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
- DUYSYHSSBDVJSM-KRWOKUGFSA-N sphingosine 1-phosphate Chemical compound CCCCCCCCCCCCC\C=C\[C@@H](O)[C@@H](N)COP(O)(O)=O DUYSYHSSBDVJSM-KRWOKUGFSA-N 0.000 title 2
- 239000000556 agonist Substances 0.000 title 1
- -1 hydroxycarbonyl group Chemical group 0.000 abstract 9
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 229920006395 saturated elastomer Polymers 0.000 abstract 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 150000004867 thiadiazoles Chemical class 0.000 abstract 1
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)
- 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.
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)
| 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)
| 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 |
-
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 not_active Ceased
- 2010-09-23 AR ARP100103466A patent/AR078311A1/es unknown
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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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |