HRP20160118T1 - HETEROCIKLIÄŚKI DERIVAT KAO INHIBITOR MIKROSOMSKIH SINTAZA PROSTAGLANDINA E (mPGEs) - Google Patents

HETEROCIKLIÄŚKI DERIVAT KAO INHIBITOR MIKROSOMSKIH SINTAZA PROSTAGLANDINA E (mPGEs) Download PDF

Info

Publication number
HRP20160118T1
HRP20160118T1 HRP20160118TT HRP20160118T HRP20160118T1 HR P20160118 T1 HRP20160118 T1 HR P20160118T1 HR P20160118T T HRP20160118T T HR P20160118TT HR P20160118 T HRP20160118 T HR P20160118T HR P20160118 T1 HRP20160118 T1 HR P20160118T1
Authority
HR
Croatia
Prior art keywords
amino
carbonyl
carboxamide
chloro
benzimidazole
Prior art date
Application number
HRP20160118TT
Other languages
English (en)
Inventor
Hironori Otsu
Original Assignee
Nippon Shinyaku Co., Ltd.
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 Nippon Shinyaku Co., Ltd. filed Critical Nippon Shinyaku Co., Ltd.
Publication of HRP20160118T1 publication Critical patent/HRP20160118T1/hr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
    • 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
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • 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
    • A61K31/433—Thidiazoles
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/04—Drugs for genital or sexual disorders; Contraceptives for inducing labour or abortion; Uterotonics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06—Antiabortive agents; Labour repressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P19/06—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
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • 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
    • 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
    • A61P31/10—Antimycotics
    • 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
    • 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
    • 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
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P9/10—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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/10—Radicals substituted by halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/12—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/14—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/16—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/26—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/12—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 linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Tropical Medicine & Parasitology (AREA)

Claims (13)

