MX2012008147A - Derivados de pirrazolopiridina. - Google Patents
Derivados de pirrazolopiridina.Info
- Publication number
- MX2012008147A MX2012008147A MX2012008147A MX2012008147A MX2012008147A MX 2012008147 A MX2012008147 A MX 2012008147A MX 2012008147 A MX2012008147 A MX 2012008147A MX 2012008147 A MX2012008147 A MX 2012008147A MX 2012008147 A MX2012008147 A MX 2012008147A
- Authority
- MX
- Mexico
- Prior art keywords
- sub
- lower alkyl
- halogen
- substituted
- hydrogen
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 10
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 101001125071 Homo sapiens Neuromedin-K receptor Proteins 0.000 abstract 2
- 102100029409 Neuromedin-K receptor Human genes 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 abstract 1
- 102100037346 Substance-P receptor Human genes 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 230000009977 dual effect Effects 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 239000002464 receptor antagonist Substances 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
Classifications
-
- 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
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Catalysts (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
La presente invención, se relaciona con un compuesto de la Fórmula (I) en donde R1 es hidrógeno, alquilo inferior, alquilo inferior substituido por halógeno, bencilo, -C(O)-alquilo inferior, -C(O)-CH2-alcoxi inferior, C-(O)cicloalquil-C3-6 -(CH2)o-C(O)-NR,R´, -(CH2)0S(O)2-alquilo inferior o -S(O)2-NR,R´; o es 0 o 1; R, R´ son independientemente uno de otro hidrógeno o alquilo inferior, o pueden formar junto con el átomo N al cual están unidos 5 o 6 miembros del anillo heterocicloalquilo; R2 es hidrógeno o alquilo inferior; R3 es halógeno, alcoxi inferior, alquilo inferior substituido por halógeno o alcoxi inferior substituido por halógeno; y pueden ser iguales o diferentes en caso de que n sea 2; n es 1 o 2; Ar es fenilo opcionalmente substituido por uno o dos sustituyentes seleccionados del alquilo inferior, halógeno, alcoxi inferior, alquilo inferior substituido por hidroxi o ciano, o es un grupo heteroarilo con cinco o seis miembros, seleccionado de tiofenilo o piridinilo que son substituidos opcionalmente por alquilo o halógeno inferior; o a una sal de adición de ácido farmacéuticamente activa. Se ha encontrado asombrosamente que los compuestos de la fórmula 1 muestran una alta afinidad simultáneamente a ambos los receptores NK1 y NK3 (antagonistas de los receptores NK1/NK3 duales), útiles en el tratamiento de esquizofrenia.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10160481 | 2010-04-20 | ||
| PCT/EP2011/055971 WO2011131571A1 (en) | 2010-04-20 | 2011-04-15 | Pyrrazolopyridine derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2012008147A true MX2012008147A (es) | 2012-08-03 |
Family
ID=43923714
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2012008147A MX2012008147A (es) | 2010-04-20 | 2011-04-15 | Derivados de pirrazolopiridina. |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8487102B2 (es) |
| EP (1) | EP2560974B1 (es) |
| JP (1) | JP5592992B2 (es) |
| KR (1) | KR101484831B1 (es) |
| CN (1) | CN102858775B (es) |
| BR (1) | BR112012026458A2 (es) |
| CA (1) | CA2786837A1 (es) |
| ES (1) | ES2562983T3 (es) |
| MX (1) | MX2012008147A (es) |
| RU (1) | RU2561276C2 (es) |
| WO (1) | WO2011131571A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013135672A1 (en) | 2012-03-13 | 2013-09-19 | Basf Se | Fungicidal pyrimidine compounds |
| WO2016021562A1 (ja) * | 2014-08-06 | 2016-02-11 | キッセイ薬品工業株式会社 | シアノチオフェン誘導体 |
| WO2016184829A1 (en) | 2015-05-18 | 2016-11-24 | Nerre Therapeutics Limited | Dual nk-1/nk-3 receptor antagonists for the treatment of sex-hormone-dependent diseases |
| SG11202008226YA (en) | 2018-03-14 | 2020-09-29 | Kandy Therapeutics Ltd | Novel pharmaceutical formulation comprising dual nk-1/nk-3 receptor antagonists |
| WO2024220539A1 (en) | 2023-04-18 | 2024-10-24 | Kallyope, Inc. | Nk3 modulators and uses thereof |
| WO2024220541A1 (en) * | 2023-04-18 | 2024-10-24 | Kallyope, Inc. | Nk3 modulators and uses thereof |
