PE20200665A1 - Compuestos espirociclicos y sus metodos de preparacion y uso - Google Patents
Compuestos espirociclicos y sus metodos de preparacion y usoInfo
- Publication number
- PE20200665A1 PE20200665A1 PE2020000297A PE2020000297A PE20200665A1 PE 20200665 A1 PE20200665 A1 PE 20200665A1 PE 2020000297 A PE2020000297 A PE 2020000297A PE 2020000297 A PE2020000297 A PE 2020000297A PE 20200665 A1 PE20200665 A1 PE 20200665A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- compound
- co2h
- compounds
- alkenyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
-
- 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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- 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
-
- 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
-
- 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
- C07D487/10—Spiro-condensed systems
Abstract
La presente invencion se refiere a compuestos espirociclicos de formulas (I), (I'), (II), (III), (IV), (VI), (V), (V'), (VII), (VIII) y a sus solvatos, hidratos, tautomeros, esteroisomeros, N-oxidos y sales farmaceutica aceptables, donde: i) En el compuesto (I), Y es -CH2- o -C(O)-; R1 y R2 son H o alquilo C1-C6; R3 es alquilo C1-C6, halogeno, entre otros; R4 es -alquinileno C2-alquilo C1-C6-CO2H y cicloalquilo C3-C8-CO2H; w es 0 a 4; n y m son 0 o 1; p y q son 0 a 2, donde cuando q es 0, p es 2; ii) En el compuesto de formula (I'), Y es -CH2-; R1 y R2 son H o alquilo C1-C6; R3 son alquilo C1-C6, halogeno, entre otros; R4 es -piperazin-CH2-CO2H, -(2,5-diazabiciclo[2.2.1]heptano)-CH2-CO2H, entre otros; w es 0 a 4; n y m son 0 o 1; p y q son 0 a 2, donde cuando q es 0, p es 2; iii) En el compuesto (II), Y es -CH2- o -C(O)-; R3 es alquilo C1-C6, alquenilo C1-C6, entre otros; p es 0 a 5; iv) En el compuesto (III), Y es -CH2- o -C(O)-; R3 es alquilo C1-C6, alquenilo C1-C6, entre otros; p es 0 a 5; v) En el compuesto de formula (IV), R1 y R2 son H o alquilo C1-C6; R3 es alquilo C1-C6, alquenilo C1-C6, entre otros; p es 0 a 5; n es 0 o 1; m es 1 o 2; donde cuando n es 0, m es 2 y cuando n es 1, m es 1; vi) En el compuesto de formula (VI), R3 es alquilo C1-C6, alquenilo C1-C6, entre otros; vii) En el compuesto (V), X es -O- o -N(R11)-; R1 es H o alquilo C1-C6; R2 es alquilo C1-C6; R3 es alquilo C1-C6, alquenilo C2-C6, entre otros; R11 es H, alquilo C1-C6, entre otros; p es 0 a 5 y v es 0 o 1; viii) En el compuesto (V'), X es -O- o -N(R11)-; R1 es H o alquilo C1-C6; R2 es alquilo C1-C6; R3 es alquilo C1-C6, halogeno, entre otros; R4 es -piperazin-CH2-CO2H, -(2,5-diazabiciclo[2.2.1]heptano)-CH2-CO2H, entre otros; R11 es H o alquilo C1-C6; p es 0 a 4; v es 0 o 1; ix) En el compuesto (VII), R1 es octahidropirrolo[3,4-c]pirrolo-R6, entre otros, donde R6 es alquilo C1-C6, entre otros; R2 es alquilo C1-C6, halogeno, entre otros; p es 0 a 4; q es 1 o 2; x) En el compuesto (VIII), R1 es octahidropirrolo[3,4-c]pirrolo-R6, entre otros, donde R6 es alquilo C1-C6, entre otros; R2 es alquilo C1-C6, halogeno, entre otros; p es 0 a 4. Son compuestos preferidos los compuestos a), b), c), d), entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos son moduladores de MAGL, siendo utiles en el tratamiento de dolor neuropatico, dolor inflamatorio, entre otros.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762551714P | 2017-08-29 | 2017-08-29 | |
| PCT/US2018/048388 WO2019046330A1 (en) | 2017-08-29 | 2018-08-28 | SPIROCYCLIC COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20200665A1 true PE20200665A1 (es) | 2020-06-11 |
Family
ID=65526036