1. Heterociklički derivat, naznačen time što ga prikazuje opća formula [1]: [image] , ili njegov tautomer ili njegova farmaceutski prihvatljiva sol, gdje je prsten A skupina koju prikazuju opće formule [2], [3] ili [4]: [image] , gdje X1 je NH, N-alkil, ili O; A1 je vodik ili alkil; A2 je i) vodik; ii) halogen; iii) alkil, izborno supstituiran s jednom do tri skupine, koje se bira iz skupine koju čine halogen, amino, monoalkilamino, dialkilamino, karbamoil, monoalkilaminokarbonil, dialkilaminokarbonil, zasićeni ciklički aminokarbonil, alkoksi, alkoksialkoksi i alkilkarboniloksi; iv) cikloalkil, izborno supstituiran s alkilom, izborno supstituiranim s jednim do tri halogena; v) alkoksi; vi) zasićena heterociklička skupina, izborno supstituirana s alkilom, alkiloksikarbonilom, alkilkarbonilom ili okso; vii) alkiltio; viii) alkilsulfonil; ix) alkilsulfinil; x) skupina s općom formulom [5]: [image] , gdje R3 i R4 su iste ili različite skupine, koje se bira između a) vodika, b) alkila, izborno supstituiranog sa skupinom koju se bira iz skupine koju čine monoalkilamino, dialkilamino, zasićeni ciklički amino, izborno supstituiran s alkilom, a zasićena heterociklička skupina, izborno supstituirana s alkilom, alkoksi, hidroksikarbonil, hidroksil, alkiloksikarbonil i alkiltio, ili c) cikloalkila; ili xi) zasićeni ciklički amino, izborno supstituiran s alkilom, amino, monoalkilamino, dialkilamino, alkoksi ili hidroksilom; R1 je fenil, benzil, naftil, cikloalkil, cikloalkilmetil, heteroaril, heteroarilmetil, 1,2,3,4-tetrahidronaftalen-5-il, 1,2,3,4-tetrahidronaftalen-6-il, 2,3-dihidro-1H-inden-4-il, 2,3-dihidro-1H-inden-5-il, 1,2-dihidrociklobutabenzen-3-il, 1,2-dihidrociklobutabenzen-4-il ili alkil, gdje su navedeni fenil, benzil, cikloalkil, cikloalkilmetil, heteroaril i heteroarilmetil izborno supstituirani s jednom do tri skupine, koje se bira iz skupine koju čine i) halogen, ii) alkil, izborno supstituiran s jednom do tri skupine, koje se bira iz skupine koju čine halogen, hidroksi i fenil, iii) alkoksi, iv) hidroksi, i v) cijano; R2 je fenil ili piridil, gdje su navedenii fenil i piridil izborno supstituirani s jednom do tri skupine, koje se bira iz skupine koju čine i) halogen, ii) alkilsulfonil, iii) alkoksi izborno supstituiran s jednim do tri halogena ili alkoksi; iv) alkinil, izborno supstituiran s alkoksialkilom ili cikloalkilom, i v) alkil, izborno supstituiran s jednom do tri skupine, koje se bira iz skupine koju čine alkoksi, alkoksialkoksi, cikloalkil, fenil i halogen.
2. Heterociklički derivat u skladu s patentnim zahtjevom 1, naznačen time što je prsten A skupina s formulom [4], a X1 je NH, ili njegov tautomer ili njegova farmaceutski prihvatljiva sol.
3. Heterociklički derivat u skladu s patentnim zahtjevom 1, naznačen time što je R1 fenil, 1,2,3,4-tetrahidronaftalen-5-il, 1,2,3,4-tetrahidronaftalen-6-il, 2,3-dihidro-1H-inden-4-il, 2,3-dihidro-1H-inden-5-il, 1,2-dihidrociklobutabenzen-3-il ili 1,2-dihidrociklobutabenzen-4-il, gdje je navedeni fenil izborno supstituiran s jednom do tri skupine, koje se bira iz skupine koju čine i) halogen, ii) alkil, izborno supstituiran s jednim do tri halogena, iii) alkoksi, i iv) cijano, ili njegov tautomer ili njegova farmaceutski prihvatljiva sol.
4. Heterociklički derivat u skladu s patentnim zahtjevom 1, naznačen time što je R2 fenil, gdje je navedeni fenil izborno supstituiran s jednom do tri skupine, koje se bira iz skupine koju čine i) halogen, ii) alkilsulfonil, iii) alkoksi izborno supstituiran s alkoksi, iv) alkinil, izborno supstituiran s alkoksialkilom ili cikloalkilom, i v) alkil, izborno supstituiran s jednom do tri skupine, koje se bira iz skupine koju čine halogen, alkoksi, alkoksialkoksi, cikloalkil i fenil, ili njegov tautomer ili njegova farmaceutski prihvatljiva sol.
5. Heterociklički derivat u skladu s patentnim zahtjevom 1, naznačen time što prsten A je skupina s formulom [4], X1 je NH, A2 je i) vodik, ii) alkil, izborno supstituiran sa skupinom koju se bira iz skupine koju čine halogen, monoalkilamino, dialkilamino, monoalkilaminokarbonil, dialkilaminokarbonil, zasićeni ciklički aminokarbonil, alkoksi, alkoksialkoksi i alkilkarboniloksi, iii) cikloalkil, izborno supstituiran s alkilom, izborno supstituiranim s jednim do tri halogena, iv) alkoksi, v) zasićena heterociklička skupina, izborno supstituirana s alkilom ili alkiloksikarbonilom, vi) alkiltio, vii) alkilsulfonil, viii) alkilsulfinil, ix) amino supstituiran s alkilom, gdje je navedeni alkil izborno supstituiran sa skupinom koju se bira iz skupine koju čine monoalkilamino, dialkilamino, zasićeni ciklički amino, izborno supstituiran s alkilom, tetrahidrofurilom, morfolino, alkoksi, hidroksikarbonilom, hidroksilom i alkiltio, x) amino supstituiran s cikloalkilom ili xi) zasićeni ciklički amino, izborno supstituiran s alkilom, dialkilamino, alkoksi ili hidroksilom, i R1 je i) fenil, izborno supstituiran s jednom do tri skupine, koje se bira iz skupine koju čine halogen, alkil, izborno supstituiran s jednim do tri halogena, alkoksi i cijano, ii) 1,2,3,4-tetrahidronaftalen-5-il, iii) 2,3-dihidro-1H-inden-5-il, iv) benzil, izborno supstituiran s halogenom ili alkilom, izborno supstituiranim s jednim do tri halogena, v) cikloalkil, vi) cikloalkilmetil, vii) naftil, viii) piridilmetil, izborno supstituiran s alkilom, izborno supstituiranim s jednim do tri halogena, ix) tienil, x) tienilmetil, xi) benzotiazolil, xii) benzotiadiazolil, xiii) indolil ili xiv) alkil, i R2 je fenil ili piridil, gdje je navedeni fenil izborno supstituiran s jednom do tri skupine, koje se bira iz skupine koju čine i) halogen, ii) alkilsulfonil, iii) alkoksi izborno supstituiran s alkoksi, iv) alkinil, izborno supstituiran s alkoksialkilom ili cikloalkilom, i v) alkil, izborno supstituiran s jednom do tri skupine, koje se bira iz skupine koju čine halogen, alkoksi, alkoksialkoksi, cikloalkil i fenil, i navedeni piridil je izborno supstituiran s halogenom, ili njegov tautomer ili njegova farmaceutski prihvatljiva sol.
6. Heterociklički derivat u skladu s patentnim zahtjevom 1, naznačen time što prsten A je skupina s formulom [4], X1 je NH, A2 je alkil supstituiran s alkoksi, dialkilamino, tetrahidrofurilom, tetrahidrofurilmetilom, alkoksialkilamino, ili cikloalkil, izborno supstituiran s alkilom, izborno supstituiranim s jednim do tri halogena, R1 je fenil supstituiran s jednim halogenom i jednim metilom, i R2 je fenil, izborno supstituiran s jednim trifluormetilom ili dva halogena, ili njegov tautomer ili njegova farmaceutski prihvatljiva sol.
