MX2011008178A - Derivados de pirrolidina como antagonistas del receptor de neuroquinina 3 (nk3). - Google Patents
Derivados de pirrolidina como antagonistas del receptor de neuroquinina 3 (nk3).Info
- Publication number
- MX2011008178A MX2011008178A MX2011008178A MX2011008178A MX2011008178A MX 2011008178 A MX2011008178 A MX 2011008178A MX 2011008178 A MX2011008178 A MX 2011008178A MX 2011008178 A MX2011008178 A MX 2011008178A MX 2011008178 A MX2011008178 A MX 2011008178A
- Authority
- MX
- Mexico
- Prior art keywords
- lower alkyl
- halogen
- hydrogen
- receptor antagonists
- substituted
- Prior art date
Links
- 102000002003 Neurokinin-3 Receptors Human genes 0.000 title abstract 2
- 108010040716 Neurokinin-3 Receptors Proteins 0.000 title abstract 2
- 239000002464 receptor antagonist Substances 0.000 title abstract 2
- 229940044551 receptor antagonist Drugs 0.000 title abstract 2
- 150000003235 pyrrolidines Chemical class 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 8
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 abstract 1
- 208000020925 Bipolar disease 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
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 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
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
-
- 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
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
- C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Abstract
La presente invención se relaciona con compuestos de la fórmula I en donde A es - NR'-, -S, -S(O)- o - S(O)2-; R´ es hidrógeno o alquilo inferior; Ar es arilo o es un grupo heteroarilo de cinco o seis miembros, que contiene uno o dos átomos de N; R es un grupo heterocíclico de cinco o seis miembros, X1 es N o CH; y X2 es -N(R1)-, -CH2-, -O-, -S, -S(O)-, o -S(O)2-, R1 es hidrógeno, alquilo inferior, S(O)2-alquilo inferior, C(O)-alquilo inferior, C(O)-cicloalquilo opcionalmente substituido por alquilo inferior; con la condición de que por lo menos uno de X1 o X2 contenga un heteroátomo, o sea un grupo heteroarilo de cinco o seis miembros, que contiene uno o dos átomos de N, cuyos grupos están sin sustituir o pueden ser substituidos por uno o dos R1; en donde R1 es un alquilo inferior o ciano; R2 es un alquilo inferior substituido por halógeno, halógeno, ciano o nitro; R3 es halógeno; R4 es hidrógeno o alquilo inferior; o es 1 o 2; en caso de que o sea 2, R2 puede ser igual o diferente; p es 1 o 2; en caso de que p sea 2, R3 puede ser igual o diferente; o una sal farmacéuticamente activa del mismo. Se ha encontrado que los presentes compuestos son antagonistas del receptor NK-3 de alto potencial para el tratamiento de depresión, dolor, psicosis, enfermedad de Parkinson, esquizofrenia, trastornos bipolares, ansiedad y trastorno de déficit de atención con hiperactividad (ADHD).
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP09153097 | 2009-02-18 | ||
PCT/EP2010/051887 WO2010094667A1 (en) | 2009-02-18 | 2010-02-16 | Pyrrolidine derivatives as nk3 receptor antagonists |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2011008178A true MX2011008178A (es) | 2011-08-17 |
Family
ID=42115644
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2011008178A MX2011008178A (es) | 2009-02-18 | 2010-02-16 | Derivados de pirrolidina como antagonistas del receptor de neuroquinina 3 (nk3). |
Country Status (12)
Country | Link |
---|---|
US (1) | US8318759B2 (es) |
EP (1) | EP2398768B1 (es) |
JP (1) | JP5452622B2 (es) |
KR (1) | KR101304130B1 (es) |
