AR098872A1 - Moduladores de tetrahidropiridopirazinas de gpr6 - Google Patents
Moduladores de tetrahidropiridopirazinas de gpr6Info
- Publication number
- AR098872A1 AR098872A1 ARP140104807A ARP140104807A AR098872A1 AR 098872 A1 AR098872 A1 AR 098872A1 AR P140104807 A ARP140104807 A AR P140104807A AR P140104807 A ARP140104807 A AR P140104807A AR 098872 A1 AR098872 A1 AR 098872A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- optionally substituted
- alkyl
- cycloalkyl
- hydrogen
- Prior art date
Links
Classifications
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- 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
- C07D471/04—Ortho-condensed systems
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
-
- 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
- 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
Abstract
Compuestos que son útiles como moduladores de GPR6, sus composiciones farmacéuticas, los métodos para el tratamiento de afecciones asociadas con GPR6, los procesos para realizar los compuestos y sus intermediarios. Reivindicación 1: El compuesto de fórmula (1) donde R¹ se selecciona del grupo que consiste en cicloalquilo C₃₋₈ opcionalmente sustituido heterociclilo C₃₋₆ opcionalmente sustituido, arilo C₆₋₁₀ opcionalmente sustituido y heteroarilo C₁₋₁₀ opcionalmente sustituido; X¹ es N y X² es CH; o X¹ es CH y X² es N; o X¹ es N y X² es N; cuando X¹ es N, Z se selecciona del grupo que consiste en alquileno C₁₋₆, haloalquileno C₁₋₆, -C(O)-, y -S(O)₂-; cuando X¹ es CH, Z se selecciona del grupo que consiste en alquileno C₁₋₆, haloalquileno C₁₋₆, -O-, -C(O)-, -NH-, -S-, -S(O)- y -S(O)₂-; q es 0, 1 ó 2; s es 0, 1 ó 2; R² es -OR⁵ o -NR⁶R⁷; R³, cada vez que se toma, se selecciona de forma independiente del grupo que consiste en alquilo C₁₋₆, cicloalquilo C₃₋₈ y trifluorometilo; p es 0, 1 ó 2; R⁴, cada vez que se toma, se selecciona de forma independiente del grupo que consiste en alquilo C₁₋₆, hidroxi y halo; r es 0 ó 1; R⁵ se selecciona del grupo que consiste en alquilo C₁₋₆ y cicloalquilo C₃₋₈; R⁶ se selecciona del grupo que consiste en hidrógeno y alquilo C₁₋₆; R⁷ se selecciona del grupo que consiste en alquilo C₁₋₆ opcionalmente sustituido, cicloalquilo C₃₋₈, arilo C₆₋₁₀ opcionalmente sustituido, heteroarilo C₁₋₁₀ opcionalmente sustituido y heterociclilo C₃₋₆ opcionalmente sustituido; X³ se selecciona del grupo que consiste en CH y CR⁴ y X⁴ es NR⁸; o X³ es NR⁸ y X⁴ se selecciona del grupo que consiste en CH y CR⁴; R⁸ se selecciona del grupo que consiste en alquilo C₁₋₆, haloalquilo C₁₋₆, cicloalquilo C₃₋₈, -S(O)₂-R⁹, -C(O)-R¹⁰, -C(O)-N(R¹¹)(R¹²) y -C(O)-OR¹³; R⁹ se selecciona del grupo que consiste en alquilo C₁₋₆, cicloalquilo C₃₋₈ y fenilo opcionalmente sustituido; R¹⁰ se selecciona del grupo que consiste en hidrógeno, alquilo C₁₋₆ opcionalmente sustituido, cicloalquilo C₃₋₈, arilo C₆₋₁₀ opcionalmente sustituido, heteroarilo C₁₋₁₀ opcionalmente sustituido y heterociclilo C₃₋₆ opcionalmente sustituido; R¹¹ fue selecciona del grupo que consiste en hidrógeno y alquilo C₁₋₆; R¹² se selecciona del grupo que consiste en hidrógeno, alquilo C₁₋₆ y cicloalquilo C₃₋₈; o R¹¹ y R¹² se toman entre si con el nitrógeno al que se unen para formar un anillo saturado de 4 a 7 miembros que tiene opcionalmente 1 heteroátomo en el anillo adicional que se selecciona del grupo N, O y S y se sustituye opcionalmente