AR037232A1 - Uso de derivados tiazolilo 2,4,5-tri-substituidos para la manufactura de medicamentos, derivados de tiazol 2,4,5-tri-trisubstituidos, composiciones farmaceuticas que los comprenden, procedimiento para preparar dichas composiciones, intermediarios, procedimientos para preparar dichos derivados, y pro - Google Patents

Uso de derivados tiazolilo 2,4,5-tri-substituidos para la manufactura de medicamentos, derivados de tiazol 2,4,5-tri-trisubstituidos, composiciones farmaceuticas que los comprenden, procedimiento para preparar dichas composiciones, intermediarios, procedimientos para preparar dichos derivados, y pro

Info

Publication number
AR037232A1
AR037232A1 ARP020103035A ARP020103035A AR037232A1 AR 037232 A1 AR037232 A1 AR 037232A1 AR P020103035 A ARP020103035 A AR P020103035A AR P020103035 A ARP020103035 A AR P020103035A AR 037232 A1 AR037232 A1 AR 037232A1
Authority
AR
Argentina
Prior art keywords
alkyl
hydroxy
amino
mono
triazolyl
Prior art date
Application number
ARP020103035A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR037232A1 publication Critical patent/AR037232A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P1/04—Drugs 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
    • 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
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/08—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
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • 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
    • A61P31/20—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
    • A61P33/14—Ectoparasiticides, e.g. scabicides
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

