PE20160751A1 - Moduladores de tetrahidropiridopirazinas de gpr6 - Google Patents
Moduladores de tetrahidropiridopirazinas de gpr6Info
- Publication number
- PE20160751A1 PE20160751A1 PE2016000838A PE2016000838A PE20160751A1 PE 20160751 A1 PE20160751 A1 PE 20160751A1 PE 2016000838 A PE2016000838 A PE 2016000838A PE 2016000838 A PE2016000838 A PE 2016000838A PE 20160751 A1 PE20160751 A1 PE 20160751A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- cycloalkyl
- gpr6
- tetrahydropyridopyrazine
- modulators
- 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
-
- 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
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Nutrition Science (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
La presente invencion se refiere a compuestos moduladores de GPR6 de Formula I donde R1 es cicloalquilo C3-C8, heterociclilo C3-C6 y heteroarilo C1-C10 cada uno opcionalmente sustituidos; X1 es N y X2 es CH o X1 es CH y X2 es N o X1 es N y X2 es N; Z es alquileno C1-C6, haloalquilenos C1-C6, entre otros; q, s y p son 0, 1 o 2; R2 es -OR5 o NR6R7; R3 es alquilo C1-C6, cicloalquilo C3-C8 y trifluorometilo; R4 es alquilo C1-C6, hidroxi o halo; r es 0 o 1; R5 es alquilo C1-C6 y cicloalquilo C3-C8; R6 es hidrogeno y alquilo C1-C6; R7 es alquilo C1-C6, cicloalquilo C3-C8, entre otros; X3 es CH y CR4 y X4 es NR8 o viceversa y R8 es alquilo C1-C6, haloalquilo C1-C6, entre otros. Son compuestos preferidos: ciclopropil-(2-(4-(2,4-difluorofenoxi)piperidin-1-il)-3-(isopropilamino)-7,8-dihidropirido[3,4-b]pirazin-6(5H)-il)metanona; 1-(2-(4-(2,4-difluorofenoxi)piperidin-1-il)-3-(isopropilamino)-7,8-dihidropirido[3,4-b]pirazin-6(5H)-il)-2-metoxietan-1-ona; entre otros. Dichos compuestos son derivados de tetrahidropiridopirazinas siendo utiles en el tratamiento de afecciones asociadas con GPR6
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361919661P | 2013-12-20 | 2013-12-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20160751A1 true PE20160751A1 (es) | 2016-08-01 |
Family
ID=52440811
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2016000838A PE20160751A1 (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 |
|---|---|---|---|---|
| KR20190007106A (ko) | 2011-12-21 | 2019-01-21 | 노비라 테라퓨틱스, 인코포레이티드 | B형 간염의 항바이러스성 제제 |
| US9487526B2 (en) | 2012-08-13 | 2016-11-08 | Takeda Pharmaceutical Company Limited | Quinoxaline derivatives as GPR6 modulators |
| NZ743463A (en) | 2012-08-28 | 2019-09-27 | Janssen Sciences Ireland Uc | Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of hepatitis b |
| DK2961732T3 (en) | 2013-02-28 | 2017-07-10 | Janssen Sciences Ireland Uc | SULFAMOYLARYLAMIDS AND USE THEREOF AS MEDICINES TO TREAT HEPATITIS B |
| WO2014161888A1 (en) | 2013-04-03 | 2014-10-09 | Janssen R&D Ireland | N-phenyl-carboxamide derivatives and the use thereof as medicaments for the treatment of hepatitis b |
| LT2997019T (lt) | 2013-05-17 | 2018-11-26 | Janssen Sciences Ireland Uc | Sulfamoiltiofenamido dariniai ir jų panaudojimas kaip vaistų hepatito b gydymui |
| JO3603B1 (ar) | 2013-05-17 | 2020-07-05 | Janssen Sciences Ireland Uc | مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي |
| LT3024819T (lt) | 2013-07-25 | 2018-06-11 | Janssen Sciences Ireland Uc | Pirolamido dariniai, turintys glioksamido pakaitų, ir jų panaudojimas kaip vaistų hepatito b gydymui |
| JP6452119B2 (ja) | 2013-10-23 | 2019-01-16 | ヤンセン・サイエンシズ・アイルランド・アンリミテッド・カンパニー | カルボキサミド誘導体およびｂ型肝炎の処置のための医薬品としてのその使用 |
| 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 |
| EP3102225B1 (en) | 2014-02-05 | 2020-03-25 | Novira Therapeutics Inc. | Combination therapy for treatment of hbv infections |
| 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 |
| WO2016149581A1 (en) | 2015-03-19 | 2016-09-22 | Novira Therapeutics, Inc. | Azocane and azonane derivatives and methods of treating hepatitis b infections |
| 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 |
| TW201718496A (zh) | 2015-09-29 | 2017-06-01 | 諾維拉治療公司 | B型肝炎抗病毒劑之晶型 |
| AU2017248828A1 (en) | 2016-04-15 | 2018-11-01 | Janssen Sciences Ireland Uc | 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 |
| CN111867582A (zh) | 2018-03-14 | 2020-10-30 | 爱尔兰詹森科学公司 | 衣壳组装调节剂给药方案 |
