AR083058A1 - Compuestos de estructura de imidazotriazinona - Google Patents
Compuestos de estructura de imidazotriazinonaInfo
- Publication number
- AR083058A1 AR083058A1 ARP110103426A ARP110103426A AR083058A1 AR 083058 A1 AR083058 A1 AR 083058A1 AR P110103426 A ARP110103426 A AR P110103426A AR P110103426 A ARP110103426 A AR P110103426A AR 083058 A1 AR083058 A1 AR 083058A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- group
- 4alkyl
- heterocycloalkyl
- Prior art date
Links
Classifications
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- 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
Abstract
Son inhibidores de fosfodiesterasa 9. La presente provee, además, procesos, composiciones farmacéuticas, preparaciones farmacéuticas y uso farmacéutico de los compuestos en el tratamiento de enfermedades o trastornos asociados con PDE9 en mamíferos, incluyendo humanos.Reivindicación 1: Un compuesto de fórmula (1) o una de sus sales aceptables desde el punto de vista farmacéutico, en donde X se selecciona de un enlace, C(O) o S(O)2; R1 se selecciona en forma independiente del grupo que consiste en H, alquilo C1-6, alcoxi C1-6, cicloalquilo C3-7, cicloalquilo C3-7-alquilo C1-4, cicloalcoxi C3-7, heterocicloalquilo, heterocicloalquil alquilo C1-4 y heterocicloalquiloxi, cada uno de los cuales puede estar sustituido en forma adicional con uno o más sustituyentes seleccionados del grupo que consiste en halógeno, -S(O)2alquilo C1-4, OH, -C(O)-alquilo C1-4, oxo, CN, alquilo C1-6, alcoxi C1-4, cicloalquilo C3-7, -C(O)NH-alquilo C1-4, -C(O)N[alquil C1-4-alquilo C1-4], alquil C1-4-C(O)-, alquilsulfonilo C1-4-, -S(O)2NH-alquilo C1-4, y -S(O)2N[alquil C1-4-alquilo C1-4]; R2 se selecciona en forma independiente del grupo que consiste en alquilo C1-6, cicloalquilo C3-10, cicloalquil C3-7-alquilo C1-4, heterocicloalquilo, heterocicloalquilalquilo C1-4, heteroarilo, heteroarilalquilo C1-4, fenilo restringido y fenilalquilo C1-4 restringido, cada uno de los cuales puede estar sustituido en forma adicional con uno o más sustituyentes seleccionados del grupo que consiste en halógeno, -S(O)2alquilo C1-4, OH, -C(O)-alquilo C1-4, oxo, CN, alquilo C1-6, alcoxi C1-4, cicloalquilo C3-7, -C(O)NH-alquilo C1-4, -C(O)N[alquil C1-4-alquilo C1-4], alquil C1-4-C(O)-, alquilsulfonilo C1-4-, -S(O)2NH-alquilo C1-4, y -S(O)2N[alquil C1-4-alquilo C1-4]; y R3 se selecciona en forma independiente del grupo que consiste en alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquilo, heterocicloalquilalquilo C1-4, heteroarilo, heteroarilalquilo C1-4, fenilo restringido y fenilalquilo C1-4 restringido, cada uno de los cuales puede estar sustituido en forma adicional con uno o más sustituyentes seleccionados del grupo que consiste en halógeno, -S(O)2alquilo C1-4, OH, -C(O)-alquilo C1-4, oxo, CN, alquilo C1-6, alcoxi C1-4, cicloalquilo C3-7, -C(O)NH-alquilo C1-4, -C(O)N[alquil C1-4-alquilo C1-4], alquil C1-4-C(O)-, alquilsulfonilo C1-4-, -S(O)2NH-alquilo C1-4, y -S(O)2N[alquil C1-4-alquilo C1-4].