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

Abstract

Uso de derivados de tiazol 2,4,5-trisustituidos de fórmula (1), un N-óxido, una sal de adición farmacéuticamente aceptable, una amina cuaternaria y una forma estereoquímicamente isomérica del mismo, donde: es halo; alquilo C1-6; alquilo C1-6 sustituido con hidroxi, carboxilo, ciano, amino, mono o di(alquilo C1-6)amino, aminocarbonilo, mono- o di(alquilo C1-6)aminocarbonilo; alquiloxicarbonilo C1-6 o alquiloxi C1-6; polihaloalquilo C1-4; alquiloxi C1-4, ciano, amino, aminocarbonilo, mono- o di(alquilo C1-6)aminocarbonilo, alquiloxicarbonilo C1-6, alquilcarboniloxi C1-6; H2N-S(=O)2-; mono- o di(alquilo C1-6)amino-S(=O)2; -C(=N-Rx)NRyRz; Rx es hidrógeno, alquilo C1-6, ciano, nitro o -S(=O)2-NH2; Ry es hidrógeno, alquilo C1-6, alquenilo C2-6 o alquinilo C2-6; Rz es hidrógeno o alquilo C1-6; es cicloalquilo C3-6, furanilo, tienilo, pirrolilo, oxazolilo, tiazolilo, imidazolilo, pirazolilo, isoxazolilo, isotiazolilo, oxadiazolilo, triazolilo, tiadiazolilo, fenilo, piridilo, pirimidinilo, pirazinilo, piridazinilo, benztiazolilo, benzoxazolilo, bencimidazolilo, indazolilo o imidazopiridilo, donde cada uno de dicho sistema de anillo puede estar opcionalmente sustituido hasta donde cada uno de dichos sustituyentes está independientemente seleccionado entre halo; hidroxi; ciano ; carboxilo; azido; amino; mono- o di(alquilo C1-6)amino; alquilcarbonilamino C1-6; alquilo C1-6; alquenilo C2-6; alquinilo C2-6; cicloalquilo C3-6; alquilo C1-6 sustituido con hidroxi, alquiloxi C1-6, amino, mono- o di(alquilo C1-4)amino; alquiloxi C1-6; alquiltio C1-6; alquilcarbonilo C1-6; alquiloxicarbonilo C1-6; arilalquiloxi C1-6; ariloxi; polihaloalquilo C1-6; polihaloalquiloxi C1-6; polihaloalquilcarbonilo C1-6; alquilo C1-4 -S(=O)n- o R1NH-S(=O)n-, donde R1 representa hidrógeno, o un radical de la fórmula (2), donde A es O, S o un radical bivalente de fórmula -CR2=N- con CR2 adherido a N de fórmula (2); y R2 es hidrógeno, alquilo C1-6 o alquiloxi C1-6; o Q es un radical de fórmulas (3), en la cual B1 y B2 son cada uno independientemente O, NR3, CH2 ó S, donde R3 es hidrógeno o alquilo C1-4; B3 es O ó NR4 es hidrógeno o alquilo C1-4; q es un número entero con un valor de 1 a 4; r es un número entero con un valor de 1 a 3; n es un número entero con un valor de 1 ó 2; L es fenilo sustituido con hasta 4 sustituyentes, estando cada sustituyente independientemente seleccionado entre alquiloxicarbonilo C1-6; alquilcarboniloxi C1-6; aminocarbonilo; mono- o di(alquilo C1-6)aminocarbonilo; alquilo C1-6-C(=O)-NH-; alquiloxi C1-6-C(=O)-NH-; H2N-C(=O)-NH-; mono- o di(alquilo C1-4)amino-C(=O)-NH-; Het-NH-; Het1 -NH-; -NH-C(=N-Rx)NRyRz; -C(=N-Rx)NRyRz; Het1; o un radical de fórmula (4): -X-C1-Y1-C2-Y2-C3-Y3-C4-Z, donde X representa NR5, O, S o un enlace directo; C1, C2, C3 y C4 representan cada uno independientemente alcanodiilo C1-6, alquenodiilo C2-6, alquinodiilo C2-6 o un enlace directo; Y1, Y2 y Y3 representan cada uno independientemente NR5, O, S o un enlace directo; Z es hidrógeno, halo, ciano, hidroxi, carboxilo, -P(=O)(OH)H, -P(=O)(OH)2, -P(=O)(OH)CH3, -P(=O)(OH)(OCH3), -P(=O)(OH)(OCH2CH3), -P(=O)(OH)NH2, -S(=O)2H, -S(=O)2(OH),-S(=O)2NH, -C(=O)-NH-S(=O)2-H, tetrazolilo, 3-hidroxi-isotiazolilo, 3-hidroxi-isoxazolilo, 3-hidroxi-tiadiazolilo, mercaptotetrazolilo, 3-mercapto-triazolilo, 3-sulfinil-triazolilo, 3-sulfonil-triazolilo; R5 es hidrógeno, alquilo C1-6 o -C(=NH)-N(Rz)2; y donde de 1 a 3 átomos de hidrógeno de los grupos alquilo C1-6, alcanodiilo C1-6 alquenodiilo C2-6 o alquinodiilo C2-6 en las definiciones de R5 y el radical de fórmula (4) pueden estar opcionalmente cada uno independientemente reemplazados con halo, hidroxi, carboxilo, -P(=O)(OH)H, -P(=O)(OH)2, -P(=O)(OH)CH3, -P(=O)(OH)(OCH3), -P(=O)(OH)(OCH2CH3), -P(=O)(OH)NH2, -S(=O)2H, -S(=O)2(OH),-S(=O)2NH, -C(=O)-NH-S(=O)2-H, tetrazolilo, 3-hidroxi-isotiazolilo, 3-hidroxi-isoxazolilo, 3-hidroxi-tiadiazolilo, mercaptotetrazolilo, 3-mercapto-triazolilo, 3-sulfinil-triazolilo, 3-sulfonil-triazolilo; o L es un heterociclo monocíclico de 5 o 6 miembros parcialmente saturado o aromático o un heterociclo bicíclico