BR112017010950B1 - Composto, composição farmacêutica de pró-fármacos de agonistas fenólicos de trpv1 e uso do composto - Google Patents

Composto, composição farmacêutica de pró-fármacos de agonistas fenólicos de trpv1 e uso do composto Download PDF

Info

Publication number
BR112017010950B1
BR112017010950B1 BR112017010950-6A BR112017010950A BR112017010950B1 BR 112017010950 B1 BR112017010950 B1 BR 112017010950B1 BR 112017010950 A BR112017010950 A BR 112017010950A BR 112017010950 B1 BR112017010950 B1 BR 112017010950B1
Authority
BR
Brazil
Prior art keywords
compound
formula
substituted
unsubstituted
alkyl
Prior art date
Application number
BR112017010950-6A
Other languages
English (en)
Portuguese (pt)
Other versions
BR112017010950A2 (pt
Inventor
Craig Husfeld
John F. Donovan
Original Assignee
Concentric Analgesics, Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Concentric Analgesics, Inc filed Critical Concentric Analgesics, Inc
Publication of BR112017010950A2 publication Critical patent/BR112017010950A2/pt
Publication of BR112017010950B1 publication Critical patent/BR112017010950B1/pt

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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Anesthesiology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
BR112017010950-6A 2014-11-25 2015-11-24 Composto, composição farmacêutica de pró-fármacos de agonistas fenólicos de trpv1 e uso do composto BR112017010950B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462084515P 2014-11-25 2014-11-25
US62/084,515 2014-11-25
US14/743,375 US9359316B1 (en) 2014-11-25 2015-06-18 Prodrugs of phenolic TRPV1 agonists
US14/743,375 2015-06-18
PCT/US2015/062531 WO2016086063A1 (en) 2014-11-25 2015-11-24 Prodrugs of phenolic trpv1 agonists

Publications (2)

Publication Number Publication Date
BR112017010950A2 BR112017010950A2 (pt) 2018-07-03
BR112017010950B1 true BR112017010950B1 (pt) 2023-12-26

Family

ID=56009519

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112017010950-6A BR112017010950B1 (pt) 2014-11-25 2015-11-24 Composto, composição farmacêutica de pró-fármacos de agonistas fenólicos de trpv1 e uso do composto

Country Status (28)

Country Link
US (1) US9359316B1 (enExample)
EP (2) EP3872063A1 (enExample)
JP (2) JP6670841B2 (enExample)
KR (1) KR102562571B1 (enExample)
CN (1) CN107205961B (enExample)
AR (1) AR102799A1 (enExample)
AU (1) AU2015353532B2 (enExample)
BR (1) BR112017010950B1 (enExample)
CA (1) CA2968061C (enExample)
CY (1) CY1124811T1 (enExample)
DK (1) DK3223805T3 (enExample)
EA (1) EA033619B1 (enExample)
ES (1) ES2871095T3 (enExample)
HR (1) HRP20210775T1 (enExample)
HU (1) HUE054449T2 (enExample)
IL (1) IL252307B (enExample)
LT (1) LT3223805T (enExample)
MX (1) MX382872B (enExample)
PH (1) PH12017500974B1 (enExample)
PL (1) PL3223805T3 (enExample)
PT (1) PT3223805T (enExample)
RS (1) RS61875B1 (enExample)
SG (1) SG11201704290VA (enExample)
SI (1) SI3223805T1 (enExample)
SM (1) SMT202100308T1 (enExample)
TW (1) TWI692465B (enExample)
WO (1) WO2016086063A1 (enExample)
ZA (1) ZA201703409B (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11634384B2 (en) 2014-11-25 2023-04-25 Concentric Analgesics, Inc. Prodrugs of phenolic TRPV1 agonists
CA3025268A1 (en) * 2016-05-25 2017-11-30 Concentric Analgesics, Inc. Prodrugs of phenolic trpv1 agonists in combination with local anesthetics and vasoconstrictors for improved local anesthesia
EP3534961A4 (en) 2016-11-02 2020-05-27 Centrexion Therapeutics Corporation STABLE AQUEOUS INJECTABLE CAPSAICIN 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
ES3018268T3 (en) 2017-07-20 2025-05-14 Centrexion Therapeutics Corp Compositions and their use for treatment of pain using capsaicin
WO2020023793A1 (en) * 2018-07-27 2020-01-30 Concentric Analgesics, Inc. Pegylated prodrugs of phenolic trpv1 agonists
TW202019887A (zh) * 2018-07-27 2020-06-01 美商同心止痛劑股份有限公司 酚系trpv1促效劑之聚乙二醇化前藥
US11254659B1 (en) 2019-01-18 2022-02-22 Centrexion Therapeutics Corporation Capsaicinoid prodrug compounds and their use in treating medical conditions
US11447444B1 (en) 2019-01-18 2022-09-20 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
EP4023631A4 (en) * 2019-09-30 2022-12-07 Nanjing Delova Biotech Co. Ltd. TRPV1 AGONIST, METHOD FOR PREPARATION AND USE
WO2022132649A1 (en) * 2020-12-14 2022-06-23 Concentric Analgesics, Inc. Pharmaceutical formulations of a phenolic trpv1 agonist prodrug
EP4263496A4 (en) * 2020-12-14 2024-11-13 Concentric Analgesics, Inc. PRODRUG OF A PHENOLIC TRPV1 AGONIST FOR THE TREATMENT OF PAIN

