AR091194A1 - TIAZOLES SUSTITUIDOS POR CARBOXAMIDA Y DERIVADOS RELACIONADOS COMO MODULADORES PARA EL RECEPTOR NUCLEAR HUERFANO RORg - Google Patents

TIAZOLES SUSTITUIDOS POR CARBOXAMIDA Y DERIVADOS RELACIONADOS COMO MODULADORES PARA EL RECEPTOR NUCLEAR HUERFANO RORg

Info

Publication number
AR091194A1
AR091194A1 ARP130101872A AR091194A1 AR 091194 A1 AR091194 A1 AR 091194A1 AR P130101872 A ARP130101872 A AR P130101872A AR 091194 A1 AR091194 A1 AR 091194A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkylene
cycloalkyl
heterocycloalkyl
independently selected
Prior art date
Application number
Other languages
English (en)
Inventor
Gege Christian
Steeneck Christoph
Dr Kinzel Olaf
Hoffmann Thomas
Dr Kleymann Gerald
Original Assignee
Phenex Pharmaceuticals Ag
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=49672489&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR091194(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Phenex Pharmaceuticals Ag filed Critical Phenex Pharmaceuticals Ag
Publication of AR091194A1 publication Critical patent/AR091194A1/es

Links

Classifications

    • 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
    • C07D277/32—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • 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
    • A61K31/426—1,3-Thiazoles
    • 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
    • C07D277/32—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • A61K31/4245—Oxadiazoles
    • 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
    • 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
    • A61K31/435—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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • 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
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic 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
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic 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
    • A61K31/495—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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/535—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
    • 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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines 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
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • 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
    • C07D277/32—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/36—Sulfur atoms
    • 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
    • C07D277/32—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/50—Nitrogen atoms bound to hetero atoms
    • C07D277/52—Nitrogen atoms bound to hetero atoms to sulfur atoms, e.g. sulfonamides
    • 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
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/38—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
    • 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
    • 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
    • C07D417/04—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
    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon 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
    • C07D417/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/02—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing not further condensed quinolizine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Los compuestos de la presente son útiles como medicamentos para tratar enfermedades inflamatorias y autoinmunes tales como la artritis, psoriasis, etc.. Reivindicación 1: Un compuesto representado por la fórmula (1) y la fórmula (2), un enantiómero, diastereómero, tautómero, N-óxido, solvato, formulación y sal farmacéuticamente aceptable de los mismos, en donde R²⁰¹ y R²⁰² son independientemente seleccionados de H, alquilo C₁₋₁₀, alquenilo C₂₋₁₀, alquinilo C₂₋₁₀, cicloalquilo C₃₋₁₀, heterocicloalquilo C₃₋₁₀, alquileno C₁₋₁₀-cicloalquilo C₃₋₁₀, alquileno C₁₋₁₀-heterocicloalquilo C₃₋₁₀, alquileno C₁₋₁₀-(heteroarilo de 5 miembros), alquileno C₁₋₁₀-(arilo de 6 miembros), alquileno C₁₋₁₀-(heteroarilo de 6 miembros), SO₂-alquilo C₁₋₁₀, en donde alquilo, alquenilo, alquinilo, alquileno, cicloalquilo, heterocicloalquilo, arilo y heteroarilo están no sustituidos o sustituidos con 1 a 7 sustituyentes seleccionados independientemente de oxo, CN, OR²¹¹, O-alquileno C₂₋₆-OR²¹¹, alquilo C₁₋₆, halo-alquilo C₁₋₆, halógeno, CO₂R²¹¹, CONR²¹¹R²¹², CONR²¹¹SO₂R²¹¹, COR²¹¹, SOˣR²¹¹, SO₃H, SO₂NR²¹¹R²¹², NR²¹¹COR²¹¹, NR²¹¹SO₂R²¹¹, NR²¹¹-CO-NR²¹¹R²¹², NR²¹¹-SO₂-NR²¹¹R²¹², cicloalquilo C₃₋₁₀, O-cicloalquilo C₃₋₁₀, heterocicloalquilo C₃₋₁₀, O-heterocicloalquilo C₃₋₁₀ y