| WO2024220543A1 (en) * | 2023-04-18 | 2024-10-24 | Kallyope, Inc. | Nk3 modulators and uses thereof |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL111960A (en) | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| ATE278687T1 (de) | 1993-12-29 | 2004-10-15 | Merck Sharp & Dohme | Substituierte morpholinderivate und ihre verwendung als therapeutische mittel |
| TW385308B (en) | 1994-03-04 | 2000-03-21 | Merck & Co Inc | Prodrugs of morpholine tachykinin receptor antagonists |
| DE69531458T2 (de) * | 1994-05-27 | 2004-08-05 | Glaxosmithkline S.P.A. | Chinolinderivate als tachykinin nk3 rezeptor antagonisten |
| US5972938A (en) | 1997-12-01 | 1999-10-26 | Merck & Co., Inc. | Method for treating or preventing psychoimmunological disorders |
| EP1319001A1 (en) * | 2000-09-22 | 2003-06-18 | Smithkline Beecham Plc | Pyrazolopyridines and pyrazolopyridazines as antidiabetics |
| EP1192952A3 (en) | 2000-09-28 | 2003-03-26 | Pfizer Products Inc. | Combination, for treating depression and anxiety, containing an NK-3 receptor antagonist and a CNS penetrant NK-1 receptor antagonist |
| AU2002222293A1 (en) * | 2000-12-19 | 2002-07-01 | Smithkline Beecham P.L.C. | Pyrazolo(3,4-c)pyridines as gsk-3 inhibitors |
| PL214231B1 (pl) * | 2001-04-27 | 2013-07-31 | Eisai R & D Man Co | Pochodne pirazolo [1,5-a] pirydyny, kompozycje je zawierajace oraz zastosowanie |
| TW200306819A (en) * | 2002-01-25 | 2003-12-01 | Vertex Pharma | Indazole compounds useful as protein kinase inhibitors |
| WO2003068773A1 (en) * | 2002-02-12 | 2003-08-21 | Glaxo Group Limited | Pyrazolopyridine derivatives |
| US7176216B2 (en) * | 2002-10-22 | 2007-02-13 | Eisai Co., Ltd. | 7-phenylpyrazolopyridine compounds |
| JP2006513159A (ja) * | 2002-11-01 | 2006-04-20 | メルク エンド カムパニー インコーポレーテッド | アンドロゲン受容体モジュレーターとしてのカルボニルアミノ−ベンズイミダゾール誘導体 |
| RU2348633C2 (ru) * | 2002-12-23 | 2009-03-10 | Глаксо Груп Лимитед | ПИРАЗОЛО[3,4-b]ПИРИДИНОВЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ ФОСФОДИЭСТЕРАЗ |
| AU2004253267B2 (en) | 2003-07-03 | 2008-12-04 | F. Hoffmann-La Roche Ag | Dual NK1/NK3 antagonists for treating schizophrenia |
| US20060030600A1 (en) | 2004-08-06 | 2006-02-09 | Patrick Schnider | Dual NK1/NK3 receptor antagonists for the treatment of schizophrenia |
| WO2007036734A1 (en) * | 2005-09-29 | 2007-04-05 | Glaxo Group Limited | Pyrazolo[3,4-b]pyridine compound, and its use as a pde4 inhibitor |
| PE20070978A1 (es) * | 2006-02-14 | 2007-11-15 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) |
-
2011
- 2011-04-11 US US13/083,636 patent/US8487102B2/en not_active Expired - Fee Related
- 2011-04-15 MX MX2012008147A patent/MX2012008147A/es active IP Right Grant
- 2011-04-15 CA CA2786837A patent/CA2786837A1/en not_active Abandoned
- 2011-04-15 KR KR1020127030061A patent/KR101484831B1/ko not_active Expired - Fee Related
- 2011-04-15 JP JP2013505421A patent/JP5592992B2/ja not_active Expired - Fee Related
- 2011-04-15 RU RU2012146874/04A patent/RU2561276C2/ru not_active IP Right Cessation
- 2011-04-15 EP EP11714558.1A patent/EP2560974B1/en not_active Not-in-force
- 2011-04-15 BR BR112012026458A patent/BR112012026458A2/pt not_active IP Right Cessation
- 2011-04-15 CN CN201180019686.3A patent/CN102858775B/zh not_active Expired - Fee Related
- 2011-04-15 WO PCT/EP2011/055971 patent/WO2011131571A1/en not_active Ceased
- 2011-04-15 ES ES11714558.1T patent/ES2562983T3/es active Active
Also Published As
| Publication number | Publication date |
|---|---|
| KR20130027513A (ko) | 2013-03-15 |
| JP5592992B2 (ja) | 2014-09-17 |
| CA2786837A1 (en) | 2011-10-27 |
| EP2560974B1 (en) | 2016-01-27 |
| WO2011131571A1 (en) | 2011-10-27 |
| US8487102B2 (en) | 2013-07-16 |
| RU2561276C2 (ru) | 2015-08-27 |
| ES2562983T3 (es) | 2016-03-09 |
| HK1174625A1 (en) | 2013-06-14 |
| CN102858775B (zh) | 2015-04-01 |
| KR101484831B1 (ko) | 2015-01-20 |
| BR112012026458A2 (pt) | 2016-08-09 |
| RU2012146874A (ru) | 2014-05-27 |
| JP2013530131A (ja) | 2013-07-25 |
| US20110257402A1 (en) | 2011-10-20 |
| CN102858775A (zh) | 2013-01-02 |
| EP2560974A1 (en) | 2013-02-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |