ECSP034710A - Derivados biarilicos nicotinamida de utilidad como inhibidores de isozimas pde4 - Google Patents

Derivados biarilicos nicotinamida de utilidad como inhibidores de isozimas pde4

Info

Publication number
ECSP034710A
ECSP034710A EC2003004710A ECSP034710A ECSP034710A EC SP034710 A ECSP034710 A EC SP034710A EC 2003004710 A EC2003004710 A EC 2003004710A EC SP034710 A ECSP034710 A EC SP034710A EC SP034710 A ECSP034710 A EC SP034710A
Authority
EC
Ecuador
Prior art keywords
optionally
carbon atom
alkyl
replaced
ring system
Prior art date
Application number
EC2003004710A
Other languages
English (en)
Inventor
Thomas Victor Magee
Anthony Marfat
Robert James Chambers
Original Assignee
Pfizer Prod 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 Prod Inc filed Critical Pfizer Prod Inc
Publication of ECSP034710A publication Critical patent/ECSP034710A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • A61P25/24—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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Biotechnology (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • AIDS & HIV (AREA)

Abstract

Compuestos de utilidad como inhibidores de PDE4 en el tratamiento de enfermedades reguladas por la activación y desgranulación de eosinófilos, especialmente asma, bronquitis crónica, y enfermedad pulmonar obstructiva crónica de fórmula: (gráfico). Donde j es 0 ó 1 con la condición de que cuando j es 0, n debe ser 2; k es 0 ó 1; m es 0, 1,, ó 2; n es 1 ó 2; W1 es -O-; o -S(=O)t-, donde t es 0,1 ó 2; o -N(R3)-; W2 es -O-CRARB-, o está ausente; y es =C(R1a)- o [N (O)k] -donde k es 0 ó 1; RA y RB son -H; -F; -CF3; alquilo C1-C4; cicloalqulo C3-C7; fenilo; 0 bencilo sustituido con 0 a 3 sustituyentes R10; o RA y RB se toman conjuntamente, pero únicamente en el caso en que m es 1, para formar un resto espiro; Re y RD tienen el mismo significado que RA y RB pero uno de ellos debe ser -H, R1 y R2 son -H; -F; -CI; -CH; -NO2; -alquilo C1-C4; - alquinilo C2-C4; -alquilo (C1-C3) fluorado; -OR16; y -C(=0)NR22a R22b; R3 es -H; -alquilo C1-C3; fenilo; bencilo; o- OR16; R4, R5 y R6 además de otros significados pueden tomarse conjuntamente para formar, por ejemplo Q1 es un sistema de anillos de carbono saturados o insaturados que es un monociclo de 3 a 7 miembros, o que es un policiclo condensado de 7 a 12 miembros; con la condición de que Q1 no es un resto biarilo discontinuo o restringido como se define en Q2; donde opcionalmente un átomo de carbono puede reemplazarse por un heterátomo seleccionado de N, O y S; donde opcionalmente un segundo átomo de carbono del mismo, y de forma adicional opcionalmente un tercer átomo de carbono del mismo pueden reemplazarse por N; Q2 es un resto blarilo discontinuo o restringido constituido por un sistema de anillo de carbono saturados o insaturados que es un monociclo de 3- a 7- miembros, o que es un policiclo condensado de 7 a 12 miembros; donde opcionalmente un átomo de carbono de dicho sistema de anillo de carbono puede reemplazarse por un heterátomo seleccionado de N,o y S, donde opcionalmente un segundo átomo de carbono del mismo y de forma adicional opcionalmente un tercer átomo de carbono del mismo pueden reemplazarse por N; Z se selecciona de: (gráfico)
EC2003004710A 2001-01-31 2003-07-31 Derivados biarilicos nicotinamida de utilidad como inhibidores de isozimas pde4 ECSP034710A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26549201P 2001-01-31 2001-01-31

Publications (1)

Publication Number Publication Date
ECSP034710A true ECSP034710A (es) 2003-09-24

Family

ID=23010671

Family Applications (2)

Application Number Title Priority Date Filing Date
EC2003004709A ECSP034709A (es) 2001-01-31 2003-07-31 Derivados de eteres utiles como agentes inhibidores de las isozimas pde4
EC2003004710A ECSP034710A (es) 2001-01-31 2003-07-31 Derivados biarilicos nicotinamida de utilidad como inhibidores de isozimas pde4