CN (1) | CN102307853B (es) |
AU (1) | AU2010215513B2 (es) |
BR (1) | BRPI1016115A8 (es) |
CA (1) | CA2748701A1 (es) |
IL (1) | IL213763A (es) |
MX (1) | MX2011008178A (es) |
SG (1) | SG173638A1 (es) |
WO (1) | WO2010094667A1 (es) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102177136A (zh) * | 2008-10-09 | 2011-09-07 | 弗·哈夫曼-拉罗切有限公司 | 吡咯烷n-苄基衍生物 |
US8618303B2 (en) * | 2011-01-07 | 2013-12-31 | Hoffmann-La Roche Inc. | Pyrrolidine derivatives |
WO2017072629A1 (en) | 2015-10-29 | 2017-05-04 | Cadila Healthcare Limited | Pharmaceutical combination of nk3 receptor antagonist and biguanides |
CN115335050B (zh) * | 2020-01-29 | 2024-05-17 | 卡玛瑞制药有限公司 | 用于治疗皮肤病症的化合物和组合物 |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2635838T3 (es) * | 2002-08-26 | 2017-10-05 | Takeda Pharmaceutical Company Limited | Compuesto modulador de receptores de calcio y su uso |
US7138423B2 (en) * | 2004-07-20 | 2006-11-21 | Bristol-Myers Squibb Company | Arylpyrrolidine derivatives as NK-1 /SSRI antagonists |
WO2006123725A1 (ja) * | 2005-05-19 | 2006-11-23 | Astellas Pharma Inc. | ピロリジン誘導体またはその塩 |
EP2148857B1 (en) | 2007-04-20 | 2010-07-28 | F. Hoffmann-La Roche AG | Pyrrolidine derivatives as dual nk1/nk3 receptors antagonists |
CN101778837A (zh) * | 2007-08-07 | 2010-07-14 | 弗·哈夫曼-拉罗切有限公司 | 作为nk3受体拮抗剂的吡咯烷芳基-醚 |
BRPI0815085A2 (pt) | 2007-08-09 | 2014-09-30 | Basf Se | Misturas fungicidas, agente fungicida, processo para combater fungos nocivos fitopatogênicos, semente, e, uso de compostos. |
CA2697325A1 (en) * | 2007-08-22 | 2009-02-26 | F. Hoffmann-La Roche Ag | Pyrrolidine aryl-ether as nk3 receptor antagonists |
US8063075B2 (en) * | 2008-06-10 | 2011-11-22 | Hoffmann-La Roche Inc. | Pyrrolidine ether derivatives as NK3 receptor antagonists |
US8022099B2 (en) * | 2008-11-03 | 2011-09-20 | Hoffmann-La Roche Inc. | N-benzyl pyrrolidine derivatives |
-
2010
- 2010-02-11 US US12/703,804 patent/US8318759B2/en not_active Expired - Fee Related
- 2010-02-16 JP JP2011549595A patent/JP5452622B2/ja not_active Expired - Fee Related
- 2010-02-16 WO PCT/EP2010/051887 patent/WO2010094667A1/en active Application Filing
- 2010-02-16 AU AU2010215513A patent/AU2010215513B2/en not_active Ceased
- 2010-02-16 CN CN201080006985.9A patent/CN102307853B/zh not_active Expired - Fee Related
- 2010-02-16 EP EP10704808.4A patent/EP2398768B1/en not_active Not-in-force
- 2010-02-16 CA CA2748701A patent/CA2748701A1/en not_active Abandoned
- 2010-02-16 BR BRPI1016115A patent/BRPI1016115A8/pt not_active IP Right Cessation
- 2010-02-16 MX MX2011008178A patent/MX2011008178A/es active IP Right Grant
- 2010-02-16 SG SG2011057742A patent/SG173638A1/en unknown
- 2010-02-16 KR KR1020117021802A patent/KR101304130B1/ko not_active IP Right Cessation
-
2011
- 2011-06-23 IL IL213763A patent/IL213763A/en not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
JP5452622B2 (ja) | 2014-03-26 |
US8318759B2 (en) | 2012-11-27 |
WO2010094667A1 (en) | 2010-08-26 |
AU2010215513B2 (en) | 2014-06-12 |
CN102307853A (zh) | 2012-01-04 |
AU2010215513A1 (en) | 2011-08-11 |
JP2012517981A (ja) | 2012-08-09 |
IL213763A0 (en) | 2011-07-31 |
BRPI1016115A2 (pt) | 2016-04-12 |
BRPI1016115A8 (pt) | 2018-01-02 |
US20100210659A1 (en) | 2010-08-19 |
KR101304130B1 (ko) | 2013-09-05 |
CA2748701A1 (en) | 2010-08-26 |
KR20110120957A (ko) | 2011-11-04 |
SG173638A1 (en) | 2011-09-29 |
CN102307853B (zh) | 2015-09-02 |
EP2398768B1 (en) | 2016-08-24 |
IL213763A (en) | 2014-12-31 |
EP2398768A1 (en) | 2011-12-28 |
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