7. Heterociklički derivat u skladu s patentnim zahtjevom 1, naznačen time što se bira između sljedećih (1)-(239), ili njihovih tautomera ili njihovih farmaceutski prihvatljivih soli: (1) N-[2-(trifluormetil)benzil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (2) N-cikloheksil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (3) N-(3-klor-2-metilfenil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (4) N-[(1-hidroksicikloheksil)metil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (5) N-[2-(trifluormetil)benzil]-5-({[2-(trifluormetil)fenil]karbonil}amino}-2,3-dihidro-1-benzofuran-7-karboksamida), (6) N-cikloheksil-5-({[2-(trifluormetil)fenil]karbonil}amino)-2,3-dihidro-1-benzofuran-7-karboksamida, (7) N-(3-klor-2-metilfenil)-5-({[2-(trifluormetil)fenil]karbonil}amino)-2,3-dihidro-1-benzofuran-7-karboksamida, (8) N-cikloheksil-5-({[2-(trifluormetil)fenil]karbonil}amino)-1H-indazol-7-karboksamida, (9) N-[2-(trifluormetil)benzil]-5-({[2-(trifluormetil)fenil]karbonil}amino)-1H-indazol-7-karboksamida, (10) N-(3-klor-2-metilfenil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (11) 2-metil-N-[2-(trifluormetil)benzil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (12) N-cikloheksil-2-metil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (13) N-(3-klor-2-metilfenil)-2-metil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (14) N-ciklopentil-2-metil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (15) N-ciklobutil-2-metil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (16) N-(3-klor-2-metilfenil)-2-etil-6-({[2-(trifluormetil)fenil]karbonil}amino)-H-benzimidazol-4-karboksamida, (17) N-cikloheksil-2-etil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (18) 2-etil-N-[2-(trifluormetil)benzil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (19) N-cikloheksil-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-H-benzimidazol-4-karboksamida, (20) 2-(metoksimetil)-N-[2-(trifluormetil)benzil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (21) 2-(metoksimetil)-N-(2-metilfenil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (22) 2-(metoksimetil)-N-(4-metilfenil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (23) N-(2-klorbenzil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (24) 2-(metoksimetil)-N-(4-metilbenzil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (25) N-(4,4-difluorcikloheksil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (26) N-(4-tert-butilfenil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (27) 2-(metoksimetil)-N-[4-(trifluormetil)fenil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (28) N-(2,4-dimetilfenil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (29) N-(2-klor-4-metilfenil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (30) N-(3,4-dimetilfenil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (31) N-(3-klor-4-metilfenil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (32) N-(2,3-dihidro-1H-inden-5-il)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (33) 2-(metoksimetil)-N-(5,6,7,8-tetrahidronaftalen-1-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (34) N-(2-fluorfenil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (35) 2-(metoksimetil)-N-(2-metoksifeny)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (36) 2-(metoksimetil)-N-(4-metoksifeny)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (37) N-(3-brom-2-metilfenil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (38) N-(3-klor-2-metilbenzil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (39) N-(2,6-difluorfenil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (40) N-(3-cijano-2-metilfenil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (41) 2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-N-{[3-(trifluormetil)piridin-2-il]metil}-1H-benzimidazol-4-karboksamida, (42) N-(2-klor-6-metilfenil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (43) 2-(2-amino-2-oksoetil)-N-(3-klor-2-metilfenil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (44) 2-(2-amino-2-oksoetil)-N-[2-(trifluormetil)benzil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (45) N-(3-klor-2-metilfenil)-1-metil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (46) N-cikloheksil-1-metil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (47) 1-metil-N-[2-(trifluormetil)benzil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (48) N-(3-klor-2-metilfenil)-1-etil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (49) N-cikloheksil-1-etil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (50) 1-etil-N-[2-(trifluormetil)benzil]-6-({[2(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (51) N-(3-klor-2-metilfenil)-2-metil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1,3-benzoksazol-4-karboksamida, (52) 2-metil-N-[2-(trifluormetil)benzil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1,3-benzoksazol-4-karboksamida, (53) N-(3-klor-2-metilfenil)-2-etil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1,3-benzoksazol-4-karboksamida, (54) N-(3-klor-2-metilfenil)-2-etoksi-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (55) 2-etoksi-N-[2-(trifluormetil)benzil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (56) N-(3-klor-2-metilfenil)-2-(1-klor-2-metilpropan-2-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-H-benzimidazol-4-karboksamida, (57) N-(3-klor-2-metilfenil)-2-[(dimetilamino)metil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (58) N-(3-klor-2-metilfenil)-2-(2-metilpropil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (59) 2-(2-metilpropil)-N-[2-(trifluormetil)benzil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (60) tert-butil-3-{4-[(3-klor-2-metilfenil)karbamoil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-2-il}azetidin-1-karboksilata, (61) N-(3-klor-2-metilfenil)-2-[(metilamino)metil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (62) {4-[(3-klor-2-metilfenil)karbamoil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-2-il}metil-acetata, (63) N-(3-klor-2-metilfenil)-2-[(2R)-tetrahidrofuran-2-il]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (64) 2-[[(2R)-tetrahidrofuran-2-il]-N-[2-(trifluormetil)benzil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-H-benzimidazol-4-karboksamida, (65) N-(3-klor-2-metilfenil)-2-[(2S)-tetrahidrofuran-2-il]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (66) 2-[[(2S)-tetrahidrofuran-2-il]-N-[2-(trifluormetil)benzil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (67) 2-(1-acetilazetidin-3-il)-N-(3-klor-2-metilfenil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (68) tert-butil-(2S)-2-{4-[(3-klor-2-metilfenil)karbamoil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-2-il}pirolidin-1-karboksilata, (69) tert-butil-(2R)-2-{4-[(3-klor-2-metilfenil)karbamoil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-2-il}pirolidin-1-karboksilata, (70) N-(3-klor-2-metilfenil)-2-[(2S)-pirolidin-2-il]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (71) N-(3-klor-2-metilfenil)-2-[(2S)-1-metilpirolidin-2-il]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (72) 2-[(2S)-1-acetilpirolidin-2-il]-N-(3-klor-2-metilfenil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (73) N-(3-klor-2-metilfenil)-2-[(2-metoksietoksi)metil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (74) N-(3-klor-2-metilfenil)-2-(1-metoksi-2-metilpropan-2-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (75) 