AR095858A1 - COMBINACIONES DE LIGANDOS DE RECEPTORES ADRENÉRGICOS a-2 Y RECEPTORES SIGMA - Google Patents
COMBINACIONES DE LIGANDOS DE RECEPTORES ADRENÉRGICOS a-2 Y RECEPTORES SIGMAInfo
- Publication number
- AR095858A1 AR095858A1 ARP140101577A ARP140101577A AR095858A1 AR 095858 A1 AR095858 A1 AR 095858A1 AR P140101577 A ARP140101577 A AR P140101577A AR P140101577 A ARP140101577 A AR P140101577A AR 095858 A1 AR095858 A1 AR 095858A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- unsubstituted
- aromatic
- nr8r9
- heterocyclyl
- Prior art date
Links
- 101150051188 Adora2a gene Proteins 0.000 title 1
- 108060003345 Adrenergic Receptor Proteins 0.000 title 1
- 102000017910 Adrenergic receptor Human genes 0.000 title 1
- 108010085082 sigma receptors Proteins 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 17
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 125000003342 alkenyl group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 150000002431 hydrogen Chemical group 0.000 abstract 5
- 239000003446 ligand Substances 0.000 abstract 5
- 239000000048 adrenergic agonist Substances 0.000 abstract 4
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 4
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 4
- BYJAVTDNIXVSPW-UHFFFAOYSA-N tetryzoline Chemical compound N1CCN=C1C1C2=CC=CC=C2CCC1 BYJAVTDNIXVSPW-UHFFFAOYSA-N 0.000 abstract 2
- YKFCISHFRZHKHY-NGQGLHOPSA-N (2s)-2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropanoic acid;trihydrate Chemical compound O.O.O.OC(=O)[C@](N)(C)CC1=CC=C(O)C(O)=C1.OC(=O)[C@](N)(C)CC1=CC=C(O)C(O)=C1 YKFCISHFRZHKHY-NGQGLHOPSA-N 0.000 abstract 1
- CNIIGCLFLJGOGP-UHFFFAOYSA-N 2-(1-naphthalenylmethyl)-4,5-dihydro-1H-imidazole Chemical compound C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 CNIIGCLFLJGOGP-UHFFFAOYSA-N 0.000 abstract 1
- VTZPAJGVRWKMAG-UHFFFAOYSA-N 3-(1h-imidazol-5-ylmethyl)-2,3-dihydro-1h-inden-5-ol Chemical compound C12=CC(O)=CC=C2CCC1CC1=CN=CN1 VTZPAJGVRWKMAG-UHFFFAOYSA-N 0.000 abstract 1
- HBLPYIOKPJVFQW-UHFFFAOYSA-N 6-ethyl-4,5,7,8-tetrahydro-[1,3]oxazolo[4,5-d]azepin-2-amine;hydron;dichloride Chemical compound Cl.Cl.C1CN(CC)CCC2=C1OC(N)=N2 HBLPYIOKPJVFQW-UHFFFAOYSA-N 0.000 abstract 1
- DHSSDEDRBUKTQY-UHFFFAOYSA-N 6-prop-2-enyl-4,5,7,8-tetrahydrothiazolo[4,5-d]azepin-2-amine Chemical compound C1CN(CC=C)CCC2=C1N=C(N)S2 DHSSDEDRBUKTQY-UHFFFAOYSA-N 0.000 abstract 1
- GJSURZIOUXUGAL-UHFFFAOYSA-N Clonidine Chemical compound ClC1=CC=CC(Cl)=C1NC1=NCCN1 GJSURZIOUXUGAL-UHFFFAOYSA-N 0.000 abstract 1
- WDZVGELJXXEGPV-YIXHJXPBSA-N Guanabenz Chemical compound NC(N)=N\N=C\C1=C(Cl)C=CC=C1Cl WDZVGELJXXEGPV-YIXHJXPBSA-N 0.000 abstract 1
- INJOMKTZOLKMBF-UHFFFAOYSA-N Guanfacine Chemical compound NC(=N)NC(=O)CC1=C(Cl)C=CC=C1Cl INJOMKTZOLKMBF-UHFFFAOYSA-N 0.000 abstract 1
- CQXADFVORZEARL-UHFFFAOYSA-N Rilmenidine Chemical compound C1CC1C(C1CC1)NC1=NCCO1 CQXADFVORZEARL-UHFFFAOYSA-N 0.000 abstract 1
- DPQAXNSOFFYKDS-UHFFFAOYSA-N Talipexole dihydrochloride Chemical compound Cl.Cl.C1CN(CC=C)CCC2=C1N=C(N)S2 DPQAXNSOFFYKDS-UHFFFAOYSA-N 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 230000000202 analgesic effect Effects 0.000 abstract 1
- 229960002610 apraclonidine Drugs 0.000 abstract 1
- IEJXVRYNEISIKR-UHFFFAOYSA-N apraclonidine Chemical compound ClC1=CC(N)=CC(Cl)=C1NC1=NCCN1 IEJXVRYNEISIKR-UHFFFAOYSA-N 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 229940083181 centrally acting adntiadrenergic agent methyldopa Drugs 0.000 abstract 1
- 229960002896 clonidine Drugs 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- JXMXDKHEZLKQPB-UHFFFAOYSA-N detomidine Chemical compound CC1=CC=CC(CC=2[N]C=NC=2)=C1C JXMXDKHEZLKQPB-UHFFFAOYSA-N 0.000 abstract 1
- 229960001894 detomidine Drugs 0.000 abstract 1
- HRLIOXLXPOHXTA-NSHDSACASA-N dexmedetomidine Chemical compound C1([C@@H](C)C=2C(=C(C)C=CC=2)C)=CN=C[N]1 HRLIOXLXPOHXTA-NSHDSACASA-N 0.000 abstract 1
- 229960004253 dexmedetomidine Drugs 0.000 abstract 1
- 229950006455 fadolmidine Drugs 0.000 abstract 1
- 229960004553 guanabenz Drugs 0.000 abstract 1
- 229960002048 guanfacine Drugs 0.000 abstract 1
- QKIQJNNDIWGVEH-UUILKARUSA-N guanoxabenz Chemical compound ONC(/N)=N/N=C/C1=C(Cl)C=CC=C1Cl QKIQJNNDIWGVEH-UUILKARUSA-N 0.000 abstract 1
- 229960001016 guanoxabenz Drugs 0.000 abstract 1
- HRLIOXLXPOHXTA-UHFFFAOYSA-N medetomidine Chemical compound C=1C=CC(C)=C(C)C=1C(C)C1=CN=C[N]1 HRLIOXLXPOHXTA-UHFFFAOYSA-N 0.000 abstract 1
- 229960002140 medetomidine Drugs 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 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
- 230000003389 potentiating effect Effects 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 229960000764 rilmenidine Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229960000337 tetryzoline Drugs 0.000 abstract 1
- XFYDIVBRZNQMJC-UHFFFAOYSA-N tizanidine Chemical compound ClC=1C=CC2=NSN=C2C=1NC1=NCCN1 XFYDIVBRZNQMJC-UHFFFAOYSA-N 0.000 abstract 1
- 229960000488 tizanidine Drugs 0.000 abstract 1
- 229960001262 tramazoline Drugs 0.000 abstract 1
- QQJLHRRUATVHED-UHFFFAOYSA-N tramazoline Chemical compound N1CCN=C1NC1=CC=CC2=C1CCCC2 QQJLHRRUATVHED-UHFFFAOYSA-N 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
- -1 ximetazoline Chemical compound 0.000 abstract 1
- BPICBUSOMSTKRF-UHFFFAOYSA-N xylazine Chemical compound CC1=CC=CC(C)=C1NC1=NCCCS1 BPICBUSOMSTKRF-UHFFFAOYSA-N 0.000 abstract 1
- 229960001600 xylazine Drugs 0.000 abstract 1
Classifications
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- 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
-
- 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
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
-
- 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
- A61K31/41—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
-
- 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
- A61K31/41—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
- A61K31/4155—1,2-Diazoles non condensed and containing further 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
- A61K31/41—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
- A61K31/4164—1,3-Diazoles
- A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
-
- 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
- A61K31/44—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
-
- 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
- A61K31/44—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
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- 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
- A61P25/06—Antimigraine agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Reivindicación 1: Combinación de al menos un ligando sigma y al menos un ligando agonista a-2-adrenérgico, para administración simultánea, separada o secuencial, en la que el ligando sigma tiene una fórmula general (1) en la que, R¹ se selecciona del grupo que consiste en hidrógeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, aromático o no aromático, heterociclilalquilo sustituido o no sustituido, -COR⁸, -C(O)OR⁸, -C(O)NR⁸R⁹, -CH=NR⁸, -CN, -OR⁸, -OC(O)R⁸, -S(O)ₜ-R⁸, -NR⁸R⁹, -NR⁸C(O)R⁹, -NO₂, -N=CR⁸R⁹ y halógeno; R² se selecciona del grupo que consiste en hidrógeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, aromático o no aromático, heterociclilalquilo sustituido o no sustituido, -COR⁸, -C(O)OR⁸, -CH=NR⁸, -CN, -OR⁸, -OC(O)R⁸, -S(O)ₜ-R⁸, -NR⁸R⁹, -NR⁸C(O)R⁹, -NO₂, -N=CR⁸R⁹ y halógeno; R³ y R⁴ se seleccionan independientemente del grupo que consiste en hidrógeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, aromático o no aromático, heterociclilalquilo sustituido o no sustituido, -COR⁸, -C(O)OR⁸, -C(O)NR⁸R⁹, -CH=NR⁸, -CN, -OR⁸, -OC(O)R⁸, -S(O)-R⁹, -NR⁸R⁹, -NR⁸C(O)R⁹, -NO₂, -N=CR⁸R⁹, y halógeno, o junto con el fenilo forman un sistema de anillos condensados opcionalmente sustituido; R⁵ y R⁶ se seleccionan independientemente del grupo que consiste en hidrógeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, aromático o no aromático, heterociclilalquilo sustituido o no sustituido,-COR⁸, -C(O)OR⁸, -C(O)NR⁸R⁹, -CH=NR⁸, -CN, -OR⁸, -OC(O)R⁸, -S(O)-R⁸, -NR⁸R⁹, -NR⁸C(O)R⁹, -NO₂, -N=CR⁸R⁹ y halógeno; o juntos forman, con el átomo de nitrógeno al que están unidos, un grupo heterociclilo sustituido o no sustituido, aromático o no aromático; n se selecciona de 1, 2, 3, 4, 5, 6, 7 y 8; t es 0, 1 ó 2; R⁸ y R⁹ se seleccionan cada uno independientemente de hidrógeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, aromático o no aromático, alcoxilo sustituido o no sustituido, ariloxilo sustituido o no sustituido y halógeno. Reivindicación 9: Combinación según la reivindicación 8, en la que el ligando agonista adrenérgico a-2 se selecciona. del grupo que consiste en clonidina, apraclonidina, tizanidina, nafazolina, ximetazolina, tetrahidrozolina, tramazolina, fadolmidina, detomidina, medetomidina, dexmedetomidina, B-HT 920 (6-alil-2-amino-5,6,7,8-tetrahidro-4H-tiazolo[4,5-d]-azepina) y B-HT 933, xilazina, rilmenidina, guanabenz, guanoxabenz, guanfacina, guanetidina y metildopa. Reivindicación 15: Ligando sigma de fórmula general (1) según una cualquiera de las reivindicaciones 1 a 7, o sal, isómero, profármaco o solvato farmaceuticamente del mismo, para su uso en la potenciación del efecto analgésico de un agonista adrenérgico a-2 cuando se usa dicho agonista adrenérgico a-2 en la profilaxis y/o el tratamiento del dolor.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13382140.5A EP2792352A1 (en) | 2013-04-16 | 2013-04-16 | Alpha-2 adrenoreceptor and sigma receptor ligand combinations |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR095858A1 true AR095858A1 (es) | 2015-11-18 |
