EA201590092A1 - АЗОТСОДЕРЖАЩИЕ 5-ЧЛЕННЫЕ ГЕТЕРОЦИКЛЫ, ЗАМЕЩЕННЫЕ КАРБОКСАМИДОМ ИЛИ СУЛЬФОНАМИДОМ, В КАЧЕСТВЕ МОДУЛЯТОРОВ ДЛЯ ЯДЕРНОГО ОРФАНОВОГО РЕЦЕПТОРА RORγ - Google Patents

АЗОТСОДЕРЖАЩИЕ 5-ЧЛЕННЫЕ ГЕТЕРОЦИКЛЫ, ЗАМЕЩЕННЫЕ КАРБОКСАМИДОМ ИЛИ СУЛЬФОНАМИДОМ, В КАЧЕСТВЕ МОДУЛЯТОРОВ ДЛЯ ЯДЕРНОГО ОРФАНОВОГО РЕЦЕПТОРА RORγ

Info

Publication number
EA201590092A1
EA201590092A1 EA201590092A EA201590092A EA201590092A1 EA 201590092 A1 EA201590092 A1 EA 201590092A1 EA 201590092 A EA201590092 A EA 201590092A EA 201590092 A EA201590092 A EA 201590092A EA 201590092 A1 EA201590092 A1 EA 201590092A1
Authority
EA
Eurasian Patent Office
Prior art keywords
modulators
carboxamide
rorγ
sulphonamide
nitrogen
Prior art date
Application number
EA201590092A
Other languages
English (en)
Other versions
EA027953B1 (ru
EA027953B9 (ru
Inventor
Кристиан Геге
Олаф Кинцель
Кристоф Штеенек
Джеральд Клейманн
Томас Хоффманн
Original Assignee
Фенекс Фармасьютикалз Аг
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=46754230&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201590092(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Фенекс Фармасьютикалз Аг filed Critical Фенекс Фармасьютикалз Аг
Publication of EA201590092A1 publication Critical patent/EA201590092A1/ru
Publication of EA027953B1 publication Critical patent/EA027953B1/ru
Publication of EA027953B9 publication Critical patent/EA027953B9/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • 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
    • 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
    • A61P17/06—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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole 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
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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
    • 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
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

В настоящем изобретении предложены модуляторы для ядерного орфанового рецептора RORγ и способы лечения заболеваний, опосредованных RORγ, путем введения указанных новых модуляторов RORγ человеку или млекопитающему, нуждающемуся в указанном лечении. В частности, в настоящем изобретении предложены циклические соединения, содержащие карбоксамид, формул (1)-(5)энантиомеры, диастереомеры, таутомеры, N-оксиды, сольваты и фармацевтически приемлемые соли указанных соединений.
EA201590092A 2012-08-09 2013-05-29 АЗОТСОДЕРЖАЩИЕ 5-ЧЛЕННЫЕ ГЕТЕРОЦИКЛЫ, ЗАМЕЩЕННЫЕ КАРБОКСАМИДОМ ИЛИ СУЛЬФОНАМИДОМ, В КАЧЕСТВЕ МОДУЛЯТОРОВ ДЛЯ ЯДЕРНОГО ОРФАНОВОГО РЕЦЕПТОРА RORγ EA027953B9 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261681296P 2012-08-09 2012-08-09
EP12005789 2012-08-09
PCT/EP2013/001594 WO2014023367A1 (en) 2012-08-09 2013-05-29 Carboxamide or sulfonamide substituted nitrogen-containing 5-membered heterocycles as modulators for the orphan nuclear receptor ror gamma

Publications (3)

Publication Number Publication Date
EA201590092A1 true EA201590092A1 (ru) 2015-08-31
EA027953B1 EA027953B1 (ru) 2017-09-29
EA027953B9 EA027953B9 (ru) 2018-01-31

Family

ID=46754230

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201590092A EA027953B9 (ru) 2012-08-09 2013-05-29 АЗОТСОДЕРЖАЩИЕ 5-ЧЛЕННЫЕ ГЕТЕРОЦИКЛЫ, ЗАМЕЩЕННЫЕ КАРБОКСАМИДОМ ИЛИ СУЛЬФОНАМИДОМ, В КАЧЕСТВЕ МОДУЛЯТОРОВ ДЛЯ ЯДЕРНОГО ОРФАНОВОГО РЕЦЕПТОРА RORγ

Country Status (28)

