AR047008A1 - Compuestos de 4-tetrazolil-4-fenilpiperidina como agonistas de los receptores opioides y agentes terapeuticos de utilidad para el tratamiento del dolor y composiciones farmaceuticas que los contienen como principio activo en combinacion con otros agentes terapéuticos. - Google Patents
Compuestos de 4-tetrazolil-4-fenilpiperidina como agonistas de los receptores opioides y agentes terapeuticos de utilidad para el tratamiento del dolor y composiciones farmaceuticas que los contienen como principio activo en combinacion con otros agentes terapéuticos.Info
- Publication number
- AR047008A1 AR047008A1 ARP030104269A ARP030104269A AR047008A1 AR 047008 A1 AR047008 A1 AR 047008A1 AR P030104269 A ARP030104269 A AR P030104269A AR P030104269 A ARP030104269 A AR P030104269A AR 047008 A1 AR047008 A1 AR 047008A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- 3alkyl
- integer ranging
- antryl
- phenanthryl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 7
- 239000000556 agonist Substances 0.000 title 1
- 239000003795 chemical substances by application Substances 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 229940124597 therapeutic agent Drugs 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 40
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 12
- 125000001624 naphthyl group Chemical group 0.000 abstract 10
- 125000005561 phenanthryl group Chemical group 0.000 abstract 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 10
- 125000002947 alkylene group Chemical group 0.000 abstract 8
- -1 4-tetrazolyl-4-phenylpiperidine compound Chemical class 0.000 abstract 7
- 150000003839 salts Chemical class 0.000 abstract 6
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 4
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 2
- OGPKTRWLBLRODW-UHFFFAOYSA-N 4-phenyl-4-(2h-tetrazol-5-yl)piperidine Chemical class C1CNCCC1(C=1C=CC=CC=1)C1=NNN=N1 OGPKTRWLBLRODW-UHFFFAOYSA-N 0.000 abstract 1
- 206010012735 Diarrhoea Diseases 0.000 abstract 1
- 102000003840 Opioid Receptors Human genes 0.000 abstract 1
- 108090000137 Opioid Receptors Proteins 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
Classifications
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- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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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
- A61K31/435—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- 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
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- 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
- A61P1/12—Antidiarrhoeals
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
- C07D211/64—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having an aryl radical as the second substituent in position 4
-
- 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
Abstract