2-tert-butil-N-(3-klor-2-metilfenil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (76) 2-tert-butil-6-({[2-(trifluormetil)fenil]karbonil}amino)-N-{[3-(trifluormetil)piridin-2-il]metil}-1H-benzimidazol-4-karboksamida, (77) N-(3-klor-2-metilfenil)-2-(2-etoksietil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (78) N-(3-klor-2-metilfenil)-2-(etoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (79) 2-(etoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-N-{[3-(trifluormetil)piridin-2-il]metil}-1H-benzimidazol-4-karboksamida, (80) N-(3-klor-2-metilfenil)-2-(2-metoksietil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (81) N-(3-klor-2-metilfenil)-2-(2,2-dimetilpropil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (82) N-(3-klor-2-metilfenil)-2-ciklopropil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (83) N-(3-klor-2-metilfenil)-2-(2-metilpentan-2-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (84) N-(3-klor-2-metilfenil)-2-(1-metilciklopropil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (85) 2-tert-butil-N-(3-klor-4-metilfenil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (86) 2-tert-butil-N-(3-klor-2-metilfenil)-6-{[(2,5-diklorfenil)karbonil]amino}-1H-benzimidazol-4-karboksamida, (87) 2-tert-butil-N-(3-klor-4-metilfenil)-6-{[(2,5-diklorfenil)karbonil]amino}-1H-benzimidazol-4-karboksamida, (88) N-(3-klor-2-metilfenil)-2-[1-(trifluormetil)ciklopropil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (89) N-(3-klor-2-metilfenil)-2-(metoksimetil)-1-metil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (90) N-(2-klorbenzil)-2-(metoksimetil)-1-metil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (91) 6-{[(2-klor-6-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-(metoksimetil)-H-benzimidazol-4-karboksamida, (92) 6-{[(2-klor-4-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-metoksimetil-1H-benzimidazol-4-karboksamida, (93) 6-{[(2-klor-5-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (94) N-(3-klor-2-metilfenil)-6-{[(2-klorfenil)karbonil]amino}-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (95) N-(3-klor-2-metilfenil)-6-{[(2-klorpiridin-3-il)karbonil]amino}-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (96) 6-{[(2-bromfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (97) N-(3-klor-2-metilfenil)-6-{[(2,6-diklorfenil)karbonil]amino}-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (98) N-(3-klor-2-metilfenil)-6-{[(2,5-diklorfenil)karbonil]amino}-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (99) 6-{[(2-klor-3-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (100) 6-{[(2-klor-3,6-difluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (101) 6-{[(2-brom-6-klorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (102) 6-{[(2-brom-6-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (103) N-(3-klor-2-metilfenil)-6-{[(2-klor-6-metilfenil)karbonil]amino}-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (104) N-(3-klor-2-metilfenil)-6-{[(2-klor-4-metilfenil)karbonil]amino}-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (105) 6-{[(5-brom-2-klorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (106) 6-{[(2-brom-5-klorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (107) N-(3-klor-2-metilfenil)-6-{[(2-klor-5-metilfenil)karbonil]amino}-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (108) N-(3-klor-2-metilfenil)-2-(metoksimetil)-6-({[5-metil-2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (109) 6-({[2,5-bis(trifluormetil)fenil]karbonil}amino)-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (110) 6-({[2,4-bis(trifluormetil)fenil]karbonil}amino)-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (111) N-(3-klor-2-metilfenil)-6-({[5-fluor-2-(trifluormetil)fenil]karbonil}amino)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (112) N-(3-klor-2-metilfenil)-6-({[2-klor-6-(trifluormetil)fenil]karbonil}amino)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (113) N-(3-klor-2-metilfenil)-6-[({2-klor-5-[2-(propan-2-iloksi)etoksi]fenil}karbonil)amino]-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (114) 6-({[2-klor-5-(2-etoksietoksi)fenil]karbonil}amino)-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (115) 6-({[2-klor-5-(3-metoksipropil)fenil]karbonil}amino)-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (116) 6-({[5-(3-tert-butoksiprop-1-in-1-il)-2-klorfenil]karbonil}amino)-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (117) 6-({[5-(3-tert-butoksipropil)-2-klorfenil]karbonil}amino)-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (118) 6-({[2-klor-5-(3-hidroksi-3-metilbutil)fenil]karbonil}amino)-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (119) 6-({[2-klor-5-(etoksimetil)fenil]karbonil}amino)-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (120) 6-[({2-klor-5-[(2-etoksietoksi)metil]fenil}karbonil)amino]-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (121) 6-({[2-klor-5-(2-ciklopropiletil)fenil]karbonil}amino)-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (122) N-(3-klor-2-metilfenil)-6-({[2-klor-5-(2-feniletil)fenil]karbonil}amino)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (123) N-(3-klor-2-metilfenil)-2-ciklopentil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (124) N-(3-klor-2-metilfenil)-2-ciklopentil-6-{[(2,5-diklorfenil)karbonil]amino}-1H-benzimidazol-4-karboksamida, (125) 6-{[(2-klor-6-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-ciklopentil-1H-benzimidazol-4-karboksamida, (126) 6-[{[(2-klor-6-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-[(2R)-tetrahidrofuran-2-il]-1H-benzimidazol-4-karboksamida, (127) N-(3-klor-2-metilfenil)-6-{[(2,6-diklorfenil)karbonil]amino}-2-[(2R)-tetrahidrofuran-2-il]-1H-benzimidazol-4-karboksamida, (128) N-(3-klor-2-metilfenil)-6-{[(2,5-diklorfenil)karbonil]amino}-2-[(2R)-tetrahidrofuran-2-il]-1H-benzimidazol-4-karboksamida, (129) N-(3-klor-2-metilfenil)-2-[(2S)-5-oksopirolidin-2-il]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (130) N-(3-klor-2-metilfenil)-2-[(2R)-5-oksopirolidin-2-il]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (131) N-(3-klor-2-metilfenil)-2-[2-okso-2-(pirolizin-1-il)etil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (132) N-(3-klor-2-metilfenil)-2-[2-(dimetilamino)-2-oksoetil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (133) N-(3-klor-2-metilfenil)-2-[2-(metilamino)-2-oksoetil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (134) 2-klor-N-(3-klor-2-metilfenil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (135) N-(3-klor-2-metilfenil)-2-[(2-metoksietil)amino]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (136) N-(3-klor-2-metilfenil)-2-[(2-hidroksietil)amino]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (137) N-(3-klor-2-metilfenil)-2-(metilamino)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (138) N-(3-klor-2-metilfenil)-2-(etilamino)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (139) N-(3-klor-2-metilfenil)-2-[(2,2-dimetilpropil)amino]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (140) N-(3-klor-2-metilfenil)-2-(ciklopentilamino)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (141) N-(3-klor-2-metilfenil)-2-(piperidin-1-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (142) N-(3-klor-2-metilfenil)-2-(4-metilpiperazin-1-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (143) 