NR²¹¹R²¹²; o R²⁰¹ y R²⁰² cuando son tomados junto con el nitrógeno al cual están unidos completan un anillo de 3 a 8 miembros que contiene átomos de carbono y que opcionalmente contiene 1 ó 2 heteroátomos seleccionados de O, S, o N, en donde el anillo está no sustituido o sustituido con 1 a 4 sustituyentes independientemente seleccionados a partir de halógeno, oxo, CN, OR²¹¹, SOˣR²¹¹, SO₃H, NR²¹¹SO₂R²¹¹, SO₂NR²¹¹R²¹², alquileno C₀₋₆-CO₂R²¹¹, CONR²¹¹R²¹², CONR²¹¹SO₂R²¹¹, COR²¹¹, NR²¹¹-CO-R²¹¹, NR²¹¹-CO-NR²¹¹R²¹², NR²-SO₂-NR²¹¹R²¹², NR²¹¹R²¹², alquilo C₁₋₆, halo-alquilo C₁₋₆, hidroxi-alquilo C₁₋₆, cicloalquilo C₃₋₈, O-cicloalquilo C₃₋₈, heterocicloalquilo C₃₋₈ y O-heterocicloalquilo C₃₋₈, en donde cicloalquilo y heterocicloalquilo están no sustituidos o sustituidos con 1 a 4 sustituyentes seleccionados independientemente de halógeno, alquilo C₁₋₃, halo-alquilo C₁₋₃, OH, O-alquilo C₁₋₃, O-halo-alquilo C₁₋₃, SO₂-alquilo C₁₋₃, COOH y oxo; R²⁰³ es seleccionado de alquilo C₁₋₁₀, fluoro-alquilo C₁₋₁₀, alquileno C₀₋₆-cicloalquilo C₃₋₁₀, alquileno C₀₋₆-heterocicloalquilo C₃₋₁₀, alquileno C₀₋₆-(arilo de 6 a 10 miembros), alquileno C₀₋₆-(heteroarilo de 5 a 10 miembros), en donde alquilo, alquileno, cicloalquilo, heterocicloalquilo, arilo y heteroarilo están no sustituidos o sustituidos con 1 a 6 sustituyentes seleccionados independientemente de oxo, halógeno, CN, alquilo C₁₋₆, halo-alquilo C₁₋₆, cicloalquilo C₃₋₆, heterocicloalquilo C₃₋₆, OR²¹², CO₂R²¹², CONR²¹²R²¹², COR²¹²; y en donde opcionalmente una unidad CH₂ en alquilo o alquileno puede ser reemplazada por O, SOˣ, NH o N(-alquilo C₁₋₃); R²⁰⁴ es un resto de fórmula (3), en donde R²⁰⁵ y R²⁰⁶ es independientemente seleccionado de H, alquilo C₁₋₆, halo-alquilo C₁₋₆, alquileno C₀₋₆-cicloalquilo C₃₋₈, alquileno C₀₋₆-heterocicloalquilo C₃₋₈, heteroarilo de 5 ó 6 miembros y arilo de 6 miembros, en donde alquilo, alquileno, cicloalquilo, heterocicloalquilo, arilo y heteroarilo están no sustituidos o sustituidos con 1 a 6 sustituyentes seleccionados independientemente de halógeno, CN, OH, oxo, alquilo C₁₋₃, halo-alquilo C₁₋₃, O-alquilo C₁₋₃, O-halo-alquilo C₁₋₃ y SO₂-alquilo C₁₋₃, NR²¹¹R²¹², CO₂R²¹² y CONR²¹¹R²¹²; y opcionalmente en donde R²⁰⁵ y R²⁰⁶ cuando se toman junto con el nitrógeno al cual están unidos completan un anillo de 3 a 8 miembros que contiene átomos de carbono y opcionalmente contiene 1 ó 2 heteroátomos seleccionados de O, S o N, en donde el anillo está no sustituido o sustituido con 1 a 4 sustituyentes seleccionados independientemente de flúor, OH, oxo, alquilo C₁₋₄ y halo-alquilo C₁₋₄; R²⁰⁷ es independientemente seleccionado de N y CR²⁰⁸; o dos R²⁰⁷ adyacentes forman un anillo insaturado o parcialmente saturado de 5 a 6 miembros que contiene átomos de carbono y que opcionalmente contiene 1 ó 2 heteroátomos seleccionados de O, S o N, en donde el anillo está no-sustituido o sustituido con uno a cuatro sustituyentes seleccionados independientemente de halógeno, OH, oxo, alquilo C₁₋₄ y fluoro-alquilo C₁₋₄; R²⁰⁸ es independientemente seleccionado de H, halógeno, CN, alquilo C₁₋₆, fluoro-alquilo C₁₋₆, alquileno C₁₋₄-OH, alquileno C₁₋₄-O-alquilo C₁₋₃, alquileno C₁₋₄-O-fluoro-alquilo C₁₋₃, OH, O-alquilo C₁₋₆, O-fluoro-alquilo C₁₋₆, cicloalquilo C₃₋₁₀, en donde alquileno está no sustituido o sustituido con 1 a 3 sustituyentes seleccionados de F y cicloalquilo está no sustituido o sustituido con 1 a 3 sustituyentes seleccionados independientemente de F, alquilo C₁₋₃ y fluoro-alquilo C₁₋₃; R²⁰⁹ es seleccionado de H, halógeno, CN, alquilo C₁₋₃ y fluoro-alquilo C₁₋₃; R²¹¹ es seleccionado independientemente de H, alquilo C₁₋₆, alquileno C₀₋₆-cicloalquilo C₃₋₁₀ y alquileno C₀₋₆-heterocicloalquilo C₃₋₁₀, en donde alquilo, alquileno, cicloalquilo y heterocicloalquilo están no sustituidos o sustituidos con 1 a 6 sustituyentes seleccionados del grupo que consiste de halógeno, CN, OH, oxo, alquilo C₁₋₃, halo-alquilo C₁₋₃, O-alquilo C₁₋₃, O-halo-alquilo C₁₋₃, NH₂, NH(alquilo C₁₋₃), N(alquilo C₁₋₃)₂, heterocicloalquilo C₃₋₆, cicloalquilo C₃₋₆ y SO₂-alquilo C₁₋₃, en donde cicloalquilo y heterocicloalquilo están no sustituidos o sustituidos con 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste de F, OH, oxo, Me y CF₃; R²¹² es seleccionado independientemente de H, alquilo C₁₋₆, halo-alquilo C₁₋₆ y cicloalquilo C₃₋₆; X²⁰⁰ es seleccionado de N y CR²⁰⁹; Y²⁰⁰ es seleccionado de O y S; x es seleccionado independientemente de 0, 1 y 2; con la condición de que 4-fenil-5-(4-sulfamoilfenil)oxazol-2-carboxamida está excluido.
ARP130101872 2012-05-31 2013-05-29 TIAZOLES SUSTITUIDOS POR CARBOXAMIDA Y DERIVADOS RELACIONADOS COMO MODULADORES PARA EL RECEPTOR NUCLEAR HUERFANO RORg AR091194A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12004186 2012-05-31