parcialmente saturado o aromático donde cada uno de dichos sistemas de anillo puede estar opcionalmente sustituido con hasta 3 sustituyentes, estando cada uno de dichos sustituyentes independientemente seleccionado entre alquiloxicarbonilo C1-6, alquilcarboniloxi C1-6, aminocarbonilo, mono- o di(alquilo C1-6)aminocarbonilo, alquilo C1-6-C(=O)-NH-; alquiloxi C1-6-C(=O)-NH-, H2N-C(=O)-NH-; mono- o di(alquilo C1-4)amino-C(=O)-NH-, Het-NH-, Het1-NH-, -NH-C(=N-Rx)NRyRz, -C(=N-Rx)NRyRz, Het1, o un radical de fórmula -X-C1-Y1-C2-Y2-C3-Y3-C4-Z (4) donde X representa NR5, O, S o un enlace directo; C1, C2, C3 y C4 representan cada uno independientemente alcanodiilo C1-6, alquenodiilo C2-6, Y1, Y2, Y3 representan cada uno independientemente NR5, O, y S ó un enlace directo Z es hidrógeno, halo, ciano, hidroxi, carboxilo, -P(=O)(OH)H, -P(=O)(OH)2, -P(=O)(OH)CH3, -P(=O)(OH)(OCH3), -P(=O)(OH)(OCH2CH3), -P(=O)(OH)NH2, -S(=O)2H, -S(=O)2(OH),-S(=O)2NH, -C(=O)-NH-S(=O)2-H, tetrazolilo, 3-hidroxi-isotiazolilo, 3-hidroxi-isoxazolilo, 3-hidroxi-tiadiazolilo, mercaptotetrazolilo, 3-mercapto-triazolilo, 3-sulfinil-triazolilo, 3-sulfonil-triazolilo; R5 es hidrógeno, alquilo C1-6 o -C(=NH)-N(Rz)2; y donde de 1 a 3 átomos de hidrógeno de los grupos alquilo C1-6, alcanodiilo C1-6, alcanodiilo C2-6 o alquinodiilo C2-6 en las definiciones de R5 y el radical de fórmulas (4) pueden estar opcionalmente cada uno independientemente reemplazados con halo, hidroxi, carboxilo, P(=O)(OH)H, -P(=O)(OH)2, -P(=O)(OH)CH3, -P(=O)(OH)(OCH3), -P(=O)(OH)(OCH2CH3), -P(=O)(OH)NH2, -S(=O)2H, -S(=O)2(OH),-S(=O)2NH, -C(=O)-NH-S(=O)2-H, tetrazolilo, 3-hidroxi-isotiazolilo, 3-hidroxi-isoxazolilo, 3-hidroxi-tiadiazolilo, mercaptotetrazolilo, 3-mercapto-triazolilo, 3-sulfinil-triazolilo, 3-sulfonil-triazolilo; Het es un heterociclo monocíclico de 5 o 6 miembros parcialmente saturado o aromático o un heterociclo bicíclico parcialmente saturado o aromático donde cada uno de dichos sistemas de anillo pueden estar opcionalmente sustituidos con hasta 3 sustituyentes, estando cada sustituyente independientemente seleccionados entre halo, hidroxi, amino, ciano, carboxilo, mono- o di(alquilo C1-6)amino, alquilo C1-6, alquilo C1-6 sustituido con hidroxi o alcoxi C1-4 o amino o mono- o di(alquilo C1-4)amino, polihaloalquilo C1-6, alquiloxi C1-6, alquiltio C1-6, alquiloxicarbonilo C1-6, alquilcarboniloxi C1-6, aminocarbonilo, mono- o di(alquilo C1-6)aminocarbonilo, alquilo C1-6-C(=O)-NH-, alquiloxi C1-6-C(=O)-NH-, H2N-C(=O)-NH- o mono- o di(alquilo C1-4)amino-C(=O)-NH-, Het1 es un heterociclo de 6 miembros saturado seleccionado entre piperidinilo, morfolinilo, tiomorfolinilo, piperazinilo, donde cada uno de dichos heterociclos saturados de 6 miembros puede estar opcionalmente sustituido con amino o alquilo C1-4 opcionalmente sustituido con arilo; arilo es fenilo, opcionalmente sustituido con hasta cinco sustituyentes cada uno independientemente seleccionado entre halo, hidroxi, alquilo C1-6, polihaloalquilo C1-6, alquiloxi C1-6, alquiltio C1-6, ciano, nitro, amino, mono- o di(alquilo C1-6)amino, para la manufactura de medicamentos para la prevención o tratamiento de enfermedades intermediarias a través de TNF-a (Factor a de Necrosis Tumoral) y/o IL-12 (interleuquina 12), que comprenden enfermedades inflamatorias o enfermedades autoinmunes como por ejemplo: artritis reumatoide, enfermedad de Crohn, enfermedad de intestino irritable, colitis, psoriasis o esclerosis múltiple. También se dan a conocer: derivados de tiazol 2,4,5-trisustituidos, composiciones farmacéuticas que los comprenden, un procedimiento para preparar dichas composiciones, intermediarios, procedimientos para preparar dichos derivados, y productos que contienen dichos derivados.
ARP020103035A 2001-08-13 2002-08-12 Uso de derivados tiazolilo 2,4,5-tri-substituidos para la manufactura de medicamentos, derivados de tiazol 2,4,5-tri-trisubstituidos, composiciones farmaceuticas que los comprenden, procedimiento para preparar dichas composiciones, intermediarios, procedimientos para preparar dichos derivados, y pro AR037232A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP01203088 2001-08-13

