ES2606839T3 - Tetraaza-ciclopenta[a]indenilo y su uso como moduladores alostéricos positivos - Google Patents
Tetraaza-ciclopenta[a]indenilo y su uso como moduladores alostéricos positivos Download PDFInfo
- Publication number
- ES2606839T3 ES2606839T3 ES12798612.3T ES12798612T ES2606839T3 ES 2606839 T3 ES2606839 T3 ES 2606839T3 ES 12798612 T ES12798612 T ES 12798612T ES 2606839 T3 ES2606839 T3 ES 2606839T3
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- hal
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- cyc
- het
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Classifications
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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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed systems
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/14—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
- A61P25/20—Hypnotics; Sedatives
-
- 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
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Compuesto de fórmula (I)**Fórmula** en la que R1, R2, R3 se seleccionan independientemente unos de otros de H, alquilo C1-C6 lineal o ramificado, alcoxilo C1- C6 lineal o ramificado, Hal o hidroxilo; Ra, Rb se seleccionan independientemente unos de otros de H, Hal, hidroxilo o A; Q indica un grupo aromático de 6 miembros o un grupo heteroaromático de 5-6 miembros que tiene de 1 a 4 heteroátomos seleccionados independientemente de N, O y S. R4 indica G, OG, SG, OCHF2, OCF2CHF2, NR5G, -COOG u OCOG; R5 indica H o un alquilo lineal o ramificado que tiene de 1 a 6 átomos de carbono. G indica -CH3, -CF3, -CH2 -A, Het, Cyc, Ar, -CH2 -Het, -CH2 -Cyc, -CH2-Ar, Hal, hidroxilo; Hal indica F, Cl, Br o I, preferiblemente F, Cl o Br; A es una cadena de carbono lineal o ramificada que tiene de 1 a 6 átomos de carbono, en la que los grupos -CH2 no adyacentes de 1 a 3 pueden reemplazarse independientemente unos de otros por un grupo seleccionado de O, NR5, S, SO, SO2, CO, y en la que los átomos de hidrógeno de 1 a 5 pueden reemplazarse independientemente unos de otros por Het, Cyc, Ar o Hal; Het indica un anillo saturado, insaturado o aromático, que es monocíclico o bicíclico o bicíclico condensado y que tiene de 3 a 8 miembros y que contiene de 1 a 4 heteroátomos seleccionados independientemente de N, NR5, O, S, CO, SO o SO2, que puede estar sustituido con de 1 a 3 sustituyentes seleccionados independientemente de A, Hal, OH y Het1; Het1 indica un anillo carbocíclico de 4, 5 ó 6 miembros en el que 1 ó 2 átomos de carbono se reemplazan por átomos de oxígeno. Ar indica un anillo aromático carbocíclico de 6 miembros o un anillo aromático bicíclico condensado o no condensado, y sustituido opcionalmente por de 1 a 3 sustituyentes seleccionados independientemente de A o Hal; Cyc indica un anillo carbocíclico saturado o insaturado que tiene desde 3 hasta 8 átomos de carbono y sustituido opcionalmente por de 1 a 3 sustituyentes seleccionados independientemente de A o Hal; y/o tautómeros, sales, solvatos y estereoisómeros farmacéuticamente utilizables de los mismos.
