AR089939A1 - COMPUESTOS BICICLICOS COMO INHIBIDORES DE mPGES-1 - Google Patents
COMPUESTOS BICICLICOS COMO INHIBIDORES DE mPGES-1Info
- Publication number
- AR089939A1 AR089939A1 ARP130100396A AR089939A1 AR 089939 A1 AR089939 A1 AR 089939A1 AR P130100396 A ARP130100396 A AR P130100396A AR 089939 A1 AR089939 A1 AR 089939A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- unsubstituted
- cycloalkyl
- alkyl
- independently selected
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen 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
- C07D215/20—Oxygen atoms
- C07D215/22—Oxygen atoms attached in position 2 or 4
- C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
- C07D217/24—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen 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
- C07D401/12—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 chain containing hetero atoms as chain links
Abstract
La presente se refiere a compuestos de fórmula (1) y sales farmacéuticamente aceptables de estos, como inhibidores de mPGES-1. Estos compuestos son inhibidores de la enzima prostaglandina E1 sintasa microsomal (mPGES-1) y por lo tanto son útiles en el tratamiento de dolor y/o inflamación de una variedad de enfermedades o afecciones, tales como asma, osteoartritis, artritis reumatoide, dolor agudo o crónico y enfermedades neurodegenerativas. Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable de este, donde Y es O, NH o NRᶜ; Z¹ y Z³, que pueden ser iguales o diferentes, se seleccionan independientemente de N y CR²; G¹ se selecciona de N y CR³; con una condición de que al menos uno de Z¹, Z³ y G¹ sea N; Q¹, Q², Q³ y Q⁴, que pueden ser iguales o diferentes, se seleccionan independientemente de N, CH y CR⁴; con una condición de que Q², Q³ y Q⁴ no sean N simultáneamente; W se selecciona de alquilo C₁₋₈ sustituido o no sustituido, alcoxi C₁₋₈alquilo C₁₋₈ sustituido o no sustituido, haloalquilo C₁₋₈ sustituido o no sustituido, hidroxialquilo C₁₋₈ sustituido o no sustituido, cicloalquilo C₃₋₁₂ sustituido o no sustituido y tetrahidrofurilo o tetrahidrofuranilo sustituido o no sustituido; R¹ se selecciona de alquilo C₁₋₈ sustituido o no sustituido, alcoxi C₁₋₈alquilo C₁₋₈ sustituido o no sustituido, haloalquilo C₁₋₈ sustituido o no sustituido, hidroxialquilo C₁₋₈ sustituido o no sustituido, cicloalquilo C₃₋₁₂ sustituido o no sustituido, arilo C₆₋₁₄ sustituido o no sustituido, heterociclilo de 3 - 15 miembros sustituido o no sustituido y heteroarilo de 5 - 14 miembros sustituido o no sustituido; cada aparición de R² y R³, que pueden ser iguales o diferentes, se selecciona independientemente de hidrógeno, halógeno, nitro, ciano, hidroxilo, alquilo C₁₋₈ sustituido o no sustituido, alcoxi C₁₋₈ sustituido o no sustituido, haloalquilo C₁₋₈ sustituido o no sustituido, hidroxialquilo C₁₋₈ sustituido o no sustituido, cicloalquilo C₃₋₁₂ sustituido o no sustituido y cicloalquil C₃₋₈alquilo C₁₋₈ sustituido o no sustituido; en cada aparición, R⁴ se selecciona independientemente de