2-[bis(2-hidroksietil)amino]-N-(3-klor-2-metilfenil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (144) N-(3-klor-2-metilfenil)-2-(dimetilamino)-6-({[2-(tritluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (145) N-(3-klor-2-metilfenil)-2-{[2-(morfolin-4-il)etil]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (146) N-(3-klor-2-metilfenil)-2-{[2-(dimetilamino)etil]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (147) N-(3-klor-2-metilfenil)-2-(3-hidroksiazetidin-1-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (148) N-(3-klor-2-metilfenil)-2-[(3S)-3-(dimetilamino)pirolizin-1-il]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (149) N-(3-klor-2-metilfenil)-2-[(3S)-3-hidroksipirolizin-1-il]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (150) N-(3-klor-2-metilfenil)-2-{[2-(dietilamino)etil]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (151) N-(3-klor-2-metilfenil)-2-{[2-(pirolizin-1-il)etil]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (152) N-(3-klor-2-metilfenil)-2-{[3-(dimetilamino)propil]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (153) N-(3-klor-2-metilfenil)-2-{[3-(dimetilamino)-2,2-dimetilpropil]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (154) N-(3-klor-2-metilfenil)-2-{[2-(dipropan-2-ilamino)etil]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (155) N-(3-klor-2-metilfenil)-2-(morfolin-4-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (156) 2-amino-N-(3-klor-2-metilfenil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (157) N-(3-klor-2-metilfenil)-2-[(3-hidroksi-2,2-dimetilpropil)amino]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (158) N-(3-klor-2-metilfenil)-2-{[(3-metiloksetan-3-il)metil]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (159) tert-butil-N-{4-[(3-klor-2-metilfenil)karbamoil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-2-il}glicinata, (160) N-{4-[(3-klor-2-metilfenil)karbamoil]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-2-il}glicina, (161) N-(3-klor-2-metilfenil)-2-[(3-hidroksi-2,2-dimetilpropil)amino]-1-metil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (162) N-(3-klor-2-metilfenil)-2-[(3-metoksi-2,2-dimetilpropil)amino]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (163) N-(3-klor-2-metilfenil)-2-(pirolizin-1-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (164) 2-(azetidin-1-il)-N-(3-klor-2-metilfenil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-H-benzimidazol-4-karboksamida, (165) N-(3-klor-2-metilfenil)-2-(3-metoksiazetidin-1-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (166) N-(3-klor-2-metilfenil)-2-[(2-hidroksi-2-metilpropil)amino]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (167) N-(3-klor-2-metilfenil)-2-{[(2S)-tetrahidrofuran-2-ilmetil]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (168) N-(3-klor-2-metilfenil)-2-{[(2R)-tetrahidrofuran-2-ilmetil]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (169) N-(3-klor-2-metilfenil)-2-{[(2S)-1-hidroksi-3-metilbutan-2-il]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (170) N-(3-klor-2-metilfenil)-2-{[(2R)-1-hidroksi-3-metilbutan-2-il]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (171) N-(3-klor-2-metilfenil)-2-{[(2S)-1-hidroksi-3,3-dimetilbutan-2-il]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (172) N-(3-klor-2-metilfenil)-2-[(3-metoksi-2,2-dimetilpropil)(metil)amino]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (173) N-(3-klor-2-metilfenil)-2-[(3-metoksipropil)amino]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (174) N-(3-klor-2-metilfenil)-2-{[2-(propan-2-iloksi)etil]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (175) 2-[(2-tert-butoksietil)amino]-N-(3-klor-2-metilfenil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (176) N-(3-klor-2-metilfenil)-2-[(2-metoksi-2-metilpropil)amino]-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (177) N-(3-klor-2-metilfenil)-2-{[2-(metilsulfanil)etil]amino}-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (178) N-(3-klor-2-metilfenil)-2-(metilsulfanil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (179) N-(3-klor-2-metilfenil)-2-(metilsulfonil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (180) N-(3-klor-2-metilfenil)-2-(metilsulfinil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (181) 6-{[(2-klor-6-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-(dimetilamino)-1H-benzimidazol-4-karboksamida, (182) N-(3-klor-2-metilfenil)-6-{[(2,6-diklorfenil)karbonil]amino}-2-(dimetilamino)-1H-benzimidazol-4-karboksamida, (183) N-(3-klor-2-metilfenil)-6-{[(2,4-diklorfenil)karbonil]amino}-2-(dimetilamino)-1H-benzimidazol-4-karboksamida, (184) N-(3-klor-2-metilfenil)-6-{[(2,5-diklorfenil)karbonil]amino}-2-(dimetilamino)-1H-benzimidazol-4-karboksamida, (185) 6-{[(2-brom-6-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-(dimetilamino)-1H-benzimidazol-4-karboksamida, (186) 6-{[(2-brom-6-klorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-(dimetilamino)-1H-benzimidazol-4-karboksamida, (187) 6-({[2-klor-5-(ciklopropiletinil)fenil]karbonil}amino)-N-(3-klor-2-metilfenil)-2-(dimetilamino)-1H-benzimidazol-4-karboksamida, (188) N-(3-klor-2-metilfenil)-6-{[(2,5-diklorfenil)karbonil]amino}-2-[(3-hidroksi-2,2-dimetilpropil)amino]-1H-benzimidazol-4-karboksamida, (189) N-(3-klor-2-metilfenil)-6-{[(2,5-diklorfenil)karbonil]amino}-2-[(3-metoksi-2,2-dimetilpropil)amino]-1H-benzimidazol-4-karboksamida, (190) N-(3-klor-2-metilfenil)-6-{[(2,5-diklorfenil)karbonil]amino}-2-[(2-hidroksi-2-metilpropil)amino]-1H-benzimidazol-4-karboksamida, (191) N-(3-klor-2-metilfenil)-6-{[(2,5-diklorfenil)karbonil]amino}-2-[(2-metoksi-2-metilpropil)amino]-1H-benzimidazol-4-karboksamida, (192) N-(3-klor-2-metilfenil)-6-{[(2,5-diklorfenil)karbonil]amino}-2-{[2-(propan-2-iloksi)etil]amino}-1H-benzimidazol-4-karboksamida, (193) 6-[{[(2-klor-6-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-{[2-(propan-2-iloksi)etil]amino}-1H-benzimidazol-4-karboksamida, (194) 2-[(2-tert-butoksietil)amino]-6-{[(2-klor-6-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-1H-benzimidazol-4-karboksamida, (195) 6-[{[(2-klor-6-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-[(3-metoksi-2,2-dimetilpropil)amino]-1H-benzimidazol-4-karboksamida, (196) 6-[{[(2-klor-6-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-[(2-metoksi-2-metilpropil)amino]-1H-benzimidazol-4-karboksamida, (197) 6-[{[(2-klor-6-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-{[(2S)-tetrahidrofuran-2-ilmetil]amino}-1H-benzimidazol-4-karboksamida, (198) 6-[{[(2-klor-6-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-{[(2R)-tetrahidrofuran-2-ilmetil]amino}-1H-benzimidazol-4-karboksamida, (199) 