Publications (1)

Publication Number Publication Date
AR037232A1 true AR037232A1 (es) 2004-11-03

Family

ID=8180791

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020103035A AR037232A1 (es) 2001-08-13 2002-08-12 Uso de derivados tiazolilo 2,4,5-tri-substituidos para la manufactura de medicamentos, derivados de tiazol 2,4,5-tri-trisubstituidos, composiciones farmaceuticas que los comprenden, procedimiento para preparar dichas composiciones, intermediarios, procedimientos para preparar dichos derivados, y pro

Country Status (26)

Country Link
US (1) US7138403B2 (es)
EP (1) EP1418911B1 (es)
JP (1) JP4491231B2 (es)
KR (1) KR100922538B1 (es)
CN (1) CN100502863C (es)
AR (1) AR037232A1 (es)
AT (1) ATE325608T1 (es)
AU (1) AU2002331227B2 (es)
BR (1) BR0211910A (es)
CA (1) CA2451981C (es)
DE (1) DE60211348T2 (es)
EA (1) EA007933B1 (es)
ES (1) ES2264734T3 (es)
HK (1) HK1077507A1 (es)
HR (1) HRP20040098B1 (es)
HU (1) HUP0401160A3 (es)
IL (2) IL160327A0 (es)
MX (1) MXPA04001400A (es)
MY (1) MY130780A (es)
NO (1) NO327345B1 (es)
NZ (1) NZ530772A (es)
PL (1) PL210475B1 (es)
TW (1) TWI268152B (es)
UA (1) UA79756C2 (es)
WO (1) WO2003015776A1 (es)
ZA (1) ZA200401164B (es)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003247959B2 (en) * 2002-07-09 2010-07-29 Vertex Pharmaceuticals Incorporated Imidazoles, oxazoles and thiazoles with protein kinase inhibiting activities
PA8578101A1 (es) * 2002-08-13 2004-05-07 Warner Lambert Co Derivados de heterobiarilo como inhibidores de metaloproteinasa de la matriz
GB0308466D0 (en) 2003-04-11 2003-05-21 Novartis Ag Organic compounds
US7560568B2 (en) 2004-01-28 2009-07-14 Smithkline Beecham Corporation Thiazole compounds
WO2006038734A1 (en) * 2004-10-08 2006-04-13 Astellas Pharma Inc. Pyridazinone derivatives cytokines inhibitors
EP1802588A4 (en) * 2004-10-15 2010-02-17 Astrazeneca Ab SUBSTITUTED AMINOPYRIMIDONE AND APPLICATIONS THEREOF
JP2008516945A (ja) * 2004-10-15 2008-05-22 アストラゼネカ・アクチエボラーグ 置換されたアミノ化合物およびそれらの使用
JP2008531537A (ja) * 2005-02-25 2008-08-14 クドス ファーマシューティカルズ リミテッド 化合物
EP1932840B1 (en) * 2005-10-03 2014-04-09 Ono Pharmaceutical Co., Ltd. Nitrogen-containing heterocyclic compound and pharmaceutical application thereof
KR20100092473A (ko) * 2007-11-01 2010-08-20 액테리온 파마슈티칼 리미티드 신규한 피리미딘 유도체
JP5581219B2 (ja) 2008-01-25 2014-08-27 ミレニアム ファーマシューティカルズ， インコーポレイテッド チオフェンおよびホスファチジルイノシトール３−キナーゼ（ｐｉ３ｋ）阻害薬としてのその使用
TWI403506B (zh) * 2008-06-16 2013-08-01 Faes Farma Sa 用於治療急性和慢性發炎疾病之５－（４－甲磺醯基－苯基）－噻唑衍生物類
JP5681105B2 (ja) 2008-07-17 2015-03-04 バイエル・クロップサイエンス・アーゲーＢａｙｅｒ Ｃｒｏｐｓｃｉｅｎｃｅ Ａｇ 殺害虫剤として使用されるヘテロ環式化合物
NZ592297A (en) * 2008-09-22 2012-11-30 Cayman Chemical Co Inc 2-Aryl-5-heteroaryl pyridine and pyrimidine derivatives as pharmaceutical active agents
US8314130B2 (en) 2008-10-01 2012-11-20 Synta Pharmaceuticals Corp. Compounds inclunding substituted pyridines for inflammation and immune-related uses
CN101391984B (zh) * 2008-11-07 2010-12-08 东华大学 碳酸二甲酯对含巯基的嘧啶杂环化合物进行甲基化的方法
