

Inhibidores de fkbp.

Info

Publication number
ES2183567T3
ES2183567T3 ES99926683T ES99926683T ES2183567T3 ES 2183567 T3 ES2183567 T3 ES 2183567T3 ES 99926683 T ES99926683 T ES 99926683T ES 99926683 T ES99926683 T ES 99926683T ES 2183567 T3 ES2183567 T3 ES 2183567T3
Authority
ES
Spain
Prior art keywords
alkyl
optionally substituted
cycloalkyl
halo
alkenyl
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES99926683T
Other languages
English (en)
Inventor
Martin James Wythes
Michael John Palmer
Mark Ian Kemp
Malcolm Christian Mackenny
Robert John Maguire
James Francis Blake Jr
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pfizer Inc
Original Assignee
Pfizer Inc
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 Pfizer Inc filed Critical Pfizer Inc
Application granted granted Critical
Publication of ES2183567T3 publication Critical patent/ES2183567T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/42Oxazoles
    • A61K31/423Oxazoles condensed with carbocyclic rings
    • 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
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • 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
    • 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
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Glass Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Un compuesto de fórmula (I): o una sal farmacéuticamente aceptable, o solvato de cualquiera de los mismos, en la que: X es O, S, NH o N(alquilo C1-6); cada uno de R1, R2, R3 y R4 es independientemente H, OH, OCO(alquilo C1-6), CO2(alquilo C1-6), CONH2, CONH(alquilo C1-6), CON(alquilo C1-6)2, halo, cicloalquilo C3-7, cicloalquiloxi C3-7, alquenilo C2-6, arilo1, alquilo C1-6 opcionalmente sustituido con uno o más sustituyentes seleccionados entre halo y cicloalquilo C3-7 y alcoxi C1-6 opcionalmente sustituido con uno o más sustituyentes seleccionados entre fluoro y cicloalquilo C3-7; A es un alquileno C3-5 no ramificado opcionalmente sustituido con hasta tres grupos alquilo C1-6; D es O o S; E es O, S, NH, N(alquilo C1-6) o CR11R12; G es alquilo C1-14 o alquenilo C2-14, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre halo, arilo, alcoxi C1-14, cicloalquilo, het y NR5R6, cada uno de R5 y R6 es independientemente H o alquilo C1-6 o se toman conjuntamente para formar, con el átomo de nitrógeno al que están unidos, un anillo heterocíclico de 4 a 7 miembros que contiene opcionalmente otro resto hetero seleccionado entre NR7, O y S(O)P y estando dicho anillo heterocíclico de 4 a 7 miembros opcionalmente sustituido con hasta 3 sustituyentes seleccionados independientemente entre alquilo C1-6 y alcoxi C1-6; R7 es H, alquilo C1-6, alquenilo C2-6, COR8, SO2R8, CONR9R10, CO2R8 o SO2NR9R10; R8 es cicloalquilo C3-7, alquenilo C2-6, arilo1 o alquilo C1-6 opcionalmente sustituidos con cicloalquilo C3- 7 o arilo1; cada uno de R9 y R10 es independientemente H, alquenilo C2-6, cicloalquilo C3-7 o alquilo C1-6 opcionalmente sustituido con cicloalquilo C3-7 o arilo; cada uno de R11 y R12 es independientemente H, arilo, alquenilo C2-8 o alquilo C1-8, estando dichos grupos alquenilo C2-8 y alquilo C1-8 opcionalmente sustituidos con unoo más sustituyentes seleccionados independientemente entre halo, NO2, alquilo C1-6, alquenilo C2-6, cicloalquilo, OH, alcoxi C1-6, alqueniloxi C2-6, feniloxi, benciloxi, NH2, arilo y het; p es 0,1 ó 2; en las que "arilo" significa fenilo o naftilo, y cada uno de ellos está opcionalmente sustituido con hasta 3 sustituyentes seleccionados independientemente entre alquilo C1-6 opcionalmente sustituido con uno o más grupos halo o cicloalquilo C3-7, alquenilo C2-6, alcoxi C1-6, alqueniloxi C2-6, OH, halo, NO2, feniloxi, benciloxi, fenilo y NH2; "arilo" significa fenilo, naftilo o bencilo, en las que cada uno de ellos está opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados independientemente entre alquilo C1-6 opcionalmente sustituido con uno o más grupos halo o cicloalquilo C3-7, alcoxi y halo; siendo "cicloalquilo" cicloalquilo C3-8 opcionalmente sustituido con hasta 3 sustituyentes seleccionados independientemente entre alqueniloC2-6, alcoxi C1-6, alqueniloxi C2-6, OH, halo y alquilo C1-6 opcionalmente sustituido con uno o más halo; y significando "het" un heterociclico monocíclico de 5 ó 6 miembros o bicíclico de 8, 9 ó 10 miembros que contiene de 1 a 3 heteroátomos seleccionados independientemente entre O, N y S y que está opcionalmente sustituido con hasta 3 sustituyentes seleccionados independientemente entre alquilo C1-6 opcionalmente sustituido con uno o más grupos halo o cicloalquilo C3-7, alquenilo C2-6, alcoxi C1-6, alqueniloxi C2-6, OH, halo, NO2, feniloxi, benciloxi y NH2; con la condición de que el compuesto no sea metil 1- (5-cloro-2-benzoxazolil)prolina.
ES99926683T 1998-07-20 1999-07-01 Inhibidores de fkbp. Expired - Lifetime ES2183567T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB9815696.1A GB9815696D0 (en) 1998-07-20 1998-07-20 Heterocyclics