6-[{[(2-klor-6-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-[(3-hidroksi-2,2-dimetilpropil)amino]-1H-benzimidazol-4-karboksamida, (200) 6-[{[(2-klor-6-fluorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-{[(2S)-1-hidroksi-3-metilbutan-2-il]amino}-1H-benzimidazol-4-karboksamida, (201) N-(3-klor-4-metilfenil)-2-(dimetilamino)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (202) N-(4-tert-butilfenil)-2-(dimetilamino)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (203) N-(2,3-dihidro-1H-inden-5-il)-2-(dimetilamino)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (204) 6-{[(2-klor-6-fluorfenil)karbonil]amino}-N-(3-klor-4-metilfenil)-2-(dimetilamino)-1H-benzimidazol-4-karboksamida, (205) N-(3-klor-4-metilfenil)-6-{[(2,6-diklorfenil)karbonil]amino}-2-(dimetilamino)-1H-benzimidazol-4-karboksamida, (206) N-(3-klor-4-metilfenil)-6-{[(2,5-diklorfenil)karbonil]amino}-2-(dimetilamino)-1H-benzimidazol-4-karboksamida, (207) N-(3-klor-2-metilfenil)-2-ciklopropil-6-{[(2,5-diklorfenil)karbonil]amino}-1H-benzimidazol-4-karboksamida, (208) N-(3-klor-4-metilfenil)-2-ciklopropil-6-{[(2,5-diklorfenil)karbonil]amino}-1H-benzimidazol-4-karboksamida, (209) N-(3-klor-2-metilfenil)-6-{[(2,5-diklorfenil)karbonil]amino}-2-(1-metilciklopropil)-1H-benzimidazol-4-karboksamida, (210) N-(3-klor-4-metilfenil)-6-{[(2,5-diklorfenil)karbonil]amino}-2-(1-metilciklopropil)-1H-benzimidazol-4-karboksamida, (211) N-(3-klor-2-metilfenil)-2-(metoksimetil)-6-({[2-(metilsulfonil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (212) N-(3-klor-4-metilfenil)-6-{[(2,5-diklorfenil)karbonil]amino}-2-(2-metoksietil)-1H-benzimidazol-4-karboksamida, (213) 2-(metoksimetil)-N-fenil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (214) 2-(metoksimetil)-N-propil-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (215) 2-(metoksimetil)-N-(piridin-3-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (216) N-benzil-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (217) N-(cikloheksilmetil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (218) 2-(metoksimetil)-N-(naftalen-1-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (219) 2-(metoksimetil)-N-(tiofen-3-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (220) N-(2,1,3-benzotiadiazol-4-il)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (221) N-(1,1-dioksid-1-benzotiofen-6-il)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (222) 2-(metoksimetil)-N-(tiofen-2-ilmetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (223) N-(1H-indol-5-il)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (224) N-(1,3-benzotiazol-2-il)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (225) N-(2,2-dimetilpropil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (226) 2-(metoksimetil)-N-(tiofen-2-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (227) N-(5-klor-1,3-benzoksazol-2-il)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (228) N-(2-benzilfenil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (229) 2-(metoksimetil)-N-(quinolin-8-il)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (230) N-(cikloheptilmetil)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (231) N-(1,3-benzoksazol-2-il)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (232) N-(6-klor-1,3-benzoksazol-2-il)-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (233) N-[3-klor-2-(hidroksimetil)fenil]-2-(metoksimetil)-6-({[2-(trifluormetil)fenil]karbonil}amino)-1H-benzimidazol-4-karboksamida, (234) N-(3-klor-2-metilfenil)-6-{[(3-fluorpiridin-2-il)karbonil]amino}-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (235) N-(3-klor-2-metilfenil)-6-{[(3-klorpiridin-4-il)karbonil]amino}-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (236) N-(3-klor-2-metilfenil)-6-{[(3,5-diklorpiridin-4-il)karbonil]amino}-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (237) 6-{[(5-butoksi-2-klorfenil)karbonil]amino}-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (238) 6-({[2-klor-5-(2,2-difluoretoksi)fenil]karbonil}amino)-N-(3-klor-2-metilfenil)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida, (239) N-(3-klor-2-metilfenil)-6-({[2-klor-5-(4,4,4-trifluorbutoksi)fenil]karbonil}amino)-2-(metoksimetil)-1H-benzimidazol-4-karboksamida.
8. Farmaceutski pripravak, naznačen time što sadrži spoj kojeg se bira iz skupine koju čini heterociklički derivat u skladu s bilo kojim od patentnih zahtjeva 1 do 7, njegov tautomer i njegovu farmaceutski prihvatljivu sol kao aktivni sastojak.
9. Spoj, kojeg se bira iz skupine koju čini heterociklički derivat u skladu s bilo kojim od patentnih zahtjeva 1 do 7, njegov tautomer i njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi kao inhibitor mPGEs.
10. Spoj, kojeg se bira iz skupine koju čini heterociklički derivat u skladu s bilo kojim od patentnih zahtjeva 1 do 7, njegov tautomer i njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u sprječavanju ili liječenju upalne bolesti crijeva, sindroma iritabilnog crijeva, migrene, glavobolje, boli u donjem dijelu leđa, spinalne stenoze, hernije diska, poremećaja temporomandibularnog zgloba, cervikalnog sindroma, cervikalne spondiloze, endometrioze, adenomioze, prijevremenog porođaja, opasnosti od prijevremenog porođaja, dismenoreje, hiperaktivnog mokraćnog mjehura, noćnog mokrenja, intersticijskog cistitisa, neurodegenerativne bolesti, psorijaze, reumatoidnog artritisa, reumatske groznice, fibromialgije, neuralgije, sindroma kompleksne regionalne boli, fascijalne disfunkcije, virusnih infekcija, bakterijske infekcije, mikoze, opekline, upale i boli nakon operacije, ozljede i vađenja zubiju, zloćudnih tumora, ateroskleroze, inzulta, gihta, artritisa, osteoartritisa, mladalačkog artritisa, ankilozantnog spondilitisa, tenosinovitisa, okoštavanja ligamenata, sistemnog eritematoznog lupusa, vaskulitisa, pankreatitisa, nefritisa, konjunktivitisa, iritisa, skleritisa, uveitisa, terapije rana, dermatitisa, egzema, osteoporoze, astme, kronične opstruktivne plućne bolesti, plućne fibroze, alergijske bolesti, porodične adenomatozne polipoze, skleroderme, bursitisa, lejomioma maternice, ili boli uzrokovane rakom.
11. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 10, naznačen time što je neurodegenerativna bolest Alzheimerova bolest ili multipla skleroza.
12. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 10, naznačen time što je virusna zarazna bolest influenca, obična prehlada, herpes zoster ili AIDS.
13. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 10, naznačen time što je zloćudni tumor rak debelog crijeva, rak dojke, rak pluća ili rak prostate.
HRP20160118TT 2011-08-18 2016-02-03 HETEROCIKLIÄŚKI DERIVAT KAO INHIBITOR MIKROSOMSKIH SINTAZA PROSTAGLANDINA E (mPGEs) HRP20160118T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2011179134 2011-08-18
EP12823510.8A EP2746265B1 (en) 2011-08-18 2012-08-17 HETEROCYCLIC DERIVATIVE AS MICROSOMAL PROSTAGLANDIN E SYNTHASE (mPGEs) INHIBITOR
PCT/JP2012/070902 WO2013024898A1 (ja) 2011-08-18 2012-08-17 ヘテロ環誘導体及び医薬