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EC2003004709A ECSP034709A (es) 2001-01-31 2003-07-31 Derivados de eteres utiles como agentes inhibidores de las isozimas pde4

Country Status (25)

Country Link
US (2) US6649633B2 (es)
EP (1) EP1355884A1 (es)
JP (1) JP2004520386A (es)
KR (1) KR20030074761A (es)
CN (1) CN1518542A (es)
BG (1) BG108038A (es)
BR (1) BR0116852A (es)
CA (1) CA2436535A1 (es)
CR (1) CR7025A (es)
CZ (1) CZ20031895A3 (es)
EA (1) EA200300621A1 (es)
EC (2) ECSP034709A (es)
EE (1) EE200300360A (es)
HU (1) HUP0400637A2 (es)
IL (1) IL156413A0 (es)
IS (1) IS6846A (es)
MA (1) MA26983A1 (es)
MX (1) MXPA03006887A (es)
NO (1) NO20033397L (es)
NZ (1) NZ526453A (es)
OA (1) OA12540A (es)
PL (1) PL364135A1 (es)
SK (1) SK8792003A3 (es)
WO (1) WO2002060875A1 (es)
ZA (1) ZA200304894B (es)

Families Citing this family (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030055026A1 (en) 2001-04-17 2003-03-20 Dey L.P. Formoterol/steroid bronchodilating compositions and methods of use thereof
KR20040007583A (ko) * 2001-05-23 2004-01-24 다나베 세이야꾸 가부시키가이샤 연골 질환의 재생치료용 조성물
MXPA03010679A (es) * 2001-05-23 2004-03-02 Tanabe Seiyaku Co Una composicion para acelerar la cicatrizacion de fractura osea.
US6951869B2 (en) * 2002-02-26 2005-10-04 Schlesinger Stephen L Use of leukotriene receptor antagonist for treatment of scarring
EP1424101A3 (en) * 2002-11-29 2004-08-18 NOZAKI, Masako Use of a leukotriene C4 and D4 receptor antagonist for the preparation of a medicament for treating or preventing brain inflammation and sepsis
US20040225077A1 (en) 2002-12-30 2004-11-11 Angiotech International Ag Drug delivery from rapid gelling polymer composition
BRPI0409229A (pt) * 2003-04-01 2006-03-28 Applied Research Systems inibidores das fosfodiesterases na infertilidade
GB0309781D0 (en) * 2003-04-29 2003-06-04 Glaxo Group Ltd Compounds
GB0317516D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as PDE4 inhibitors
GB0317482D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
US7153870B2 (en) 2003-07-25 2006-12-26 Pfizer Inc. Nicotinamide derivatives useful as PDE4 inhibitors
US7132435B2 (en) * 2003-07-25 2006-11-07 Pfizer Inc. Compounds
US20050020587A1 (en) * 2003-07-25 2005-01-27 Pfizer Inc Nicotinamide derivatives useful as PDE4 inhibitors
GB0317498D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Compounds
GB0317484D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
US7534894B2 (en) * 2003-09-25 2009-05-19 Wyeth Biphenyloxy-acids
US20050154006A1 (en) * 2004-01-09 2005-07-14 Boehringer Ingelheim International Gmbh Pharmaceutical compositions based on a scopineester and nicotinamide derivatives
US20090042951A1 (en) * 2004-02-20 2009-02-12 Robert Danziger Blood Pressure Reduction in Salt-Sensitive Hypertension
WO2005087236A1 (en) * 2004-03-11 2005-09-22 Glaxo Group Limited Novel m3 muscarinic acetylcholine receptor antagonists
JP4793692B2 (ja) * 2004-04-26 2011-10-12 小野薬品工業株式会社 新規なｂｌｔ２介在性疾患、ｂｌｔ２結合剤および化合物
US7704522B2 (en) 2004-09-08 2010-04-27 Clyde Morgan Topical medicament
EP1844136B1 (en) 2004-12-29 2014-08-27 Hadasit Medical Research Services And Development Ltd. Stem cells culture systems
US8597947B2 (en) 2004-12-29 2013-12-03 Hadasit Medical Research Services & Development Limited Undifferentiated stem cell culture systems
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス，インコーポレイティド ムスカリン性受容体調節による神経発生
AU2006304787A1 (en) 2005-10-21 2007-04-26 Braincells, Inc. Modulation of neurogenesis by PDE inhibition
CA2625210A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
TWI385169B (zh) 2005-10-31 2013-02-11 Eisai R&D Man Co Ltd 經雜環取代之吡啶衍生物及含有彼之抗真菌劑
NZ568694A (en) 2005-11-09 2011-09-30 Zalicus Inc Method, compositions, and kits for the treatment of medical conditions