Compuestos de 4-tetrazolil-4-fenilpiperidina, composiciones que comprenden una cantidad efectiva de un compuesto de 4-tetrazolil-4-fenilpiperidina, utiles para tratar o prevenir dolor o diarrea en un animal y para estimular la funcion el receptor opioide en una célula. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1a) o una sal farmacéuticamente aceptable del mismo, en donde: Ar1 es cicloalquilo C3-8, fenilo, naftilo, antrilo, fenantrilo o -heteroarilo (de 5 a 7 miembros), estando cada uno insustituido o sustituido con uno o varios grupos R2; Ar2 es fenilo, naftilo, antrilo, fenantrilo o -heteroarilo (de 5 a 7 miembros), estando cada uno insustituido o sustituido con uno o varios grupos R2; G es -H, -L- (CH2)nCO2R4, -L-(CH2)nR5, -(alquilen C1-5)CO2R4, o -(alquilen C1-5)R5; L es -C(O)-, -SO2- o -SO-; R1 es -H, -C(O)NH2, -C(O)NHOH, -CO2R4, -CHO, -CN, -(alquilo C1-4), -C(O)NH(alquilo C1-4), -C(O)N(alquilo C1-4)2, o un resto seleccionado del grupo de formulas (2); R2 y R3 son cada uno, de modo independiente, -halogeno, -alquilo C1-3, -O(alquilo C1-3), -NH(alquilo C1-3) o -N(alquilo C1-3)2; R4 = -H, alquilo C1-10, -CH2O(alquilo C1-4), -CH2N(alquilo C1-4)2 o -CH2NH(alquilo C1-4); R5 = -NH2, - NHSO2R4, -C(O)NH2, -C(O)NHOH, -SO2NH2, -C(O)NH(alquilo C1-4), -C(O)N(alquilo C1-4)2., -SO2NH(alquilo C1-4), -SO2N(alquilo C1-4)2, -H, -OH, -CN, -cicloalquilo C3-8, fenilo, naftilo, antrilo, fenantrilo, o -heteroarilo (de 5 a 7 miembros), estando cada uno insustituido o sustituido con uno o varios grupos R2; m = un numero entero que va de 0 a 4; n = un numero entero que va de 1 a 4; p = 0 o 1; q = un numero entero que va de 0 a 3 y r = un numero entero que va de 1 a 6. Reivindicacion 21: Un compuesto caracterizado porque tiene la formula (1b), o una sal farmacéuticamente aceptable del mismo, en donde: Ar1 es cicloalquilo C3-8, fenilo, naftilo, antrilo, fenantrilo o -heteroarilo (de 5 a 7 miembros), estando cada uno insustituido o sustituido con uno o varios grupos R2; Ar2 es fenilo, naftilo, antrilo, fenantrilo o -heteroarilo (de 5 a 7 miembros), estando cada uno insustituido o sustituido con uno o varios grupos R2; G es -H, -L-(CH2)nC(O)OR4, -L-(CH2)nR5, -(alquilen C1- 5)COOR4, o -(alquileno C1-5)R5; L es -C(O)-, -SO2- o -SO-; R1 es -H, -C(O)NH2, -C(O)NHOH, -CO2R4, -CHO, -CN, -(alquilo C1-4), -C(O)NH(alquilo C1-4), -C(O)N(alquilo C1-4)2, o un resto seleccionado del grupo de formulas (2); R2 y R3 son cada uno, de modo independiente, -halogeno, -alquilo C1-3, -O(alquilo C1-3), -NH(alquilo C1-3) o -N(alquilo C1-3)2; R4 = -H, alquilo C1-10, -CH2O(alquilo C1-4), -CH2N(alquilo C1-4)2 o -CH2NH(alquilo C1-4); R5 = -NH2, -NHSO2R4, -C(O)NH2, -C(O)NHOH, -SO2NH2, - C(O)NH(alquilo C1-4), -C(O)N(alquilo C1-4)2, -SO2NH(alquilo C1-4), -SO2N(alquilo C1-4)2, -H, -OH, -CN, -cicloalquilo C3-8, fenilo, naftilo, antrilo, fenantrilo, o -heteroarilo (de 5 a 7 miembros), estando cada uno insustituido o sustituido con uno o varios grupos R2; m = un numero entero que va de 0 a 4; n = un numero entero que va de 1 a 4; p = 0 o 1; q = un numero entero que va de 0 a 3 y r = un numero entero que va de 1 a 6. Reivindicacion 41: Un compuesto caracterizado porque tiene la formula (1c) o una sal farmacéuticamente aceptable del mismo, en donde; Ar3 es fenilo, naftilo, antrilo, fenantrilo o -heteroarilo (de 5 a 7 miembros), estando cada uno insustituido o sustituido con uno o varios grupos R2; G = -H, -L-(CH2)nC(O)OR4, - L-(CH2)nR5, -(alquilen C1-5)COOR4, o -(alquilen C1-5)R5; L es -C(O)-, -SO2- o -SO-; R1 es -H, -C(O)NH2, -C(O)NHOH, -CO2R4, -CHO, -CN, -(alquilo C1-4), -C(O)NH(alquilo C1-4), -C(O)N(alquilo