BR112019009880A2 - inibidores de magl - Google Patents
inibidores de magl Download PDFInfo
- Publication number
- BR112019009880A2 BR112019009880A2 BR112019009880A BR112019009880A BR112019009880A2 BR 112019009880 A2 BR112019009880 A2 BR 112019009880A2 BR 112019009880 A BR112019009880 A BR 112019009880A BR 112019009880 A BR112019009880 A BR 112019009880A BR 112019009880 A2 BR112019009880 A2 BR 112019009880A2
- Authority
- BR
- Brazil
- Prior art keywords
- solvate
- pharmaceutically acceptable
- compound
- acceptable salt
- formula
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 1165
- 208000002193 Pain Diseases 0.000 claims abstract description 24
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 21
- 150000003839 salts Chemical class 0.000 claims description 1109
- 239000012453 solvate Substances 0.000 claims description 1072
- 229910052736 halogen Inorganic materials 0.000 claims description 124
- 150000002367 halogens Chemical class 0.000 claims description 124
- 238000000034 method Methods 0.000 claims description 103
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 60
- 125000000217 alkyl group Chemical group 0.000 claims description 48
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 47
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 42
- 125000001072 heteroaryl group Chemical group 0.000 claims description 42
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 38
- 201000010099 disease Diseases 0.000 claims description 36
- 229910052739 hydrogen Inorganic materials 0.000 claims description 36
- 125000003118 aryl group Chemical group 0.000 claims description 32
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- 208000035475 disorder Diseases 0.000 claims description 24
- 229910052757 nitrogen Inorganic materials 0.000 claims description 24
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 22
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 20
- 238000011282 treatment Methods 0.000 claims description 16
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 13
- 206010015037 epilepsy Diseases 0.000 claims description 13
- 208000008795 neuromyelitis optica Diseases 0.000 claims description 13
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims description 12
- 229910052731 fluorine Inorganic materials 0.000 claims description 11
- 201000006417 multiple sclerosis Diseases 0.000 claims description 10
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- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 7
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 6
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- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims description 3
- -1 bicyclic carbamates Chemical class 0.000 abstract description 307
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- 235000002639 sodium chloride Nutrition 0.000 description 1065
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 106
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 80
- 239000000243 solution Substances 0.000 description 78
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- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 57
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- 238000003786 synthesis reaction Methods 0.000 description 36
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- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 12
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- 239000002904 solvent Substances 0.000 description 11
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- 108020002334 Monoacylglycerol lipase Proteins 0.000 description 10
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- 125000001424 substituent group Chemical group 0.000 description 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 10
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- YHYNJGHMBMXAFB-UHFFFAOYSA-N 2-hydroxy-4-(trifluoromethyl)benzaldehyde Chemical compound OC1=CC(C(F)(F)F)=CC=C1C=O YHYNJGHMBMXAFB-UHFFFAOYSA-N 0.000 description 5
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- 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
- A61P25/08—Antiepileptics; Anticonvulsants
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- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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| WO2017197192A1 (en) * | 2016-05-12 | 2017-11-16 | Abide Therapeutics, Inc. | Spirocycle compounds and methods of making and using same |
| JOP20190107A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| JOP20190105A1 (ar) * | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| MA58133B1 (fr) | 2016-11-16 | 2024-02-29 | H Lundbeck As | Une forme cristalline d'un inhibiteur de magl |
| WO2018093950A1 (en) | 2016-11-16 | 2018-05-24 | Abide Therapeutics, Inc. | Pharmaceutical formulations |
| AU2018271876B2 (en) | 2017-05-23 | 2021-10-21 | H. Lundbeck A/S. | Pyrazole MAGL inhibitors |
| US10927105B1 (en) | 2017-05-23 | 2021-02-23 | Lundbeck La Jolla Research Center, Inc. | Pyrazole MAGL inhibitors |
| PE20200664A1 (es) | 2017-08-29 | 2020-06-11 | Lundbeck La Jolla Research Center Inc | Compuestos espirociclicos y sus metodos de preparacion y uso |
| PE20200665A1 (es) | 2017-08-29 | 2020-06-11 | Lundbeck La Jolla Research Center Inc | Compuestos espirociclicos y sus metodos de preparacion y uso |
| CA3106510A1 (en) * | 2018-07-19 | 2020-01-23 | Pfizer Inc. | Heterocyclic spiro compounds as magl inhibitors |
| EP4474017A3 (en) | 2018-08-13 | 2025-02-26 | F. Hoffmann-La Roche AG | New heterocyclic compounds |
| MX2022013224A (es) | 2020-04-21 | 2022-11-14 | H Lundbeck As | Sintesis de un inhibidor de la monoacilglicerol lipasa. |
| UY39516A (es) | 2020-11-13 | 2022-05-31 | H Lundbeck As | Composición para el tratamiento de una enfermedad vascular, composición para la prevención de una enfermedad vascular, composición para el tratamiento de la hipertensión, y composición para la prevención de la hipertensión |