halógeno, nitro, ciano, hidroxilo, alquilo C₁₋₈ sustituido o no sustituido, alcoxi C₁₋₈ sustituido o no sustituido, alcoxi C₁₋₈alquilo C₁₋₈ sustituido o no sustituido, haloalquilo C₁₋₈ sustituido o no sustituido, hidroxialquilo C₁₋₈ sustituido o no sustituido y cicloalquilo C₃₋₁₂ sustituido o no sustituido y cicloalquilo C₃₋₈alquilo C₁₋₈ sustituido o no sustituido; en cada aparición, Rᶜ se selecciona independientemente de alquilo C₁₋₈ sustituido o no sustituido y aril C₆₋₁₄alquil C₁₋₈ sustituido o no sustituido; o RC y R¹, junto con el N al que están unidos, forman un anillo de morfolina; cada aparición de RX y Rʸ, que pueden ser iguales o diferentes, se seleccionan independientemente de hidrógeno, alquilo C₁₋₈ sustituido o no sustituido y aril C₆₋₁₄alquilo C₁₋₈ sustituido o no sustituido; y n es un entero que se encuentra en el intervalo de 1 a 4, ambos inclusive.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN372MU2012 | 2012-02-09 | ||
| US201261602227P | 2012-02-23 | 2012-02-23 | |
| IN1302MU2012 | 2012-04-24 | ||
| US201261645193P | 2012-05-10 | 2012-05-10 | |
| IN2576MU2012 | 2012-09-05 | ||
| US201261707838P | 2012-09-28 | 2012-09-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR089939A1 true AR089939A1 (es) | 2014-10-01 |
Family
ID=48946104
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130100396 AR089939A1 (es) | 2012-02-09 | 2013-02-07 | COMPUESTOS BICICLICOS COMO INHIBIDORES DE mPGES-1 |
Country Status (3)
| Country | Link |
|---|---|
| US (1) | US9006257B2 (es) |
| AR (1) | AR089939A1 (es) |
| WO (1) | WO2013118071A1 (es) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014127214A1 (en) | 2013-02-15 | 2014-08-21 | Kala Pharmaceuticals, Inc. | Therapeutic compounds and uses thereof |
| AU2014219024B2 (en) | 2013-02-20 | 2018-04-05 | KALA BIO, Inc. | Therapeutic compounds and uses thereof |
| US9688688B2 (en) | 2013-02-20 | 2017-06-27 | Kala Pharmaceuticals, Inc. | Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof |
| US9890173B2 (en) | 2013-11-01 | 2018-02-13 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| AU2014342042B2 (en) | 2013-11-01 | 2017-08-17 | KALA BIO, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| RU2681537C2 (ru) * | 2014-04-14 | 2019-03-07 | Шанхай Хэнжуй Фармасьютикал Ко., Лтд. | Амидные производные и их фармацевтически приемлемые соли, способ их получения и медицинское применение |
| US20200347038A1 (en) | 2014-08-29 | 2020-11-05 | Russell Dahl | Quinolines that modulate serca and their use for treating disease |
| US20170281611A1 (en) * | 2014-08-29 | 2017-10-05 | Eiger Biopharmaceuticals, Inc. | Quinolines and their use for treating endoplasmic reticulum stress-caused diseases |
| CN105237476A (zh) * | 2015-10-31 | 2016-01-13 | 高大元 | 一种4-氯-8-氨基喹啉的合成方法 |
| CA3036336A1 (en) | 2016-09-08 | 2018-03-15 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| BR112019004463A2 (pt) | 2016-09-08 | 2019-05-28 | Kala Pharmaceuticals Inc | formas cristalinas de compostos terapêuticos, seus processos de obtenção e seus métodos de uso |