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9139589B2 (en) 2009-01-30 2015-09-22 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9090601B2 (en) * 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
BR112012028280A2 (pt) 2010-05-05 2015-09-15 Bayer Ip Gmbh derivados de tiazole como pesticidas
WO2012021611A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2012021696A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US8859768B2 (en) 2010-08-11 2014-10-14 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
CN103237450A (zh) 2010-10-13 2013-08-07 米伦纽姆医药公司 杂芳基化合物和其用途
US20120129843A1 (en) * 2010-11-18 2012-05-24 Yan Zhang Pyridyl-thiazolyl inhibitors of pro-matrix metalloproteinase activation
WO2012109573A1 (en) * 2011-02-11 2012-08-16 Purdue Research Foundation Substituted thiazoles for use as antiviral agents
GEP201706748B (en) 2012-08-10 2017-10-10 Boehringer Ingelheim Int Heteroaromatic compounds as bruton's tyrosine kinase (btk) inhibitors
US20150284380A1 (en) * 2012-10-31 2015-10-08 Bayer Cropscience Ag Novel heterocyclic compounds as pest control agents
BR112015011497B1 (pt) 2012-11-27 2023-01-10 Thomas Helledays Stiftelse För Medicinsk Forskning Composto, e, formulação farmacêutica
JP6486954B2 (ja) 2014-01-29 2019-03-20 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｂｔｋ阻害剤としてのピラゾール化合物
CA2948601A1 (en) 2014-06-04 2015-12-10 Thomas Helledays Stiftelse For Medicinsk Forskning Mth1 inhibitors for treatment of inflammatory and autoimmune conditions
WO2015187088A1 (en) 2014-06-04 2015-12-10 Thomas Helledays Stiftelse För Medicinsk Forskning Mth1 inhibitors for treatment of cancer
JOP20200117A1 (ar) 2014-10-30 2017-06-16 Janssen Pharmaceutica Nv كحولات ثلاثي فلوروميثيل كمُعدلات للمستقبل النووي جاما تي المرتبط بحمض الريتيونَويك ROR?t
HUE046888T2 (hu) * 2014-10-30 2020-03-30 Janssen Pharmaceutica Nv Amid-szubsztituált tiazolok mint ROR-gamma-t modulátorok
ES2708025T3 (es) * 2014-10-30 2019-04-08 Janssen Pharmaceutica Nv Tiazoles como moduladores de RORyt
SI3390390T1 (sl) 2015-12-16 2021-12-31 Boehringer Ingelheim International Gmbh Bipirazolilni derivati, uporabni za zdravljenje avtoimunskih bolezni
WO2017123695A1 (en) 2016-01-13 2017-07-20 Boehringer Ingelheim International Gmbh Isoquinolones as btk inhibitors
TW201803869A (zh) 2016-04-27 2018-02-01 健生藥品公司 作為ＲＯＲγＴ調節劑之６－胺基吡啶－３－基噻唑
US10414759B2 (en) * 2017-05-08 2019-09-17 Purdue Research Foundation Phenylthiazoles and uses thereof
ES2929140T3 (es) 2018-06-18 2022-11-25 Janssen Pharmaceutica Nv Imidazoles sustituidos con fenilo y piridinilo como moduladores de RORgammat
CN112566901A (zh) 2018-06-18 2021-03-26 詹森药业有限公司 作为RORγt的调节剂的苯基取代的吡唑类
WO2019244001A1 (en) 2018-06-18 2019-12-26 Janssen Pharmaceutica Nv 6-aminopyridin-3-yl pyrazoles as modulators of roryt
EP3807261B1 (en) 2018-06-18 2022-07-13 Janssen Pharmaceutica NV Pyridinyl pyrazoles as modulators of roryt
CN110746325A (zh) * 2018-07-24 2020-02-04 上海和辉光电有限公司 一种基于胍骨架的n型掺杂化合物及其应用
CN110452224B (zh) * 2019-08-30 2022-06-03 西南大学 嘧啶唑醇类化合物及其制备方法和应用
WO2022155941A1 (en) * 2021-01-25 2022-07-28 Qilu Regor Therapeutics Inc. Cdk2 inhibitors

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE258165C (es)
US3499762A (en) 1966-11-03 1970-03-10 Eastman Kodak Co Photographic elements comprising novel u.v.-absorbing optical brightening agents
DE1959307A1 (de) 1969-11-26 1971-06-03 Basf Ag Optische Aufheller
BE795907A (fr) * 1972-02-25 1973-06-18 Luso Farmaco Inst 2-amino-4-arylthiazoles 5-substitues et leur preparation
US4649146A (en) 1983-01-31 1987-03-10 Fujisawa Pharmaceutical Co., Ltd. Thiazole derivatives and pharmaceutical composition comprising the same
JPH03144612A (ja) 1989-10-31 1991-06-20 Nec Corp 接続方法
JPH04368375A (ja) * 1991-06-17 1992-12-21 Otsuka Pharmaceut Factory Inc イソオキサゾール誘導体
US5240929A (en) * 1992-08-03 1993-08-31 Warner-Lambert Company 2-heterocyclic-5-hydroxy-1,3-pyrimidines useful as antiinflammatory agents
JPH10504542A (ja) * 1994-07-27 1998-05-06 ジー．ディー．サール アンド カンパニー 炎症処置用の置換チアゾール化合物
JPH10507205A (ja) 1995-08-02 1998-07-14 ホータ．ウリアッヒ イ シイア．エセ．アー． 抗真菌活性を有する新規カルボンアミド
AR008395A1 (es) * 1996-07-09 2000-01-19 Astra Pharma Prod Compuesto derivado de pirimidina, composicion farmaceutica que lo comprende, procedimiento para prepararlo, y compuesto intermediario util parallevar a cabo dicho procedimiento.
EP0920426B9 (de) 1996-08-26 2005-04-06 ALTANA Pharma AG Neue thiazol-derivate mit phosphodiesterase inhibierender wirkung
AU4015497A (en) 1996-08-26 1998-03-19 Byk Gulden Lomberg Chemische Fabrik Gmbh Thiazole derivatives useful as selective inhibitors of pde-iv
WO2000035911A1 (en) * 1998-12-16 2000-06-22 Aventis Pharma Limited Heteroaryl-cyclic acetals
DE10001644A1 (de) * 1999-01-19 2000-07-20 Clariant Gmbh Fluorierte Azole und ihre Verwendung in flüssigkristallinen Mischungen
DE60024480T2 (de) 1999-10-27 2006-07-27 Novartis Ag Thiazol und imidazo[4,5-b]pyridin verbindungen und ihre verwendung als pharmazeutika
CN1230166C (zh) * 2000-01-18 2005-12-07 沃泰克斯药物股份有限公司 回旋酶抑制剂及其用途
AU3740101A (en) 2000-03-01 2001-09-12 Janssen Pharmaceutica Nv 2,4-disubstituted thiazolyl derivatives
HUP0300382A3 (en) * 2000-03-29 2006-11-28 Cyclacel Ltd 2-substituted 4-heteroaryl-pyrimidines and their use in the treatmetn of proliferative disorders and pharmaceutical compositions containing the compounds
JP2004517100A (ja) * 2000-12-20 2004-06-10 グラクソ　グループ　リミテッド ｈＰＰＡＲアルファアゴニストとしての置換オキサゾールおよびチアゾール
GB0031103D0 (en) * 2000-12-20 2001-01-31 Glaxo Group Ltd Chemical compounds
GB0031109D0 (en) * 2000-12-20 2001-01-31 Glaxo Group Ltd Chemical compounds
GB0031107D0 (en) * 2000-12-20 2001-01-31 Glaxo Group Ltd Chemical compounds