| EP4457213A4 (en) | 2021-12-29 | 2025-12-17 | Psy Therapeutics Inc | INHIBITION OF MONOACYLGLYCEROL LIPASE (MAGL) |
| WO2023213854A1 (en) | 2022-05-04 | 2023-11-09 | H. Lundbeck A/S | Crystalline form of 1,1,1,3,3,3-hexafluoropropan-2-yl (s)-1-(pyridazin-3-ylcarbamoyl)-6 azaspiro[2.5]octane-6-carboxylate as monoacylglycerol lipase inhibitor. |
| WO2024168426A1 (en) | 2023-02-13 | 2024-08-22 | Apogee Pharmaceuticals, Inc. | Small molecules as monoacylglycerol lipase (magl) inhibitors, compositions and use thereof |
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| US1003002A (en) | 1910-10-10 | 1911-09-12 | Gustave J Martel | Tire-patching device. |
| WO2002070523A1 (en) | 2001-03-07 | 2002-09-12 | Pfizer Products Inc. | Modulators of chemokine receptor activity |
| EP1948630A2 (en) | 2005-11-05 | 2008-07-30 | AstraZeneca AB | Novel compounds |
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| FR2941696B1 (fr) | 2009-02-05 | 2011-04-15 | Sanofi Aventis | Derives d'azaspiranyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique |
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| US8575296B2 (en) | 2009-09-29 | 2013-11-05 | Polyone Corporation | Polyester articles having simulated metallic or pearlescent appearance |
| ES2735411T3 (es) | 2009-10-23 | 2019-12-18 | Janssen Pharmaceutica Nv | Octahidropirrolo[3,4-c]pirroles disustituidos como moduladores del receptor de orexina |
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| EP2444084A1 (en) | 2010-10-21 | 2012-04-25 | Centro Nacional de Investigaciones Oncológicas (CNIO) | Use of PI3K inibitors for the treatment of obesity |
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| JP2014005245A (ja) | 2012-06-26 | 2014-01-16 | Dainippon Sumitomo Pharma Co Ltd | 二環性ピリミジン誘導体を含有する医薬組成物 |
| MA37940B1 (fr) | 2012-09-25 | 2018-09-28 | Hoffmann La Roche | Derives d'octahydro-cyclopenta(c)pyrrole substitues inhibiteurs de l'autotaxine, utiles pour traiter les affections renales, hepatiques et inflammatoires, les affections du systeme nerveux, les maladies fibreuses. |
| WO2015003002A1 (en) | 2013-07-03 | 2015-01-08 | Abide Therapeutics, Inc. | Pyrrolo-pyrrole carbamate and related organic compounds, pharmaceutical compositions, and medical uses thereof |
| AP2016009496A0 (en) | 2014-04-04 | 2016-10-31 | X-Rx Inc | Substituted spirocydic inhibitors of autotaxin |
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| WO2016149401A2 (en) * | 2015-03-18 | 2016-09-22 | Abide Therapeutics, Inc. | Piperazine carbamates and methods of making and using same |
| CN107849021A (zh) | 2015-05-11 | 2018-03-27 | 阿比德治疗公司 | 治疗炎症或神经性疼痛的方法 |
| CN107849017B (zh) | 2015-07-31 | 2021-03-30 | 辉瑞公司 | 作为magl抑制剂的1,1,1-三氟-3-羟基丙-2-基氨基甲酸酯衍生物及1,1,1-三氟-4-羟基丁-2-基氨基甲酸酯衍生物 |
| WO2017087858A1 (en) | 2015-11-20 | 2017-05-26 | Abide Therapeutics, Inc. | Pyrazole compounds and methods of making and using same |
| EP3377060B1 (en) | 2015-11-20 | 2020-08-19 | Lundbeck La Jolla Research Center, Inc. | Pyrazole derivatives, processes for their preparation and uses thereof |
| CN109715613B (zh) | 2016-03-31 | 2021-07-30 | 武田药品工业株式会社 | 杂环化合物 |
| WO2017197192A1 (en) | 2016-05-12 | 2017-11-16 | Abide Therapeutics, Inc. | Spirocycle compounds and methods of making and using same |
| JOP20190049A1 (ar) | 2016-09-23 | 2019-03-20 | Bial Portela & C? S A | مثبطات دوبامين-b-هيدروكسيلاز |
| WO2018093950A1 (en) | 2016-11-16 | 2018-05-24 | Abide Therapeutics, Inc. | Pharmaceutical formulations |
| JOP20190106A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| JOP20190105A1 (ar) * | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| MA58133B1 (fr) | 2016-11-16 | 2024-02-29 | H Lundbeck As | Une forme cristalline d'un inhibiteur de magl |
| JOP20190107A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| PL3595665T3 (pl) | 2017-03-13 | 2025-01-13 | Lundbeck La Jolla Research Center, Inc. | Podwójne inhibitory magl i faah |
| AU2018271876B2 (en) | 2017-05-23 | 2021-10-21 | H. Lundbeck A/S. | Pyrazole MAGL inhibitors |
| JOP20190267A1 (ar) | 2017-05-23 | 2019-11-18 | Lundbeck La Jolla Research Center Inc | مثبطات بيرازول magl |
| PE20200664A1 (es) | 2017-08-29 | 2020-06-11 | Lundbeck La Jolla Research Center Inc | Compuestos espirociclicos y sus metodos de preparacion y uso |
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| UY39516A (es) | 2020-11-13 | 2022-05-31 | H Lundbeck As | Composición para el tratamiento de una enfermedad vascular, composición para la prevención de una enfermedad vascular, composición para el tratamiento de la hipertensión, y composición para la prevención de la hipertensión |
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2017
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- 2017-11-15 KR KR1020197017201A patent/KR20190080935A/ko not_active Ceased
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2019
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2021
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| B25A | Requested transfer of rights approved |
Owner name: H. LUNDBECK A/S (DK) |
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| B15K | Others concerning applications: alteration of classification |
Free format text: AS CLASSIFICACOES ANTERIORES ERAM: C07D 498/08 , C07D 471/10 , C07D 295/205 , C07D 403/04 , C07D 295/26 Ipc: C07D 498/08 (2006.01), C07D 471/10 (2006.01), C07D |
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| B06W | Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette] | ||
| B350 | Update of information on the portal [chapter 15.35 patent gazette] | ||
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 6A ANUIDADE. |
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| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2748 DE 05-09-2023 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013. |