Country Link
US (1) US9458104B2 (ru)
EP (2) EP3118189A1 (ru)
JP (1) JP6097829B2 (ru)
KR (1) KR101732973B1 (ru)
CN (1) CN104603105B (ru)
AR (1) AR091193A1 (ru)
AU (1) AU2013301914B2 (ru)
BR (1) BR112015002738A2 (ru)
CA (1) CA2879478C (ru)
CL (1) CL2015000300A1 (ru)
CO (1) CO7310529A2 (ru)
EA (1) EA027953B9 (ru)
GT (1) GT201500024A (ru)
HK (1) HK1211584A1 (ru)
IL (1) IL236695A (ru)
IN (1) IN2015DN01815A (ru)
JO (1) JO3215B1 (ru)
MX (1) MX364453B (ru)
NO (1) NO344067B1 (ru)
NZ (1) NZ704512A (ru)
PE (1) PE20150463A1 (ru)
PH (1) PH12015500142B1 (ru)
SG (1) SG11201500955RA (ru)
TW (2) TW201527278A (ru)
UA (1) UA115145C2 (ru)
UY (1) UY34833A (ru)
WO (1) WO2014023367A1 (ru)
ZA (1) ZA201500534B (ru)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI659019B (zh) * 2014-02-28 2019-05-11 日商帝人製藥股份有限公司 吡唑醯胺衍生物
US9868724B2 (en) * 2014-05-28 2018-01-16 Glaxosmithkline Intellectual Property Development Limited Compounds
CA2949559C (en) * 2014-06-06 2023-08-29 Research Triangle Institute Apelin receptor (apj) agonists and uses thereof
JOP20200117A1 (ar) 2014-10-30 2017-06-16 Janssen Pharmaceutica Nv كحولات ثلاثي فلوروميثيل كمُعدلات للمستقبل النووي جاما تي المرتبط بحمض الريتيونَويك ROR?t
TR201820513T4 (tr) 2014-10-30 2019-02-21 Janssen Pharmaceutica Nv Roryt modülatörleri olarak tiazoller.
EP3101006A1 (en) * 2015-06-05 2016-12-07 Lead Pharma Cel Models IP B.V. Ror gamma (rory) modulators
EP3170822A1 (en) 2015-11-18 2017-05-24 AGV Discovery Azaindole derivatives and their use as erk kinase inhibitors
RU2021133849A (ru) 2015-12-09 2022-03-21 Рисерч Трайэнгл Инститьют Улучшенные агонисты апелинового рецептора (apj) и их использование
MX2018011214A (es) * 2016-03-15 2019-03-28 Bayer Cropscience Ag Sulfonamidas sustituidas para controlar plagas animales.
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
US11926612B2 (en) * 2016-10-12 2024-03-12 Research Triangle Institute Heterocyclic apelin receptor (APJ) agonists and uses thereof
TW201822637A (zh) 2016-11-07 2018-07-01 德商拜耳廠股份有限公司 用於控制動物害蟲的經取代磺醯胺類
JP2020059651A (ja) * 2016-12-26 2020-04-16 科研製薬株式会社 ピラゾール誘導体及びそれを含有する医薬
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
US10654828B2 (en) 2017-07-28 2020-05-19 Novartis Ag Indole derivatives and uses thereof
CN109485595B (zh) * 2017-09-12 2022-05-27 江苏恒瑞医药股份有限公司 亲水性基团取代的吲哚甲酰胺类衍生物、其制备方法及其在医药上的应用
WO2019053090A1 (en) 2017-09-13 2019-03-21 Novartis Ag DIPHENYL DERIVATIVES AND USES THEREOF
PE20210550A1 (es) * 2018-02-28 2021-03-17 Japan Tobacco Inc Compuestos de 4-metildihidropirimidinona y su uso farmaceutico
CN112334450A (zh) * 2018-06-18 2021-02-05 詹森药业有限公司 作为RORγt的调节剂的苯基和吡啶基取代的咪唑
EP3790865A1 (en) * 2018-06-18 2021-03-17 Janssen Pharmaceutica NV Phenyl substituted pyrazoles as modulators of roryt
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
CA3103771A1 (en) 2018-06-18 2019-12-26 Janssen Pharmaceutica Nv 6-aminopyridin-3-yl pyrazoles as modulators of roryt
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
KR20220038402A (ko) 2019-07-23 2022-03-28 바이엘 악티엔게젤샤프트 살충제로서의 신규 헤테로아릴-트리아졸 화합물
EP4055010A1 (de) 2019-11-07 2022-09-14 Bayer Aktiengesellschaft Substituierte sulfonylamide zur bekämpfung tierischer schädlinge
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-***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***化合物
EP4212531A1 (en) 2022-01-14 2023-07-19 AGV Discovery Azaindole derivatives and their use as erk kinase inhibitors