Publications (1)

Publication Number Publication Date
ES2183567T3 true ES2183567T3 (es) 2003-03-16

Family

ID=10835773

Family Applications (1)

Application Number Title Priority Date Filing Date
ES99926683T Expired - Lifetime ES2183567T3 (es) 1998-07-20 1999-07-01 Inhibidores de fkbp.

Country Status (45)

Country Link
US (2) US6166011A (es)
EP (1) EP1098894B1 (es)
JP (1) JP3545341B2 (es)
KR (1) KR20010083130A (es)
CN (1) CN1315951A (es)
AP (1) AP2001002045A0 (es)
AR (1) AR016501A1 (es)
AT (1) ATE225346T1 (es)
AU (1) AU756769B2 (es)
BG (1) BG105249A (es)
BR (1) BR9912307A (es)
CA (1) CA2338276C (es)
CO (1) CO5080761A1 (es)
CZ (1) CZ2001224A3 (es)
DE (1) DE69903319T2 (es)
DK (1) DK1098894T3 (es)
DZ (1) DZ2848A1 (es)
EA (1) EA200100051A1 (es)
EE (1) EE200100043A (es)
ES (1) ES2183567T3 (es)
GB (1) GB9815696D0 (es)
GT (1) GT199900113A (es)
HK (1) HK1040706A1 (es)
HN (1) HN1999000101A (es)
HR (1) HRP20010053A2 (es)
HU (1) HUP0103020A3 (es)
ID (1) ID27022A (es)
IL (1) IL140243A0 (es)
IS (1) IS5799A (es)
MA (1) MA26661A1 (es)
NO (1) NO20010299L (es)
NZ (1) NZ508839A (es)
OA (1) OA11586A (es)
PA (1) PA8477601A1 (es)
PE (1) PE20000867A1 (es)
PL (1) PL345705A1 (es)
PT (1) PT1098894E (es)
SI (1) SI1098894T1 (es)
SK (1) SK702001A3 (es)
TN (1) TNSN99146A1 (es)
TR (1) TR200100133T2 (es)
UA (1) UA60368C2 (es)
WO (1) WO2000005231A1 (es)
YU (1) YU83100A (es)
ZA (1) ZA200100229B (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9815696D0 (en) * 1998-07-20 1998-09-16 Pfizer Ltd Heterocyclics
GB9815880D0 (en) * 1998-07-21 1998-09-16 Pfizer Ltd Heterocycles
GB0008939D0 (en) 2000-04-11 2000-05-31 Glaxo Group Ltd Process for preparing substituted benzimidazole compounds
AU2002241524A1 (en) * 2000-11-28 2002-06-11 Wyeth Expression analysis of FKBP nucleic acids and polypeptides useful in the diagnosis and treatment of prostate cancer
US7186518B2 (en) * 2003-11-21 2007-03-06 Dade Behring Inc. Method and composition useful for determining FK 506
WO2009154754A2 (en) * 2008-06-17 2009-12-23 Concert Pharmaceuticals, Inc. Synthesis of deuterated morpholine derivatives
DE102008060549A1 (de) 2008-12-04 2010-06-10 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Wirkstoff-Peptid-Konstrukt zur extrazellulären Anreicherung
TWI534142B (zh) 2011-03-15 2016-05-21 大正製藥股份有限公司 Azole derivatives
EP2705856A1 (en) 2012-09-07 2014-03-12 Deutsches Zentrum für Neurodegenerative Erkrankungen e.V. Compounds for the treatment of neurodegenerative disorders
CN106138044B (zh) * 2016-07-15 2017-05-03 鲁俊东 一种治疗腰椎间盘突出症的药物

