AR047812A1 - Compuestos de tetrazol y su uso como antagonistas del receptor de glutamato metabotropico - Google Patents
Compuestos de tetrazol y su uso como antagonistas del receptor de glutamato metabotropicoInfo
- Publication number
- AR047812A1 AR047812A1 ARP050100615A ARP050100615A AR047812A1 AR 047812 A1 AR047812 A1 AR 047812A1 AR P050100615 A ARP050100615 A AR P050100615A AR P050100615 A ARP050100615 A AR P050100615A AR 047812 A1 AR047812 A1 AR 047812A1
- Authority
- AR
- Argentina
- Prior art keywords
- 6alkyl
- 4alkyl
- nr5r6
- ring
- 6alkylnr5
- Prior art date
Links
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 title 1
- CWRVKFFCRWGWCS-UHFFFAOYSA-N Pentrazole Chemical class C1CCCCC2=NN=NN21 CWRVKFFCRWGWCS-UHFFFAOYSA-N 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 229930195712 glutamate Natural products 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 9
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 7
- -1 OC1-6alkyl Chemical group 0.000 abstract 7
- 229910052799 carbon Inorganic materials 0.000 abstract 6
- 229910052760 oxygen Inorganic materials 0.000 abstract 6
- 229910052717 sulfur Inorganic materials 0.000 abstract 6
- 229910052757 nitrogen Inorganic materials 0.000 abstract 5
- 125000004429 atom Chemical group 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 4
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 abstract 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 150000003852 triazoles Chemical class 0.000 abstract 2
- 125000006592 (C2-C3) alkenyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- CPIMLQSFGIXVKQ-UHFFFAOYSA-N 1-[4-(4-acetylphenyl)piperazin-1-yl]-2-[5-(5-methylfuran-2-yl)tetrazol-2-yl]ethanone Chemical compound C1=CC(C(=O)C)=CC=C1N1CCN(C(=O)CN2N=C(N=N2)C=2OC(C)=CC=2)CC1 CPIMLQSFGIXVKQ-UHFFFAOYSA-N 0.000 abstract 1
- PKDPUENCROCRCH-UHFFFAOYSA-N 1-piperazin-1-ylethanone Chemical compound CC(=O)N1CCNCC1 PKDPUENCROCRCH-UHFFFAOYSA-N 0.000 abstract 1
- SGZLSBWGNCQYJP-UHFFFAOYSA-N 2-[5-(5-methylfuran-2-yl)tetrazol-2-yl]-n-(2-phenylbenzotriazol-5-yl)acetamide Chemical compound O1C(C)=CC=C1C1=NN(CC(=O)NC2=CC3=NN(N=C3C=C2)C=2C=CC=CC=2)N=N1 SGZLSBWGNCQYJP-UHFFFAOYSA-N 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 101001134805 Homo sapiens Protocadherin alpha-13 Proteins 0.000 abstract 1
- 102100033442 Protocadherin alpha-13 Human genes 0.000 abstract 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000005213 alkyl heteroaryl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
- C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D257/04—Five-membered rings
-
- 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
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic 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
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
-
- 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