Also Published As

Publication number Publication date
DE60211348D1 (de) 2006-06-14
MY130780A (en) 2007-07-31
ES2264734T3 (es) 2007-01-16
US7138403B2 (en) 2006-11-21
EP1418911B1 (en) 2006-05-10
CA2451981C (en) 2012-02-21
AU2002331227B2 (en) 2008-01-24
ATE325608T1 (de) 2006-06-15
KR100922538B1 (ko) 2009-10-21
HK1077507A1 (en) 2006-02-17
PL210475B1 (pl) 2012-01-31
HRP20040098B1 (en) 2012-08-31
EA200400305A1 (ru) 2004-08-26
EP1418911A1 (en) 2004-05-19
IL160327A0 (en) 2004-07-25
ZA200401164B (en) 2005-07-27
NO20040631L (no) 2004-03-12
JP4491231B2 (ja) 2010-06-30
CN100502863C (zh) 2009-06-24
BR0211910A (pt) 2004-10-19
DE60211348T2 (de) 2007-02-08
HUP0401160A2 (hu) 2004-09-28
KR20040043134A (ko) 2004-05-22
CA2451981A1 (en) 2003-02-27
NO327345B1 (no) 2009-06-15
MXPA04001400A (es) 2004-05-27
IL160327A (en) 2010-05-17
JP2005504767A (ja) 2005-02-17
EA007933B1 (ru) 2007-02-27
TWI268152B (en) 2006-12-11
US20040254192A1 (en) 2004-12-16
HUP0401160A3 (en) 2008-01-28
PL368241A1 (en) 2005-03-21
UA79756C2 (en) 2007-07-25
HRP20040098A2 (en) 2004-06-30
NZ530772A (en) 2006-03-31
CN1633294A (zh) 2005-06-29
WO2003015776A1 (en) 2003-02-27