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI91859C (fi) * 1987-06-17 1994-08-25 Eisai Co Ltd Analogiamenetelmä antiallergisena aineena aktiivisen bentsotiatsolijohdannaisen valmistamiseksi
FR2696176B1 (fr) * 1992-09-28 1994-11-10 Synthelabo Dérivés de pipéridine, leur préparation et leur application en thérapeutique.
CO4520280A1 (es) * 1993-10-26 1997-10-15 Boehringer Ingelheim Pharma Derivados de pirrolidina, inhibidores de la bioscientesis de leucotrienos
US5801187A (en) * 1996-09-25 1998-09-01 Gpi-Nil Holdings, Inc. Heterocyclic esters and amides
GB9700597D0 (en) * 1997-01-14 1997-03-05 Sandoz Pharma Uk Organic compounds
US5721256A (en) * 1997-02-12 1998-02-24 Gpi Nil Holdings, Inc. Method of using neurotrophic sulfonamide compounds
GB9815696D0 (en) * 1998-07-20 1998-09-16 Pfizer Ltd Heterocyclics
US6686357B1 (en) * 1999-07-15 2004-02-03 Pfizer, Inc. FKBP inhibitors
GB9815880D0 (en) * 1998-07-21 1998-09-16 Pfizer Ltd Heterocycles

Also Published As

Publication number Publication date
PT1098894E (pt) 2003-02-28
CA2338276A1 (en) 2000-02-03
TR200100133T2 (tr) 2001-06-21
ZA200100229B (en) 2002-04-09
AU4385599A (en) 2000-02-14
NO20010299L (no) 2001-03-15
CA2338276C (en) 2007-01-09
US20040058905A1 (en) 2004-03-25
CZ2001224A3 (cs) 2001-08-15
HN1999000101A (es) 2000-11-11
BG105249A (en) 2001-11-30
AP2001002045A0 (en) 2001-03-31
MA26661A1 (fr) 2004-12-20
KR20010083130A (ko) 2001-08-31
EA200100051A1 (ru) 2001-08-27
SI1098894T1 (en) 2002-12-31
AR016501A1 (es) 2001-07-04
DK1098894T3 (da) 2002-10-28
HK1040706A1 (zh) 2002-06-21
EP1098894A1 (en) 2001-05-16
DE69903319D1 (de) 2002-11-07
BR9912307A (pt) 2001-05-02
OA11586A (en) 2004-07-26
GB9815696D0 (en) 1998-09-16
TNSN99146A1 (fr) 2005-11-10
NZ508839A (en) 2003-01-31
PA8477601A1 (es) 2000-09-29
JP2002521381A (ja) 2002-07-16
EP1098894B1 (en) 2002-10-02
ATE225346T1 (de) 2002-10-15
IS5799A (is) 2000-12-29
ID27022A (id) 2001-02-22
UA60368C2 (uk) 2003-10-15
EE200100043A (et) 2002-06-17
WO2000005231A1 (en) 2000-02-03
IL140243A0 (en) 2002-02-10
SK702001A3 (en) 2001-12-03
PE20000867A1 (es) 2000-08-31
CN1315951A (zh) 2001-10-03
GT199900113A (es) 2001-01-09
PL345705A1 (en) 2002-01-02
YU83100A (sh) 2003-04-30
JP3545341B2 (ja) 2004-07-21
AU756769B2 (en) 2003-01-23
NO20010299D0 (no) 2001-01-18
DE69903319T2 (de) 2003-01-30
HUP0103020A2 (hu) 2002-05-29
CO5080761A1 (es) 2001-09-25
DZ2848A1 (fr) 2003-12-01
HRP20010053A2 (en) 2001-12-31
HUP0103020A3 (en) 2002-10-28
US6166011A (en) 2000-12-26

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