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38469410P | 2010-09-20 | 2010-09-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR083058A1 true AR083058A1 (es) | 2013-01-30 |
Family
ID=44720178
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110103426A AR083058A1 (es) | 2010-09-20 | 2011-09-20 | Compuestos de estructura de imidazotriazinona |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US20120157458A1 (es) |
| EP (2) | EP2619208B1 (es) |
| JP (2) | JP5855109B2 (es) |
| CN (1) | CN103313988B (es) |
| AR (1) | AR083058A1 (es) |
| AU (2) | AU2011305568B2 (es) |
| BR (1) | BR112013008140A8 (es) |
| CA (1) | CA2811714C (es) |
| DK (1) | DK2619208T3 (es) |
| ES (1) | ES2610360T3 (es) |
| HK (1) | HK1187908A1 (es) |
| MX (1) | MX2013003093A (es) |
| PL (1) | PL2619208T3 (es) |
| RU (1) | RU2603140C2 (es) |
| TW (1) | TWI541244B (es) |
| UY (1) | UY33616A (es) |
| WO (1) | WO2012040230A1 (es) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2619208B1 (en) | 2010-09-20 | 2016-11-09 | Ironwood Pharmaceuticals, Inc. | Imidazotriazinone compounds |
| MX370433B (es) | 2011-10-10 | 2019-12-13 | H Lundbeck As | Derivados de 7h-imidazo [1-5-a] pirazin-8-ona como inhibidores de la fosfodiasterasa 9(pde9); y el uso de los mismos en el tratamiento de trastornos neurodegenerativos. |
| AP2014007820A0 (en) | 2012-01-26 | 2014-07-31 | Lundbeck & Co As H | PDE9 inhibitors with imidazo triazinone backbone |
| EP2828262A4 (en) | 2012-03-19 | 2015-09-23 | Forum Pharmaceuticals Inc | IMIDAZOTRIAZINONVERBINDUNGEN |
| WO2014024125A1 (en) | 2012-08-08 | 2014-02-13 | Celon Pharma S.A. | Pyrazolo[4,3-d]pyrimidin-7(6h)-one derivatives as pde9 inhibitors |
| CN102786525B (zh) | 2012-08-08 | 2014-12-17 | 中山大学 | N-取代吡唑并[3,4-d]嘧啶酮类化合物、其制备方法及其应用 |
| WO2014067962A1 (de) | 2012-10-31 | 2014-05-08 | Bayer Cropscience Ag | Neue heterocylische verbindungen als schädlingsbekämpfungsmittel |
| TW201629064A (zh) | 2014-10-10 | 2016-08-16 | Ｈ 朗德貝克公司 | 作爲ｐｄｅ１抑制劑之三唑並吡酮 |
| US20180044343A1 (en) * | 2015-03-16 | 2018-02-15 | Sumitomo Dainippon Pharma Co., Ltd. | Bicyclic imidazolo derivative |
| US20160311831A1 (en) * | 2015-04-22 | 2016-10-27 | H. Lundbeck A/S | Imidazotriazinones as PDE1 Inhibitors |
| JO3627B1 (ar) | 2015-04-30 | 2020-08-27 | H Lundbeck As | إيميدازو بيرازينونات على هيئة مثبطات pde1 |
| DK3303339T3 (da) | 2015-07-07 | 2021-04-12 | H Lundbeck As | Pde9-inhibitorer med imidazotriazinonskelet og imidazopyrazinonskelet til behandling af perifere sygdomme |
| WO2017070293A1 (en) * | 2015-10-20 | 2017-04-27 | Ironwood Pharmaceuticals, Inc. | Phosphodiesterase 9 inhibitor and levodopa therapy |
| CN105669680B (zh) * | 2016-03-24 | 2018-02-23 | 南京药捷安康生物科技有限公司 | 吡咯并[2,1‑f][1,2,4]三嗪‑4(1H)‑酮衍生物类PDE9A抑制剂 |
| TWI729109B (zh) | 2016-04-12 | 2021-06-01 | 丹麥商Ｈ 朗德貝克公司 | 作爲PDE1抑制劑的1,5-二氫-4H-吡唑并[3,4-d]嘧啶-4-酮和1,5-二氫-4H-吡唑并[4,3-c]吡啶-4-酮 |