Similar Documents

Publication Publication Date Title
AR037232A1 (es) Uso de derivados tiazolilo 2,4,5-tri-substituidos para la manufactura de medicamentos, derivados de tiazol 2,4,5-tri-trisubstituidos, composiciones farmaceuticas que los comprenden, procedimiento para preparar dichas composiciones, intermediarios, procedimientos para preparar dichos derivados, y pro
CA2844054C (en) Inhibitors of influenza viruses replication
DK1442019T3 (da) Amidderivater som glycogensynthasekinase 3- beta-inhibitorer
PE20220931A1 (es) Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina
AR030553A1 (es) Uso de derivados de tiazolilo 2,4-disustituidos para la fabricacion de un medicamento para la prevencion o el tratamiento de enfermedades mediadas a traves de citoquinas, derivados de tiazolilo 2,4-disustituidos, composiciones farmaceuticas que los comprenden, procesos para preparar dichos derivados
AR057979A1 (es) PIRAZOLPIRIMIDINAS COMO INHIBIDORAS DE PROTEíNA QUINASA. COMPOSICIONES FARMACEUTICAS.
MX2009005449A (es) Compuesto heteromonociclico y uso del mismo.
AR048316A1 (es) Aril piperidinas o piperazinas sustituidas con heterociclos de cinco miembros inhibidoras de la mtp, metodos para su preparacion, composiciones farmaceuticas que las contienen y su uso en la fabricacion de medicamentos para el tratamiento de trastornos del metabolismo.
AR053784A1 (es) Compuestos y derivados tetrazolicos de dibencil amina. composiciones farmaceuticas.
CO6241157A2 (es) "derivados de 6-(pirrolidin-3-il)-1h-pirazolo{3,4-d}pirimidin-4(5h)-ona utiles como inhibidores de pde9"
AR063680A1 (es) Derivados de pirazolo[1, 5-a]pirimidina, metodos e intermediario para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion de mglur5.
AR036106A1 (es) Compuestos azaindoles inhibidores de quinasa selectivos, composiciones farmaceuticas y el uso de dicha composicion para la fabricacion de un medicamento
NO20041911L (no) Heteroarylaminer som glykogensyntase-kinase 3beta-inhibitorer (GSK3-inhibitorer)
AR099511A1 (es) Derivados del ácido piridin-3-ilacético como inhibidores de la replicación del virus de inmunodeficiencia humana
MX2020005874A (es) Acidos carbamoil ciclohexilicos n-enlazados a pirazol como antagonistas de receptores del acido lisofosfatidico (lpa).
AR050189A1 (es) Derivados sustituidos de propenil piperazina como inhibidores de histona desacetilasa
BR122015023612B8 (pt) compostos derivados de pirimidina, seu uso, composição farmacêutica e produto
EA200400616A1 (ru) ПРОИЗВОДНЫЕ АМИНОБЕНЗАМИДОВ В КАЧЕСТВЕ ИНГИБИТОРОВ ГЛИКОГЕНСИНТАЗА-КИНАЗЫ 3β
JP2012522759A (ja) イミダゾ［２，１−ｂ］［１，３，４］チアジアゾール誘導体
AR071314A1 (es) Antagonistas de receptor de cgrp
MX2019012945A (es) Formas cristalinas de un compuesto inhibidor de jak.
TW200626605A (en) Novel bis-azaindole derivatives, their preparation and their pharmaceutical use as kinase inhibitors
NO20082975L (no) Nye cykliske ureaderivater, fremstilling derav og farmasoytisk anvendelse derav som kinaseinhibitorer
AR066154A1 (es) Derivados de piperidina / piperazina
PH12018500294A1 (en) 5-(n-benzyl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication

Legal Events

Date Code Title Description
FG Grant, registration
FG Grant, registration