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
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
- C07D285/125—1,3,4-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
- C07D285/135—Nitrogen atoms
-
- 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
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pulmonology (AREA)
- Transplantation (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Plural Heterocyclic Compounds (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.
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 (29)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
LT2474545T (lt) | 2005-12-13 | 2017-02-27 | Incyte Holdings Corporation | Heteroarilu pakeisti pirolo[2,3-b]piridinai ir pirolo[2,3-b]pirimidinai kaip janus kinazės inhibitoriai |
CA2689663C (en) | 2007-06-13 | 2016-08-09 | Incyte Corporation | Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
BRPI1012159B1 (pt) | 2009-05-22 | 2022-01-25 | Incyte Holdings Corporation | Compostos derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d] pirimidinas e pirrol-3-il-pirrolo[2,3-d] pirimidinas como inibidores de janus cinase, composições farmacêuticas compreendendo os referidos compostos e usos dos mesmos |
DK2432472T3 (da) | 2009-05-22 | 2019-11-18 | Incyte Holdings Corp | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octan- eller heptan-nitril som jak-inhibitorer |
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 |
KR20220015492A (ko) | 2010-03-10 | 2022-02-08 | 인사이트 홀딩스 코포레이션 | Jak1 저해제로서의 피페리딘4일 아제티딘 유도체 |
PL2574168T3 (pl) | 2010-05-21 | 2016-10-31 | Preparaty inhibitora kinazy janusowej do stosowania miejscowego | |
CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
ES2536415T3 (es) | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores 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 |
WO2013173720A1 (en) | 2012-05-18 | 2013-11-21 | Incyte Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
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 |
PE20200175A1 (es) | 2012-11-15 | 2020-01-24 | Incyte Holdings Corp | Formas de dosificacion de ruxolitinib de liberacion sostenida |
UA120162C2 (uk) | 2013-03-06 | 2019-10-25 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки при отриманні інгібітора jak |
WO2015003723A1 (en) * | 2013-07-12 | 2015-01-15 | Københavns Universitet | Substituted 4-proline derivatives as iglur antagonists |
CA3155500A1 (en) | 2013-08-07 | 2015-02-12 | Incyte Corporation | Sustained release dosage forms for a jak1 inhibitor |
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 |
US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
CN112105608B (zh) | 2018-01-30 | 2023-07-14 | 因赛特公司 | 制备(1-(3-氟-2-(三氟甲基)异烟碱基)哌啶-4-酮)的方法 |
MX2020010322A (es) | 2018-03-30 | 2022-11-30 | Incyte Corp | Tratamiento de la hidradenitis supurativa mediante el uso de inhibidores de actividad de la cinasa janus (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 |
CN115298173A (zh) | 2020-03-31 | 2022-11-04 | 田边三菱制药株式会社 | 羟基吡咯烷衍生物及其医药用途 |
US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
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WO1994000943A1 (en) | 1992-06-23 | 1994-01-06 | Motorola, Inc. | Multi-modulation scheme compatible radio |
PT837710E (pt) | 1995-06-21 | 2002-05-31 | Sofotec Gmbh & Co Kg | Cartucho de po farmaceutico com dispositivo de doseamento integrado e inalador para medicamentos em po |
DE10129703A1 (de) | 2001-06-22 | 2003-01-02 | Sofotec Gmbh & Co Kg | Zerstäubungssystem für eine Pulvermischung und Verfahren für Trockenpulverinhalatoren |
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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 |
CA2539033C (en) | 2003-09-12 | 2013-03-05 | Neuronova Ab | Treatment of disease or injury of the nervous system 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 |
US8455658B2 (en) * | 2006-01-25 | 2013-06-04 | Synta Pharmaceuticals Corp. | Thiazole and thiadiazole compounds for inflammation and immune-related uses |
RU2008134702A (ru) | 2006-01-27 | 2010-03-10 | Юниверсити Оф Вирждиния Пэтент Фаундейшн (Us) | Способ лечения невропатической боли |
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 |
WO2008016674A1 (en) * | 2006-08-01 | 2008-02-07 | Praecis Pharmaceuticals Incorporated | Agonists of the sphingosine- 1- phosphate receptor (slp) |
JP5216769B2 (ja) | 2006-08-17 | 2013-06-19 | ザ・ユニバーシティ・オブ・シカゴ | 炎症性疾患の処置 |
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 |
-
2009
- 2009-09-25 EP EP09382184A patent/EP2305660A1/en not_active Withdrawn
-
2010
- 2010-09-07 UY UY0001032880A patent/UY32880A/es unknown
- 2010-09-17 TW TW099131607A patent/TW201113277A/zh unknown
- 2010-09-22 WO PCT/EP2010/005801 patent/WO2011035900A1/en active Application Filing
- 2010-09-23 AR ARP100103466A patent/AR078311A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
WO2011035900A1 (en) | 2011-03-31 |
UY32880A (es) | 2011-02-28 |
EP2305660A1 (en) | 2011-04-06 |
TW201113277A (en) | 2011-04-16 |
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