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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Virology (AREA)
- Ophthalmology & Optometry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Anesthesiology (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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 (16)
| Country | Link |
|---|---|
| US (3) | US20120157458A1 (es) |
| EP (2) | EP3181566A1 (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) |
| 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 (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3181566A1 (en) | 2010-09-20 | 2017-06-21 | Ironwood Pharmaceuticals, Inc. | Imidazotriazinone compounds |
| HK1211023A1 (zh) * | 2011-10-10 | 2016-05-13 | H. Lundbeck A/S | 具有咪唑并吡嗪骨架pde9i |
| HK1199879A1 (en) | 2012-01-26 | 2015-07-24 | H.隆德贝克有限公司 | 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 |
| EP2914587A1 (de) | 2012-10-31 | 2015-09-09 | 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 |
| TW201643167A (zh) * | 2015-04-22 | 2016-12-16 | Ｈ 朗德貝克公司 | 作爲ｐｄｅ１抑制劑之咪唑並三酮 |
| JO3627B1 (ar) | 2015-04-30 | 2020-08-27 | H Lundbeck As | إيميدازو بيرازينونات على هيئة مثبطات pde1 |
| LT3865484T (lt) | 2015-07-07 | 2024-02-12 | H. Lundbeck A/S | Pde9 inhibitorius su imidazopirazinono karkasu, skirtas periferinių ligų gydymui |
| 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 |
| IL295973A (en) | 2016-07-06 | 2022-10-01 | H Lundbeck As | pde9 inhibitors for the treatment of peripheral diseases |
| EP3529250B1 (en) | 2016-10-18 | 2023-12-06 | H. Lundbeck A/S | Imidazopyrazinones, pyrazolopyrimidinones and pyrazolopyridinones as pde1 inhibitors |
| HUE050403T2 (hu) | 2016-10-28 | 2020-12-28 | H Lundbeck As | Imidazopirazinonokkal végzett kombinációs kezelések pszichiátriai és/vagy kognitív betegségek kezelésére |
| WO2018078042A1 (en) | 2016-10-28 | 2018-05-03 | H. Lundbeck A/S | Combination treatments comprising administration of imidazopyrazinones |
| US11370795B2 (en) * | 2017-05-26 | 2022-06-28 | Imara Inc. | Process for the synthesis of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-3-tetrahydropyran-4-yl-7H-imidazo[1,5-a]pyrazin-8-one |
| HRP20240363T1 (hr) | 2018-05-25 | 2024-06-07 | Cardurion Pharmaceuticals, Inc. | Monohidratni i kristalni oblici 6-[(3s,4s)-4-metil-1-(pirimidin-2-ilmetil)pirolidin-3-il]-3-tetrahidropiran-4-il-7h-imidazo [1,5-a] pirazin-8-ona |
| WO2020047311A1 (en) | 2018-08-31 | 2020-03-05 | Imara Inc. | Pde9 inhibitors for treating sickle cell disease |
| WO2020102374A1 (en) * | 2018-11-14 | 2020-05-22 | The Board Of Trustees Of The Leland Stanford Junior University | Targeting of makap-pde4d3 complexes in neurodegenerative disease |
| KR102712818B1 (ko) * | 2018-12-06 | 2024-09-30 | 한국화학연구원 | Pde9a 저해 활성을 가지는 화합물 및 이들의 의약 용도 |
| CA3155013A1 (en) * | 2019-10-21 | 2021-04-29 | Ki Ho Lee | Use of imidazopyrimidine or imidazotriazine compound for prevention, alleviation, or treatment of developmental disability |
| 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 |
| GB2632307A (en) * | 2023-08-02 | 2025-02-05 | Duke Street Bio Ltd | PARP1 inhibitor compounds |
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 |
| HRP20020585B1 (hr) | 1997-11-12 | 2013-02-28 | Bayer Schering Pharma Aktiengesellschaft | 2-fenil supstituirani imidazotriazinoni kao inhibitori fosfodiesteraze |
| US7087605B2 (en) | 2001-06-01 | 2006-08-08 | Bayer Aktiengesellschaft | 5-Ethyl-imidazotriazinones |