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP2377531A2 (en) 2006-05-09 2011-10-19 Braincells, Inc. Neurogenesis by modulating angiotensin
EP2026813A2 (en) 2006-05-09 2009-02-25 Braincells, Inc. 5 ht receptor mediated neurogenesis
US7998971B2 (en) 2006-09-08 2011-08-16 Braincells Inc. Combinations containing a 4-acylaminopyridine derivative
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
EP2129381A1 (en) 2007-01-24 2009-12-09 Glaxo Group Limited Pharmaceutical compositions comprising 3, 5-diamin0-6- (2, 3-dichl0phenyl) -l, 2, 4-triazine or r (-) -2, 4-diamino-5- (2, 3-dichlorophenyl) -6-fluoromethyl pyrimidine and an nk1
JP5395058B2 (ja) 2007-04-18 2014-01-22 ハダシット メディカル リサーチ サーヴィシーズ アンド ディヴェロップメント リミテッド 幹細胞に由来する網膜色素上皮細胞
US8513287B2 (en) 2007-12-27 2013-08-20 Eisai R&D Management Co., Ltd. Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
JP6148007B2 (ja) 2009-05-12 2017-06-14 コーニンクレッカ フィリップス エヌ ヴェＫｏｎｉｎｋｌｉｊｋｅ Ｐｈｉｌｉｐｓ Ｎ．Ｖ． 前立腺癌マーカーとしてのホスホジエステラーゼ４ｄ７
KR20120036842A (ko) 2009-05-12 2012-04-18 코닌클리케 필립스 일렉트로닉스 엔.브이. 악성의 호르몬 민감성 전립선 암에 대한 마커로서의 포스포디에스테라제 4ｄ7
BR112012004677A2 (pt) 2009-09-01 2020-11-03 Catabasis Pharmaceuticals, Inc. conjugados de ácido graxo niacina e seus usos
USRE46608E1 (en) 2009-09-01 2017-11-14 Catabasis Pharmaceuticals, Inc. Fatty acid niacin conjugates and their uses
WO2011044141A1 (en) * 2009-10-05 2011-04-14 Catabasis Pharmaceuticals, Inc. Fatty acid fibrate derivatives and their uses
EP2804603A1 (en) 2012-01-10 2014-11-26 President and Fellows of Harvard College Beta-cell replication promoting compounds and methods of their use
DK3013796T3 (da) * 2013-06-27 2020-03-16 Lg Chemical Ltd Biarylderivater som gpr120-agonister
AP2016009080A0 (en) * 2013-09-17 2016-03-31 Vectus Biosystems Pty Ltd Compositions for the treatment of hypertension and/or fibrosis
WO2016108240A1 (en) 2014-12-30 2016-07-07 Cell Cure Neurosciences Ltd. Assessing retinal pigment epithelial cell populations
JP6882981B2 (ja) 2014-12-30 2021-06-02 セル キュア ニューロサイエンシズ リミテッド Ｒｐｅ細胞集団およびそれを作製する方法
US11230696B2 (en) 2015-07-29 2022-01-25 Hadasit Medical Research Services And Development Ltd. Large scale production of retinal pigment epithelial cells
AU2016303632B2 (en) 2015-08-05 2022-09-29 Cell Cure Neurosciences Ltd. Preparation of retinal pigment epithelium cells
EA201890442A1 (ru) 2015-08-05 2018-07-31 Селл Кьюр Нейросайансес Лтд. Получение фоторецепторов для лечения заболеваний сетчатки
EP3368661A1 (en) 2015-10-26 2018-09-05 Cell Cure Neurosciences Ltd. Preparation of retinal pigment epithelium cells
US9725406B1 (en) 2016-10-13 2017-08-08 Resolvex Pharmaceuticals Inc. Substituted hydroxystilbenes and their therapeutic applications
EP3595687A1 (en) 2017-03-16 2020-01-22 Lineage Cell Therapeutics, Inc. Methods for measuring therapeutic effects of retinal disease therapies
BR112020013238A2 (pt) 2017-12-29 2020-12-01 Cell Cure Neurosciences Ltd. composição e método para formular células do epitélio pigmentar da retina bem como uso da dita composição para tratar uma condição retiniana
CN112312899A (zh) * 2018-05-04 2021-02-02 治疗方案股份有限公司 靶向癌症干细胞的癌症治疗
CN113038951B (zh) 2018-09-20 2024-04-30 耶达研究及发展有限公司 治疗肌萎缩侧索硬化的方法
US11116737B1 (en) 2020-04-10 2021-09-14 University Of Georgia Research Foundation, Inc. Methods of using probenecid for treatment of coronavirus infections
CN111888349B (zh) * 2020-07-29 2021-10-22 温州医科大学附属第二医院、温州医科大学附属育英儿童医院 印楝素在制备促进缺血超长随意皮瓣存活药物的作用
EP4351334A1 (en) 2021-06-09 2024-04-17 Lineage Cell Therapeutics, Inc. Methods and compositions for treating retinal diseases and conditions
KR20240038013A (ko) 2021-07-28 2024-03-22 리니지 셀 테라퓨틱스, 인크. 망막 색소 상피 세포의 확장
WO2023211857A1 (en) 2022-04-25 2023-11-02 Lineage Cell Therapeutics, Inc. Methods and compositions for treating vision loss