| US10392399B2 (en) | 2016-09-08 | 2019-08-27 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| AU2017357503B2 (en) | 2016-11-11 | 2022-02-17 | Bayer Animal Health Gmbh | New anthelmintic quinoline-3-carboxamide derivatives |
| US11254661B2 (en) | 2017-08-04 | 2022-02-22 | Bayer Animal Health Gmbh | Quinoline derivatives for treating infections with helminths |
| WO2019101826A1 (en) | 2017-11-22 | 2019-05-31 | Khondrion Ip B.V. | Compounds as mpges-1 inhibitors |
| TWI809018B (zh) | 2017-12-15 | 2023-07-21 | 德商拜耳動物保健有限公司 | 用於製備喹啉衍生物之方法 |
| PT3790874T (pt) | 2018-05-09 | 2023-05-31 | Bayer Animal Health Gmbh | Derivados de quinolina antelmínticos |
| CA3104647A1 (en) | 2018-06-27 | 2020-01-02 | Bristol-Myers Squibb Company | Naphthyridinone compounds useful as t cell activators |
| WO2020006018A1 (en) | 2018-06-27 | 2020-01-02 | Bristol-Myers Squibb Company | Substituted naphthyridinone compounds useful as t cell activators |
| US20210275516A1 (en) * | 2018-07-02 | 2021-09-09 | Ecole Polytechnique Federale De Lausanne (Epfl) | Lactate enhancing compounds and uses thereof |
| CA3142513A1 (en) | 2019-06-25 | 2020-12-30 | Gilead Sciences, Inc. | Flt3l-fc fusion proteins and methods of use |
| AR119821A1 (es) | 2019-08-28 | 2022-01-12 | Bristol Myers Squibb Co | Compuestos de piridopirimidinonilo sustituidos útiles como activadores de células t |
| AU2020365113A1 (en) | 2019-10-18 | 2022-04-07 | Forty Seven, Inc. | Combination therapies for treating myelodysplastic syndromes and acute myeloid leukemia |
| MX2022005123A (es) | 2019-10-31 | 2022-05-30 | Forty Seven Inc | Tratamiento basado en anti-cd47 y anti-cd20 para cancer hematologico. |
| TWI778443B (zh) | 2019-11-12 | 2022-09-21 | 美商基利科學股份有限公司 | Mcl1抑制劑 |
| CN111018777B (zh) * | 2019-11-25 | 2021-02-12 | 武汉智顿科技发展有限公司 | 一种地喹氯铵的制备方法 |
| CN110963967B (zh) * | 2019-11-25 | 2021-02-12 | 武汉智顿科技发展有限公司 | 一种2-甲基-4-氨基喹啉的制备方法 |
| AR120823A1 (es) | 2019-12-23 | 2022-03-23 | Bristol Myers Squibb Co | Compuestos bicíclicos sustituidos útiles como activadores de células t |
| CA3165735A1 (en) | 2019-12-24 | 2021-07-01 | Carna Biosciences, Inc. | Diacylglycerol kinase modulating compounds |
| BR112022014623A2 (pt) | 2020-02-14 | 2022-09-13 | Jounce Therapeutics Inc | Anticorpos e proteínas de fusão que se ligam a ccr8 e usos dos mesmos |
| US20230039553A1 (en) | 2020-05-01 | 2023-02-09 | Gilead Sciences, Inc. | Cd73 compounds |
| US11730729B2 (en) | 2020-07-20 | 2023-08-22 | Neurodon Corporation | Quinolines that modulate SERCA and their use for treating disease |
| TW202302145A (zh) | 2021-04-14 | 2023-01-16 | 美商基利科學股份有限公司 | ＣＤ４７／ＳＩＲＰα結合及ＮＥＤＤ８活化酶Ｅ１調節次單元之共抑制以用於治療癌症 |
| TW202313094A (zh) | 2021-05-18 | 2023-04-01 | 美商基利科學股份有限公司 | 使用ＦＬＴ３Ｌ—Ｆｃ融合蛋白之方法 |
| AU2022298639A1 (en) | 2021-06-23 | 2023-12-07 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| US11926628B2 (en) | 2021-06-23 | 2024-03-12 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| CA3220923A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| US11976072B2 (en) | 2021-06-23 | 2024-05-07 | Gilead Sciences, Inc. | Diacylglycerol kinase modulating compounds |
