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AR078311A1 - Derivados de tiadiazol como agonistas de los receptores de esfingosina-1-fosfato (s1p1) - Google Patents

Derivados de tiadiazol como agonistas de los receptores de esfingosina-1-fosfato (s1p1)

Info

Publication number
AR078311A1
AR078311A1 ARP100103466A ARP100103466A AR078311A1 AR 078311 A1 AR078311 A1 AR 078311A1 AR P100103466 A ARP100103466 A AR P100103466A AR P100103466 A ARP100103466 A AR P100103466A AR 078311 A1 AR078311 A1 AR 078311A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
optionally substituted
hydroxycarbonyl
substituted
Prior art date
Application number
ARP100103466A
Other languages
English (en)
Inventor
Belart Emma Terricabras
Ferrer Jordi Gracia
Coll Gaspar Casals
Izquierdo Nuria Aguilar
Cepeda Marta Mir
Riera Marta Carrascal
Poveda Pedro Manuel Grima
Original Assignee
Almirall Sa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Almirall Sa filed Critical Almirall Sa
Publication of AR078311A1 publication Critical patent/AR078311A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/121,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/1251,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)

Abstract

Derivados de tiadiazol que tienen la estructura química representada por la formula (1) o una sal o N-oxido o estereoisomero del mismo farmacéuticamente aceptable, en donde: ò L representa un enlace directo o un grupo -NH-, ò R1 representa un grupo fenilo, piridilo o bencilo que está opcionalmente sustituido con uno o más sustituyentes seleccionados de átomos de halogeno, un grupo alquilo C14, un grupo alcoxi C1-4, un grupo cicloalquilo C3-7 y grupos -CN, -CONH2 y CF3. ò R2 representa un grupo alquilo C1-6 o alquil C1-4-cicloalquilo C3-7, ò R3, R4 y R6 independientemente representan un átomo de hidrogeno, un átomo de halogeno, un grupo alquilo C1-4 o un grupo -CF3, ò R5 representa un -O(CH2)(0-2)-Ra, -O-(CH2)(2-4)-NR'Rö, -O-(CH2)(2-4)-NH-(CH2)(1-4)-Rö, -(CH2)(1-2)-NR'Rö, -(CH2)(1-4)-NH-(CH2)(1-4)-Rö o -(CO)-NR'Rö, en donde - Ra representa un grupo heterocíclico saturado que contiene N, de 4 a 6 miembros, opcionalmente sustituido con uno o más sustituyentes seleccionados de un grupo hidroxicarbonilo y un grupo alquilo C1-4 sustituido con un grupo hidroxicarbonilo, o un grupo cicloalquilo C3-7 sustituido con un grupo di-(alquil C1-4)amino que, a su vez, está opcionalmente sustituido con un grupo hidroxicarbonilo, - R' representa un átomo de hidrogeno o un grupo alquilo C1-4, - Rö representa un grupo metilsulfonamido, grupo alcanoilo C2-4, que está opcionalmente sustituido con un grupo hidroxi; un grupo alquilo C1-4 sustituido con uno o más sustituyentes seleccionados de un grupo hidroxi, y un grupo hidroxicarbonilo; un grupo heterocíclico saturado o insaturado de 5 a 6 miembros que contiene uno o más heteroátomos seleccionados de átomos de nitrogeno y oxígeno y que está opcionalmente sustituido con un grupo hidroxi; o un grupo cicloalquilo C4-6 sustituido con un grupo hidroxicarbonilo, o - R' y Rö junto con el átomo de nitrogeno al que están unidos forman un grupo heterocíclico saturado o insaturado, de 4 a 6 miembros, que contiene, como heteroátomos, el átomo de N al que R' y Rö están unidos y 0, 1 o 2 átomos de N adicionales, grupo heterocíclico que está opcionalmente sustituido con uno o más sustituyentes seleccionados de un grupo ciano, carbamoílo, hidroxicarbonilo, alcoxicarbonilo C1-3 y 1H-tetrazolilo y un grupo alquilo C1-3 que está opcionalmente sustituido con un grupo hidroxicarbonilo.
ARP100103466A 2009-09-25 2010-09-23 Derivados de tiadiazol como agonistas de los receptores de esfingosina-1-fosfato (s1p1) AR078311A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09382184A EP2305660A1 (en) 2009-09-25 2009-09-25 New thiadiazole derivatives