| MA55020A (fr) | 2019-02-22 | 2021-12-29 | Janssen Sciences Ireland Unlimited Co | Dérivés d'amide utiles dans le traitement d'une infection par le virus de l'hépatite b ou de maladies induites par le virus de l'hépatite b |
| JP2022532526A (ja) | 2019-05-06 | 2022-07-15 | ヤンセン・サイエンシズ・アイルランド・アンリミテッド・カンパニー | Ｈｂｖ感染又はｈｂｖ誘導性疾患の処置において有用なアミド誘導体 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0804575A1 (en) * | 1994-08-11 | 1997-11-05 | Takeda Chemical Industries, Ltd. | G protein coupled receptor protein, production, and use thereof |
| WO2001062765A2 (en) | 1999-02-26 | 2001-08-30 | Arena Pharmaceuticals, Inc. | Small molecule modulators of g protein-coupled receptor six |
| AU2001239549A1 (en) | 2000-03-24 | 2001-10-03 | Akzo Nobel N.V. | Keratinocyte growth inhibitors and hydroxamic acid derivatives |
| AU2003274005A1 (en) * | 2002-10-24 | 2004-05-13 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with human g-protein coupled receptor 6 (gpr6) |
| WO2004069162A2 (en) | 2003-01-31 | 2004-08-19 | 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 |
| JP2009535393A (ja) | 2006-05-01 | 2009-10-01 | ファイザー・プロダクツ・インク | 置換２−アミノ縮合複素環式化合物 |
| 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 |
| CN106928194B (zh) | 2009-06-12 | 2019-11-12 | Abivax公司 | 用于治疗过早衰老和尤其是早衰的化合物 |
| WO2013087808A1 (en) | 2011-12-15 | 2013-06-20 | Merz Pharma Gmbh & Co. Kgaa | Pharmaceutical composition comprising a pyrazolopyrimidme and cyclodextrin |
| WO2013087815A1 (en) | 2011-12-15 | 2013-06-20 | Merz Pharma Gmbh & Co. Kgaa | Liquid pharmaceutical composition containing a pyrazolopyrimidine derivative and pharmaceutical uses thereof |
| AU2013259551B2 (en) | 2012-05-09 | 2017-11-02 | Sunovion Pharmaceuticals Inc. | Heteroaryl compounds and methods of use thereof |
| US9487526B2 (en) | 2012-08-13 | 2016-11-08 | 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 BR BR112016014020-6A patent/BR112016014020B1/pt active IP Right Grant
- 2014-12-19 UY UY0001035908A patent/UY35908A/es not_active Application Discontinuation
- 2014-12-19 TW TW110118089A patent/TWI809395B/zh active
- 2014-12-19 CN CN201480069550.7A patent/CN105829309B/zh active Active
- 2014-12-19 CN CN201810356710.6A patent/CN108658978A/zh active Pending
- 2014-12-19 SI SI201430995T patent/SI3083620T1/sl unknown
- 2014-12-19 MX MX2016008188A patent/MX2016008188A/es active IP Right Grant
- 2014-12-19 CA CA2934247A patent/CA2934247C/en active Active
- 2014-12-19 EP EP14833425.3A patent/EP3083620B1/en active Active
- 2014-12-19 LT LTEP14833425.3T patent/LT3083620T/lt unknown
- 2014-12-19 HU HUE14833425A patent/HUE042443T2/hu unknown
- 2014-12-19 TW TW103144660A patent/TWI730937B/zh 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 WO PCT/US2014/071543 patent/WO2015095728A1/en active Application Filing
- 2014-12-19 CR CR20160321A patent/CR20160321A/es unknown
- 2014-12-19 PE PE2016000838A patent/PE20160751A1/es unknown
- 2014-12-19 SG SG11201604921TA patent/SG11201604921TA/en unknown
- 2014-12-19 DK DK14833425.3T patent/DK3083620T3/en active
- 2014-12-19 TN TN2016000244A patent/TN2016000244A1/en unknown
- 2014-12-19 US US14/577,480 patent/US9181249B2/en active Active
- 2014-12-19 PL PL14833425T patent/PL3083620T4/pl unknown
- 2014-12-19 RS RS20181548A patent/RS58092B1/sr unknown
- 2014-12-19 MA MA39193A patent/MA39193B1/fr unknown
- 2014-12-19 UA UAA201606659A patent/UA120427C2/uk unknown
- 2014-12-19 AR ARP140104807A patent/AR098872A1/es active IP Right Grant
- 2014-12-19 NZ NZ721723A patent/NZ721723A/en unknown
- 2014-12-19 GE GEAP201414210A patent/GEP201706783B/en unknown
- 2014-12-19 TR TR2019/00038T patent/TR201900038T4/tr unknown
- 2014-12-19 ES ES14833425T patent/ES2702187T3/es active Active
- 2014-12-19 JP JP2016541330A patent/JP6538697B2/ja active Active
- 2014-12-19 AU AU2014368992A patent/AU2014368992C1/en active Active
- 2014-12-19 EP EP18187138.5A patent/EP3453709A1/en not_active Withdrawn
- 2014-12-19 PT PT14833425T patent/PT3083620T/pt unknown
- 2014-12-19 EA EA201691272A patent/EA032443B1/ru 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/PH12016501192A1/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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