sobre cualquiera de los átomos de carbono del anillo con 1 a 5 sustituyentes que se seleccionan de forma independiente del grupo que consiste en ciano, halo, hidroxi, amino, heterociclilo C₃₋₆ opcionalmente sustituido, amida C₁₋₉, alquilo C₁₋₆ opcionalmente sustituido y alcoxi C₁₋₄ y se sustituye sobre cualquier nitrógeno en el anillo adicional por un sustituyente que se selecciona del grupo que consiste en hidrógeno, cicloalquilo C₃₋₈ y alquilo C₁₋₆ opcionalmente sustituido; R¹³ se selecciona del grupo que consiste en alquilo C₁₋₆ y cicloalquilo C₃₋₈; o su sal farmacéuticamente aceptable.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361919661P | 2013-12-20 | 2013-12-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR098872A1 true AR098872A1 (es) | 2016-06-22 |
Family
ID=52440811
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140104807A AR098872A1 (es) | 2013-12-20 | 2014-12-19 | Moduladores de tetrahidropiridopirazinas de gpr6 |
Country Status (41)
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI519515B (zh) | 2011-12-21 | 2016-02-01 | 諾維拉治療公司 | Ｂ型肝炎抗病毒劑 |
| EP2882722B1 (en) | 2012-08-13 | 2016-07-27 | Takeda Pharmaceutical Company Limited | Quinoxaline derivatives as gpr6 modulators |
| EA027280B1 (ru) | 2012-08-28 | 2017-07-31 | Янссен Сайенсиз Айрлэнд Юси | Сульфамоил-ариламиды и их применение в качестве лекарственных препаратов для лечения гепатита b |
| CA2899706C (en) | 2013-02-28 | 2021-10-19 | Janssen Sciences Ireland Uc | Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of hepatitis b |
| US9895349B2 (en) | 2013-04-03 | 2018-02-20 | Janssen Sciences Ireland Us | N-phenyl-carboxamide derivatives and the use thereof as medicaments for the treatment of hepatitis B |
| BR112015028538A2 (pt) | 2013-05-17 | 2017-07-25 | Janssen Sciences Ireland Uc | derivados de sulfamoiltiofenamida e o uso dos mesmos como medicamentos para o tratamento da hepatite b |
| JO3603B1 (ar) | 2013-05-17 | 2020-07-05 | Janssen Sciences Ireland Uc | مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي |
| NO3024819T3 (es) | 2013-07-25 | 2018-07-21 | ||
| CA2923712C (en) | 2013-10-23 | 2021-11-02 | Janssen Sciences Ireland Uc | Carboxamide derivatives and the use thereof as medicaments for the treatment of hepatitis b |
| JO3466B1 (ar) * | 2013-12-20 | 2020-07-05 | Takeda Pharmaceuticals Co | مواد ضابطة لتترا هيدرو بيريدوبيرازينات من gpr6 |
| US10392349B2 (en) | 2014-01-16 | 2019-08-27 | Novira Therapeutics, Inc. | Azepane derivatives and methods of treating hepatitis B infections |
| US9169212B2 (en) | 2014-01-16 | 2015-10-27 | Novira Therapeutics, Inc. | Azepane derivatives and methods of treating hepatitis B infections |
| RU2702109C1 (ru) | 2014-02-05 | 2019-10-04 | Новира Терапьютикс, Инк. | Комбинированная терапия для лечения инфекций вгв |
| CN110483484A (zh) | 2014-02-06 | 2019-11-22 | 爱尔兰詹森科学公司 | 氨磺酰基吡咯酰胺衍生物及其作为药物用于治疗乙型肝炎的用途 |
| JP6526034B2 (ja) * | 2014-02-14 | 2019-06-05 | 武田薬品工業株式会社 | Ｇｐｒ６のピリドピラジンモジュレーター |
| CN107847762A (zh) | 2015-03-19 | 2018-03-27 | 诺维拉治疗公司 | 氮杂环辛烷和氮杂环壬烷衍生物以及治疗乙型肝炎感染的方法 |
| US10875876B2 (en) | 2015-07-02 | 2020-12-29 | Janssen Sciences Ireland Uc | Cyclized sulfamoylarylamide derivatives and the use thereof as medicaments for the treatment of hepatitis B |
| EP3356328A1 (en) | 2015-09-29 | 2018-08-08 | Novira Therapeutics, Inc. | Crystalline forms of a hepatitis b antiviral agent |