- 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
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- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Procesos para su preparacion, composiciones farmacéuticas que contienen dichos compuestos y el uso terapéutico de los mismos. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1), en donde: X3 y X4 se seleccionan entre N y C, de modo que cuando X3 es N, X4 es C y cuando X3 es C, X4 es N; P se selecciona entre arilo y heteroarilo; si m = 1 entonces R1 se une a P a través de un átomo de carbono en el anillo P en una meta-posicion del anillo P respecto del punto de union de P a X3, y si m = 2 entonces R1 se une a P vía carbon átomos en el anillo P en las posiciones 2 y 5 del anillo P; R1 se selecciona entre el grupo formado por hidroxi, halo, nitro, C1-6 alquilhalo, OC1-6alquilhalo, C1-6 alquilo, OC1-6alquilo, C2-6 alquenilo, OC2-6alquenilo, C2-6 alquinilo, OC2-6alquinilo, C0-6alquilC3-6cicloalquilo, OC0-6alquilC3-6cicloalquilo, C0-6 alquilarilo, OC0-6alquilarilo, CHO, (CO)R5, O(CO)R5, O(CO)OR5, O(CNR5)OR5, C1-6alquilOR5, OC2-6alquilOR5, C1-6alquil(CO)R5, OC1- 6alquil(CO)R5, C0-6alquilCO2R5, OC1-6alquilCO2R5, C0-6 alquilciano, OC2-6alquilciano, C0-6alquilNR5R6, OC2-6alquilNR5R6, C1-6alquil(CO)NR5R6, OC1-6alquil(CO)NR5R6, C0-6alquilNR5(CO)R6, OC2-6alquilNR5(CO)R6, C0-6alquilNR5(CO)NR5R6, C0-6alquilSR5, OC2- 6alquilSR5, C0-6alquil(SO)R5, OC2-6alquil(SO)R5, C0-6alquilSO2R5, OC2-6alquilSO2R5, C0-6alquil(SO2)NR5R6, OC2-6alquil(SO2)NR5R6, C0-6alquilNR5(SO2)R6, OC2-6alquilNR5(SO2)R6, C0-6alquilNR5(SO2)NR5R6, OC2-6alquilNR5(SO2)NR5R6, (CO)NR5R6, O(CO)NR5R6, NR5OR6, C0-6alquilNR5(CO)OR6, OC2-6alquilNR5(CO)OR6, SO3R5 y un anillo de 5 o 6 miembros que contiene uno o más átomos seleccionados en forma independiente entre el grupo formado por C, N, O y S; X1 se seleccionan entre el grupo formado por C2-3 alquilo, C2-3 alquenilo, NR3, O, S, CR3R4, SO, SO2; X2 se seleccionan entre el grupo formado por un enlace CR3R4, O, S, NR3, SO, SO2; R3 y R4 se seleccionan en forma independiente entre un grupo formado por hidrogeno, hidroxi, C-6 alquilo, C0-6 alquilciano, oxo, =NR5, =NOR5, C1-4 alquilhalo, halo, C1-4alquilC3-7cicloalquilo, C3-7 cicloalquilo, O(CO)C1-4alquilo, (CO)C1-4alquilo, C1-4alquil(SO)C0-4alquilo, C1-4alquil(SO2)C0-4alquilo, (SO)C0-4alquilo, (SO2)C0-4alquilo, OC1-4alquilo, C1- 4alquilOR5 y C0-4alquilNR5R6; Q es ya sea seleccionado entre triazol, piperazina, y imidazol, o bien Q es cualquier otro anillo heterocíclico de 4,5, 6 o 7 miembros que contienen uno o más heteroátomos seleccionados entre N, O y S y está fusionado a un anillo y triazol; R2 se selecciona entre el grupo formado por hidroxi, C0-6 alquilciano, =NR5, =O, =NOR5, C1-4 alquilhalo, halo, C1-6 alquilo, C3-6 cicloalquilo, C0-6 alquilarilo, C0-6 alquilheteroarilo, C0-6 alquilcicloalquilo, C0-6 alquilheterocicloalquilo, OC1-4alquilo, OC0-6alquilarilo, O(CO)C1-4alquilo, (CO)OC1-4alquilo, C0-4alquil(S)C0-4alquilo, C1-4alquil(SO)C0-4alquilo, C1-4alquil(SO2)C0-4alquilo, (SO)C0-4alquilo, (SO2)C0-4alquilo, C1-4alquilOR5, C0-4alquilNR5R6 y un anillo de 5 o 6 miembros que contiene uno o más átomos seleccionados en forma independiente entre C, N, O y S, y dicho anillo opcionalmente puede fusionarse con un anillo de 5 o 6 miembros que contiene uno o más átomos seleccionados en forma independiente entre el grupo formado por C, N y O y en donde dicho anillo y dicho anillo fusionado pueden sustituirse con uno o más A; y cualquier C1-6 alquilo, arilo o heteroarilo definido bajo R1, R2 y R3 puede sustituirse con uno o más A; y A se selecciona entre el grupo formado por hidrogeno, hidroxi, halo, nitro, oxo, C0-6 alquilciano, C0-4alquilC3-6cicloalquilo, C1-6 alquilo, -OC1-6alquilo, C1-6 alquilhalo, OC1-6alquilhalo, C2-6 alquenilo, C0-3 alquilarilo, C0-6alquilOR5, OC2-6alquilOR5, C1-6alquilSR5, OC2-6alquilSR5, (CO)R5, O(CO)R5, OC2-6alquilciano, OC1-6alquilCO2R5, O(CO)OR5, OC1-6alquil(CO)R5, C1-6alquil(CO)R5, NR5OR6, C0-6NR5R6, OC2-6alquilNR5R6, C0-6alquil(CO)NR5R6, OC1-6alquil(CO)NR5R6, OC2-6alquilNR5(CO)R6, C0- 6alquilNR5(CO)R6, C0-6alquilNR5(CO)NR5R6, O(CO)NR5R6, C0-6alquil(SO2)NR5R6, OC2-6alquil(SO2)NR5R6, C0-6alquilNR5(SO2)R6, OC2-6alquilNR5(SO2)R6, SO3R5, C1-6alquilNR5(SO2)NR5R6, OC2-6alquil(SO2)R5, C0-6alquil(SO2)R5, C0-6alquil(SO)R5, OC2- 6alquil(SO)R5 y un anillo de 5 o 6 miembros que contiene uno o más átomos seleccionados en forma independiente entre el grupo formado por C, N, O y S; R5 y R6 se seleccionan en forma independiente entre H, C1-6 alquilo, C3-7 cicloalquilo y arilo; y sus sales e hidratos; m se selecciona entre 1 o 2; p se selecciona entre 0, 1, 2, 3 y 4, o una sal o hidrato del mismo; con la salvedad de que el compuesto no sea: 1-(2-benzotiazolil)-4-[[5-(5-metil-2-furanil)-2H-tetrazol-2-il]acetil-piperazina; 1- (4-acetilfenil)-4-[[5-(5-metil-2-furanil)-2H-tetrazol-2-il]acetil]-piperazina; o 5-(5-metil-2-furanil)-N-(2-fenil-2H-benzotriazol-5-il)-2H-tetrazol-2-acetamida.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US54529104P | 2004-02-18 | 2004-02-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR047812A1 true AR047812A1 (es) | 2006-02-22 |
Family
ID=34886129
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050100615A AR047812A1 (es) | 2004-02-18 | 2005-02-18 | Compuestos de tetrazol y su uso como antagonistas del receptor de glutamato metabotropico |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US20070197549A1 (es) |
| EP (1) | EP1716125B1 (es) |
| JP (1) | JP5084269B2 (es) |
| KR (1) | KR20070027504A (es) |
| CN (2) | CN1918137B (es) |
| AR (1) | AR047812A1 (es) |
| AU (1) | AU2005214379B2 (es) |
| BR (1) | BRPI0507498A (es) |
| CA (1) | CA2556263A1 (es) |
| IL (1) | IL177056A0 (es) |