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2140772A5 (en) 1971-06-07 1973-01-19 Aries Robert Phenoxynicotinoylaminophenols - analgesics tranquillisers antipyretics, anti-inflammatories and antirheumatics
US4270946A (en) * 1979-10-01 1981-06-02 Stauffer Chemical Company N-Aryl,2-phenoxy nicotinamide compounds and the herbicidal use thereof
US4692185A (en) * 1986-01-13 1987-09-08 Stauffer Chemical Company N-(ortho-substituted) benzyl, 3-trifluoromethylphenoxy nicotinamides as herbicides
US4861891A (en) * 1988-08-31 1989-08-29 Pfizer Inc. Antidepressant N-substituted nicotinamide compounds
DE69130605T2 (de) 1991-02-27 1999-05-20 Lacer Sa Antihypertensive N-(alpha-substituiertes Pyridyl)-carbonyldipeptide
DE4200323A1 (de) 1992-01-09 1993-07-15 Bayer Ag Herbizide und pflanzennematizide mittel auf basis von mercaptonicotinsaeurederivaten
US5552438A (en) 1992-04-02 1996-09-03 Smithkline Beecham Corporation Compounds useful for treating allergic and inflammatory diseases
EP1466598A3 (en) 1993-06-18 2007-06-27 Smithkline Beecham Corporation PDE-IV inhibitors
JP3406689B2 (ja) 1994-03-15 2003-05-12 株式会社大塚製薬工場 ナフチリジン及びピリドピラジン誘導体
US5618027A (en) * 1994-07-20 1997-04-08 Nevrekar; Venkatesh R. Gate valve
EP0796096A4 (en) 1994-12-23 1998-04-29 Smithkline Beecham Corp 4,4- (DISUBSTITUTED) CYCLOHEXAN-1-CARBOXYLATE MONOMERS AND RELATED COMPOUNDS
TW429148B (en) * 1995-10-27 2001-04-11 Pfizer Pharmaceutical agents for the treatment of acute and chronic inflammatory diseases
GB9622386D0 (en) 1996-10-28 1997-01-08 Sandoz Ltd Organic compounds
US5922557A (en) 1997-01-09 1999-07-13 Merck & Co., Inc. System for stably expressing a high-affinity camp phosphodiesterase and use thereof
EA003528B1 (ru) 1997-04-04 2003-06-26 Пфайзер Продактс Инк. Производные никотинамида, их применение, фармацевтическая композиция, способ лечения и способ ингибирования изоферментов фдэ4 d
GB9715584D0 (en) * 1997-07-23 1997-10-01 Eisai Co Ltd Compounds
UA67753C2 (uk) 1997-10-10 2004-07-15 Смітклайн Бічам Корпорейшн Спосіб отримання заміщених 4-феніл-4-ціанциклогексанових кислот
AR015966A1 (es) 1997-10-17 2001-05-30 Smithkline Beecham Corp Uso de un compuesto inhibidor de pde4 para la preparacion de un medicamento util para el tratamiento de prurito
MA24682A1 (fr) 1997-10-23 1999-07-01 Smithkline Beecham Corp Formes polymorphes nouvelles de cipamfylline, procede pour leur preparation et compositions les contenant
DE60103976T2 (de) * 2000-01-31 2005-07-21 Pfizer Products Inc., Groton Pyrimidinylcarboxamiden als inhibitoren der pde4 isoenzyme
BR0107964A (pt) * 2000-01-31 2002-10-29 Pfizer Prod Inc Derivados de nicotinamida benzofundida com heterociclica úteis como inibidores seletivos de isozimas pde4