| EP3442524A2 (en) | 2016-04-15 | 2019-02-20 | Novira Therapeutics Inc. | Combinations and methods comprising a capsid assembly inhibitor |
| JOP20180057A1 (ar) * | 2017-06-15 | 2019-01-30 | Takeda Pharmaceuticals Co | مركبات رابع هيدروبيريدو بيرازين والتي تعمل كمعدلات gpr6 |
| US10973801B2 (en) | 2018-03-14 | 2021-04-13 | Janssen Sciences Ireland Unlimited Company | Capsid assembly modulator dosing regimen |
| US11096931B2 (en) | 2019-02-22 | 2021-08-24 | Janssen Sciences Ireland Unlimited Company | Amide derivatives useful in the treatment of HBV infection or HBV-induced diseases |
| US11491148B2 (en) | 2019-05-06 | 2022-11-08 | Janssen Sciences Ireland Unlimited Company | Amide derivatives useful in the treatment of HBV infection or HBV-induced diseases |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2195768A1 (en) * | 1994-08-11 | 1996-02-22 | Shuji Hinuma | G protein coupled receptor protein, production, and use thereof |
| JP2004515449A (ja) * | 1999-02-26 | 2004-05-27 | アリーナ・フアーマシユーチカルズ・インコーポレーテツド | 第６ｇタンパク質共役型受容体の小分子調節物質 |
| AU2001239549A1 (en) | 2000-03-24 | 2001-10-03 | Akzo Nobel N.V. | Keratinocyte growth inhibitors and hydroxamic acid derivatives |
| WO2004038416A1 (en) * | 2002-10-24 | 2004-05-06 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with human g-protein coupled receptor 6 (gpr6) |
| US7388019B2 (en) | 2003-01-31 | 2008-06-17 | Merck & Co., Inc. | 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| SE0400285D0 (sv) * | 2004-02-10 | 2004-02-10 | Astrazeneca Ab | Pyrroloquinoline and piperidoquinoline derivatives, preparation thereof, compositions containing them and uses thereof |
| US20070054916A1 (en) | 2004-10-01 | 2007-03-08 | Amgen Inc. | Aryl nitrogen-containing bicyclic compounds and methods of use |
| RS51885B (en) * | 2006-04-21 | 2012-02-29 | Pfizer Products Inc. | PYRIDIN [3,4-b] PYRAZINNES |
| WO2007125405A2 (en) | 2006-05-01 | 2007-11-08 | Pfizer Products Inc. | Substituted 2-amino-fused heterocyclic compounds |
| CN101766001B (zh) | 2007-06-05 | 2012-11-28 | 阿斯特里姆有限公司 | 远程测试***和方法 |
| GB0710844D0 (en) | 2007-06-06 | 2007-07-18 | Lectus Therapeutics Ltd | Potassium ion channel modulators & uses thereof |
| GB2449929A (en) | 2007-06-08 | 2008-12-10 | Snell & Wilcox Ltd | Hierarchical spatial resolution building processes to fill holes in an interpolated image |
| DK2440545T3 (da) | 2009-06-12 | 2019-07-22 | Abivax | Forbindelser, der er anvendelige til behandling af cancer |
| WO2013087815A1 (en) | 2011-12-15 | 2013-06-20 | Merz Pharma Gmbh & Co. Kgaa | Liquid pharmaceutical composition containing a pyrazolopyrimidine derivative and pharmaceutical uses thereof |
| WO2013087808A1 (en) | 2011-12-15 | 2013-06-20 | Merz Pharma Gmbh & Co. Kgaa | Pharmaceutical composition comprising a pyrazolopyrimidme and cyclodextrin |
| JP6345651B2 (ja) | 2012-05-09 | 2018-06-20 | サノビオン ファーマシューティカルズ インクＳｕｎｏｖｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃ． | ヘテロアリール化合物及びその使用方法 |
| EP2882722B1 (en) * | 2012-08-13 | 2016-07-27 | Takeda Pharmaceutical Company Limited | Quinoxaline derivatives as gpr6 modulators |
| FR2995937B1 (fr) | 2012-09-21 | 2014-09-26 | Exoes | Ensemble de production d'electricite a moteur a pression de vapeur |
| JO3466B1 (ar) * | 2013-12-20 | 2020-07-05 | Takeda Pharmaceuticals Co | مواد ضابطة لتترا هيدرو بيريدوبيرازينات من gpr6 |
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2014
