BR112013000253A2 - derivados de (3-metilpirrolidin-3-il) metil piridinil éter e seu uso como antagonistas do receptor nk-3 - Google Patents
derivados de (3-metilpirrolidin-3-il) metil piridinil éter e seu uso como antagonistas do receptor nk-3Info
- Publication number
- BR112013000253A2 BR112013000253A2 BR112013000253A BR112013000253A BR112013000253A2 BR 112013000253 A2 BR112013000253 A2 BR 112013000253A2 BR 112013000253 A BR112013000253 A BR 112013000253A BR 112013000253 A BR112013000253 A BR 112013000253A BR 112013000253 A2 BR112013000253 A2 BR 112013000253A2
- Authority
- BR
- Brazil
- Prior art keywords
- lower alkyl
- substituted
- cyano
- halogen
- methyl
- Prior art date
Links
- 102000002003 Neurokinin-3 Receptors Human genes 0.000 title abstract 3
- 108010040716 Neurokinin-3 Receptors Proteins 0.000 title abstract 3
- 239000002464 receptor antagonist Substances 0.000 title abstract 3
- 229940044551 receptor antagonist Drugs 0.000 title abstract 3
- WQZMBSPAIOEJKF-UHFFFAOYSA-N 2-[(3-methylpyrrolidin-3-yl)methoxy]pyridine Chemical class CC1(COc2ccccn2)CCNC1 WQZMBSPAIOEJKF-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- -1 methyl pyridinol ether derivatives Chemical class 0.000 abstract 2
- XUWHAWMETYGRKB-UHFFFAOYSA-N piperidin-2-one Chemical compound O=C1CCCCN1 XUWHAWMETYGRKB-UHFFFAOYSA-N 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 abstract 1
- 208000020401 Depressive disease Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 208000028017 Psychotic disease Diseases 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/22—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
- A61P25/24—Antidepressants
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
derivados de (33-metilpirrolidin-3-il) metil piridinol éter e seu uso como antogonistas do receptor nk-3. a presente invenção refere-se a um composto de fórmula geral em que a é selecionado dentre os grupos (a), (b) ou (c): (a) ou (b) é cicloalquila, opcionalmente substtituído por alquila inferior (c); ar1 é fenila ou uma heteroarila de seis membros; x1 é n ou ch; x2 é n-r ou o; r1 é s(o)2-alquila inferior, c(o)-cicloalquila substituída por alquila inferior, ou é c(o)-alquila inferior, alquila inferior, ciano, cicloalquila ou é uma heteroarila de seis membros substtituída por alquila nferior, ciano, c(o)-alquila infeior, halogênio, alquila infeior substituída por halogênio ou alcóxi inferior; ou é fenila substtituída pro ciano ou halogênio; r2 é alquila inferior, halogênio, pirazolila, 3-metil-[1,2,4]oxazolila, 5-metil-[1,2,4]oxadiazol-3-ila, piridila substituída por ciano, ou é fenila substituída por halogênio, ou é ciano, alcóxi inferior, ou é piperidin-2-ona; ou a sais farmaceuticamente ativos, formas estereoisoméricas, incluindo diastereoisiômeros e enantiômeros individuais do composto de fórmula i assim como misturas racêmicas e não racêmicas dos mesmos. descobrimos que os presentes compostos são antagonistas do receptor nk-3 com alto potencial para o tratamento de depressão, dor, psicose, mal de parkinson, esquizofrenia, ansiedade e trasntorno do déficit de atenção com hiperatividade (adhd)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10168688.9 | 2010-07-07 | ||
| EP10168688 | 2010-07-07 | ||
| PCT/EP2011/061168 WO2012004207A1 (en) | 2010-07-07 | 2011-07-04 | (3 -methylpyrrolidin- 3 - yl) methyl pyridinyl ether derivatives and their use as nk-3 receptor antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR112013000253A2 true BR112013000253A2 (pt) | 2016-05-24 |