Publications (1)

Publication Number Publication Date
AR091194A1 true AR091194A1 (es) 2015-01-21

Family

ID=49672489

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130101872 AR091194A1 (es) 2012-05-31 2013-05-29 TIAZOLES SUSTITUIDOS POR CARBOXAMIDA Y DERIVADOS RELACIONADOS COMO MODULADORES PARA EL RECEPTOR NUCLEAR HUERFANO RORg

Country Status (26)

Country Link
US (1) US10301272B2 (es)
EP (1) EP2855440A1 (es)
JP (1) JP6225178B2 (es)
KR (1) KR101742954B1 (es)
CN (2) CN107007597A (es)
AR (1) AR091194A1 (es)
AU (1) AU2013270036B2 (es)
BR (1) BR112014029868A2 (es)
CA (1) CA2873877C (es)
CL (1) CL2014003277A1 (es)
CO (1) CO7160113A2 (es)
CR (1) CR20150003A (es)
EA (2) EA201791271A1 (es)
GT (1) GT201400275A (es)
HK (1) HK1209117A1 (es)
IL (1) IL235626B (es)
MX (1) MX2014014614A (es)
NO (1) NO20141395A1 (es)
NZ (1) NZ702539A (es)
PE (1) PE20150229A1 (es)
PH (1) PH12014502570A1 (es)
SG (1) SG11201407919WA (es)
TW (1) TWI511960B (es)
UA (1) UA117913C2 (es)
UY (1) UY34832A (es)
WO (1) WO2013178362A1 (es)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9926309B2 (en) 2011-10-05 2018-03-27 The Board Of Trustees Of The Leland Stanford Junior University Pi-kinase inhibitors with anti-infective activity
JO3407B1 (ar) 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
JO3215B1 (ar) 2012-08-09 2018-03-08 Phenex Pharmaceuticals Ag حلقات غير متجانسة بها 5 ذرات تحتوي على النيتروجين بها استبدال بكربوكساميد أو سلفوناميد كمعدلات لمستقبل نووي غير محمي RORy
LT3027603T (lt) * 2013-08-02 2018-08-10 Pfizer Inc. Heterobicikloarilo rorc2 inhibitoriai ir jų panaudojimo būdai
JP2017502070A (ja) * 2014-01-10 2017-01-19 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ＲＯＲｃモジュレーターとしてのヘテロアリールスルタム誘導体
SG11201606080SA (en) 2014-02-03 2016-08-30 Vitae Pharmaceuticals Inc Dihydropyrrolopyridine inhibitors of ror-gamma
RU2705800C2 (ru) 2014-06-06 2019-11-12 Рисерч Трайэнгл Инститьют Агонисты рецептора апелина (apj) и их применение
MA40759A (fr) 2014-09-26 2017-08-01 Pfizer Modulateurs de rorc2 de type pyrrolopyridine substitué par un méthyle et trifluorométhyle et leurs procédés d'utilisation
PT3207043T (pt) 2014-10-14 2019-03-25 Vitae Pharmaceuticals Llc Inibidores de di-hidropirrolopiridina de ror-gama
JOP20200117A1 (ar) * 2014-10-30 2017-06-16 Janssen Pharmaceutica Nv كحولات ثلاثي فلوروميثيل كمُعدلات للمستقبل النووي جاما تي المرتبط بحمض الريتيونَويك ROR?t
CN108064224B (zh) * 2014-10-30 2022-03-29 詹森药业有限公司 作为Rorγt的调节剂的酰胺取代的噻唑
JP6661630B2 (ja) 2014-10-30 2020-03-11 ヤンセン ファーマシューティカ エヌ．ベー． ＲＯＲγｔのモジュレーターとしてのチアゾール
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
US9845308B2 (en) 2014-11-05 2017-12-19 Vitae Pharmaceuticals, Inc. Isoindoline inhibitors of ROR-gamma
EP3101008A1 (en) * 2015-06-05 2016-12-07 Lead Pharma Cel Models IP B.V. Ror gamma (rory) modulators
EP3101009A1 (en) * 2015-06-05 2016-12-07 Lead Pharma Cel Models IP B.V. Ror gamma (rory) modulators