| MX (1) | MXPA06009019A (es) |
| MY (1) | MY145075A (es) |
| NO (1) | NO20063470L (es) |
| RU (1) | RU2372347C2 (es) |
| SG (1) | SG150539A1 (es) |
| TW (1) | TW200533664A (es) |
| UA (1) | UA85576C2 (es) |
| UY (1) | UY28763A1 (es) |
| WO (1) | WO2005080356A1 (es) |
| ZA (1) | ZA200606594B (es) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1918137B (zh) * | 2004-02-18 | 2012-08-01 | 阿斯利康(瑞典)有限公司 | 四唑化合物及其作为代谢型谷氨酸受体拮抗剂的应用 |
| TW200538108A (en) | 2004-02-19 | 2005-12-01 | Astrazeneca Ab | Fused heterocyclic compounds and their use as metabotropic glutamate receptor antagonists |
| GB0420722D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| WO2006080533A1 (ja) * | 2005-01-31 | 2006-08-03 | Mochida Pharmaceutical Co., Ltd. | ３－アミノ－１,２,４－トリアゾール誘導体 |
| AU2006202083A1 (en) * | 2005-06-03 | 2006-12-21 | Reto Brun | Linear dicationic terphenyls and their aza analogues as antiparasitic agents |
| US7964619B2 (en) | 2005-06-03 | 2011-06-21 | The University Of North Carolina At Chapel Hill | Teraryl components as antiparasitic agents |
| AR058807A1 (es) | 2005-09-29 | 2008-02-27 | Astrazeneca Ab | 5-(fenilisoxazoletoxi)-triazol-3-il piridinas sustituidas, para el tratamiento de trastornos mediados por el receptor mglur5 |
| HUP0500921A2 (en) * | 2005-10-05 | 2007-07-30 | Richter Gedeon Nyrt | Tetrazole derivatives, process for their preparation and their use |
| AR059898A1 (es) * | 2006-03-15 | 2008-05-07 | Janssen Pharmaceutica Nv | Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2 |
| TW200811157A (en) | 2006-05-05 | 2008-03-01 | Astrazeneca Ab | mGluR5 modulators I |
| TW200808800A (en) * | 2006-05-05 | 2008-02-16 | Astrazeneca Ab | MGluR5 modulators V |
| TW200811179A (en) * | 2006-05-05 | 2008-03-01 | Astrazeneca Ab | mGluR5 modulators VI |
| TW200845978A (en) | 2007-03-07 | 2008-12-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives |
| AR065622A1 (es) * | 2007-03-07 | 2009-06-17 | Ortho Mcneil Janssen Pharm | Derivados de 3-ciano -4- (4-fenil- piperidin -1- il) piridin -2- ona |
| TW200900065A (en) * | 2007-03-07 | 2009-01-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives |
| CA2696948C (en) | 2007-09-14 | 2013-04-30 | Jose Maria Cid-Nunez | 1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones |
| EP2200985B1 (en) | 2007-09-14 | 2011-07-13 | Ortho-McNeil-Janssen Pharmaceuticals, Inc. | 1,3-disubstituted 4-(aryl-x-phenyl)-1h-pyridin-2-ones |
| NZ584148A (en) * | 2007-09-14 | 2011-05-27 | Ortho Mcneil Janssen Pharm | 1,3-disubstituted-4-phenyl-1 h-pyridin-2-ones |
| MX2010004272A (es) * | 2007-10-19 | 2010-04-30 | Astrazeneca Ab | Derivados de tetrazol como moduladores de receptores de glutamato metabotropicos (mglurs). |
| WO2009054785A1 (en) * | 2007-10-26 | 2009-04-30 | Astrazeneca Ab | 1,2,4-triazole ether derivatives as modulators of mglur5 |