Family
ID=48227118
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140101577A AR095858A1 (es) | 2013-04-16 | 2014-04-11 | COMBINACIONES DE LIGANDOS DE RECEPTORES ADRENÉRGICOS a-2 Y RECEPTORES SIGMA |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20160058771A1 (es) |
| EP (2) | EP2792352A1 (es) |
| JP (1) | JP2016516792A (es) |
| KR (1) | KR20150143754A (es) |
| CN (1) | CN105228606A (es) |
| AR (1) | AR095858A1 (es) |
| AU (1) | AU2014255837A1 (es) |
| BR (1) | BR112015026259A2 (es) |
| CA (1) | CA2908926A1 (es) |
| HK (1) | HK1219431A1 (es) |
| MX (1) | MX2015014441A (es) |
| PH (1) | PH12015502282A1 (es) |
| RU (1) | RU2015148766A (es) |
| SG (1) | SG11201508102XA (es) |
| TN (1) | TN2015000440A1 (es) |
| WO (1) | WO2014170319A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2116539A1 (en) | 2008-04-25 | 2009-11-11 | Laboratorios Del. Dr. Esteve, S.A. | 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof |
| EP2353598A1 (en) | 2010-02-04 | 2011-08-10 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for use in the prevention and/or treatment of postoperative pain |
| EP2353591A1 (en) | 2010-02-04 | 2011-08-10 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof |
| EP2388005A1 (en) | 2010-05-21 | 2011-11-23 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy |
| EP2415471A1 (en) | 2010-08-03 | 2012-02-08 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in opioid-induced hyperalgesia |
| EP2524694A1 (en) | 2011-05-19 | 2012-11-21 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in diabetes type-2 associated pain |
| TW201607538A (zh) | 2013-12-17 | 2016-03-01 | 以斯提夫博士實驗室股份有限公司 | 血清素－去甲腎上腺素再攝取抑制劑（ＳＮＲＩＳ）和σ受體配體組合物 |
| EP3886854A4 (en) | 2018-11-30 | 2022-07-06 | Nuvation Bio Inc. | PYRROLE AND PYRAZOLE COMPOUNDS AND METHODS OF USE THERE |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE469143T1 (de) * | 2002-11-15 | 2010-06-15 | Du Pont | Neue insektizide vom anthranilamid-typ |
| JP5139061B2 (ja) | 2004-08-27 | 2013-02-06 | ラボラトリオス デル ドクトール エステベ エセ．ア． | シグマ受容体阻害剤 |
| US8889173B2 (en) * | 2008-04-18 | 2014-11-18 | Warsaw Orthopedic, Inc. | Alpha adrenergic receptor agonists for treatment of pain and/or inflammation |
| EP2116539A1 (en) | 2008-04-25 | 2009-11-11 | Laboratorios Del. Dr. Esteve, S.A. | 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof |
| CA2762107A1 (en) * | 2009-05-15 | 2010-11-18 | Recro Pharma, Inc. | Sublingual dexmedetomidine compositions and methods of use thereof |
| EP2292236A1 (en) | 2009-08-14 | 2011-03-09 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for the prevention or treatment of pain induced by chemotherapy |
| US20130143884A1 (en) | 2009-11-25 | 2013-06-06 | Maria Rosa Cuberes-Altisent | 4-[2-[ [5-methyl-1-(2-naphtalenyl)-1h-pyrazol-3-yl]oxy]ethyl] morpholine salts |
| EP2335688A1 (en) | 2009-11-25 | 2011-06-22 | Laboratorios Del. Dr. Esteve, S.A. | Pharmaceutical compositions comprising sigma receptor ligands |
| AR080133A1 (es) | 2010-02-04 | 2012-03-14 | Esteve Labor Dr | Clorhidrato de 4-(-2-((5-metil-1-(2-naftalenil)-1h-pirazol-3-il)oxi)etil)morfolina y formas cristalinas del mismo |
| US20110269727A1 (en) * | 2010-04-29 | 2011-11-03 | Toledano Annette C | Composition to reduce allodynic back pain and related method of use |
| EP2388005A1 (en) | 2010-05-21 | 2011-11-23 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy |
| EP2415471A1 (en) | 2010-08-03 | 2012-02-08 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in opioid-induced hyperalgesia |
| EP2426111A1 (en) | 2010-08-09 | 2012-03-07 | Laboratorios Del. Dr. Esteve, S.A. | 4-[-2-[[5-methyl-1-(2-naphtalenyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride amorphous solid forms |
| EP2460519A1 (en) | 2010-12-03 | 2012-06-06 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in bone cancer pain |
| EP2524694A1 (en) * | 2011-05-19 | 2012-11-21 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in diabetes type-2 associated pain |
-
2013
- 2013-04-16 EP EP13382140.5A patent/EP2792352A1/en not_active Withdrawn
-
2014
- 2014-04-11 AR ARP140101577A patent/AR095858A1/es unknown
- 2014-04-15 US US14/784,736 patent/US20160058771A1/en not_active Abandoned
- 2014-04-15 SG SG11201508102XA patent/SG11201508102XA/en unknown
- 2014-04-15 CN CN201480021541.0A patent/CN105228606A/zh active Pending
- 2014-04-15 BR BR112015026259A patent/BR112015026259A2/pt not_active Application Discontinuation
- 2014-04-15 CA CA2908926A patent/CA2908926A1/en not_active Abandoned
- 2014-04-15 MX MX2015014441A patent/MX2015014441A/es unknown
- 2014-04-15 WO PCT/EP2014/057608 patent/WO2014170319A1/en active Application Filing
- 2014-04-15 KR KR1020157032620A patent/KR20150143754A/ko not_active Application Discontinuation
- 2014-04-15 AU AU2014255837A patent/AU2014255837A1/en not_active Abandoned
- 2014-04-15 EP EP14718049.1A patent/EP2986284A1/en not_active Withdrawn
- 2014-04-15 JP JP2016508133A patent/JP2016516792A/ja active Pending
- 2014-04-15 RU RU2015148766A patent/RU2015148766A/ru not_active Application Discontinuation
-
2015
- 2015-09-29 TN TN2015000440A patent/TN2015000440A1/en unknown
- 2015-10-01 PH PH12015502282A patent/PH12015502282A1/en unknown
-
2016
- 2016-06-29 HK HK16107566.1A patent/HK1219431A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| HK1219431A1 (zh) | 2017-04-07 |
| KR20150143754A (ko) | 2015-12-23 |
| CN105228606A (zh) | 2016-01-06 |
| SG11201508102XA (en) | 2015-11-27 |
| WO2014170319A1 (en) | 2014-10-23 |
| BR112015026259A2 (pt) | 2017-07-25 |
| JP2016516792A (ja) | 2016-06-09 |
| CA2908926A1 (en) | 2014-10-23 |
| RU2015148766A (ru) | 2017-05-18 |
| MX2015014441A (es) | 2016-06-21 |
| TN2015000440A1 (en) | 2017-01-03 |
| PH12015502282A1 (en) | 2016-02-01 |
| EP2986284A1 (en) | 2016-02-24 |
| RU2015148766A3 (es) | 2018-03-29 |
| AU2014255837A1 (en) | 2015-11-05 |
| EP2792352A1 (en) | 2014-10-22 |
| US20160058771A1 (en) | 2016-03-03 |
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