EP3101006A1 (en) * 2015-06-05 2016-12-07 Lead Pharma Cel Models IP B.V. Ror gamma (rory) modulators
CN105017143B (zh) * 2015-07-21 2018-06-26 中国科学院上海有机化学研究所 N-三氟甲氧基吡啶盐类化合物及其制备方法和用途
ES2856931T3 (es) 2015-08-05 2021-09-28 Vitae Pharmaceuticals Llc Moduladores de ROR-gamma
AR105821A1 (es) * 2015-09-09 2017-11-15 Lilly Co Eli COMPUESTOS ÚTILES PARA INHIBIR ROR-g-T
EP3377482B1 (en) 2015-11-20 2021-05-12 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
MA43417A (fr) 2015-12-09 2018-10-17 Res Triangle Inst Agonistes améliorés du récepteur de l'apéline (apj) et leurs utilisations
TWI757266B (zh) 2016-01-29 2022-03-11 美商維它藥物有限責任公司 ＲＯＲ－γ調節劑
TWI691486B (zh) * 2016-01-29 2020-04-21 日商東麗股份有限公司 環狀胺衍生物及其醫藥用途
WO2017147526A1 (en) 2016-02-26 2017-08-31 The Board Of Trustees Of The Leland Stanford Junior University Pi-kinase inhibitors with anti-infective activity
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
US9481674B1 (en) 2016-06-10 2016-11-01 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
US11926612B2 (en) * 2016-10-12 2024-03-12 Research Triangle Institute Heterocyclic apelin receptor (APJ) agonists and uses thereof
JP2020142989A (ja) * 2017-06-21 2020-09-10 Ｍｅｉｊｉ Ｓｅｉｋａファルマ株式会社 イミダゾール誘導体及びそれを含有する医薬
AR112461A1 (es) 2017-07-24 2019-10-30 Vitae Pharmaceuticals Inc PROCESOS PARA LA PRODUCCIÓN DE SALES Y FORMAS CRISTALINAS DE INHIBIDORES DE RORg
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
CN110913859A (zh) * 2017-07-27 2020-03-24 东丽株式会社 圆形脱毛症的治疗剂或预防剂
WO2019022234A1 (ja) * 2017-07-27 2019-01-31 東レ株式会社 炎症性腸疾患の治療剤又は予防剤
CN109593068B (zh) * 2017-09-30 2022-12-27 广东东阳光药业有限公司 一种RORγ抑制剂的中间体及其制备方法
WO2019244001A1 (en) 2018-06-18 2019-12-26 Janssen Pharmaceutica Nv 6-aminopyridin-3-yl pyrazoles as modulators of roryt
ES2929140T3 (es) 2018-06-18 2022-11-25 Janssen Pharmaceutica Nv Imidazoles sustituidos con fenilo y piridinilo como moduladores de RORgammat
US10975037B2 (en) 2018-06-18 2021-04-13 Janssen Pharmaceutica Nv Phenyl substituted pyrazoles as modulators of RORγt
CN112292373A (zh) 2018-06-18 2021-01-29 詹森药业有限公司 作为RORγt的调节剂的吡啶基吡唑类
CN111484505B (zh) * 2019-01-28 2022-11-15 正大天晴药业集团股份有限公司 一种双环RORγ抑制剂的盐酸盐结晶型
IL285889B1 (en) 2019-03-12 2024-05-01 Cyteir Therapeutics Inc RAD51 inhibitors
CN111728967A (zh) * 2019-03-25 2020-10-02 深圳先进技术研究院 穿心莲内酯在抑制破骨细胞形成及其活化中的应用
CA3148216A1 (en) 2019-07-23 2021-01-28 Bayer Aktiengesellschaft Novel heteroaryl-triazole compounds as pesticides
MX2022005260A (es) * 2019-10-31 2022-06-09 Jiangsu Hengrui Medicine Co Sal de adicion acida de regulador rorgamma.
TW202136248A (zh) 2019-11-25 2021-10-01 德商拜耳廠股份有限公司 作為殺蟲劑之新穎雜芳基-三唑化合物
TW202208347A (zh) 2020-05-06 2022-03-01 德商拜耳廠股份有限公司 作為殺蟲劑之新穎雜芳基三唑化合物
CN111658651B (zh) * 2020-06-08 2021-08-03 重庆医科大学附属第一医院 CQMU151在制备治疗Th17细胞介导自身免疫病药物中的应用
CN113717080A (zh) * 2021-10-09 2021-11-30 西安瑞联新材料股份有限公司 一种4-氯-2-氰基苯磺酰氯的合成方法