Family Cites Families (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9012936D0 (en) * 1990-06-11 1990-08-01 Fujisawa Pharmaceutical Co Thiophene derivatives,processes for preparation thereof and pharmaceutical composition comprising the same
HRP950330A2 (en) 1994-07-05 1997-10-31 Ciba Geigy Ag New herbicides
US5776954A (en) 1996-10-30 1998-07-07 Merck & Co., Inc. Substituted pyridyl pyrroles, compositions containing such compounds and methods of use
DE19744026A1 (de) 1997-10-06 1999-04-08 Hoechst Marion Roussel De Gmbh Pyrazol-Derivate, ihre Herstellung und ihre Verwendung in Arzneimitteln
WO2000024739A1 (en) 1998-10-23 2000-05-04 Dow Agrosciences Llc 3-(substituted phenyl)-5-(substituted heterocyclyl)-1,2,4-triazole compounds
EP1224173B1 (en) 1999-10-18 2005-10-12 The University Of Connecticut Pyrazole derivatives as cannabinoid receptor antagonists
US8084467B2 (en) 1999-10-18 2011-12-27 University Of Connecticut Pyrazole derivatives as cannabinoid receptor antagonists
US7393842B2 (en) 2001-08-31 2008-07-01 University Of Connecticut Pyrazole analogs acting on cannabinoid receptors
EP1259504A1 (en) 2000-03-03 2002-11-27 Pfizer Products Inc. Pyrazole ether derivatives as anti-inflammatory/analgesic agents
SE0102315D0 (sv) 2001-06-28 2001-06-28 Astrazeneca Ab Compounds
CA2457922A1 (en) 2001-08-31 2003-03-13 University Of Connecticut Novel pyrazole analogs acting on cannabinoid receptors
WO2003037335A1 (en) 2001-11-02 2003-05-08 Pfizer Products Inc. 5-heteroatom-substituted pyrazoles
US20050113283A1 (en) 2002-01-18 2005-05-26 David Solow-Cordero Methods of treating conditions associated with an EDG-4 receptor
US7244753B2 (en) 2002-07-29 2007-07-17 Nitromed, Inc. Cyclooxygenase-2 selective inhibitors, compositions and methods of use
AU2003259749A1 (en) 2002-08-12 2004-02-25 Sugen, Inc. 3-pyrrolyl-pyridopyrazoles and 3-pyrrolyl-indazoles as novel kinase inhibitors
EP1433788A1 (en) 2002-12-23 2004-06-30 Aventis Pharma Deutschland GmbH Pyrazole-derivatives as factor Xa inhibitors
BR0317926A (pt) * 2003-01-02 2005-11-29 Hoffmann La Roche Compostos, processo para a sua manufatura, composições farmacêuticas que os compreendem, método para o tratamento e/ou profilaxia de enfermidades que estão associadas com a modulação de receptores de cb1 e utilização dos mesmos
WO2004092140A1 (en) 2003-04-03 2004-10-28 Merck & Co., Inc. Biaryl substituted pyrazoles as sodium channel blockers
JPWO2004094407A1 (ja) 2003-04-21 2006-07-13 第一製薬株式会社 ５員複素環誘導体
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
WO2005108393A1 (en) * 2004-05-10 2005-11-17 F. Hoffmann-La Roche Ag Pyrrole or imidazole amides for treating obesity
CN101228160A (zh) * 2004-06-30 2008-07-23 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吖吲哚
EP1765819B1 (en) 2004-06-30 2014-03-12 Vertex Pharmaceuticals Inc. Azaindoles useful as inhibitors of protein kinases
EA011725B1 (ru) 2004-08-26 2009-04-28 Пфайзер Инк. Пиразолзамещённые аминогетероарильные соединения в качестве ингибиторов протеинкиназы
EP1881991A1 (en) 2005-05-19 2008-01-30 Cv Therapeutics, Inc. A1 adenosine receptor agonists
WO2006133926A1 (en) * 2005-06-17 2006-12-21 Carex Sa Pyrazole derivates as cannabinoid receptor modulators
CA2613517A1 (en) 2005-06-27 2007-01-04 Exelixis, Inc. Pyrazole based lxr modulators
TW200720255A (en) * 2005-07-13 2007-06-01 Taiho Pharmaceutical Co Ltd Benzoimidazole compound capable of inhibiting prostaglandin d synthetase
WO2007024744A2 (en) 2005-08-21 2007-03-01 Exelixis, Inc. Heterocyclic carboxamide compounds as steroid nuclear receptor ligands
US20100256357A1 (en) * 2006-08-09 2010-10-07 Agouron Pharmaceuticals, Inc. Heterocycles useful as inhibitors of carbonic anhydrase
AU2007336068B2 (en) 2006-12-18 2013-05-02 7Tm Pharma A/S Modulators of CB1 receptors
EP1946778A1 (en) * 2007-01-16 2008-07-23 Laboratorios del Dr. Esteve S.A. Active substance combination for the treatment of diabetes
JP2010517970A (ja) 2007-02-02 2010-05-27 ノイロサーチ アクティーゼルスカブ ピリジニル−ピラゾール誘導体及びカリウムチャネル調節剤としてのそれらの使用
US20090069288A1 (en) 2007-07-16 2009-03-12 Breinlinger Eric C Novel therapeutic compounds
US8415358B2 (en) 2007-09-17 2013-04-09 Neurosearch A/S Pyrazine derivatives and their use as potassium channel modulators
KR100917037B1 (ko) 2007-11-01 2009-09-10 한국과학기술연구원 피라졸릴카르복스아미도알킬피페라진 유도체 및 이의제조방법
WO2009080227A2 (en) 2007-12-26 2009-07-02 Sanofi-Aventis Pyrazole-carboxamide derivatives as p2y12 antagonists
