AR102799A1 - Profármacos de agonistas fenólicos de trpv1 - Google Patents
Profármacos de agonistas fenólicos de trpv1Info
- Publication number
- AR102799A1 AR102799A1 ARP150103868A ARP150103868A AR102799A1 AR 102799 A1 AR102799 A1 AR 102799A1 AR P150103868 A ARP150103868 A AR P150103868A AR P150103868 A ARP150103868 A AR P150103868A AR 102799 A1 AR102799 A1 AR 102799A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- unsubstituted
- trpv1
- phenolic
- atoms
- Prior art date
Links
- 239000000556 agonist Substances 0.000 title abstract 2
- 102000003566 TRPV1 Human genes 0.000 title 1
- 101150016206 Trpv1 gene Proteins 0.000 title 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol group Chemical group C1(=CC=CC=C1)O ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 abstract 2
- 102100029613 Transient receptor potential cation channel subfamily V member 1 Human genes 0.000 abstract 1
- 108050004388 Transient receptor potential cation channel subfamily V member 1 Proteins 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 230000001052 transient effect Effects 0.000 abstract 1
Classifications
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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
- A61K31/16—Amides, e.g. hydroxamic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
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- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P23/00—Anaesthetics
- A61P23/02—Local anaesthetics
-
- 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
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- 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
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- 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]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/40—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings
- C07C271/42—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/52—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
- C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
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- 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
- C07D211/08—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/26—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/195—Radicals derived from nitrogen analogues of carboxylic acids
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Virology (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Anesthesiology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Molecular Biology (AREA)
- Emergency Medicine (AREA)
- AIDS & HIV (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Reproductive Health (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Se describen compuestos, composiciones farmacéuticas y medicamentos que los incluyen, y métodos de uso de dichos compuestos para modular la actividad del receptor de potencial transitorio del receptor vanilloide 1 (TRPV1). Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de fórmula (1), donde: Y es un agonista de TRPV1 fenólico, donde el átomo de hidrógeno del grupo hidroxilo fenólico se reemplaza por un enlace covalente con -C(O)-X-(C(R¹)(R²))ₙ-Z; X es -C(R¹)(R²)-, -O-, -N(R⁵)- o -S-; n es un entero entre 1 y 10; Z es -NR³R⁴ o -CO₂H; R⁵ es hidrógeno, alquilo sustituido o no sustituido, o arilo sustituido o no sustituido, y cada R¹ y R² es cada uno en forma independiente hidrógeno, alquilo sustituido o no sustituido, arilo sustituido o no sustituido, o acilo sustituido o no sustituido, o dos grupos R¹ o R² en átomos de carbono adyacentes, junto con los átomos de carbono a los cuales se encuentran unidos, forman un grupo cicloalquilo sustituido o no sustituido, o grupos R¹ y R⁵ en átomos adyacentes, junto con los átomos a los cuales están unidos, forman un grupo heterocicloalquilo sustituido o no sustituido; y R³ y R⁴ es cada uno en forma independiente hidrógeno, alquilo sustituido o no sustituido, o arilo sustituido o no sustituido; o una sal aceptable farmacéuticamente, solvato aceptable farmacéuticamente, o hidrato del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462084515P | 2014-11-25 | 2014-11-25 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR102799A1 true AR102799A1 (es) | 2017-03-22 |
Family
ID=56009519
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP150103868A AR102799A1 (es) | 2014-11-25 | 2015-11-25 | Profármacos de agonistas fenólicos de trpv1 |
Country Status (28)
Country | Link |
---|---|
US (1) | US9359316B1 (es) |
EP (2) | EP3872063A1 (es) |
JP (2) | JP6670841B2 (es) |
KR (1) | KR102562571B1 (es) |
CN (1) | CN107205961B (es) |
AR (1) | AR102799A1 (es) |
AU (1) | AU2015353532B2 (es) |
BR (1) | BR112017010950B1 (es) |
CA (1) | CA2968061C (es) |
CY (1) | CY1124811T1 (es) |
DK (1) | DK3223805T3 (es) |
EA (1) | EA033619B1 (es) |
ES (1) | ES2871095T3 (es) |
HK (1) | HK1244672A1 (es) |
HR (1) | HRP20210775T1 (es) |
HU (1) | HUE054449T2 (es) |
IL (1) | IL252307B (es) |
LT (1) | LT3223805T (es) |
MX (1) | MX2017006818A (es) |
PH (1) | PH12017500974A1 (es) |
PL (1) | PL3223805T3 (es) |
PT (1) | PT3223805T (es) |
RS (1) | RS61875B1 (es) |
SG (1) | SG11201704290VA (es) |
SI (1) | SI3223805T1 (es) |
TW (1) | TWI692465B (es) |
WO (1) | WO2016086063A1 (es) |
ZA (1) | ZA201703409B (es) |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US11634384B2 (en) | 2014-11-25 | 2023-04-25 | Concentric Analgesics, Inc. | Prodrugs of phenolic TRPV1 agonists |
EP3463576A4 (en) * | 2016-05-25 | 2020-01-15 | Concentric Analgesics, Inc. | PRODRUGS BY PHENOLIC TRPV1 AGONISTS IN COMBINATION WITH LOCAL ANESTHETIC AND VASOCONSTRICTORS FOR IMPROVED LOCAL ANESTHESIA |
CA3041121A1 (en) | 2016-11-02 | 2018-05-11 | Centrexion Therapeutics Corporation | Stable aqueous capsaicin injectable formulations and medical uses thereof |
CN108069898B (zh) * | 2016-11-16 | 2021-11-23 | 南华大学 | 含烟酸辣椒碱酯衍生物、制备方法及其用途 |
WO2018217937A1 (en) * | 2017-05-24 | 2018-11-29 | Concentric Analgesics, Inc. | Prodrugs of phenolic trpv1 agonists in combination with local anesthetics and vasoconstrictors for improved local anesthesia |
MX2020000488A (es) | 2017-07-20 | 2020-10-28 | Centrexion Therapeutics Corp | Metodos y composiciones para el tratamiento del dolor usando capsaicina. |
WO2020023793A1 (en) * | 2018-07-27 | 2020-01-30 | Concentric Analgesics, Inc. | Pegylated prodrugs of phenolic trpv1 agonists |
AU2019310118A1 (en) | 2018-07-27 | 2021-03-11 | Concentric Analgesics, Inc. | Pegylated prodrugs of phenolic TRPV1 agonists |
US11447444B1 (en) | 2019-01-18 | 2022-09-20 | Centrexion Therapeutics Corporation | Capsaicinoid prodrug compounds and their use in treating medical conditions |
US11254659B1 (en) | 2019-01-18 | 2022-02-22 | Centrexion Therapeutics Corporation | Capsaicinoid prodrug compounds and their use in treating medical conditions |
WO2021034863A1 (en) * | 2019-08-19 | 2021-02-25 | Chorda Pharma, Inc. | Chemical derivatives and methods for synthesizing and compounding chemical derivatives related to capsaicin palmitate and capsaicin prodrugs |
US20220371988A1 (en) * | 2019-09-30 | 2022-11-24 | Nanjing Delova Biotech Co. Ltd. | Trpv1 agonist and preparation method therefor and use thereof |
US20240058316A1 (en) * | 2020-12-14 | 2024-02-22 | Concentric Analgesics, Inc. | Prodrug of a phenolic trpv1 agonist for the treatment of pain |
US20240050421A1 (en) * | 2020-12-14 | 2024-02-15 | Concentric Analgesics, Inc. | Pharmaceutical formulations of a phenolic trpv1 agonist prodrug |
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