Family Cites Families (86)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3669160D1 (en) 1985-03-27 1990-04-05 Zenyaku Kogyo Kk Thiazolderivate.
CA2012716A1 (en) 1989-03-22 1990-09-22 Akito Tanaka Thiazole compounds, processes for the preparation thereof and pharmaceutical composition comprising the same
GB9012936D0 (en) 1990-06-11 1990-08-01 Fujisawa Pharmaceutical Co Thiophene derivatives,processes for preparation thereof and pharmaceutical composition comprising the same
US5571810A (en) * 1990-06-11 1996-11-05 Fujisawa Pharmaceutical Co., Ltd. Thiophene derivatives
US5519040A (en) 1994-04-29 1996-05-21 Allergan Substituted thiazole sulfonamides as antiglaucoma agents
WO1996003392A1 (en) 1994-07-27 1996-02-08 G.D. Searle & Co. Substituted thiazoles for the treatment of inflammation
EP0825989A1 (en) 1995-05-19 1998-03-04 G.D. Searle & Co. Substituted oxazoles for the treatment of inflammation
ATE236890T1 (de) 1996-12-23 2003-04-15 Bristol Myers Squibb Pharma Co Sauerstoff oder schwefel enthaltende 5-gliedrige heteroaromatishe derivative als factor xa hemmer
PT853083E (pt) * 1997-01-06 2001-12-28 Pfizer Composto de piridilfurano e piridiltiofeno e sua utilizacao farmaceutica
US6413997B1 (en) 1998-10-23 2002-07-02 Dow Agrosciences Llc 3-(substituted phenyl)-5-(substituted heterocyclyl)-1,2,4-triazole compounds
AU2164300A (en) 1998-12-04 2000-06-26 N.V. Organon Substituted thiazoles for treatment of human diseases involving modulators of p-, l- and e- selectin
SE0102315D0 (sv) 2001-06-28 2001-06-28 Astrazeneca Ab Compounds
US20030236293A1 (en) 2001-09-18 2003-12-25 Pharmacia Corporation Compositions of tricyclic cyclooxygenase-2 selective inhibitors and acetaminophen for treatment and prevention of inflammation, inflammation-mediated disorders and pain
JP2005511613A (ja) * 2001-11-08 2005-04-28 ファルマシア アンド アップジョン カンパニー リミティド ライアビリティー カンパニー 疾患治療用アザビシクロ置換ヘテロアリール化合物
US20050113283A1 (en) 2002-01-18 2005-05-26 David Solow-Cordero Methods of treating conditions associated with an EDG-4 receptor
US20070060584A1 (en) 2003-04-18 2007-03-15 Chakravarty Prasun K Biaryl substituted thiazoles, oxazoles and imidazoles as sodium channel blockers
NZ544040A (en) * 2003-05-22 2009-03-31 Nycomed Gmbh Composition comprising a PDE4 inhibitor and a PDE5 inhibitor
TWI376370B (en) 2003-07-23 2012-11-11 Synta Pharmaceuticals Corp Compounds for inflammation and immune-related uses
US7211668B2 (en) * 2003-07-28 2007-05-01 Panagene, Inc. PNA monomer and precursor
EP1653952A4 (en) * 2003-08-06 2007-04-04 Pfizer Prod Inc OXAZOLE COMPOUNDS FOR THE TREATMENT OF NEURODEEGENERATIVE DISORDER
JP2007502307A (ja) 2003-08-15 2007-02-08 アストラゼネカ アクチボラグ グルタミン酸ラセマーゼ（ｍｕｒｉ）の阻害剤としての縮合複素環
SA04250288B1 (ar) * 2003-09-19 2008-07-19 سولفاي فارماسوتيكالز بي . في مشتقات ثيازول thiazole كمعدلات لمستقبل المكونات الكيميائية للقنب cannabinoid
TW200529860A (en) 2003-12-22 2005-09-16 Astrazeneca Ab Nicotinic acetylcholine receptor ligands
US7297168B2 (en) 2004-02-02 2007-11-20 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
CA2561724A1 (en) * 2004-04-02 2005-11-03 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of rock and other protein kinases
AU2005236055B2 (en) * 2004-04-20 2011-10-06 Transtech Pharma, Llc Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators
ZA200700751B (en) * 2004-06-30 2008-08-27 Vertex Pharma Azalndoles useful as inhibitors of protein kinases