| GB0113343D0 (en) * | 2001-06-01 | 2001-07-25 | Bayer Ag | Novel Heterocycles 2 |
| BR0213817A (pt) * | 2001-11-02 | 2004-10-19 | Pfizer Prod Inc | Tratamento de sìndrome de resistência à insulina e diabete do tipo 2 com inibidores da pde9 |
| 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 |
| JP2008543968A (ja) | 2005-06-28 | 2008-12-04 | オーキッド リサーチ ラボラトリーズ リミテッド | 新規なピラゾロピリミジノン誘導体 |
| PT2152712E (pt) * | 2007-05-11 | 2012-02-29 | Pfizer | Compostos amino-heterocíclicos |
| AU2009262241B2 (en) | 2008-06-25 | 2014-05-22 | Forum Pharmaceuticals Inc. | 1, 2 disubstituted heterocyclic compounds |
| EP3181566A1 (en) | 2010-09-20 | 2017-06-21 | Ironwood Pharmaceuticals, Inc. | Imidazotriazinone compounds |
| HK1199879A1 (en) | 2012-01-26 | 2015-07-24 | H.隆德贝克有限公司 | Pde9 inhibitors with imidazo triazinone backbone |
| EP2828262A4 (en) | 2012-03-19 | 2015-09-23 | Forum Pharmaceuticals Inc | IMIDAZOTRIAZINONVERBINDUNGEN |
-
2011
- 2011-09-20 EP EP16197573.5A patent/EP3181566A1/en not_active Withdrawn
- 2011-09-20 AR ARP110103426A patent/AR083058A1/es unknown
- 2011-09-20 TW TW100133825A patent/TWI541244B/zh not_active IP Right Cessation
- 2011-09-20 ES ES11761793.6T patent/ES2610360T3/es active Active
- 2011-09-20 US US13/237,795 patent/US20120157458A1/en not_active Abandoned
- 2011-09-20 CA CA2811714A patent/CA2811714C/en not_active Expired - Fee Related
- 2011-09-20 UY UY0001033616A patent/UY33616A/es unknown
- 2011-09-20 EP EP11761793.6A patent/EP2619208B1/en not_active Not-in-force
- 2011-09-20 CN CN201180055157.9A patent/CN103313988B/zh not_active Expired - Fee Related
- 2011-09-20 MX MX2013003093A patent/MX2013003093A/es active IP Right Grant
- 2011-09-20 WO PCT/US2011/052399 patent/WO2012040230A1/en not_active Ceased
- 2011-09-20 DK DK11761793.6T patent/DK2619208T3/en active
- 2011-09-20 PL PL11761793T patent/PL2619208T3/pl unknown
- 2011-09-20 AU AU2011305568A patent/AU2011305568B2/en not_active Ceased
- 2011-09-20 JP JP2013530234A patent/JP5855109B2/ja not_active Expired - Fee Related
- 2011-09-20 BR BR112013008140A patent/BR112013008140A8/pt not_active IP Right Cessation
- 2011-09-20 RU RU2013118362/04A patent/RU2603140C2/ru not_active IP Right Cessation
-
2014
- 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 |
|---|---|
| US9540380B2 (en) | 2017-01-10 |
| CA2811714A1 (en) | 2012-03-29 |
| CN103313988B (zh) | 2016-06-08 |
| RU2603140C2 (ru) | 2016-11-20 |
| JP2013540755A (ja) | 2013-11-07 |
| EP2619208A1 (en) | 2013-07-31 |
| TWI541244B (zh) | 2016-07-11 |
| CN103313988A (zh) | 2013-09-18 |
| US20120157458A1 (en) | 2012-06-21 |
| DK2619208T3 (en) | 2017-01-30 |
| JP2016104747A (ja) | 2016-06-09 |
| BR112013008140A8 (pt) | 2018-04-03 |
| JP5855109B2 (ja) | 2016-02-09 |
| EP2619208B1 (en) | 2016-11-09 |
| AU2011305568A1 (en) | 2013-04-04 |
| MX2013003093A (es) | 2013-10-28 |
| WO2012040230A1 (en) | 2012-03-29 |
| US20170152265A1 (en) | 2017-06-01 |
| ES2610360T3 (es) | 2017-04-27 |
| EP3181566A1 (en) | 2017-06-21 |
| AU2011305568B2 (en) | 2015-12-10 |
| HK1187908A1 (en) | 2014-04-17 |
| TW201217381A (en) | 2012-05-01 |
| BR112013008140A2 (pt) | 2017-12-05 |
| US20140330014A1 (en) | 2014-11-06 |
| CA2811714C (en) | 2017-11-21 |
| AU2016200970A1 (en) | 2016-03-03 |
| UY33616A (es) | 2012-04-30 |
| RU2013118362A (ru) | 2014-10-27 |
| PL2619208T3 (pl) | 2017-03-31 |
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