AR084730A1 - Ligandos heterociclicos nitrogenados de receptores sigma utiles para el tratamiento de dolor por cancer de huesos - Google Patents
Ligandos heterociclicos nitrogenados de receptores sigma utiles para el tratamiento de dolor por cancer de huesosInfo
- Publication number
- AR084730A1 AR084730A1 ARP110104502A ARP110104502A AR084730A1 AR 084730 A1 AR084730 A1 AR 084730A1 AR P110104502 A ARP110104502 A AR P110104502A AR P110104502 A ARP110104502 A AR P110104502A AR 084730 A1 AR084730 A1 AR 084730A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- unsubstituted
- aromatic
- nr8r9
- heterocyclyl
- Prior art date
Links
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
- A61K31/41—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
- A61K31/4152—1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- 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
- C07D231/18—One oxygen or sulfur atom
- C07D231/20—One oxygen atom attached in position 3 or 5
- C07D231/22—One oxygen atom attached in position 3 or 5 with aryl radicals attached to ring nitrogen 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
- A61K31/41—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
- A61K31/435—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
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- 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
-
- 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
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
- 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
- A61P35/00—Antineoplastic agents
Abstract
Reivindicación 4: Ligando sigma según cualquier reivindicación anterior, que tiene la 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 no aromático sustituido o no sustituido, heterociclilo aromático sustituido o no sustituido, 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 aromático o no aromático, sustituido o no sustituido, 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; 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 aromático o no aromático, sustituido o no sustituido, 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, o forman juntos 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 aromático o no aromático, sustituido o no sustituido, 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, o forman juntos, con el átomo de nitrógeno al que están unidos, un grupo heterociclilo aromático o no aromático, sustituido o no sustituido; n se selecciona de 1, 2, 3, 4, 5, 6, 7 y 8; t es 1, 2 ó 3; R8 y R9 se seleccionan cada uno 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, heterociclilo aromático o no aromático, sustituido o no sustituido, alcoxilo sustituido o no sustituido, ariloxilo sustituido o no sustituido y halógeno; o una sal, isómero, profármaco o solvato farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP10382330A EP2460519A1 (en) | 2010-12-03 | 2010-12-03 | Use of sigma ligands in bone cancer pain |
Publications (1)
Publication Number | Publication Date |
---|---|
AR084730A1 true AR084730A1 (es) | 2013-06-05 |
Family
ID=43629676
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110104502A AR084730A1 (es) | 2010-12-03 | 2011-12-02 | Ligandos heterociclicos nitrogenados de receptores sigma utiles para el tratamiento de dolor por cancer de huesos |
Country Status (33)
Country | Link |
---|---|
US (1) | US20130324535A1 (es) |
EP (2) | EP2460519A1 (es) |
JP (1) | JP6027014B2 (es) |
KR (1) | KR101855358B1 (es) |
CN (1) | CN103313709B (es) |
AR (1) | AR084730A1 (es) |
BR (1) | BR112013013369A8 (es) |
CA (1) | CA2819442C (es) |
CO (1) | CO6781549A2 (es) |
CY (1) | CY1119030T1 (es) |
DK (1) | DK2646025T3 (es) |
ES (1) | ES2626672T3 (es) |
HR (1) | HRP20170818T1 (es) |
HU (1) | HUE033488T2 (es) |
IL (1) | IL226706A (es) |
LT (1) | LT2646025T (es) |
MA (1) | MA34878B1 (es) |
ME (1) | ME02852B (es) |
MX (1) | MX343773B (es) |
MY (1) | MY171994A (es) |
NZ (1) | NZ612119A (es) |
PL (1) | PL2646025T3 (es) |
PT (1) | PT2646025T (es) |
RS (1) | RS56081B1 (es) |
RU (1) | RU2585095C2 (es) |
SG (1) | SG190745A1 (es) |
SI (1) | SI2646025T1 (es) |
TN (1) | TN2013000227A1 (es) |
TR (1) | TR201708567T4 (es) |
TW (1) | TWI629060B (es) |
UA (1) | UA112638C2 (es) |
WO (1) | WO2012072782A1 (es) |
ZA (1) | ZA201304966B (es) |
Families Citing this family (18)
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 |
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 |
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 |
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 |
EP2524694A1 (en) | 2011-05-19 | 2012-11-21 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in diabetes type-2 associated pain |