US20090197895A1 (en) 2008-01-31 2009-08-06 The Scripps Research Institute Oxazole-pyrrole-piperazine alpha-helix mimetic
CN101544631B (zh) 2008-03-26 2012-05-23 中国科学院上海药物研究所 吡唑类5-脂氧酶小分子抑制剂及其制备方法、药物组合物和应用
US8895558B2 (en) 2008-10-02 2014-11-25 Green Cross Corporation Arylpiperazine-containing pyrrole 3-carboxamide derivatives for treating depressive disorders
US20110230536A1 (en) 2008-10-24 2011-09-22 Calcimedica, Inc. Phenylpyrazole inhibitors of store operated calcium release
EP2181710A1 (en) 2008-10-28 2010-05-05 Phenex Pharmaceuticals AG Ligands for modulation of orphan receptor-gamma (NR1F3) activity
JP2012513409A (ja) 2008-12-23 2012-06-14 アボット・ラボラトリーズ 抗ウイルス化合物
EP2289883A1 (en) 2009-08-19 2011-03-02 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
TW201124409A (en) 2009-10-07 2011-07-16 Karobio Ab Novel estrogen receptor ligands
UY33200A (es) 2010-01-26 2011-08-31 Sanofi Aventis Derivados de ácido 3-heteroaroilamino-propiónico sustituidos con oxígeno y su uso como productos farmacéuticos
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
WO2011112264A1 (en) 2010-03-11 2011-09-15 New York University Compounds as rorϒt modulators and uses thereof
EP3002008B8 (en) 2010-03-11 2018-10-24 New York University Amido compounds as roryt modulators and uses thereof
WO2011115892A1 (en) 2010-03-15 2011-09-22 Griffin Patrick R Modulators of the retinoic acid receptor-related orphan receptors
WO2012027965A1 (en) 2010-09-01 2012-03-08 Glaxo Group Limited Novel compounds
WO2012028100A1 (en) 2010-09-01 2012-03-08 Glaxo Group Limited Novel compounds
WO2012064744A2 (en) 2010-11-08 2012-05-18 Lycera Corporation Tetrahydroquinoline and related bicyclic compounds for inhibition of rorϒ activity and the treatment of disease
US8722709B2 (en) 2010-11-10 2014-05-13 Boehringer Ingelheim International Gmbh Mineralocorticoid receptor antagonists
WO2012074547A2 (en) 2010-11-29 2012-06-07 New York University STEROID COMPOUNDS AS RORγt 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
JP5883034B2 (ja) 2011-01-28 2016-03-09 ４エスツェー ディスカバリー ゲゼルシャフト ミット ベシュレンクテル ハフツング 自己免疫性炎症の治療のためのＩＬ１７及びＩＦＮ−γ阻害
PT2668182T (pt) 2011-01-28 2018-01-31 4Sc Discovery Gmbh Inibição de il-7 e de ifn gama para o tratamento de inflamação autoimune
EP2487159A1 (en) 2011-02-11 2012-08-15 MSD Oss B.V. RorgammaT inhibitors
CA2736441A1 (en) 2011-04-06 2012-10-06 The Regents Of The University Of California Pyrazolylthiazole compounds as .delta.f508-cystic fibrosis transmembrane conductance regulator correctors
WO2012139930A1 (en) 2011-04-11 2012-10-18 Nerviano Medical Sciences S.R.L. Pyrazolyl-pyrimidine derivatives as kinase 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
AR086156A1 (es) 2011-04-28 2013-11-20 Japan Tobacco Inc Compuesto de amida y su uso medicinal
US9586928B2 (en) 2011-05-16 2017-03-07 The Scripps Research Institute Modulators of the nuclear hormone receptor ROR
CA2840406A1 (en) 2011-06-27 2013-01-03 Galderma Research & Development New th-17 differentiation markers for rosacea and uses thereof
CN103930565B (zh) 2011-06-27 2017-06-30 高德美研究及发展公司 用于痤疮的新th17分化标志物及其用途
ES2560381T3 (es) 2011-07-26 2016-02-18 Sanofi Derivados de ácido 3-heteroaroilamino-propiónico y su uso como productos farmacéuticos
WO2013019682A1 (en) 2011-07-29 2013-02-07 Tempero Pharmaceuticals, Inc. Compounds and methods
WO2013018695A1 (ja) 2011-07-29 2013-02-07 武田薬品工業株式会社 複素環化合物
US20140155419A1 (en) 2011-07-29 2014-06-05 Erkan Baloglu Compounds and methods
EP2736332A4 (en) 2011-07-29 2015-03-18 Tempero Pharmaceuticals Inc CONNECTIONS AND METHODS
US20140256740A1 (en) 2011-07-29 2014-09-11 Tempero Pharmaceuticals, Inc. Compounds and methods
WO2013029338A1 (en) 2011-09-01 2013-03-07 Glaxo Group Limited Novel compounds
JP2014528933A (ja) 2011-09-09 2014-10-30 ニューヨーク ユニバーシティ ＲＯＲγｔモジュレーターとしてのアミド化合物およびその使用
US9777036B2 (en) 2011-09-19 2017-10-03 ETH Zürich ROR gamma modulators
WO2013042782A1 (ja) 2011-09-22 2013-03-28 武田薬品工業株式会社 縮合複素環化合物
GB201116641D0 (en) 2011-09-27 2011-11-09 Glaxo Group Ltd Novel compounds
WO2013079223A1 (en) * 2011-12-02 2013-06-06 Phenex Pharmaceuticals Ag Pyrrolo carboxamides as modulators of orphan nuclear receptor rar-related orphan receptor-gamma (rorϒ, nr1f3) activity and for the treatment of chronic inflammatory and autoimmune diseases
SG11201407919WA (en) 2012-05-31 2014-12-30 Phenex Pharmaceuticals Ag Carboxamide or sulfonamide substituted thiazoles and related derivatives as modulators for the orphan nuclear receptor ror[gamma]

Also Published As

Publication number Publication date
AU2013301914A8 (en) 2015-02-12
NZ704512A (en) 2016-09-30
US20150344423A1 (en) 2015-12-03
PE20150463A1 (es) 2015-04-23
EA027953B1 (ru) 2017-09-29
CN104603105A (zh) 2015-05-06
GT201500024A (es) 2017-08-24
UY34833A (es) 2013-12-31
PH12015500142A1 (en) 2015-03-16
EA027953B9 (ru) 2018-01-31
EP2882710B1 (en) 2016-09-07
KR101732973B1 (ko) 2017-05-08
JO3215B1 (ar) 2018-03-08
IL236695A0 (en) 2015-02-26
MX2015001728A (es) 2015-04-14
AU2013301914B2 (en) 2016-08-18
NO20150112A1 (en) 2015-01-23
BR112015002738A2 (pt) 2018-05-22
CL2015000300A1 (es) 2015-07-10
AR091193A1 (es) 2015-01-21
EP2882710A1 (en) 2015-06-17
CO7310529A2 (es) 2015-06-30
WO2014023367A1 (en) 2014-02-13
JP2015524449A (ja) 2015-08-24
ZA201500534B (en) 2016-10-26
IL236695A (en) 2017-07-31
PH12015500142B1 (en) 2015-03-16
HK1211584A1 (en) 2016-05-27
IN2015DN01815A (ru) 2015-05-29
CN104603105B (zh) 2017-09-08
SG11201500955RA (en) 2015-03-30
NO344067B1 (en) 2019-08-26
TWI488839B (zh) 2015-06-21
EP3118189A1 (en) 2017-01-18
AU2013301914A1 (en) 2015-02-05
MX364453B (es) 2019-04-26
KR20150040354A (ko) 2015-04-14
CA2879478A1 (en) 2014-02-13
CA2879478C (en) 2017-08-22
UA115145C2 (uk) 2017-09-25
TW201527278A (zh) 2015-07-16
JP6097829B2 (ja) 2017-03-15
TW201406723A (zh) 2014-02-16
US9458104B2 (en) 2016-10-04