EP2325184A1 (en) * 2004-06-30 2011-05-25 Vertex Pharmceuticals Incorporated Azaindoles useful as inhibitors of protein kinases
JP5122280B2 (ja) * 2004-06-30 2013-01-16 バーテックス ファーマシューティカルズ インコーポレイテッド タンパク質キナーゼのインヒビターとして有用なアザインドール
JP4942654B2 (ja) 2004-08-23 2012-05-30 イーライ リリー アンド カンパニー ヒスタミンｈ３受容体薬剤、製剤及び治療的使用
JPWO2006082952A1 (ja) 2005-02-01 2008-06-26 武田薬品工業株式会社 アミド化合物
US7759337B2 (en) * 2005-03-03 2010-07-20 Amgen Inc. Phthalazine compounds and methods of use
EP1894930A4 (en) 2005-06-23 2010-06-23 Kyowa Hakko Kirin Co Ltd THIAZOLE DERIVATIVE
JP5121453B2 (ja) 2005-08-02 2013-01-16 協和発酵キリン株式会社 睡眠障害の治療および／または予防剤
KR20140107671A (ko) 2005-12-30 2014-09-04 머크 샤프 앤드 돔 코포레이션 Ｃｅｔｐ 억제제로서 유용한 1,3-옥사졸리딘-2-온 유도체
TWI417096B (zh) 2006-01-25 2013-12-01 Synta Pharmaceuticals Corp 用於發炎及免疫相關用途之苯基及吡啶基化合物
US8455658B2 (en) * 2006-01-25 2013-06-04 Synta Pharmaceuticals Corp. Thiazole and thiadiazole compounds for inflammation and immune-related uses
WO2007125049A1 (en) 2006-04-27 2007-11-08 Solvay Pharmaceuticals Gmbh Use of cbx cannabinoid receptor modulators as potassium channel modulators
CN101432400B (zh) * 2006-05-01 2012-11-14 国际壳牌研究有限公司 气化反应器及其应用
CN101096363B (zh) 2006-06-27 2011-05-11 中国人民解放军军事医学科学院毒物药物研究所 2,4,5-三取代噻唑类化合物、其制备方法、药物组合物及其制药用途
WO2008022281A1 (en) 2006-08-16 2008-02-21 The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone Small molecule inhibitors of kynurenine-3-monooxygenase
WO2008083070A1 (en) 2006-12-29 2008-07-10 Neurogen Corporation Crf1 receptor ligands comprising fused bicyclic heteroaryl moieties
US20090317360A1 (en) 2007-06-12 2009-12-24 Genelabs Technologies, Inc. Anti-viral inhibitors and methods of use
WO2009037247A1 (en) 2007-09-17 2009-03-26 Neurosearch A/S Pyrazine derivatives and their use as potassium channel modulators
EP2320737B1 (en) 2008-08-05 2013-07-17 Merck Sharp & Dohme Corp. Pyrazolo-[1,5-a]-pyridines as mark inhibitors
EP2181710A1 (en) 2008-10-28 2010-05-05 Phenex Pharmaceuticals AG Ligands for modulation of orphan receptor-gamma (NR1F3) activity
EP2367824B1 (en) 2008-12-23 2016-03-23 AbbVie Inc. Anti-viral derivatives of pyrimidine
WO2010083145A1 (en) 2009-01-16 2010-07-22 Merck Sharp & Dohme Corp. IMIDAZO[1,2-a]PYRIDINES AND IMIDAZO[1,2-b]PYRIDAZINES AS MARK INHIBITORS
US8946231B2 (en) 2009-03-23 2015-02-03 Merck Sharp & Dohme Corp. P2X3, receptor antagonists for treatment of pain
NZ596388A (en) 2009-04-22 2013-05-31 Actelion Pharmaceuticals Ltd Thiazole derivatives and their use as p2y12 receptor antagonists
EP2368886A1 (en) 2010-03-01 2011-09-28 Phenex Pharmaceuticals AG Novel compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (ROR gamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune desease
CN104592205A (zh) 2010-03-01 2015-05-06 Gtx公司 用于治疗癌的化合物
WO2011112264A1 (en) 2010-03-11 2011-09-15 New York University Compounds as rorϒt modulators and uses thereof
US9492439B2 (en) 2010-03-11 2016-11-15 New York University Amido compounds as RORγt modulators and uses thereof
US8343970B2 (en) 2010-03-12 2013-01-01 Omeros Corporation PDE10 inhibitors and related compositions and methods
WO2011115892A1 (en) * 2010-03-15 2011-09-22 Griffin Patrick R Modulators of the retinoic acid receptor-related orphan receptors
WO2012007500A2 (de) * 2010-07-15 2012-01-19 Bayer Cropscience Ag Neue heterocyclische verbindungen als schädlingsbekämpfungsmittel