| AU2017292650A1 (en) | 2016-07-06 | 2018-12-13 | H. Lundbeck A/S | PDE9 inhibitors for treatment of peripheral diseases |
| WO2018073251A1 (en) | 2016-10-18 | 2018-04-26 | H. Lundbeck A/S | Imidazopyrazinones, pyrazolopyrimidinones and pyrazolopyridinones as pde1 inhibitors |
| CN109803653A (zh) | 2016-10-28 | 2019-05-24 | H.隆德贝克有限公司 | 包括给予咪唑并吡嗪酮的组合治疗 |
| DK3532064T3 (da) | 2016-10-28 | 2020-08-24 | H Lundbeck As | Kombinationsbehandlinger omfattende imidazopyrazinoner til behandlingen af psykiatriske og/eller kognitive lidelser |
| WO2018218104A1 (en) * | 2017-05-26 | 2018-11-29 | Imara, Inc. | Methods of making and using pde9 inhibitors |
| EP3880256A4 (en) * | 2018-11-14 | 2022-08-03 | The Board of Trustees of the Leland Stanford Junior University | TARGETING MAKAPP-PDE4D3 COMPLEXES IN NEURODEGENERATIVE DISEASES |
| KR20200068996A (ko) * | 2018-12-06 | 2020-06-16 | 한국화학연구원 | Pde9a 저해 활성을 가지는 화합물 및 이들의 의약 용도 |
| KR20220086607A (ko) * | 2019-10-21 | 2022-06-23 | 에스케이바이오팜 주식회사 | 발달 장애의 예방, 경감 또는 치료를 위한 이미다조피리미딘 또는 이미다조트리아진 화합물의 용도 |
| CN112724079A (zh) * | 2021-02-04 | 2021-04-30 | 康化（上海）新药研发有限公司 | 一种6-甲氧基吡啶甲酸甲酯的合成方法 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT72878B (en) | 1980-04-24 | 1983-03-29 | Merck & Co Inc | Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents |
| DE19750085A1 (de) * | 1997-11-12 | 1999-05-20 | Bayer Ag | 2-Phenyl-substituierte Imidazotriazinone |
| EP1049695B1 (de) | 1997-11-12 | 2002-02-13 | Bayer Ag | 2-phenyl-substituierte imidazotriazinone als phosphodiesterase inhibitoren |
| GB0113343D0 (en) * | 2001-06-01 | 2001-07-25 | Bayer Ag | Novel Heterocycles 2 |
| US7087605B2 (en) | 2001-06-01 | 2006-08-08 | Bayer Aktiengesellschaft | 5-Ethyl-imidazotriazinones |
| IL161155A0 (en) * | 2001-11-02 | 2004-08-31 | Pfizer Prod Inc | Treatment of insulin resistance syndrome and type 2 diabetes with pde9 inhibitors |
| DE10229778A1 (de) * | 2002-07-03 | 2004-01-29 | Bayer Ag | Neue Verwendung von Imidazotriazinonen |
| JP2007524596A (ja) | 2003-02-28 | 2007-08-30 | トランスフォーム・ファーマシューティカルズ・インコーポレイテッド | 共結晶医薬組成物 |
| US20040220186A1 (en) | 2003-04-30 | 2004-11-04 | Pfizer Inc. | PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease |
| US20060264624A1 (en) | 2005-05-20 | 2006-11-23 | Alexander Heim-Riether | Methods for synthesizing imidazotriazinones |
| EP1896476A2 (en) | 2005-06-28 | 2008-03-12 | Orchid Research Laboratories Limited | Novel pyrazolopyrimidinone derivatives |
| EP2152712B1 (en) * | 2007-05-11 | 2012-01-11 | Pfizer Inc. | Amino-heterocyclic compounds |
| CN102131801B (zh) | 2008-06-25 | 2015-04-08 | 福拉姆医药股份有限公司 | 1,2-二取代的杂环化合物 |
| EP2619208B1 (en) * | 2010-09-20 | 2016-11-09 | Ironwood Pharmaceuticals, Inc. | Imidazotriazinone compounds |
| AP2014007820A0 (en) | 2012-01-26 | 2014-07-31 | Lundbeck & Co As H | PDE9 inhibitors with imidazo triazinone backbone |
| EP2828262A4 (en) | 2012-03-19 | 2015-09-23 | Forum Pharmaceuticals Inc | IMIDAZOTRIAZINONVERBINDUNGEN |
-
2011
- 2011-09-20 EP EP11761793.6A patent/EP2619208B1/en not_active Not-in-force
- 2011-09-20 UY UY0001033616A patent/UY33616A/es unknown
- 2011-09-20 MX MX2013003093A patent/MX2013003093A/es active IP Right Grant
- 2011-09-20 TW TW100133825A patent/TWI541244B/zh not_active IP Right Cessation
- 2011-09-20 CN CN201180055157.9A patent/CN103313988B/zh not_active Expired - Fee Related
- 2011-09-20 ES ES11761793.6T patent/ES2610360T3/es active Active
- 2011-09-20 JP JP2013530234A patent/JP5855109B2/ja not_active Expired - Fee Related
- 2011-09-20 DK DK11761793.6T patent/DK2619208T3/en active
- 2011-09-20 EP EP16197573.5A patent/EP3181566A1/en not_active Withdrawn
- 2011-09-20 BR BR112013008140A patent/BR112013008140A8/pt not_active IP Right Cessation
- 2011-09-20 US US13/237,795 patent/US20120157458A1/en not_active Abandoned
- 2011-09-20 PL PL11761793T patent/PL2619208T3/pl unknown
- 2011-09-20 AU AU2011305568A patent/AU2011305568B2/en not_active Ceased
- 2011-09-20 WO PCT/US2011/052399 patent/WO2012040230A1/en active Application Filing
- 2011-09-20 CA CA2811714A patent/CA2811714C/en not_active Expired - Fee Related
- 2011-09-20 RU RU2013118362/04A patent/RU2603140C2/ru not_active IP Right Cessation
- 2011-09-20 AR ARP110103426A patent/AR083058A1/es unknown
-
2014
- 2014-01-29 HK HK14100968.2A patent/HK1187908A1/zh not_active IP Right Cessation
- 2014-07-17 US US14/334,073 patent/US9540380B2/en not_active Expired - Fee Related
-
2015
- 2015-12-08 JP JP2015239514A patent/JP2016104747A/ja active Pending
-
2016
- 2016-02-16 AU AU2016200970A patent/AU2016200970A1/en not_active Abandoned
- 2016-12-07 US US15/371,935 patent/US20170152265A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN103313988B (zh) | 2016-06-08 |
| TWI541244B (zh) | 2016-07-11 |
| WO2012040230A1 (en) | 2012-03-29 |
| US20170152265A1 (en) | 2017-06-01 |
| RU2603140C2 (ru) | 2016-11-20 |
| JP2013540755A (ja) | 2013-11-07 |
| CA2811714A1 (en) | 2012-03-29 |
| AU2011305568B2 (en) | 2015-12-10 |
| AU2011305568A1 (en) | 2013-04-04 |
| TW201217381A (en) | 2012-05-01 |
| BR112013008140A2 (pt) | 2017-12-05 |
| AU2016200970A1 (en) | 2016-03-03 |
| BR112013008140A8 (pt) | 2018-04-03 |
| PL2619208T3 (pl) | 2017-03-31 |
| DK2619208T3 (en) | 2017-01-30 |
| JP5855109B2 (ja) | 2016-02-09 |
| CA2811714C (en) | 2017-11-21 |
| US20140330014A1 (en) | 2014-11-06 |
| RU2013118362A (ru) | 2014-10-27 |
| JP2016104747A (ja) | 2016-06-09 |
| EP2619208A1 (en) | 2013-07-31 |
| US9540380B2 (en) | 2017-01-10 |
| HK1187908A1 (zh) | 2014-04-17 |
| ES2610360T3 (es) | 2017-04-27 |
| CN103313988A (zh) | 2013-09-18 |
| MX2013003093A (es) | 2013-10-28 |
| EP3181566A1 (en) | 2017-06-21 |
| EP2619208B1 (en) | 2016-11-09 |
| UY33616A (es) | 2012-04-30 |
| US20120157458A1 (en) | 2012-06-21 |
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