| BR112013000253B1 BR112013000253B1 (pt) | 2021-10-13 |
Family
ID=44276056
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112013000253-0A BR112013000253B1 (pt) | 2010-07-07 | 2011-07-04 | Derivados de (3-metilpirrolidin-3-il) metil piridinil éter, seu uso e processo de preparação e composição farmacêutica que os compreende |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8507535B2 (pt) |
| EP (1) | EP2590963B1 (pt) |
| JP (1) | JP5717154B2 (pt) |
| KR (1) | KR101485272B1 (pt) |
| CN (1) | CN102971310B (pt) |
| BR (1) | BR112013000253B1 (pt) |
| CA (1) | CA2803717C (pt) |
| ES (1) | ES2528370T3 (pt) |
| MX (1) | MX2012015268A (pt) |
| RU (1) | RU2625798C2 (pt) |
| WO (1) | WO2012004207A1 (pt) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2011253003B2 (en) * | 2010-05-13 | 2014-05-01 | Amgen Inc. | Heteroaryloxyheterocyclyl compounds as PDE10 inhibitors |
| EP3183248B1 (en) | 2014-08-21 | 2020-11-11 | Bristol-Myers Squibb Company | Tied-back benzamide derivatives as potent rock inhibitors |
| LT3344248T (lt) | 2015-09-02 | 2022-06-27 | Trevena, Inc. | 6-narių azaheterociklinių junginių, kurių sudėtyje yra deltaopioidų receptorius moduliuojančių junginių, panaudojimo ir gamybos būdai |
| KR20190129867A (ko) * | 2017-02-17 | 2019-11-20 | 트레베나, 인코포레이티드. | 5-원 아자-헤테로고리 함유 델타-오피오이드 수용체 조절 화합물, 및 그의 사용 및 제조 방법 |
| BR112019016775A2 (pt) | 2017-02-17 | 2020-03-31 | Trevena, Inc. | Compostos moduladores de receptor delta-opioide contendo aza-heterocíclico com 7 membros, métodos de uso e produção dos mesmos |
| WO2021030335A1 (en) * | 2019-08-12 | 2021-02-18 | Millendo Therapeutics, Inc. | A stereoisomerically pure nk-3 receptor antagonist and crystalline forms thereof |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO2696B1 (en) * | 2002-12-23 | 2013-03-03 | شركة جانسين فارماسوتيكا ان. في | Derivatives of 1-piperdine-4-yl-4-biprolidine-3-yl-piperazine substituted and used as quinine antagonists |
| US7138423B2 (en) * | 2004-07-20 | 2006-11-21 | Bristol-Myers Squibb Company | Arylpyrrolidine derivatives as NK-1 /SSRI antagonists |
| KR101163847B1 (ko) | 2007-04-20 | 2012-07-09 | 에프. 호프만-라 로슈 아게 | 이중 ｎｋ1/ｎｋ3 수용체 길항제로서의 피롤리딘 유도체 |
| AU2008285718A1 (en) * | 2007-08-07 | 2009-02-12 | F. Hoffmann-La Roche Ag | Pyrrolidine aryl-ether as NK3 receptor antagonists |
| KR101194467B1 (ko) | 2007-08-22 | 2012-10-24 | 에프. 호프만-라 로슈 아게 | Ｎｋ3 수용체 길항제로서의 피롤리딘 아릴-에터 |
| US8063075B2 (en) * | 2008-06-10 | 2011-11-22 | Hoffmann-La Roche Inc. | Pyrrolidine ether derivatives as NK3 receptor antagonists |
-
2011
- 2011-06-29 US US13/171,507 patent/US8507535B2/en active Active
- 2011-07-04 EP EP11728862.1A patent/EP2590963B1/en active Active
- 2011-07-04 RU RU2013102399A patent/RU2625798C2/ru active
- 2011-07-04 ES ES11728862.1T patent/ES2528370T3/es active Active
- 2011-07-04 KR KR1020137003090A patent/KR101485272B1/ko active Active
- 2011-07-04 CA CA2803717A patent/CA2803717C/en active Active
- 2011-07-04 BR BR112013000253-0A patent/BR112013000253B1/pt active IP Right Grant
- 2011-07-04 JP JP2013517325A patent/JP5717154B2/ja active Active
- 2011-07-04 MX MX2012015268A patent/MX2012015268A/es active IP Right Grant
- 2011-07-04 CN CN201180033350.2A patent/CN102971310B/zh active Active
- 2011-07-04 WO PCT/EP2011/061168 patent/WO2012004207A1/en active Application Filing
Also Published As
| Publication number | Publication date |