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2020000297A PE20200665A1 (es) | 2017-08-29 | 2018-08-28 | Compuestos espirociclicos y sus metodos de preparacion y uso |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US11161856B2 (es) |
| EP (1) | EP3675848B1 (es) |
| JP (1) | JP7177825B2 (es) |
| KR (1) | KR20200046053A (es) |
| CN (1) | CN111032034B (es) |
| AU (1) | AU2018326497A1 (es) |
| BR (1) | BR112020003946A2 (es) |
| CA (1) | CA3072926A1 (es) |
| CL (1) | CL2020000463A1 (es) |
| CO (1) | CO2020001715A2 (es) |
| CR (1) | CR20200088A (es) |
| DO (1) | DOP2020000040A (es) |
| EA (1) | EA202090296A1 (es) |
| EC (1) | ECSP20013332A (es) |
| ES (1) | ES2914363T3 (es) |
| IL (1) | IL272578A (es) |
| JO (1) | JOP20200022A1 (es) |
| MA (1) | MA50045A (es) |
| MX (1) | MX2020002254A (es) |
| PE (1) | PE20200665A1 (es) |
| PH (1) | PH12020500371A1 (es) |
| RU (1) | RU2020107039A (es) |
| SG (1) | SG11202000984YA (es) |
| WO (1) | WO2019046330A1 (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3698782B1 (en) | 2012-01-06 | 2024-05-15 | H. Lundbeck A/S | Carbamate compounds for use in therapy |
| WO2017197192A1 (en) | 2016-05-12 | 2017-11-16 | Abide Therapeutics, Inc. | Spirocycle compounds and methods of making and using same |
| JP7042804B2 (ja) | 2016-09-19 | 2022-03-28 | ルンドベック ラ ホーヤ リサーチ センター，インク． | ピペラジンカルバメート、及びその製造と使用の方法 |
| JOP20190107A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| MX2020002251A (es) | 2017-08-29 | 2020-07-20 | Lundbeck La Jolla Research Center Inc | Compuestos espirociclicos y sus metodos de preparacion y uso. |
| EA202090296A1 (ru) | 2017-08-29 | 2020-08-03 | Лундбекк Ла-Хойя Рисерч Сентер, Инк. | Спироциклические соединения и способы их получения и применения |
| US10570106B2 (en) | 2018-05-15 | 2020-02-25 | Lundbeck La Jolla Research Center, Inc. | MAGL inhibitors |
| CN111505410B (zh) * | 2020-04-02 | 2022-07-29 | 矽力杰半导体技术(杭州)有限公司 | 调光模式检测电路、方法和无调光检测电路及照明系统 |
| JP2023523219A (ja) | 2020-04-21 | 2023-06-02 | ハー・ルンドベック・アクチエゼルスカベット | モノアシルグリセロールリパーゼ阻害剤の合成 |
| TW202229255A (zh) | 2020-11-13 | 2022-08-01 | 丹麥商Ｈ 朗德貝克公司 | Magl抑制劑 |
| 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. |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002070523A1 (en) * | 2001-03-07 | 2002-09-12 | Pfizer Products Inc. | Modulators of chemokine receptor activity |
| CA2665804A1 (en) * | 2006-08-23 | 2008-02-28 | Astellas Pharma Inc. | Urea compound or salt thereof |
| RU2010140613A (ru) | 2008-03-05 | 2012-04-10 | Таргасепт, Инк. (Us) | Амиды диазабициклоалканов, селективные в отношении подтипа никотиновых ацетилхолиновых рецепторов |
| WO2010141817A1 (en) | 2009-06-05 | 2010-12-09 | Janssen Pharmaceutica Nv | Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase |
| JP5759470B2 (ja) | 2009-10-23 | 2015-08-05 | ヤンセン ファーマシューティカ エヌ．ベー． | オレキシン受容体調節因子としての二置換オクタヒドロピロロ［３，４−ｃ］ピロール |
| EP2542083B1 (en) | 2010-03-04 | 2015-05-06 | Merck Sharp & Dohme Corp. | Positive allosteric modulators of mglur2 |
| FR2960875B1 (fr) * | 2010-06-04 | 2012-12-28 | Sanofi Aventis | Derives de carbamates d'hexafluoroisopropyle, leur preparation et leur application en therapeutique |
| EP2444084A1 (en) | 2010-10-21 | 2012-04-25 | Centro Nacional de Investigaciones Oncológicas (CNIO) | Use of PI3K inibitors for the treatment of obesity |
| EP3698782B1 (en) * | 2012-01-06 | 2024-05-15 | H. Lundbeck A/S | Carbamate compounds for use in therapy |
| EP3590940B1 (en) | 2012-09-25 | 2021-06-09 | F. Hoffmann-La Roche AG | Hexahydropyrrolo[3,4-c]pyrrole derivatives and related compounds as autotaxin (atx) inhibitors and as inhibitors of the lysophosphatidic acid (lpa) production for treating e.g. renal diseases |