Publications (1)

Publication Number Publication Date
HRP20160118T1 true HRP20160118T1 (hr) 2016-02-26

Family

ID=47715213

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20160118TT HRP20160118T1 (hr) 2011-08-18 2016-02-03 HETEROCIKLIÄŚKI DERIVAT KAO INHIBITOR MIKROSOMSKIH SINTAZA PROSTAGLANDINA E (mPGEs)

Country Status (24)

Country Link
US (2) US9216968B2 (hr)
EP (1) EP2746265B1 (hr)
JP (1) JP5601422B2 (hr)
KR (1) KR101778354B1 (hr)
CN (1) CN103857657B (hr)
AU (1) AU2012295805B2 (hr)
BR (1) BR112014003496B1 (hr)
CA (1) CA2844794C (hr)
CO (1) CO6910189A2 (hr)
DK (1) DK2746265T3 (hr)
ES (1) ES2561105T3 (hr)
HR (1) HRP20160118T1 (hr)
HU (1) HUE026671T2 (hr)
IL (1) IL230786A (hr)
MX (1) MX348548B (hr)
MY (1) MY166866A (hr)
PL (1) PL2746265T3 (hr)
PT (1) PT2746265E (hr)
RU (1) RU2632908C2 (hr)
SA (1) SA112330791B1 (hr)
SI (1) SI2746265T1 (hr)
UA (1) UA108950C2 (hr)
WO (1) WO2013024898A1 (hr)
ZA (1) ZA201400742B (hr)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY166866A (en) * 2011-08-18 2018-07-24 Nippon Shinyaku Co Ltd Heterocyclic derivative and pharmaceutical drug
CA2909477A1 (en) * 2013-04-30 2014-11-06 F. Hoffmann-La Roche Ag Pd-catalyzed coupling of pyrazole amides
EP3036227B1 (en) * 2013-08-22 2020-01-08 Genentech, Inc. Process for preparing a compound
CA2966583A1 (en) 2014-11-06 2016-05-12 Lysosomal Therapeutics Inc. Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders
AU2015342883B2 (en) 2014-11-06 2020-07-02 Bial - R&D Investments, S.A. Substituted pyrrolo(1,2-a)pyrimidines and their use in the treatment of medical disorders
ES2958391T3 (es) 2014-11-06 2024-02-08 Bial R&D Invest S A Imidazo[1,5-a]pirimidinas sustituidas y su uso en el tratamiento de trastornos médicos
ES2902127T3 (es) 2015-10-29 2022-03-25 Aska Pharm Co Ltd Derivado de pirimidina
GB201603311D0 (en) * 2016-02-25 2016-04-13 Jakobsson Per Johan New uses and methods
CA3020305A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics Inc. Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
KR20230104752A (ko) 2016-04-06 2023-07-10 비알 - 알&디 인베스트먼츠, 에스.에이. 피라졸로[1,5-a]피리미디닐 카르복스아미드 화합물및 의학적 장애의 치료에서의 그의 용도
EP3440081A4 (en) 2016-04-06 2019-09-18 Lysosomal Therapeutics Inc. PYRROLO [1,2-A] PYRIMIDINYL CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
WO2017192931A1 (en) * 2016-05-05 2017-11-09 Lysosomal Therapeutics Inc. SUBSTITUTED IMDAZO[1,2-α]PYRIDINES, SUBSTITUTED IMIDAZO[1,2-α]PYRAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
CA3022670A1 (en) 2016-05-05 2017-11-09 Lysosomal Therapeutics Inc. Substituted imidazo[1,2-b]pyridazines, substituted imidazo[1,5-b]pyridazines, related compounds, and their use in the treatment of medical 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
AU2018362046B2 (en) 2017-11-06 2023-04-13 Jubilant Prodel LLC Pyrimidine derivatives as inhibitors of PD1/PD-L1 activation
AU2019234185A1 (en) 2018-03-13 2020-10-01 Jubilant Prodel LLC. Bicyclic compounds as inhibitors of PD1/PD-L1 interaction/activation
MX2021015452A (es) 2019-06-25 2022-02-11 Gilead Sciences Inc Proteinas de fusion flt3l-fc y metodos de uso.
JP7371243B2 (ja) 2019-10-18 2023-10-30 フォーティ セブン， インコーポレイテッド 骨髄異形成症候群及び急性骨髄性白血病を治療するための併用療法
CN114599392A (zh) 2019-10-31 2022-06-07 四十七公司 基于抗cd47和抗cd20的血癌治疗
TWI778443B (zh) 2019-11-12 2022-09-21 美商基利科學股份有限公司 Mcl1抑制劑
MX2022007930A (es) 2019-12-24 2022-08-08 Carna Biosciences Inc Compuestos moduladores de diacilglicerol quinasa.
WO2021132472A1 (ja) * 2019-12-25 2021-07-01 日本新薬株式会社 慢性前立腺炎／慢性骨盤痛症候群の予防及び／又は治療剤
CA3165893A1 (en) * 2019-12-25 2021-07-01 Nippon Shinyaku Co., Ltd. Antitumor drug for use in combination with immune checkpoint inhibitor
CN111072634B (zh) * 2020-01-03 2022-07-22 中国医科大学 1-取代-3-取代-5-取代酰胺-1h-吲哚类化合物及其制备方法和应用
WO2021163064A2 (en) 2020-02-14 2021-08-19 Jounce Therapeutics, Inc. Antibodies and fusion proteins that bind to ccr8 and uses thereof
AU2021264550A1 (en) 2020-05-01 2022-11-17 Gilead Sciences, Inc. CD73 inhibiting 2,4-dioxopyrimidine compounds
US20240083867A1 (en) 2021-02-02 2024-03-14 Aska Pharmaceutical Co., Ltd. Pyrimidine derivative
TW202302145A (zh) 2021-04-14 2023-01-16 美商基利科學股份有限公司 ＣＤ４７／ＳＩＲＰα結合及ＮＥＤＤ８活化酶Ｅ１調節次單元之共抑制以用於治療癌症
US20220389394A1 (en) 2021-05-18 2022-12-08 Gilead Sciences, Inc. METHODS OF USING FLT3L-Fc FUSION PROTEINS
WO2022271677A1 (en) 2021-06-23 2022-12-29 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
EP4359413A1 (en) 2021-06-23 2024-05-01 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
AU2022299051A1 (en) 2021-06-23 2023-12-07 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
CA3222439A1 (en) 2021-06-23 2022-12-29 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
AU2022375782A1 (en) 2021-10-28 2024-05-02 Gilead Sciences, Inc. Pyridizin-3(2h)-one derivatives
AU2022376954A1 (en) 2021-10-29 2024-05-02 Gilead Sciences, Inc. Cd73 compounds
WO2023122581A2 (en) 2021-12-22 2023-06-29 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
AU2022417491A1 (en) 2021-12-22 2024-05-23 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
TW202340168A (zh) 2022-01-28 2023-10-16 美商基利科學股份有限公司 Ｐａｒｐ７抑制劑
WO2023178181A1 (en) 2022-03-17 2023-09-21 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
US20230355796A1 (en) 2022-03-24 2023-11-09 Gilead Sciences, Inc. Combination therapy for treating trop-2 expressing cancers
TW202345901A (zh) 2022-04-05 2023-12-01 美商基利科學股份有限公司 用於治療結腸直腸癌之組合療法
TW202400138A (zh) 2022-04-21 2024-01-01 美商基利科學股份有限公司 Ｋｒａｓ ｇ１２ｄ調節化合物
WO2024005197A1 (ja) * 2022-06-30 2024-01-04 日本新薬株式会社 固体分散体、固体分散体を含む製剤、及びそれらの製造方法
WO2024006929A1 (en) 2022-07-01 2024-01-04 Gilead Sciences, Inc. Cd73 compounds
WO2024064668A1 (en) 2022-09-21 2024-03-28 Gilead Sciences, Inc. FOCAL IONIZING RADIATION AND CD47/SIRPα DISRUPTION ANTICANCER COMBINATION THERAPY