| JP2011500798A (ja) * | 2007-10-26 | 2011-01-06 | アストラゼネカ・アクチエボラーグ | ｍＧｌｕＲ５のモジュレーターとしてのアミノ１，２，４−トリアゾール誘導体 |
| CN101861316B (zh) | 2007-11-14 | 2013-08-21 | 奥梅-杨森制药有限公司 | 咪唑并[1,2-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途 |
| CN102171214B (zh) | 2008-08-06 | 2015-06-24 | 生物马林药物股份有限公司 | 聚(adp-核糖)聚合酶(parp)的二氢吡啶并酞嗪酮抑制剂 |
| CN102143955B (zh) | 2008-09-02 | 2013-08-14 | Omj制药公司 | 作为代谢型谷氨酸受体调节剂的3-氮杂二环[3.1.0]己烷衍生物 |
| WO2010043396A1 (en) | 2008-10-16 | 2010-04-22 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors |
| JP5690277B2 (ja) | 2008-11-28 | 2015-03-25 | ジャンセン ファーマシューティカルズ， インコーポレイテッド． | 代謝型グルタミン酸受容体の調節因子としてのインドールおよびベンゾオキサジン誘導体 |
| CN102245592A (zh) * | 2008-12-12 | 2011-11-16 | 阿斯利康(瑞典)有限公司 | 制备4-[4-甲基-5-(c1-10 烷基硫基/c5-10芳基-c1-6 烷基硫基)-4h-1,2,4-三唑-3-基]吡啶的新方法 |
| EP2379531A1 (en) * | 2008-12-18 | 2011-10-26 | AstraZeneca AB | Processes for the manufacture of 3-{4-methyl-5- [ (ir) -1- (2- (3-methylphenyl) -2h-tetrazol-5-yl) -ethoxy]-4h- [1,2, 4]triazol-3-yl} -pyridine, 4-methyl-3-methylthio-5- (3- pyridyl)-l,2,4-triazole, and (ir) -1- [2- (3-methylphenyl) -2h- tetrazol-5-yl]ethanol |
| US8349852B2 (en) | 2009-01-13 | 2013-01-08 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
| US20100273805A1 (en) * | 2009-04-23 | 2010-10-28 | Astrazeneca Ab | Sulphide bridged derivatives as modulators of mglur5 733 |
| MY153913A (en) | 2009-05-12 | 2015-04-15 | Janssen Pharmaceuticals Inc | 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| ES2440001T3 (es) | 2009-05-12 | 2014-01-27 | Janssen Pharmaceuticals, Inc. | Derivados de 1,2,4-triazolo[4,3-A]piridina y su uso para el tratamiento o prevención de trastornos neurológicos y psiquiátricos |
| CN102439015B (zh) | 2009-05-12 | 2015-05-13 | 杨森制药有限公司 | 1,2,4-三唑并[4,3-a]吡啶衍生物和其作为mGluR2受体的正向变构调节剂的用途 |
| US8883827B2 (en) | 2009-06-05 | 2014-11-11 | Oslo University Hospital Hf | Azole derivatives as WTN pathway inhibitors |
| EP2519521B1 (en) * | 2009-12-29 | 2013-11-20 | Eli Lilly and Company | Tetrahydrotriazolopyridine compounds as selective mglu5 receptor potentiators useful for the treatment of schizophrenia |
| US20120295942A1 (en) | 2010-02-01 | 2012-11-22 | Nicholas James Devereux | Pyrazolo[5,1b]oxazole Derivatives as CRF-1 Receptor Antagonists |
| WO2011092293A2 (en) | 2010-02-01 | 2011-08-04 | Novartis Ag | Cyclohexyl amide derivatives as crf receptor antagonists |
| CN102753527B (zh) | 2010-02-02 | 2014-12-24 | 诺华股份有限公司 | 用作crf受体拮抗剂的环己基酰胺衍生物 |
| CN106943406A (zh) | 2010-02-03 | 2017-07-14 | 麦迪韦逊科技有限公司 | 用于pten基因缺失相关疾病的治疗的聚(adp‑核糖)聚合酶(parp)的二氢吡啶并酞嗪酮抑制剂 |
| JP5735988B2 (ja) | 2010-02-08 | 2015-06-17 | ビオマリン プハルマセウトイカル インコーポレイテッド | ジヒドロピリドフタラジノン誘導体を合成する方法 |
| SG10201710578TA (en) | 2010-10-21 | 2018-02-27 | Medivation Technologies Inc | Crystalline (8s,9r)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1h-1,2,4-triazol-5-yl)-8,9-dihydro-2h-pyrido[4,3,2-de]phthalazin-3(7h)-one tosylate salt |