| WO2015003002A1 (en) | 2013-07-03 | 2015-01-08 | Abide Therapeutics, Inc. | Pyrrolo-pyrrole carbamate and related organic compounds, pharmaceutical compositions, and medical uses thereof |
| CA2979537C (en) * | 2015-03-18 | 2023-08-29 | Abide Therapeutics, Inc. | Piperazine carbamates and methods of making and using same |
| BR112018000041A2 (pt) | 2015-07-31 | 2018-09-04 | Pfizer Inc. | Derivados de carbamato de 1,1,1-trifluoro-3- hidroxipropan-2-ila e derivados de carbamato de 1,1,1-trifluoro-4-hidroxibutan-2-ila como inibidores de magl |
| CN108601769B (zh) * | 2015-11-20 | 2021-09-03 | H.隆德贝克有限公司 | 吡唑化合物及其制备和使用方法 |
| 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) |
| MX2020002251A (es) | 2017-08-29 | 2020-07-20 | Lundbeck La Jolla Research Center Inc | Compuestos espirociclicos y sus metodos de preparacion y uso. |
| EA202090296A1 (ru) | 2017-08-29 | 2020-08-03 | Лундбекк Ла-Хойя Рисерч Сентер, Инк. | Спироциклические соединения и способы их получения и применения |
-
2018
- 2018-08-28 EA EA202090296A patent/EA202090296A1/ru unknown
- 2018-08-28 SG SG11202000984YA patent/SG11202000984YA/en unknown
- 2018-08-28 BR BR112020003946-2A patent/BR112020003946A2/pt not_active Application Discontinuation
- 2018-08-28 WO PCT/US2018/048388 patent/WO2019046330A1/en unknown
- 2018-08-28 AU AU2018326497A patent/AU2018326497A1/en not_active Abandoned
- 2018-08-28 ES ES18852217T patent/ES2914363T3/es active Active
- 2018-08-28 MX MX2020002254A patent/MX2020002254A/es unknown
- 2018-08-28 US US16/642,713 patent/US11161856B2/en active Active
- 2018-08-28 EP EP18852217.1A patent/EP3675848B1/en active Active
- 2018-08-28 KR KR1020207007712A patent/KR20200046053A/ko unknown
- 2018-08-28 JP JP2020512612A patent/JP7177825B2/ja active Active
- 2018-08-28 RU RU2020107039A patent/RU2020107039A/ru unknown
- 2018-08-28 MA MA050045A patent/MA50045A/fr unknown
- 2018-08-28 CR CR20200088A patent/CR20200088A/es unknown
- 2018-08-28 CN CN201880054296.1A patent/CN111032034B/zh active Active
- 2018-08-28 PE PE2020000297A patent/PE20200665A1/es unknown
- 2018-08-28 JO JOP/2020/0022A patent/JOP20200022A1/ar unknown
- 2018-08-28 CA CA3072926A patent/CA3072926A1/en not_active Abandoned
-
2020
- 2020-02-10 IL IL272578A patent/IL272578A/en unknown
- 2020-02-14 CO CONC2020/0001715A patent/CO2020001715A2/es unknown
- 2020-02-21 EC ECSENADI202013332A patent/ECSP20013332A/es unknown
- 2020-02-21 DO DO2020000040A patent/DOP2020000040A/es unknown
- 2020-02-24 PH PH12020500371A patent/PH12020500371A1/en unknown
- 2020-02-25 CL CL2020000463A patent/CL2020000463A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BR112020003946A2 (pt) | 2020-09-08 |
| AU2018326497A1 (en) | 2020-02-20 |
| ES2914363T3 (es) | 2022-06-09 |
| JOP20200022A1 (ar) | 2020-02-02 |
| RU2020107039A (ru) | 2021-09-30 |
| CA3072926A1 (en) | 2019-03-07 |
| US11161856B2 (en) | 2021-11-02 |
| MX2020002254A (es) | 2020-07-20 |
| KR20200046053A (ko) | 2020-05-06 |
| CL2020000463A1 (es) | 2020-07-10 |
| CN111032034B (zh) | 2023-05-02 |
| CR20200088A (es) | 2020-04-08 |
| MA50045A (fr) | 2020-07-08 |
| PH12020500371A1 (en) | 2020-12-07 |
| CN111032034A (zh) | 2020-04-17 |
| IL272578A (en) | 2020-03-31 |
| DOP2020000040A (es) | 2020-08-31 |
| JP7177825B2 (ja) | 2022-11-24 |
| EP3675848B1 (en) | 2022-03-23 |
| CO2020001715A2 (es) | 2020-02-28 |
| US20210214375A1 (en) | 2021-07-15 |
| WO2019046330A1 (en) | 2019-03-07 |
| SG11202000984YA (en) | 2020-03-30 |
| EP3675848A1 (en) | 2020-07-08 |
| EP3675848A4 (en) | 2021-03-10 |
| ECSP20013332A (es) | 2020-04-22 |
| EA202090296A1 (ru) | 2020-08-03 |
| JP2020532547A (ja) | 2020-11-12 |
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