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161578931P | 2011-12-22 | 2011-12-22 | |
| US201161578931P | 2011-12-22 | ||
| EP11195214 | 2011-12-22 | ||
| EP11195214.9A EP2607364A1 (en) | 2011-12-22 | 2011-12-22 | Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators |
| US201261657978P | 2012-06-11 | 2012-06-11 | |
| US201261657978P | 2012-06-11 | ||
| EP12171415.8A EP2674434A1 (en) | 2012-06-11 | 2012-06-11 | Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators |
| EP12171415 | 2012-06-11 | ||
| PCT/EP2012/004968 WO2013091773A1 (en) | 2011-12-22 | 2012-11-30 | Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2606839T3 true ES2606839T3 (es) | 2017-03-28 |
Family
ID=48667735
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES12798612.3T Active ES2606839T3 (es) | 2011-12-22 | 2012-11-30 | Tetraaza-ciclopenta[a]indenilo y su uso como moduladores alostéricos positivos |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US9403835B2 (es) |
| EP (1) | EP2794608B1 (es) |
| JP (1) | JP6112316B2 (es) |
| CN (1) | CN104039789B (es) |
| AU (1) | AU2012357169B2 (es) |
| CA (1) | CA2860008C (es) |
| ES (1) | ES2606839T3 (es) |
| WO (1) | WO2013091773A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2813505A1 (en) | 2013-06-14 | 2014-12-17 | Asceneuron SA | Tetraaza-cyclopenta[a]indenyl derivatives |
| GB201317363D0 (en) | 2013-10-01 | 2013-11-13 | Eisai Ltd | Novel compounds |
| TR201908031T4 (tr) * | 2014-08-26 | 2019-06-21 | Astellas Pharma Inc | İdrar kesesi hastalıklarının tedavisine yönelik muskarinik m3 ligandları olarak 2-aminotiyazol türevleri veya bunların tuzu. |
| ES2712627T3 (es) * | 2015-02-11 | 2019-05-14 | Sunovion Pharmaceuticals Inc | Compuestos dihidro-4H-pirazolo[5,1-c][1,4]oxazinilo fusionados y análogos para el tratamiento de trastornos del SNC |
| KR102630720B1 (ko) | 2015-08-28 | 2024-01-29 | 세키스이 메디칼 가부시키가이샤 | 벤질 화합물 |
| MX2019000982A (es) | 2016-07-29 | 2019-07-04 | Sunovion Pharmaceuticals Inc | Compuestos y composiciones y usos de los mismos. |
| CN111183138A (zh) | 2017-08-02 | 2020-05-19 | 赛诺维信制药公司 | 异色满化合物以及用途 |
| CA3085353A1 (en) | 2017-12-21 | 2019-06-27 | Ribon Therapeutics Inc. | Quinazolinones as parp14 inhibitors |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2276936T3 (es) * | 2001-03-27 | 2007-07-01 | Neurogen Corporation | (oxo-pirazolo(1,5a)pirimidin-2-il)alquilcarboxamidas. |
| CN100586951C (zh) * | 2004-12-15 | 2010-02-03 | 弗·哈夫曼-拉罗切有限公司 | 作为甘氨酸转运体l(GlyT-1)抑制剂用于治疗阿尔茨海默氏病的二环和三环取代的苯甲酮化合物 |
| US7855206B2 (en) * | 2006-11-14 | 2010-12-21 | Merck Sharp & Dohme Corp. | Tricyclic heteroaromatic compounds as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes |
| WO2011137049A1 (en) * | 2010-04-30 | 2011-11-03 | Merck Sharp & Dohme Corp. | Heterocyclic quinolizine derived m1 receptor positive allosteric modulators |
| EP2813505A1 (en) * | 2013-06-14 | 2014-12-17 | Asceneuron SA | Tetraaza-cyclopenta[a]indenyl derivatives |
-
2012
- 2012-11-30 CN CN201280062522.3A patent/CN104039789B/zh active Active
- 2012-11-30 ES ES12798612.3T patent/ES2606839T3/es active Active
- 2012-11-30 EP EP12798612.3A patent/EP2794608B1/en active Active
- 2012-11-30 US US14/366,901 patent/US9403835B2/en active Active
- 2012-11-30 CA CA2860008A patent/CA2860008C/en active Active
- 2012-11-30 WO PCT/EP2012/004968 patent/WO2013091773A1/en active Application Filing
- 2012-11-30 JP JP2014547736A patent/JP6112316B2/ja active Active
- 2012-11-30 AU AU2012357169A patent/AU2012357169B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| WO2013091773A1 (en) | 2013-06-27 |
| EP2794608A1 (en) | 2014-10-29 |
| CA2860008C (en) | 2020-11-10 |
| US9403835B2 (en) | 2016-08-02 |
| JP2015502371A (ja) | 2015-01-22 |
| CA2860008A1 (en) | 2013-06-27 |
| AU2012357169B2 (en) | 2017-03-30 |
| AU2012357169A1 (en) | 2014-08-07 |
| US20150018343A1 (en) | 2015-01-15 |
| CN104039789B (zh) | 2016-09-07 |
| CN104039789A (zh) | 2014-09-10 |
| JP6112316B2 (ja) | 2017-04-12 |
| EP2794608B1 (en) | 2016-09-14 |
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