WO2012028100A1 (en) * 2010-09-01 2012-03-08 Glaxo Group Limited Novel compounds
WO2012027965A1 (en) 2010-09-01 2012-03-08 Glaxo Group Limited Novel compounds
EP2638014B1 (en) 2010-11-08 2017-01-04 Lycera Corporation N-sulfonylated tetrahydroquinolines and related bicyclic compounds for inhibition of ror-gamma activity and the treatment of diseases
US9505798B2 (en) 2010-11-29 2016-11-29 New York University Steroid compounds as RORyt modulators and uses thereof
WO2012100732A1 (en) * 2011-01-24 2012-08-02 Glaxo Group Limited Retinoid-related orphan receptor gamma modulators, composition containing them and uses thereof
WO2012100734A1 (en) 2011-01-24 2012-08-02 Glaxo Group Limited Compounds useful as retinoid-related orphan receptor gamma modulators
RU2013139662A (ru) 2011-01-28 2015-03-10 4-Эс-Си Дискавери Гмбх Ингибирование il17 и ifn-гамма для лечения аутоиммунного воспаления
PL2668182T3 (pl) 2011-01-28 2018-11-30 Immunic Ag Inhibitowanie IL17 i IFN-gamma do leczenia zapalenia autoimmunologicznego
EP2487159A1 (en) 2011-02-11 2012-08-15 MSD Oss B.V. RorgammaT inhibitors
EP2511263A1 (en) 2011-04-14 2012-10-17 Phenex Pharmaceuticals AG Pyrrolo sulfonamide compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (RORgamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases
WO2012145254A2 (en) 2011-04-16 2012-10-26 Board Of Regents, The University Of Texas System Methods of using inhibitors of rorϒt to treat disease
BR112013027670B1 (pt) 2011-04-28 2021-11-09 Japan Tobacco Inc Composto de amida, composição farmacêutica e medicamento que o compreende e antagonista de rory
US9586928B2 (en) 2011-05-16 2017-03-07 The Scripps Research Institute Modulators of the nuclear hormone receptor ROR
WO2013000871A1 (en) 2011-06-27 2013-01-03 Galderma Research & Development New th-17 differentiation markers for rosacea and uses thereof
US20140235475A1 (en) 2011-06-27 2014-08-21 Isabelle Carlavan Th17 differentiation markers for acne and uses thereof
CA2841905A1 (en) 2011-07-26 2013-01-31 Sanofi 3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals
RU2617843C2 (ru) 2011-07-26 2017-04-28 Санофи Замещенные производные 3-тиазолоаминопропионовой кислоты и их применение в качестве фармацевтических препаратов
US20140155419A1 (en) 2011-07-29 2014-06-05 Erkan Baloglu Compounds and methods
US20140256740A1 (en) 2011-07-29 2014-09-11 Tempero Pharmaceuticals, Inc. Compounds and methods
EP2736332A4 (en) 2011-07-29 2015-03-18 Tempero Pharmaceuticals Inc CONNECTIONS AND METHODS
EP2738170B1 (en) 2011-07-29 2017-08-30 Takeda Pharmaceutical Company Limited Heterocyclic compound
WO2013019682A1 (en) 2011-07-29 2013-02-07 Tempero Pharmaceuticals, Inc. Compounds and methods
WO2013029338A1 (en) 2011-09-01 2013-03-07 Glaxo Group Limited Novel compounds
KR20140072090A (ko) 2011-09-09 2014-06-12 뉴욕 유니버시티 ＲＯＲγｔ 조정제로서의 아미도 화합물 및 이의 용도
BR112014003704A2 (pt) 2011-09-19 2017-03-07 Eth Zuerich moduladores ror gama
US9120776B2 (en) 2011-09-22 2015-09-01 Takeda Pharmaceutical Company Limited Condensed heterocyclic compound
GB201116641D0 (en) 2011-09-27 2011-11-09 Glaxo Group Ltd Novel compounds
JP5918859B2 (ja) 2011-12-02 2016-05-18 フェネックス ファーマシューティカルス アーゲー オーファン核内受容体ＲＡＲに関連するオーファン受容体−ガンマ（ＲＯＲγ、ＮＲ１Ｆ３）活性の調整剤としての、慢性の炎症性疾患および自己免疫性疾患を治療するためのピロロカルボキサミド
US9388196B2 (en) * 2012-03-06 2016-07-12 Lupin Limited Thiazole derivatives as alpha 7 nAChR modulators