- 2014-12-18 JO JOP/2014/0369A patent/JO3466B1/ar active
- 2014-12-19 SG SG11201604921TA patent/SG11201604921TA/en unknown
- 2014-12-19 DK DK14833425.3T patent/DK3083620T3/en active
- 2014-12-19 KR KR1020167019644A patent/KR102441531B1/ko active IP Right Grant
- 2014-12-19 MY MYPI2016001142A patent/MY177031A/en unknown
- 2014-12-19 EA EA201691272A patent/EA032443B1/ru unknown
- 2014-12-19 PT PT14833425T patent/PT3083620T/pt unknown
- 2014-12-19 TN TN2016000244A patent/TN2016000244A1/en unknown
- 2014-12-19 AU AU2014368992A patent/AU2014368992C1/en active Active
- 2014-12-19 MA MA39193A patent/MA39193B1/fr unknown
- 2014-12-19 EP EP14833425.3A patent/EP3083620B1/en active Active
- 2014-12-19 CA CA2934247A patent/CA2934247C/en active Active
- 2014-12-19 WO PCT/US2014/071543 patent/WO2015095728A1/en active Application Filing
- 2014-12-19 PE PE2016000838A patent/PE20160751A1/es unknown
- 2014-12-19 UY UY0001035908A patent/UY35908A/es not_active Application Discontinuation
- 2014-12-19 TW TW103144660A patent/TWI730937B/zh active
- 2014-12-19 RS RS20181548A patent/RS58092B1/sr unknown
- 2014-12-19 PL PL14833425T patent/PL3083620T3/pl unknown
- 2014-12-19 UA UAA201606659A patent/UA120427C2/uk unknown
- 2014-12-19 TW TW110118089A patent/TWI809395B/zh active
- 2014-12-19 AR ARP140104807A patent/AR098872A1/es active IP Right Grant
- 2014-12-19 CN CN201810356710.6A patent/CN108658978A/zh active Pending
- 2014-12-19 US US14/577,480 patent/US9181249B2/en active Active
- 2014-12-19 MX MX2016008188A patent/MX2016008188A/es active IP Right Grant
- 2014-12-19 EP EP18187138.5A patent/EP3453709A1/en not_active Withdrawn
- 2014-12-19 SI SI201430995T patent/SI3083620T1/sl unknown
- 2014-12-19 GE GEAP201414210A patent/GEP201706783B/en unknown
- 2014-12-19 JP JP2016541330A patent/JP6538697B2/ja active Active
- 2014-12-19 ES ES14833425T patent/ES2702187T3/es active Active
- 2014-12-19 HU HUE14833425A patent/HUE042443T2/hu unknown
- 2014-12-19 BR BR112016014020-6A patent/BR112016014020B1/pt active IP Right Grant
- 2014-12-19 CN CN201480069550.7A patent/CN105829309B/zh active Active
- 2014-12-19 LT LTEP14833425.3T patent/LT3083620T/lt unknown
- 2014-12-19 TR TR2019/00038T patent/TR201900038T4/tr unknown
- 2014-12-19 NZ NZ721723A patent/NZ721723A/en unknown
- 2014-12-19 CR CR20160321A patent/CR20160321A/es unknown
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2015
- 2015-10-14 US US14/883,174 patent/US9708313B2/en active Active
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2016
- 2016-06-13 IL IL24617716A patent/IL246177B/en active IP Right Grant
- 2016-06-17 DO DO2016000144A patent/DOP2016000144A/es unknown
- 2016-06-17 PH PH12016501192A patent/PH12016501192B1/en unknown
- 2016-06-20 CL CL2016001595A patent/CL2016001595A1/es unknown
- 2016-07-08 ZA ZA2016/04703A patent/ZA201604703B/en unknown
- 2016-07-20 EC ECIEPI201661758A patent/ECSP16061758A/es unknown
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2017
- 2017-06-13 US US15/621,761 patent/US10077266B2/en active Active
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2018
- 2018-08-07 US US16/057,350 patent/US10738046B2/en active Active
- 2018-11-27 HR HRP20182004TT patent/HRP20182004T1/hr unknown
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2019
- 2019-01-03 CY CY20191100008T patent/CY1121395T1/el unknown
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