C1-4)2, o un resto seleccionado del grupo de formulas (2); R2 y R3 son cada uno, de modo independiente, -halogeno, -alquilo C1-3, -O(alquilo C1-3), -NH(alquilo C1-3) o -N(alquilo C1-3)2; R4 = -H, alquilo C1-10, -CH2O(alquilo C1-4), -CH2N(alquilo C1-4)2 o -CH2NH(alquilo C1-4); R5 = -NH2, -NHSO2R4, -C(O)NH2, - C(O)NHOH, -SO2NH2, -C(O)NH(alquilo C1-4), -C(O)N(alquilo C1-4)2, -SO2NH(alquilo C1-4), -SO2N(alquilo C1-4)2, -H, -OH, -CN, -cicloalquilo C3-8, fenilo, naftilo, antrilo, fenantrilo, o -heteroarilo (de 5 a 7 miembros), estando cada uno insustituido o sustituido con uno o varios grupos R2; m = un numero entero que va de 0 a 4; n = un numero entero que va de 1 a 4; p = 0 o 1; q = un numero entero que va de 0 a 3 y r = un numero entero que va de 1 a 6. Reivindicacion 61: Un compuesto caracterizado porque tiene la formula (1d) o una sal farmacéuticamente aceptable del mismo, en donde: Ar3 es fenilo, naftilo, antrilo, fenantrilo o -heteroarilo (de 5 a 7 miembros), estando cada uno insustituido o sustituido con uno o varios grupos R2; G = -H, -L- (CH2)nC(O)OR4, -L-(CH2)nR5, -(alquilen C1-5)COOR4, o -(alquilen C1-5)R5; L es -C(O)-, -SO2- o -SO-; R1 es -H, -C(O)NH2, -C(O)NHOH, -CO2R4, -CHO, -CN, -(alquilo C1-4), -C(O)NH(alquilo C1-4), -C(O)N(alquilo C1-4)2, o un resto seleccionado del grupo de formulas (2); R2 y R3 son cada uno, de modo independiente, -halogeno, -alquilo C1-3, -O(alquilo C1-3), -NH(alquilo C1-3) o -N(alquilo C1-3)2; R4 = -H, alquilo C1-10, -CH2O(alquilo C1-4), -CH2N(alquilo C1-4)2 o -CH2NH(alquilo C1-4); R5 = -NH2, - NHSO2R4, -C(O)NH2, -C(O)NHOH, -SO2NH2, -C(O)NH(alquilo C1-4), -C(O)N(alquilo C1-4)2, -SO2NH(alquilo C1-4), -SO2N(alquilo C1-4)2, -H, -OH, -CN, -cicloalquilo C3-8, fenilo, naftilo, antrilo, fenantrilo, o -heteroarilo (de 5 a 7 miembros), estando cada uno insustituido o sustituido con uno o varios grupos R2; m = un numero entero que va de 0 a 4; n = un numero entero que va de 1 a 4; p = 0 o 1; q = un numero entero que va de 0 a 3 y r = un numero entero que va de 1 a 6. Reivindicacion 110: Un compuesto caracterizado porque tiene la formula (3) o una sal farmacéutica del mismo. Reivindicacion 111: Un compuesto caracterizado porque tiene la formula (4) o una sal farmacéutica del mismo.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
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US42738102P | 2002-11-18 | 2002-11-18 | |
US46027803P | 2003-04-03 | 2003-04-03 | |
US48848803P | 2003-07-17 | 2003-07-17 | |
US10/714,066 US7202259B2 (en) | 2002-11-18 | 2003-11-13 | Therapeutic agents useful for treating pain |
Publications (1)
Publication Number | Publication Date |
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AR047008A1 true AR047008A1 (es) | 2006-01-04 |
Family
ID=32777221
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP030104269A AR047008A1 (es) | 2002-11-18 | 2003-11-19 | Compuestos de 4-tetrazolil-4-fenilpiperidina como agonistas de los receptores opioides y agentes terapeuticos de utilidad para el tratamiento del dolor y composiciones farmaceuticas que los contienen como principio activo en combinacion con otros agentes terapéuticos. |
Country Status (37)
Country | Link |
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US (3) | US7202259B2 (es) |