Also Published As

Publication number Publication date
CN104603118A (zh) 2015-05-06
UA117913C2 (uk) 2018-10-25
MX2014014614A (es) 2015-02-12
IL235626B (en) 2018-11-29
CA2873877C (en) 2018-08-07
US10301272B2 (en) 2019-05-28
CO7160113A2 (es) 2015-01-15
AU2013270036B2 (en) 2016-12-01
TWI511960B (zh) 2015-12-11
TW201400465A (zh) 2014-01-01
NO20141395A1 (no) 2014-12-30
UY34832A (es) 2013-12-31
GT201400275A (es) 2017-08-24
CN104603118B (zh) 2017-10-03
KR101742954B1 (ko) 2017-06-02
BR112014029868A2 (pt) 2017-06-27
EA201791271A1 (ru) 2018-01-31
PH12014502570A1 (en) 2015-01-21
CL2014003277A1 (es) 2015-07-10
EA028330B1 (ru) 2017-11-30
SG11201407919WA (en) 2014-12-30
JP2015521193A (ja) 2015-07-27
HK1209117A1 (en) 2016-03-24
IL235626A0 (en) 2015-02-01
EP2855440A1 (en) 2015-04-08
EA201491943A1 (ru) 2015-07-30
PE20150229A1 (es) 2015-03-02
CR20150003A (es) 2015-04-23
WO2013178362A1 (en) 2013-12-05
CN107007597A (zh) 2017-08-04
JP6225178B2 (ja) 2017-11-01
US20150175562A1 (en) 2015-06-25
AU2013270036A1 (en) 2014-11-27
KR20150015031A (ko) 2015-02-09
NZ702539A (en) 2016-11-25
CA2873877A1 (en) 2013-12-05

Similar Documents

Publication Publication Date Title
AR091194A1 (es) TIAZOLES SUSTITUIDOS POR CARBOXAMIDA Y DERIVADOS RELACIONADOS COMO MODULADORES PARA EL RECEPTOR NUCLEAR HUERFANO RORg
HRP20191901T1 (hr) Ciklizirani derivati sulfamoilarilamida i njihova uporaba kao lijekova za liječenje hepatitisa b
AR091193A1 (es) HETEROCICLOS DE 5 MIEMBROS QUE CONTIENEN NITROGENO SUSTITUIDO POR CARBOXAMIDA O SULFONAMIDA COMO MODULADORES PARA EL RECEPTOR NUCLEAR HUERFANO RORg
ECSP18094790A (es) Piridinas sustituidas con heteroarilo y métodos de uso referencia cruzada a solicitudes relacionadas
AR086019A1 (es) COMPUESTOS DE PIRROLO SULFONAMIDA PARA MODULACION DE LA ACTIVIDAD DEL RECEPTOR HUERFANO g RELACIONADO AL RECEPTOR NUCLEAR HUERFANO RAR (RORg, NR1F3) Y PARA EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS Y AUTOINMUNES CRONICAS
AR103064A1 (es) Compuestos moduladores de fxr (nr1h4)
AR105845A1 (es) Compuestos de heteroarilo bicíclicos fusionados como moduladores de la función irak4
AR113909A1 (es) Compuestos y sus composiciones farmacéuticas para el tratamiento de hepatitis b
AR097431A1 (es) Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de quinasas pim
AR100442A1 (es) Derivados de pirido[1,2-a]pirimidin-4-ona para tratar atrofia muscular espinal
EA201690989A1 (ru) Ингибиторы syk
AR095609A1 (es) Compuestos de pirrolopiridina
RU2016135922A (ru) Терапевтические соединения и композиции
AR079226A1 (es) Espiroindolinona- pirrolidinas, procesos de preparacion y uso de los mismos para el tratamiento y profilaxis del cancer
ES2631611T3 (es) Amidas de piperidina de Pirano-Espirociclico como moduladores de canales iónicos
AR085549A1 (es) DERIVADOS TRIAZOLIL PIPERAZINA Y TRIAZOLIL PIPERIDINA SUSTITUIDOS COMO MODULADORES DE g SECRETASA
AR085489A1 (es) Derivados de triazolopiridinas, composiciones farmaceuticas que los contienen, proceso para prepararlos, intermediarios de dicho proceso y uso de los mismos para el tratamiento de enfermedades autoinmunes e inflamatorias
EA201690135A1 (ru) Трициклические соединения бензоксаборола и их применение
EA201391558A1 (ru) Тетрагидропиразоло[1,5-а]пиримидины как противотуберкулезные соединения
ES2626801T3 (es) Compuestos de triazolopiridina como inhibidores de pde10a
AR098522A1 (es) Compuesto de triazolo-piridina
EA201791816A1 (ru) Ингибиторы kv1.3 и их применение в медицине
AR092749A1 (es) Compuestos farmaceuticos
EA201791671A1 (ru) 4-замещенные соединения бензоксаборола и их применение
MY185971A (en) Pyranodipyridine compound

Legal Events

Date Code Title Description
FB Suspension of granting procedure