| CA2814998C (en) | 2010-11-08 | 2019-10-29 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| US9271967B2 (en) | 2010-11-08 | 2016-03-01 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors |
| ES2552879T3 (es) | 2010-11-08 | 2015-12-02 | Janssen Pharmaceuticals, Inc. | Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de receptores mGluR2 |
| JP2013544874A (ja) | 2010-12-08 | 2013-12-19 | オスロ ユニヴァーシティー ホスピタル エイチエフ | Ｗｎｔシグナル伝達経路阻害薬としてのトリアゾール誘導体 |
| KR101235100B1 (ko) * | 2010-12-15 | 2013-02-20 | 서강대학교산학협력단 | 트리아졸을 포함하는 삼중연결고리 3차 아민 화합물, 이의 제조방법 및 응용 |
| US9199975B2 (en) | 2011-09-30 | 2015-12-01 | Asana Biosciences, Llc | Biaryl imidazole derivatives for regulating CYP17 |
| US8809372B2 (en) | 2011-09-30 | 2014-08-19 | Asana Biosciences, Llc | Pyridine derivatives |
| JO3368B1 (ar) | 2013-06-04 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2 |
| JO3367B1 (ar) | 2013-09-06 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2 |
| CN105916846A (zh) * | 2013-11-07 | 2016-08-31 | 麦迪韦逊科技有限公司 | 用于合成经保护的n-烷基三唑甲醛的三唑中间体 |
| EA033889B1 (ru) | 2014-01-21 | 2019-12-05 | Янссен Фармацевтика Нв | Комбинация на основе лиганда sv2a и положительного аллостерического модулятора метаботропного глутаматергического рецептора 2 подтипа |
| LT3431106T (lt) | 2014-01-21 | 2021-02-10 | Janssen Pharmaceutica Nv | Deriniai, apimantys 2 potipio metabotropinio glutamaterginio receptoriaus teigiamus alosterinius moduliatorius arba ortosterinius agonistus, ir jų panaudojimas |
| CN111269192A (zh) * | 2020-02-25 | 2020-06-12 | 成都睿智化学研究有限公司 | 一种5-羟甲基四氮唑及其衍生物的合成方法 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3509153A (en) * | 1967-03-24 | 1970-04-28 | Miles Lab | 5-phenyl (or 5-phenylalkyl)-2-(omega-(4-phenyl-1-piperazinyl)alkyl)tetrazoles |
| US4663332A (en) * | 1985-10-10 | 1987-05-05 | Hoffman-La Roche Inc. | 5-substituted N-alkylated tetrazoles |
| EP0596933A1 (en) | 1991-08-03 | 1994-05-18 | Smithkline Beecham Plc | 5-ht4 receptor antagonists |
| GB9205320D0 (en) * | 1992-03-11 | 1992-04-22 | Ici Plc | Anti-tumour compounds |
| TW544448B (en) * | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
| DE10023430A1 (de) | 2000-05-12 | 2001-11-15 | Bayer Ag | Substituierte N-Benzoyl-N'-(tetrazolylphenyl)-harnstoffe |
| GB0115862D0 (en) | 2001-06-28 | 2001-08-22 | Smithkline Beecham Plc | Compounds |
| GB0121033D0 (en) | 2001-08-30 | 2001-10-24 | Novartis Ag | Organic compounds |
| CA2462289C (en) * | 2001-10-04 | 2010-02-23 | Nicholas D. Cosford | Heteroaryl substituted tetrazole modulators of metabotropic glutamate receptor-5 |
| EP1458383B1 (en) * | 2001-12-18 | 2007-11-21 | Merck & Co., Inc. | Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5 |
| WO2003077918A1 (en) * | 2002-03-12 | 2003-09-25 | Merck & Co., Inc. | Di-aryl substituted tetrazole modulators of metabotropic glutamate receptor-5 |