EP (2) | EP1562932B9 (es) |
JP (2) | JP4601429B2 (es) |
KR (1) | KR20050115221A (es) |
CN (2) | CN101648941A (es) |
AP (1) | AP2210A (es) |
AR (1) | AR047008A1 (es) |
AT (2) | ATE402167T1 (es) |
AU (2) | AU2003294313B2 (es) |
BR (1) | BR0316305A (es) |
CA (1) | CA2506242C (es) |
CO (1) | CO5690588A2 (es) |
CR (2) | CR7877A (es) |
CY (2) | CY1107682T1 (es) |
DE (2) | DE60313021T2 (es) |
DK (2) | DK1562932T3 (es) |
EA (1) | EA008621B1 (es) |
EC (1) | ECSP055840A (es) |
ES (2) | ES2312150T3 (es) |
GE (1) | GEP20084539B (es) |
HK (1) | HK1086829A1 (es) |
IL (1) | IL209352A0 (es) |
IS (2) | IS2720B (es) |
MA (1) | MA27565A1 (es) |
ME (1) | MEP48108A (es) |
MX (1) | MXPA05004669A (es) |
MY (1) | MY135647A (es) |
NI (1) | NI200500087A (es) |
NO (1) | NO20052894L (es) |
NZ (2) | NZ572685A (es) |
OA (1) | OA13010A (es) |
PT (2) | PT1562932E (es) |
RS (1) | RS51047B (es) |
SG (1) | SG165998A1 (es) |
SI (2) | SI1562932T1 (es) |
TW (2) | TWI343917B (es) |
WO (1) | WO2004046132A1 (es) |
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US7202259B2 (en) * | 2002-11-18 | 2007-04-10 | Euro-Celtique S.A. | Therapeutic agents useful for treating pain |
EP1641441B1 (en) | 2003-04-30 | 2014-03-12 | Purdue Pharma L.P. | Tamper-resistant transdermal dosage form comprising an active agent component and an adverse agent component at the distal site of the active agent layer |
US8790689B2 (en) * | 2003-04-30 | 2014-07-29 | Purdue Pharma L.P. | Tamper resistant transdermal dosage form |
AU2005210496B2 (en) | 2004-01-30 | 2009-04-23 | Euro-Celtique S.A. | Methods for making 4-Tetrazolyl-4-Phenylpiperidine compounds |
SE0401656D0 (sv) * | 2004-06-24 | 2004-06-24 | Astrazeneca Ab | Chemical compounds |
BRPI0619679A2 (pt) * | 2005-11-21 | 2011-10-11 | Purdue Pharma Lp | compostos 4-oxadiazolil-piperidina e seus usos |
US20080051380A1 (en) | 2006-08-25 | 2008-02-28 | Auerbach Alan H | Methods and compositions for treating cancer |
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US8969358B2 (en) | 2013-03-15 | 2015-03-03 | Purdue Pharma L.P. | Buprenorphine analogs |
WO2015097546A1 (en) | 2013-12-26 | 2015-07-02 | Purdue Pharma L.P. | Propellane-based compounds and their use as opioid receptor modulators |
EP3087078B1 (en) | 2013-12-26 | 2019-05-15 | Purdue Pharma LP | 7-beta-alkyl analogs of orvinols |
EP3087073B1 (en) | 2013-12-26 | 2018-07-04 | Purdue Pharma LP | 10-substituted morphinan hydantoins |
US9656962B2 (en) | 2013-12-26 | 2017-05-23 | Purdue Pharma L.P. | Ring-contracted morphinans and the use thereof |
WO2015097545A1 (en) | 2013-12-26 | 2015-07-02 | Purdue Pharma L.P. | Opioid receptor modulating oxabicyclo[2.2.2]octane morphinans |
WO2015099863A1 (en) | 2013-12-27 | 2015-07-02 | Purdue Pharma L.P. | 6-substituted and 7-substituted morphinan analogs and the use thereof |
US10030021B2 (en) | 2014-05-27 | 2018-07-24 | Purdue Pharma L.P. | Spirocyclic morphinans and use thereof |
JP6360915B2 (ja) | 2014-06-13 | 2018-07-18 | パーデュー、ファーマ、リミテッド、パートナーシップ | アザモルフィナン誘導体及びその使用 |
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WO2017165558A1 (en) | 2016-03-22 | 2017-09-28 | Regents Of The University Of Minnesota | Combination for treating pain |
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