Publications (1)

Publication Number Publication Date
AR078311A1 true AR078311A1 (es) 2011-10-26

Family

ID=41426442

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100103466A AR078311A1 (es) 2009-09-25 2010-09-23 Derivados de tiadiazol como agonistas de los receptores de esfingosina-1-fosfato (s1p1)

Country Status (5)

Country Link
EP (1) EP2305660A1 (es)
AR (1) AR078311A1 (es)
TW (1) TW201113277A (es)
UY (1) UY32880A (es)
WO (1) WO2011035900A1 (es)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI3184526T1 (sl) 2005-12-13 2019-03-29 Incyte Holdings Corporation Derivati pirolo(2,3-D)pirimidina kot inhibitorji Janus kinaze
MX2009013402A (es) 2007-06-13 2010-02-24 Incyte Corp Sales de inhibidor de janus cinasa (r)-3-(4-(7h-pirrolo[2,3-d]piri midin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanitrilo.
WO2010135621A1 (en) 2009-05-22 2010-11-25 Incyte Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
WO2010135650A1 (en) 2009-05-22 2010-11-25 Incyte Corporation N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
PE20130038A1 (es) 2010-03-10 2013-01-28 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de jak1
SG10201503983QA (en) 2010-05-21 2015-06-29 Incyte Corp Topical Formulation for a JAK Inhibitor
EP2640725B1 (en) 2010-11-19 2015-01-07 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
BR112013012502A2 (pt) 2010-11-19 2019-03-06 Incyte Corporation pirrolopiridina ciclobutil substituída e derivados de pirrolopirimidina derivativos como inibidores de jak
EP2511275A1 (en) * 2011-04-12 2012-10-17 Bioprojet Novel piperidinyl monocarboxylic acids as S1P1 receptor agonists
EP2721028B1 (en) 2011-06-20 2015-11-04 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
AR091079A1 (es) 2012-05-18 2014-12-30 Incyte Corp Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak
US8846729B2 (en) * 2012-11-14 2014-09-30 Allergan, Inc. 2-thio-1,3,4-oxadiazoles azetidine derivatives as sphingosine-1 phosphate receptors modulators
US8729110B1 (en) * 2012-11-14 2014-05-20 Allergan, Inc. 2-thio-1,3,4-oxadiazoles derivatives as sphingosine-1 phosphate receptors modulators
PL2919766T3 (pl) 2012-11-15 2021-10-04 Incyte Holdings Corporation Postacie dawkowania ruksolitynibu o przedłużonym uwalnianiu
EP3489239B1 (en) 2013-03-06 2021-09-15 Incyte Holdings Corporation Processes and intermediates for making a jak inhibitor
WO2015003723A1 (en) * 2013-07-12 2015-01-15 Københavns Universitet Substituted 4-proline derivatives as iglur antagonists
LT3030227T (lt) 2013-08-07 2020-06-10 Incyte Corporation Prailginto atpalaidavimo jak1 inhibitoriaus dozavimo formos
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
ES2751698T3 (es) * 2014-11-03 2020-04-01 Olon Spa Procedimiento para la preparación del éster etílico del ácido 1-(2-halogen-etil)-4-piperidina-carboxílico
MA41139A (fr) 2014-12-11 2017-10-17 Actelion Pharmaceuticals Ltd Combinaison pharmaceutique comportant un agoniste sélectif du récepteur sip1
MX379273B (es) 2014-12-11 2025-03-11 Actelion Pharmaceuticals Ltd Regimen de dosificación para un agonista selectivo de receptor s1p1.
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