| WO2023076983A1 (en) | 2021-10-28 | 2023-05-04 | Gilead Sciences, Inc. | Pyridizin-3(2h)-one derivatives |
| WO2023122581A2 (en) | 2021-12-22 | 2023-06-29 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| US20230242508A1 (en) | 2021-12-22 | 2023-08-03 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| TW202333681A (zh) * | 2021-12-28 | 2023-09-01 | 日商日本新藥股份有限公司 | 吲唑化合物及醫藥 |
| TW202340168A (zh) | 2022-01-28 | 2023-10-16 | 美商基利科學股份有限公司 | Ｐａｒｐ７抑制劑 |
| TW202346277A (zh) | 2022-03-17 | 2023-12-01 | 美商基利科學股份有限公司 | Ｉｋａｒｏｓ鋅指家族降解劑及其用途 |
| US20230355796A1 (en) | 2022-03-24 | 2023-11-09 | Gilead Sciences, Inc. | Combination therapy for treating trop-2 expressing cancers |
| TW202345901A (zh) | 2022-04-05 | 2023-12-01 | 美商基利科學股份有限公司 | 用於治療結腸直腸癌之組合療法 |
| TW202400138A (zh) | 2022-04-21 | 2024-01-01 | 美商基利科學股份有限公司 | Ｋｒａｓ ｇ１２ｄ調節化合物 |
| CN115124463B (zh) * | 2022-07-01 | 2023-11-28 | 浙江工业大学 | 取代喹啉类化合物及其制备方法和应用 |
| US20240116928A1 (en) | 2022-07-01 | 2024-04-11 | Gilead Sciences, Inc. | Cd73 compounds |
| US20240091351A1 (en) | 2022-09-21 | 2024-03-21 | Gilead Sciences, Inc. | FOCAL IONIZING RADIATION AND CD47/SIRPa DISRUPTION ANTICANCER COMBINATION THERAPY |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7442716B2 (en) | 2004-12-17 | 2008-10-28 | Merck Frosst Canada Ltd. | 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors |
| JP5086809B2 (ja) | 2004-12-17 | 2012-11-28 | メルク カナダ インコーポレイテッド | ｍＰＧＥＳ−１阻害剤としての２−（フェニルまたはヘテロ環式）−１Ｈ−フェナントロ［９，１０−ｄ］イミダゾール |
| UY32138A (es) * | 2008-09-25 | 2010-04-30 | Boehringer Ingelheim Int | Amidas sustituidas del ácido 2-(2,6-dicloro-fenilamino)-6-fluoro-1-metil-1h-bencimidazol-5-carboxílico y sus sales farmacéuticamente aceptables |
| UY32470A (es) | 2009-03-05 | 2010-10-29 | Boehringer Ingelheim Int | Derivados de 2-{2-cloro-5-[(sustituido) metil]fenilamino} -1-metil]fenilamino}-1-metilbencimidazol-5-carboxamidas-n-(sustituidas) y sus sales fisiológicamente aceptables, composiciones conteniéndolos y aplicaciones |
| WO2011023812A1 (en) * | 2009-08-27 | 2011-03-03 | Novasaid Ab | Microsomal prostaglandin e synthase-1 (mpges1) inhibitors |
| TW201305178A (zh) * | 2010-10-29 | 2013-02-01 | Glenmark Pharmaceuticals Sa | 作為ｍＰＧＥＳ－１抑制物的三環化合物 |
| WO2012110860A1 (en) | 2011-02-17 | 2012-08-23 | Glenmark Pharmaceuticals S.A. | TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS |
| EP2495244A1 (en) * | 2011-03-02 | 2012-09-05 | NovaSaid AB | Piperidinyl benzoimidazole derivatives as mPGEs-1 inhibitors |
-
2013
- 2013-02-07 AR ARP130100396 patent/AR089939A1/es unknown
- 2013-02-07 US US13/761,937 patent/US9006257B2/en not_active Expired - Fee Related
- 2013-02-07 WO PCT/IB2013/051004 patent/WO2013118071A1/en active Application Filing
Also Published As
| Publication number | Publication date |
|---|---|
| US20130210844A1 (en) | 2013-08-15 |
| US9006257B2 (en) | 2015-04-14 |
| WO2013118071A1 (en) | 2013-08-15 |
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