Similar Documents

Publication Publication Date Title
EA201590092A1 (ru) АЗОТСОДЕРЖАЩИЕ 5-ЧЛЕННЫЕ ГЕТЕРОЦИКЛЫ, ЗАМЕЩЕННЫЕ КАРБОКСАМИДОМ ИЛИ СУЛЬФОНАМИДОМ, В КАЧЕСТВЕ МОДУЛЯТОРОВ ДЛЯ ЯДЕРНОГО ОРФАНОВОГО РЕЦЕПТОРА RORγ
EA201791271A1 (ru) ТИАЗОЛЫ, ЗАМЕЩЕННЫЕ КАРБОКСАМИДОМ ИЛИ СУЛЬФОНАМИДОМ, И РОДСТВЕННЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ ДЛЯ ОРФАННОГО ЯДЕРНОГО РЕЦЕПТОРА RORγ
PH12019501321B1 (en) Use of pyrazolopyrimidine derivatives for the treatment of pi3k-delta related disorders
SA518392101B1 (ar) ROR-Gamma مشتقات البنزيميدازول في صورة مُعدلات لـ
EA201891191A1 (ru) 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения
EA202090256A1 (ru) 5-членные и бициклические гетероциклические амиды в качестве ингибиторов rock
EA201891501A1 (ru) Фталазиноны и изохинолиноны в качестве ингибиторов rock
EA200901157A1 (ru) Конденсированные кольцевые гетероциклические модуляторы киназы
EA201691368A1 (ru) ПИРРОЛИДИНИЛСУЛЬФОНОВЫЕ МОДУЛЯТОРЫ RORγ
EA201492166A1 (ru) N-замещенные бензамиды и их применение в лечении боли
EA201390717A1 (ru) 3-(аминоарил)пиридиновые соединения
EA201290103A1 (ru) Гетероциклические соединения и их использование
EA201490269A1 (ru) Новое производное 1,2,3,4-тетрагидрохинолина, подходящее для лечения диабета
EA201792374A1 (ru) Азабензимидазолы и их применение в качестве модуляторов рецептора ampa
EA201790327A1 (ru) Соединения замещенного пиперидина
MX2018004664A (es) Antagonistas de ep4.
EA201300436A8 (ru) Совместные кристаллы и соли ингибиторов ccr3
EA201692300A1 (ru) Производные карбоксамида
EA201491227A1 (ru) Новые производные морфолинила, подходящие для применения в качестве ингибиторов mogat-2
EA201170447A1 (ru) Производные изохинолинона в качестве антагонистов nk3
EA201691133A1 (ru) (r)-3-((3s,4s)-3-фтор-4-(4-гидроксифенил)пиперидин-1-ил)-1-(4-метилбензил)пирролидин-2-он и его пролекарственные средства для лечения психиатрических нарушений
EA201491878A8 (ru) Замещенные ксантиновые производные
ECSP15007708A (es) Heterociclos de 5 miembros que contienen nitrógeno sustituidos por carboxamida o sulfonamida como moduladores para el receptor nuclear huérfano ror[gamma]
ECSP14033496A (es) Tiazoles sustituidos por carboxamida o sulfonamida y derivados relacionados como moduladores para el receptor nuclear huérfano ror[gamma]
EA201591023A1 (ru) Твердая форма производного дигидропиридооксазина

Legal Events

Date Code Title Description
TH4A Publication of the corrected specification to eurasian patent
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM RU