MX2020007973A (es) 2018-01-30 2020-12-07 Incyte Corp Procesos para preparar (1-(3-fluoro-2-(trifluorometil)isonicotinil )piperidin-4-ona).
SI3773593T1 (sl) 2018-03-30 2024-08-30 Incyte Corporation Zdravljenje hidradenitisa suppurative z zaviralci jak
WO2020254530A1 (en) 2019-06-18 2020-12-24 Syngenta Crop Protection Ag 7-sulfonyl-n-(1,3,4-thiadiazol-2-yl)-quinoxaline-6-carboxamide derivatives and the respective -benzimidazole-5-, -imidazo[4,5-b]pyridine-5-, -3h-furo[3,2b]pyridine-5-, -quinoline-2-, and -naphthalene-2-carboxamide derivatives as pesticides
EP4129402A4 (en) 2020-03-31 2024-06-12 Mitsubishi Tanabe Pharma Corporation HYDROXYPYRROLIDINE DERIVATIVE AND MEDICAL USE THEREOF
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2303792A (en) 1992-06-23 1994-01-24 Motorola, Inc. Multi-modulation scheme compatible radio
WO1997000703A1 (en) 1995-06-21 1997-01-09 Asta Medica Aktiengesellschaft Pharmaceutical powder cartridge with integrated metering device and inhaler for powdered medicaments
DE10129703A1 (de) 2001-06-22 2003-01-02 Sofotec Gmbh & Co Kg Zerstäubungssystem für eine Pulvermischung und Verfahren für Trockenpulverinhalatoren
DE10202940A1 (de) 2002-01-24 2003-07-31 Sofotec Gmbh & Co Kg Patrone für einen Pulverinhalator
AU2003240655B2 (en) 2002-05-16 2007-09-06 Novartis Ag Use of EDG receptor binding agents in cancer
GB0217152D0 (en) 2002-07-24 2002-09-04 Novartis Ag Organic compounds
EP1484057A1 (en) 2003-06-06 2004-12-08 Aventis Pharma Deutschland GmbH Use of 2-amino-1-3-propanediol derivatives for the manufacture of a medicament for the treatment of various types of pain
WO2005025553A2 (en) 2003-09-12 2005-03-24 Neuronova Ab Treatment of disorders of nervous systemsystem with fty720
US20050124664A1 (en) * 2003-10-30 2005-06-09 Eric Sartori Urea thiadiazole inhibitors of plasminogen activator inhibior-1
GB0329498D0 (en) 2003-12-19 2004-01-28 Novartis Ag Organic compounds
TWI444370B (zh) * 2006-01-25 2014-07-11 Synta Pharmaceuticals Corp 用於發炎及免疫相關用途之噻唑及噻二唑化合物
AU2007209961A1 (en) 2006-01-27 2007-08-09 University Of Virginia Patent Foundation Method for treatment of neuropathic pain
TWI389683B (zh) 2006-02-06 2013-03-21 Kyorin Seiyaku Kk A therapeutic agent for an inflammatory bowel disease or an inflammatory bowel disease treatment using a 2-amino-1,3-propanediol derivative as an active ingredient
EP2046315B1 (en) 2006-06-02 2013-04-10 The Ohio State University Research Foundation Therapeutic agents for the treatment of mantle cell lymphoma
GB0612721D0 (en) 2006-06-27 2006-08-09 Novartis Ag Organic compounds
EP2046766A1 (en) * 2006-08-01 2009-04-15 Praecis Pharmaceuticals Incorporated Agonists of the sphingosine- 1- phosphate receptor (slp)
DK2056807T3 (da) 2006-08-17 2012-10-22 Univ Chicago Behandling af inflammatoriske sygdomme
JP2010511728A (ja) * 2006-12-05 2010-04-15 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Il−8受容体アンタゴニスト
GB0704394D0 (en) * 2007-03-07 2007-04-11 Senexis Ltd Compounds

Also Published As

Publication number Publication date
EP2305660A1 (en) 2011-04-06
WO2011035900A1 (en) 2011-03-31
UY32880A (es) 2011-02-28
TW201113277A (en) 2011-04-16

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