EP2792352A1 (en) | 2013-04-16 | 2014-10-22 | Laboratorios Del. Dr. Esteve, S.A. | Alpha-2 adrenoreceptor and sigma receptor ligand combinations |
EP2818166A1 (en) * | 2013-06-26 | 2014-12-31 | Laboratorios del Dr. Esteve S.A. | Use of sigma receptor ligands for the prevention and treatment of pain associated to interstitial cystitis/bladder pain syndrome (IC/BPS) |
TW201605433A (zh) * | 2013-09-12 | 2016-02-16 | 以斯提夫博士實驗室股份有限公司 | NSAID與西克馬(sigma)受體配位體之組合 |
MA39147B1 (fr) | 2013-12-17 | 2019-12-31 | Esteve Labor Dr | Combinaisons d'inhibiteurs de la recapture de sérotonine-norépinéphrine (snri) et de ligands des récepteurs sigma |
MA39146A1 (fr) | 2013-12-17 | 2017-11-30 | Esteve Labor Dr | Combinaisons de gabapentanoïdes et de ligands des récepteurs sigma |
EP2929883A1 (en) * | 2014-04-08 | 2015-10-14 | Institut Pasteur | Pyrazole derivatives as dihydroorotate dehydrogenase (DHODH) inhibitors |
ES2701975R1 (es) * | 2016-07-12 | 2019-03-01 | Esteve Pharmaceuticals Sa | Uso de ligandos del receptor sigma en el dolor post-herpetico |
EP3796929A1 (en) * | 2018-05-21 | 2021-03-31 | Ipsen Biopharm Limited | Suppression of bone cancer-induced allodynia |
US11034669B2 (en) | 2018-11-30 | 2021-06-15 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
CN112341397B (zh) * | 2019-08-09 | 2023-05-23 | 成都苑东生物制药股份有限公司 | 吡嗪类衍生物或盐、异构体、其制备方法及用途 |
KR20210151572A (ko) | 2020-06-05 | 2021-12-14 | 주식회사 허밍아비스 | 발열체 조성물 및 이를 이용한 마스크 제조방법 |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SI2298743T1 (sl) * | 2003-06-26 | 2012-12-31 | Novartis Ag | Inhibitorji p38-kinaze na osnovi 5-ÄŤlenskih heterociklov |
EP1781618B1 (en) * | 2004-08-27 | 2012-10-03 | Laboratorios Del Dr. Esteve, S.A. | Sigma receptor inhibitors |
RU2417987C2 (ru) * | 2004-08-27 | 2011-05-10 | Лабораторьос Дель Др.Эстеве, С.А. | Ингибиторы сигма-рецептора |
WO2007098953A1 (en) * | 2006-03-01 | 2007-09-07 | Laboratorios Del Dr. Esteve, S.A. | Pyrazole derivatives as sigma receptor inhibitors |
EP2113501A1 (en) * | 2008-04-25 | 2009-11-04 | Laboratorios Del. Dr. Esteve, S.A. | 5-Methyl-1-(naphthalen-2-YL)-1H-Pyrazoles useful as sigma receptor inhibitors |
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 |
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 |
-
2010
- 2010-12-03 EP EP10382330A patent/EP2460519A1/en not_active Withdrawn
-
2011
- 2011-02-12 UA UAA201308348A patent/UA112638C2/uk unknown
- 2011-11-25 TW TW100143323A patent/TWI629060B/zh not_active IP Right Cessation
- 2011-12-02 SG SG2013042569A patent/SG190745A1/en unknown
- 2011-12-02 AR ARP110104502A patent/AR084730A1/es unknown
- 2011-12-02 SI SI201131191A patent/SI2646025T1/sl unknown
- 2011-12-02 PT PT117940825T patent/PT2646025T/pt unknown
- 2011-12-02 DK DK11794082.5T patent/DK2646025T3/en active
- 2011-12-02 KR KR1020137017344A patent/KR101855358B1/ko active IP Right Grant
- 2011-12-02 US US13/991,282 patent/US20130324535A1/en not_active Abandoned
- 2011-12-02 CA CA2819442A patent/CA2819442C/en not_active Expired - Fee Related
- 2011-12-02 ME MEP-2017-120A patent/ME02852B/me unknown
- 2011-12-02 WO PCT/EP2011/071584 patent/WO2012072782A1/en active Application Filing
- 2011-12-02 BR BR112013013369A patent/BR112013013369A8/pt not_active Application Discontinuation
- 2011-12-02 JP JP2013541369A patent/JP6027014B2/ja not_active Expired - Fee Related
- 2011-12-02 MY MYPI2013001961A patent/MY171994A/en unknown
- 2011-12-02 RS RS20170575A patent/RS56081B1/sr unknown
- 2011-12-02 EP EP11794082.5A patent/EP2646025B1/en active Active
- 2011-12-02 RU RU2013130222/15A patent/RU2585095C2/ru not_active IP Right Cessation
- 2011-12-02 ES ES11794082.5T patent/ES2626672T3/es active Active
- 2011-12-02 MX MX2013006140A patent/MX343773B/es active IP Right Grant
- 2011-12-02 PL PL11794082T patent/PL2646025T3/pl unknown
- 2011-12-02 HU HUE11794082A patent/HUE033488T2/en unknown
- 2011-12-02 MA MA36072A patent/MA34878B1/fr unknown
- 2011-12-02 CN CN201180065232.XA patent/CN103313709B/zh not_active Expired - Fee Related
- 2011-12-02 LT LTEP11794082.5T patent/LT2646025T/lt unknown
- 2011-12-02 TR TR2017/08567T patent/TR201708567T4/tr unknown
- 2011-12-02 NZ NZ612119A patent/NZ612119A/en not_active IP Right Cessation
-
2013
- 2013-05-29 TN TNP2013000227A patent/TN2013000227A1/fr unknown
- 2013-06-03 IL IL226706A patent/IL226706A/en active IP Right Grant
- 2013-07-02 CO CO13155721A patent/CO6781549A2/es not_active Application Discontinuation
- 2013-07-03 ZA ZA2013/04966A patent/ZA201304966B/en unknown
-
2017
- 2017-05-30 HR HRP20170818TT patent/HRP20170818T1/hr unknown
- 2017-06-08 CY CY20171100604T patent/CY1119030T1/el unknown
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