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU171244B (hu) * 1974-05-02 1977-12-28 Chinoin Gyogyszer Es Vegyeszet Sposob poluchenija novykh proizvodnykh benzimidazola i gerbicidy soderzhahhie takie soedinenija
US4888353A (en) 1986-02-28 1989-12-19 Erbamont, Inc. Carboxamides useful as antiemetic or antipsychotic agents
HUP9900973A3 (en) 1996-01-03 2000-04-28 Smithkline Beecham Plc Carbamoyloxy derivatives of mutiline with antibacterial activity, pharmaceutical compns. contg. them and process for preparing the said compds.
US6387938B1 (en) 1996-07-05 2002-05-14 Mochida Pharmaceutical Co., Ltd. Benzimidazole derivatives
FR2812876B1 (fr) 2000-08-08 2002-09-27 Galderma Res & Dev Nouveaux composes bi-aromatiques activateurs des recepteurs de type ppar-gamma et leur utilisation dans des compositions cosmetiques ou pharmaceutiques
WO2003064422A1 (fr) 2002-01-31 2003-08-07 Daiichi Pharmaceutical Co., Ltd. Derive imidazo[1,2-a]pyridine
US20040034078A1 (en) 2002-06-14 2004-02-19 Agouron Pharmaceuticals, Inc. Benzimidazole inhibitors of poly(ADP-ribosyl) polymerase
WO2005023773A1 (en) 2003-09-04 2005-03-17 Pfizer Limited Process for the preparation of substituted aryl pyrazoles
US7442716B2 (en) * 2004-12-17 2008-10-28 Merck Frosst Canada Ltd. 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
EP1828143B1 (en) * 2004-12-17 2013-03-20 Merck Frosst Canada Ltd. 2-(phenyl or heterocyclic)-1h-phenantrho[9,10-d]imidazoles as mpges-1 inhibitors
CA2589221A1 (en) 2005-01-28 2006-08-03 Janssen Pharmaceutica N.V. Anthelmintic imidazol-thiazole derivates
EP2457901A1 (en) * 2005-03-14 2012-05-30 High Point Pharmaceuticals, LLC Benzazole derivatives, compositions, and methods of use as B-secretase inhibitors
TWI370820B (en) 2005-04-27 2012-08-21 Takeda Pharmaceutical Fused heterocyclic compounds
CA2620223A1 (en) 2005-09-02 2007-03-08 Abbott Laboratories Novel imidazo based heterocycles
JP2007197416A (ja) 2005-12-28 2007-08-09 Fujifilm Corp 殺菌用水性組成物の製造方法
GB0611587D0 (en) 2006-06-12 2006-07-19 Glaxo Group Ltd Novel compounds
ITMI20061368A1 (it) * 2006-07-14 2008-01-15 Acraf Composto 2-arilindolico sostituito in posizione 5, composizione farmaceutica che lo comprende nonche' composti intermedi e procedimento per prepararlo
EA200900613A1 (ru) 2006-11-29 2009-10-30 Пфайзер Продактс Инк. Спирокетоновые ингибиторы ацетил-коа-карбоксилаз
WO2008071944A1 (en) * 2006-12-14 2008-06-19 Boehringer Ingelheim International Gmbh Benzoxazoles useful in the treatment of inflammation
US20100179109A1 (en) 2007-04-05 2010-07-15 Baldwin Jonh J Renin inhibitors
US20090076062A1 (en) 2007-09-13 2009-03-19 Juergen Klaus Maibaum Organic Compounds
AU2008319735A1 (en) 2007-10-31 2009-05-07 Nissan Chemical Industries, Ltd. Pyridazinone derivatives and use thereof as P2X7 receptor inhibitors
WO2009068512A1 (en) 2007-11-30 2009-06-04 Palau Pharma, S. A. 2 -amino-pyrimidine derivatives as histamine h4 antagonists
WO2009084695A1 (ja) 2007-12-28 2009-07-09 Carna Biosciences Inc. ２－アミノキナゾリン誘導体
CN101981031A (zh) 2008-01-22 2011-02-23 武田药品工业株式会社 具有促肾上腺皮质激素释放因子拮抗活性的三环化合物和含有它们的药物组合物
WO2009103778A1 (en) * 2008-02-19 2009-08-27 Novasaid Ab Compounds and methods
CA2762680C (en) 2009-05-21 2018-04-17 Chlorion Pharma, Inc. Methyl sulfanyl pyrmidmes useful as antiinflammatories, analgesics, and antiepileptics
JP5579862B2 (ja) 2009-10-23 2014-08-27 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 ミクロソームプロスタグランジンｅ２シンターゼ−１のインヒビター
MY166866A (en) * 2011-08-18 2018-07-24 Nippon Shinyaku Co Ltd Heterocyclic derivative and pharmaceutical drug

Also Published As

Publication number Publication date
PT2746265E (pt) 2016-03-11
KR101778354B1 (ko) 2017-09-13
SI2746265T1 (sl) 2016-03-31
AU2012295805A1 (en) 2014-02-20
CN103857657A (zh) 2014-06-11
MX348548B (es) 2017-06-19
EP2746265B1 (en) 2015-11-18
AU2012295805B2 (en) 2017-05-04
CA2844794C (en) 2018-02-20
EP2746265A1 (en) 2014-06-25
KR20140054193A (ko) 2014-05-08
JPWO2013024898A1 (ja) 2015-03-05
US9732066B2 (en) 2017-08-15
NZ620610A (en) 2016-04-29
CA2844794A1 (en) 2013-02-21
BR112014003496A2 (pt) 2017-03-01
MX2014001665A (es) 2014-03-31
IL230786A0 (en) 2014-03-31
IL230786A (en) 2017-03-30
UA108950C2 (uk) 2015-06-25
SA112330791B1 (ar) 2015-08-24
BR112014003496B1 (pt) 2022-02-22
PL2746265T3 (pl) 2016-04-29
WO2013024898A1 (ja) 2013-02-21
US20140221339A1 (en) 2014-08-07
ZA201400742B (en) 2014-11-26
MY166866A (en) 2018-07-24
JP5601422B2 (ja) 2014-10-08
HUE026671T2 (en) 2016-07-28
RU2632908C2 (ru) 2017-10-11
EP2746265A4 (en) 2015-02-11
RU2014110172A (ru) 2015-09-27
CN103857657B (zh) 2016-04-20
ES2561105T3 (es) 2016-02-24
US9216968B2 (en) 2015-12-22
DK2746265T3 (da) 2016-02-01
CO6910189A2 (es) 2014-03-31
US20160046612A1 (en) 2016-02-18

Similar Documents

Publication Publication Date Title
HRP20160118T1 (hr) HETEROCIKLIÄŚKI DERIVAT KAO INHIBITOR MIKROSOMSKIH SINTAZA PROSTAGLANDINA E (mPGEs)
RU2401265C2 (ru) Соединения и композиции в качестве ингибиторов протеинкиназы
HRP20201337T1 (hr) Inhibitori lizin-specifične demetilaze-1
RU2386630C2 (ru) Соединения и композиции в качестве ингибиторов протеинтирозинкиназы
HRP20200854T1 (hr) Novi biciklički inhibitori bromodomene
JP2013544256A5 (hr)
RU2013124101A (ru) Гетероциклические амины и их применения
RU2018137194A (ru) Ингибиторы бромдомена
HRP20201469T1 (hr) Derivati tetrahidroizokinolina
JP2016523911A5 (hr)
JP2009541268A5 (hr)
HRP20180382T1 (hr) Inhibitori protein kinaze
HRP20201746T1 (hr) Aromatski derivati sulfonamida
HRP20160574T1 (hr) Pozitivni alosterni modulatori m1 receptora na bazi hinolin amida
CA2663366A1 (en) Compounds and compositions as protein kinase inhibitors
JP2011520908A5 (hr)
JP2012526803A5 (hr)
HRP20100292T1 (hr) Spojevi tropana
RU2009101911A (ru) Производные пиридина и пиразина в качестве ингибиторов mnk-киназы
RU2014153628A (ru) Производные пиридинона и пиридазинона
CA2671744A1 (en) Compounds and compositions as protein kinase inhibitors
JP2004536814A5 (hr)
JP2013528591A5 (hr)
HRP20130106T1 (hr) Imidazotriazini i imidazopirimidini kao inhibitori kinaze
JP2017500364A5 (hr)