Also Published As

Publication number Publication date
JP2004520386A (ja) 2004-07-08
HUP0400637A2 (hu) 2004-06-28
CZ20031895A3 (cs) 2004-08-18
US20020193612A1 (en) 2002-12-19
CN1518542A (zh) 2004-08-04
IS6846A (is) 2003-06-16
PL364135A1 (en) 2004-12-13
US6953810B2 (en) 2005-10-11
EA200300621A1 (ru) 2003-12-25
EE200300360A (et) 2003-12-15
IL156413A0 (en) 2004-01-04
MXPA03006887A (es) 2003-11-13
KR20030074761A (ko) 2003-09-19
SK8792003A3 (en) 2004-09-08
WO2002060875A8 (en) 2003-07-31
US6649633B2 (en) 2003-11-18
US20040048903A1 (en) 2004-03-11
BR0116852A (pt) 2004-02-25
BG108038A (en) 2004-07-30
OA12540A (en) 2006-06-05
ECSP034709A (es) 2003-09-24
CR7025A (es) 2003-11-25
EP1355884A1 (en) 2003-10-29
ZA200304894B (en) 2004-06-24
WO2002060875A1 (en) 2002-08-08
MA26983A1 (fr) 2004-12-20
NO20033397L (no) 2003-09-19
NZ526453A (en) 2005-01-28
CA2436535A1 (en) 2002-08-08
NO20033397D0 (no) 2003-07-30

Similar Documents

Publication Publication Date Title
ECSP034710A (es) Derivados biarilicos nicotinamida de utilidad como inhibidores de isozimas pde4
BG108039A (en) Thiazolyl-, oxazolyl-, pyrrolyl- and amidazolyl-acid amide derivatives useful as inhibitors of pde4 isozymes
AR027337A1 (es) Derivados de nicotinamida benzocondensada heterocicliclo utiles como inhibidores selectivos de las isozimas pde4.
DE602006007012D1 (de) Pyridinderivate als dipeptedyl-peptidase-hemmer
DK1585739T3 (da) Substituerede arylcyclopropylacetamider som glucokinaseaktivatorer
PE20091687A1 (es) Derivados de piridina o pirazina como inhibidores de cinasa-pi-3
MX2007005694A (es) Nuevos derivados de betulina, preparacion y uso de los mismos.
PE20050076A1 (es) Nuevos compuestos de isotiazol e isoxazol como inhibidores del factor de crecimiento transformador (tgf)
AR078833A1 (es) Derivados de heteroarilos que contienen nitrogeno como inhibidores dela cinasa jak3
CO5611127A2 (es) Derivados de indolilmaleimida
TW200616979A (en) Non-nucleoside reverse transcriptase inhibitors
MY144895A (en) Macrocylic inhibitors of hepatitis c virus
AR048641A1 (es) Compuestos de aril- o heteroarilamida ortosustituidos utiles como antago-nistas del receptor de prostaglandinas e2; composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicame
HRP20050688A2 (en) Pyrimidine derivatives for the prevention of hiv infection
ATE537830T1 (de) Nicotinamid derivate und ihre verwendung als therapeutika
NO20074641L (no) 1-Acetic Acid-Indole Derivatives with PGD2 Antagonist Activity
BR0213660A (pt) Composto, composição farmacêutica e método para tratar pacientes
AR055744A1 (es) Derivados de acido pirimidincarboxilico, su uso para preparar medicamentos y preparacion de dicjhos compuestos
EA200801134A1 (ru) Замещенные бициклические пиримидоновые производные
DK1751093T3 (da) Substituerede cyklohexyleddikesyre-derivater
DK1885187T3 (da) Fremgangsmåde til behandling af lægemiddelresistent cancer
ECSP045469A (es) El uso de cianopirrolidinas sustituidas y preparaciones de combinacion que las contienen para tratar hiperlipidemia y enfermedades asociadas
DK1745010T3 (da) Substituerede cyklohexyl-1,4-diaminderivater
ATE464296T1 (de) Selektive nichtsteroidale glucocorticoid-rezeptor-modulatoren
ATE386037T1 (de) Nicht-nucleosidische inhibitoren der reverse transkriptase