| KR100557093B1 (ko) * | 2003-10-07 | 2006-03-03 | 한미약품 주식회사 | 다약제 내성 저해 활성을 갖는 테트라졸 유도체 및 그의제조방법 |
| CN1918137B (zh) * | 2004-02-18 | 2012-08-01 | 阿斯利康(瑞典)有限公司 | 四唑化合物及其作为代谢型谷氨酸受体拮抗剂的应用 |
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2005
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- 2005-02-17 UA UAA200608678A patent/UA85576C2/ru unknown
- 2005-02-17 WO PCT/US2005/005217 patent/WO2005080356A1/en not_active Ceased
- 2005-02-17 BR BRPI0507498-3A patent/BRPI0507498A/pt not_active IP Right Cessation
- 2005-02-17 JP JP2006554236A patent/JP5084269B2/ja not_active Expired - Fee Related
- 2005-02-17 US US10/588,756 patent/US20070197549A1/en not_active Abandoned
- 2005-02-17 AU AU2005214379A patent/AU2005214379B2/en not_active Expired - Fee Related
- 2005-02-17 TW TW094104641A patent/TW200533664A/zh unknown
- 2005-02-17 CA CA002556263A patent/CA2556263A1/en not_active Abandoned
- 2005-02-17 CN CN201010113361A patent/CN101845023A/zh active Pending
- 2005-02-17 MX MXPA06009019A patent/MXPA06009019A/es active IP Right Grant
- 2005-02-17 KR KR1020067015943A patent/KR20070027504A/ko not_active Ceased
- 2005-02-17 EP EP05713793.7A patent/EP1716125B1/en not_active Expired - Lifetime
- 2005-02-17 SG SG200901214-7A patent/SG150539A1/en unknown
- 2005-02-17 MY MYPI20050601A patent/MY145075A/en unknown
- 2005-02-17 RU RU2006127573/04A patent/RU2372347C2/ru not_active IP Right Cessation
- 2005-02-18 AR ARP050100615A patent/AR047812A1/es unknown
- 2005-02-18 UY UY28763A patent/UY28763A1/es unknown
- 2005-02-18 US US11/060,463 patent/US7691892B2/en not_active Expired - Fee Related
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- 2006-07-25 IL IL177056A patent/IL177056A0/en unknown
- 2006-07-28 NO NO20063470A patent/NO20063470L/no not_active Application Discontinuation
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|---|---|
| AU2005214379B2 (en) | 2012-03-22 |
| JP2007523182A (ja) | 2007-08-16 |
| RU2006127573A (ru) | 2008-03-27 |
| US20060004021A1 (en) | 2006-01-05 |
| NO20063470L (no) | 2006-11-17 |
| EP1716125A1 (en) | 2006-11-02 |
| MY145075A (en) | 2011-12-15 |
| JP5084269B2 (ja) | 2012-11-28 |
| UA85576C2 (ru) | 2009-02-10 |
| RU2372347C2 (ru) | 2009-11-10 |
| AU2005214379A1 (en) | 2005-09-01 |
| UY28763A1 (es) | 2005-06-30 |
| KR20070027504A (ko) | 2007-03-09 |
| WO2005080356A1 (en) | 2005-09-01 |
| CA2556263A1 (en) | 2005-09-01 |
| IL177056A0 (en) | 2006-12-10 |
| CN101845023A (zh) | 2010-09-29 |
| SG150539A1 (en) | 2009-03-30 |
| US7691892B2 (en) | 2010-04-06 |
| ZA200606594B (en) | 2007-11-28 |
| CN1918137A (zh) | 2007-02-21 |
| CN1918137B (zh) | 2012-08-01 |
| TW200533664A (en) | 2005-10-16 |
| BRPI0507498A (pt) | 2007-07-10 |
| EP1716125B1 (en) | 2013-06-19 |
| US20070197549A1 (en) | 2007-08-23 |
| MXPA06009019A (es) | 2007-03-08 |
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