|---|---|
| CA2803717C (en) | 2018-01-30 |
| EP2590963A1 (en) | 2013-05-15 |
| HK1179619A1 (en) | 2013-10-04 |
| CA2803717A1 (en) | 2012-01-12 |
| WO2012004207A1 (en) | 2012-01-12 |
| EP2590963B1 (en) | 2014-12-03 |
| CN102971310B (zh) | 2015-06-03 |
| ES2528370T3 (es) | 2015-02-09 |
| JP5717154B2 (ja) | 2015-05-13 |
| KR101485272B1 (ko) | 2015-01-21 |
| JP2013531668A (ja) | 2013-08-08 |
| KR20130051474A (ko) | 2013-05-20 |
| RU2625798C2 (ru) | 2017-07-19 |
| RU2013102399A (ru) | 2014-08-20 |
| MX2012015268A (es) | 2013-02-07 |
| US8507535B2 (en) | 2013-08-13 |
| US20120010212A1 (en) | 2012-01-12 |
| CN102971310A (zh) | 2013-03-13 |
| BR112013000253B1 (pt) | 2021-10-13 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR062937A1 (es) | Compuestos que modulan el receptor cb2 | |
| EA201591703A1 (ru) | Замещенные 2-азабициклы и их применение в качестве модуляторов рецепторов орексина | |
| BR112013000253A2 (pt) | derivados de (3-metilpirrolidin-3-il) metil piridinil éter e seu uso como antagonistas do receptor nk-3 | |
| AR078168A1 (es) | Derivados de piperidinas y piperazinas, procesos para prepararlos y sus usos como moduladores de gpr119 | |
| PE20212247A1 (es) | Compuestos de 3-((3-aminofenil)amino)piperidina-2,6-diona sustituida, composiciones de estos y metodos de tratamiento con estos | |
| EA201391341A1 (ru) | Производные гетероциклических аминов | |
| MX2015015893A (es) | 2-fenilimidazo[1,2-a]pirimidinas como agentes formadores de imagen. | |
| AR083813A1 (es) | Derivados de pirazol aminopirimidina como moduladores de lrrk2 | |
| AR085960A1 (es) | 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2 | |
| BR112015015812A2 (pt) | derivados de pirimidina fundidos a pirido ou pirrolo como inibidores de autotaxina para tratamento de dor | |
| HRP20140687T1 (hr) | Derivati benzofurana | |
| PE20141167A1 (es) | Piridopirazinas sustituidas como inhibidores novedosos de ptk | |
| PE20140934A1 (es) | Derivados de pirazol | |
| AR085615A1 (es) | Derivados de fluoropiridinona utiles como agentes antibacterianos y composiciones farmaceuticas que los contienen | |
| BR112014007898A2 (pt) | derivados de etinila como moduladores alostéricos de mglur5 | |
| BR112015032637A2 (pt) | derivados de pirrolopiridina ou pirazolopiridina | |
| JP2013509392A5 (pt) | ||
| AR087915A1 (es) | N-(3-(2-amino-6,6-difluor-4,4a,5,6,7,7a-hexahidro-ciclopenta-[e][1,3]oxazin-4-il)-fenil)-amidas como inhibidores de la bace1 | |
| AR086554A1 (es) | Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina | |
| BR112013021848A2 (pt) | 5-(fenil/piridinil-etinil)-2-piridina/2-pirimidina-carboxamidas como moduladores de mglur5 | |
| BR112014015832A8 (pt) | derivados heterocíclicos como receptores associados com aminas vistigiais (taars) | |
| EA201391815A1 (ru) | Замещенные производные бензамида | |
| EA201071012A1 (ru) | Производные азетидинов, способ их получения и применение их в терапии | |
| BR112014004275A2 (pt) | derivados de isoxazolina como compostos inseticidas | |
| PE20141168A1 (es) | Derivados de pirazolidin-3-ona |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] |
Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI |
|
| B06T | Formal requirements before examination [chapter 6.20 patent gazette] | ||
| B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 04/07/2011, OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF, QUE DETERMINA A ALTERACAO DO PRAZO DE CONCESSAO. |