AR045069A1 - Derivados de pirazol-fenil urea como moduladores del receptor 5ht 2a de serotonina, utiles para la profilaxis y tratamiento de desordenes relacionados con el mismo - Google Patents
Derivados de pirazol-fenil urea como moduladores del receptor 5ht 2a de serotonina, utiles para la profilaxis y tratamiento de desordenes relacionados con el mismoInfo
- Publication number
- AR045069A1 AR045069A1 ARP040102586A ARP040102586A AR045069A1 AR 045069 A1 AR045069 A1 AR 045069A1 AR P040102586 A ARP040102586 A AR P040102586A AR P040102586 A ARP040102586 A AR P040102586A AR 045069 A1 AR045069 A1 AR 045069A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkoxy
- group
- alkyl
- carboxy
- alkynyl
- Prior art date
Links
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 title abstract 3
- 238000011282 treatment Methods 0.000 title abstract 3
- 102000049773 5-HT2A Serotonin Receptor Human genes 0.000 title 1
- 108010072564 5-HT2A Serotonin Receptor Proteins 0.000 title 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 title 1
- 239000004202 carbamide Substances 0.000 title 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 10
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 10
- 229910052736 halogen Inorganic materials 0.000 abstract 10
- 150000002367 halogens Chemical class 0.000 abstract 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 9
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 9
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 8
- -1 C 1-6 alkylureyl Chemical group 0.000 abstract 8
- 125000005431 alkyl carboxamide group Chemical group 0.000 abstract 8
- 125000004422 alkyl sulphonamide group Chemical group 0.000 abstract 8
- 125000005392 carboxamide group Chemical class NC(=O)* 0.000 abstract 8
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 8
- 125000005432 dialkylcarboxamide group Chemical group 0.000 abstract 8
- 125000004995 haloalkylthio group Chemical group 0.000 abstract 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 7
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 7
- 125000002252 acyl group Chemical group 0.000 abstract 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 7
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 6
- 125000004423 acyloxy group Chemical group 0.000 abstract 6
- 125000003545 alkoxy group Chemical group 0.000 abstract 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 6
- 208000035475 disorder Diseases 0.000 abstract 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 6
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 5
- 125000004749 (C1-C6) haloalkylsulfinyl group Chemical group 0.000 abstract 5
- 125000004741 (C1-C6) haloalkylsulfonyl group Chemical group 0.000 abstract 5
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000003396 thiol group Chemical class [H]S* 0.000 abstract 5
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 abstract 4
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 4
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 4
- 208000028017 Psychotic disease Diseases 0.000 abstract 4
- 125000005363 dialkylsulfonamide group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 229940124530 sulfonamide Drugs 0.000 abstract 4
- 150000003456 sulfonamides Chemical class 0.000 abstract 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 3
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 201000000980 schizophrenia Diseases 0.000 abstract 3
- 125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 abstract 2
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 abstract 2
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 abstract 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 2
- 125000004771 (C1-C4) haloalkylsulfinyl group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004441 haloalkylsulfonyl group Chemical group 0.000 abstract 2
- LNEPOXFFQSENCJ-UHFFFAOYSA-N haloperidol Chemical compound C1CC(O)(C=2C=CC(Cl)=CC=2)CCN1CCCC(=O)C1=CC=C(F)C=C1 LNEPOXFFQSENCJ-UHFFFAOYSA-N 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 238000011321 prophylaxis Methods 0.000 abstract 2
- 208000024891 symptom Diseases 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 abstract 1
- 125000006705 (C5-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 206010002383 Angina Pectoris Diseases 0.000 abstract 1
- 206010003658 Atrial Fibrillation Diseases 0.000 abstract 1
- 208000020925 Bipolar disease Diseases 0.000 abstract 1
- 101150049660 DRD2 gene Proteins 0.000 abstract 1
- 229940121891 Dopamine receptor antagonist Drugs 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- 208000011963 Substance-induced psychotic disease Diseases 0.000 abstract 1
- 231100000393 Substance-induced psychotic disorder Toxicity 0.000 abstract 1
- 238000013019 agitation Methods 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000005277 alkyl imino group Chemical group 0.000 abstract 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 abstract 1
- 125000005422 alkyl sulfonamido group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 230000003542 behavioural effect Effects 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 230000035602 clotting Effects 0.000 abstract 1
- 208000029078 coronary artery disease Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 239000003210 dopamine receptor blocking agent Substances 0.000 abstract 1
- 201000002545 drug psychosis Diseases 0.000 abstract 1
- 230000002964 excitative effect Effects 0.000 abstract 1
- 210000002816 gill Anatomy 0.000 abstract 1
- 229960003878 haloperidol Drugs 0.000 abstract 1
- 230000000302 ischemic effect Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 208000010125 myocardial infarction Diseases 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229940076279 serotonin Drugs 0.000 abstract 1
- 208000019116 sleep disease Diseases 0.000 abstract 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
- 230000001052 transient effect Effects 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
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- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- 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
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- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
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Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US48957203P | 2003-07-22 | 2003-07-22 | |
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