Family Cites Families (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3598122A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3598123A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3993073A (en) 1969-04-01 1976-11-23 Alza Corporation Novel drug delivery device
US3710795A (en) 1970-09-29 1973-01-16 Alza Corp Drug-delivery device with stretched, rate-controlling membrane
US4069307A (en) 1970-10-01 1978-01-17 Alza Corporation Drug-delivery device comprising certain polymeric materials for controlled release of drug
US3731683A (en) 1971-06-04 1973-05-08 Alza Corp Bandage for the controlled metering of topical drugs to the skin
US3996934A (en) 1971-08-09 1976-12-14 Alza Corporation Medical bandage
US3742951A (en) 1971-08-09 1973-07-03 Alza Corp Bandage for controlled release of vasodilators
BE795384A (fr) 1972-02-14 1973-08-13 Ici Ltd Pansements
US3921636A (en) 1973-01-15 1975-11-25 Alza Corp Novel drug delivery device
US3993072A (en) 1974-08-28 1976-11-23 Alza Corporation Microporous drug delivery device
US4151273A (en) 1974-10-31 1979-04-24 The Regents Of The University Of California Increasing the absorption rate of insoluble drugs
US3972995A (en) 1975-04-14 1976-08-03 American Home Products Corporation Dosage form
US4077407A (en) 1975-11-24 1978-03-07 Alza Corporation Osmotic devices having composite walls
US4031894A (en) 1975-12-08 1977-06-28 Alza Corporation Bandage for transdermally administering scopolamine to prevent nausea
US4060084A (en) 1976-09-07 1977-11-29 Alza Corporation Method and therapeutic system for providing chemotherapy transdermally
US4201211A (en) 1977-07-12 1980-05-06 Alza Corporation Therapeutic system for administering clonidine transdermally
JPS5562012A (en) 1978-11-06 1980-05-10 Teijin Ltd Slow-releasing preparation
US4230105A (en) 1978-11-13 1980-10-28 Merck & Co., Inc. Transdermal delivery of drugs
US4229447A (en) 1979-06-04 1980-10-21 American Home Products Corporation Intraoral methods of using benzodiazepines
CA1146866A (en) 1979-07-05 1983-05-24 Yamanouchi Pharmaceutical Co. Ltd. Process for the production of sustained release pharmaceutical composition of solid medical material
US4291015A (en) 1979-08-14 1981-09-22 Key Pharmaceuticals, Inc. Polymeric diffusion matrix containing a vasodilator
US4327725A (en) 1980-11-25 1982-05-04 Alza Corporation Osmotic device with hydrogel driving member
US4476116A (en) 1982-12-10 1984-10-09 Syntex (U.S.A.) Inc. Polypeptides/chelating agent nasal compositions having enhanced peptide absorption
US5116817A (en) 1982-12-10 1992-05-26 Syntex (U.S.A.) Inc. LHRH preparations for intranasal administration
US4596795A (en) 1984-04-25 1986-06-24 The United States Of America As Represented By The Secretary, Dept. Of Health & Human Services Administration of sex hormones in the form of hydrophilic cyclodextrin derivatives
US4624848A (en) 1984-05-10 1986-11-25 Ciba-Geigy Corporation Active agent containing hydrogel devices wherein the active agent concentration profile contains a sigmoidal concentration gradient for improved constant release, their manufacture and use
JPS624233A (ja) 1985-07-01 1987-01-10 Toyobo Co Ltd 組織性プラスミノ−ゲン活性化因子の製造法
GB8518301D0 (en) 1985-07-19 1985-08-29 Fujisawa Pharmaceutical Co Hydrodynamically explosive systems
DE3684446D1 (de) 1985-12-28 1992-04-23 Sumitomo Pharma Arzneimittel mit verzoegerter stossweiser freisetzung.
US4755386A (en) 1986-01-22 1988-07-05 Schering Corporation Buccal formulation
US5312325A (en) 1987-05-28 1994-05-17 Drug Delivery Systems Inc Pulsating transdermal drug delivery system
US4812590A (en) * 1987-06-25 1989-03-14 Merck & Co., Inc. Carbamates of 4-hydroxyanisole as prodrugs for chemotherapy of melanoma
US4968509A (en) 1987-07-27 1990-11-06 Mcneilab, Inc. Oral sustained release acetaminophen formulation and process
IL92966A (en) 1989-01-12 1995-07-31 Pfizer Dispensing devices powered by hydrogel
US5739136A (en) 1989-10-17 1998-04-14 Ellinwood, Jr.; Everett H. Intraoral dosing method of administering medicaments
US5017381A (en) 1990-05-02 1991-05-21 Alza Corporation Multi-unit pulsatile delivery system
US5633009A (en) 1990-11-28 1997-05-27 Sano Corporation Transdermal administration of azapirones
US5094782A (en) * 1990-12-24 1992-03-10 National Science Council Of Republic Of China Synthesis of capsacin derivatives and their use as an analgesic drug and vessel dilation drug
DE69222847T3 (de) 1991-04-16 2005-09-15 Nippon Shinyaku Co., Ltd. Verfahren zur herstellung einer festen dispersion
JPH0778037B2 (ja) * 1991-06-13 1995-08-23 ナショナル サイエンス カウンシル カプサイシン誘導体又はその酸エステルを有効成分とする鎮痛剤、血管拡張剤
US5229135A (en) 1991-11-22 1993-07-20 Prographarm Laboratories Sustained release diltiazem formulation
CA2122479C (en) 1991-11-22 1998-08-25 Richard John Dansereau Risedronate delayed-release compositions
US5340591A (en) 1992-01-24 1994-08-23 Fujisawa Pharmaceutical Co., Ltd. Method of producing a solid dispersion of the sparingly water-soluble drug, nilvadipine
US5461140A (en) 1992-04-30 1995-10-24 Pharmaceutical Delivery Systems Bioerodible polymers for solid controlled release pharmaceutical compositions
US5260068A (en) 1992-05-04 1993-11-09 Anda Sr Pharmaceuticals Inc. Multiparticulate pulsatile drug delivery system
US5281420A (en) 1992-05-19 1994-01-25 The Procter & Gamble Company Solid dispersion compositions of tebufelone
AU4198793A (en) 1992-07-24 1994-01-27 Takeda Chemical Industries Ltd. Microparticle preparation and production thereof
US5700485A (en) 1992-09-10 1997-12-23 Children's Medical Center Corporation Prolonged nerve blockade by the combination of local anesthetic and glucocorticoid
EP0665010B1 (en) 1992-10-16 2002-09-11 Nippon Shinyaku Company, Limited Method of manufacturing wax matrices
US5260069A (en) 1992-11-27 1993-11-09 Anda Sr Pharmaceuticals Inc. Pulsatile particles drug delivery system
US5686105A (en) 1993-10-19 1997-11-11 The Procter & Gamble Company Pharmaceutical dosage form with multiple enteric polymer coatings for colonic delivery
US5665378A (en) 1994-09-30 1997-09-09 Davis; Roosevelt Transdermal therapeutic formulation
US5567441A (en) 1995-03-24 1996-10-22 Andrx Pharmaceuticals Inc. Diltiazem controlled release formulation
CA2220451A1 (en) 1995-05-17 1996-11-21 Cedars-Sinai Medical Center Methods and compositions for improving digestion and absorption in the small intestine
SE9502244D0 (sv) 1995-06-20 1995-06-20 Bioglan Ab A composition and a process for the preparation thereof
US5837284A (en) 1995-12-04 1998-11-17 Mehta; Atul M. Delivery of multiple doses of medications
US5858401A (en) 1996-01-22 1999-01-12 Sidmak Laboratories, Inc. Pharmaceutical composition for cyclosporines
US6929801B2 (en) 1996-02-19 2005-08-16 Acrux Dds Pty Ltd Transdermal delivery of antiparkinson agents
US6923983B2 (en) 1996-02-19 2005-08-02 Acrux Dds Pty Ltd Transdermal delivery of hormones
US6458373B1 (en) 1997-01-07 2002-10-01 Sonus Pharmaceuticals, Inc. Emulsion vehicle for poorly soluble drugs
WO1998040070A1 (en) 1997-03-13 1998-09-17 Campbell James N Compositions containing capsaicin or capsaicin analogues and a local anesthetic
US5840329A (en) 1997-05-15 1998-11-24 Bioadvances Llc Pulsatile drug delivery system
US6391452B1 (en) 1997-07-18 2002-05-21 Bayer Corporation Compositions for nasal drug delivery, methods of making same, and methods of removing residual solvent from pharmaceutical preparations
US5869090A (en) 1998-01-20 1999-02-09 Rosenbaum; Jerry Transdermal delivery of dehydroepiandrosterone
US6946144B1 (en) 1998-07-08 2005-09-20 Oryxe Transdermal delivery system
DE60039379D1 (de) 1999-02-10 2008-08-21 Pfizer Prod Inc Pharmazeutische feste Dispersionen
US6395300B1 (en) 1999-05-27 2002-05-28 Acusphere, Inc. Porous drug matrices and methods of manufacture thereof
JP2004511488A (ja) * 2000-10-10 2004-04-15 オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド 新規標識レシニフェラトキシン誘導体
US6465014B1 (en) 2001-03-21 2002-10-15 Isp Investments Inc. pH-dependent sustained release, drug-delivery composition
US6960563B2 (en) 2001-08-31 2005-11-01 Morton Grove Pharmaceuticals, Inc. Spontaneous emulsions containing cyclosporine
US20040161481A1 (en) 2002-12-18 2004-08-19 Algorx Administration of capsaicinoids
US20050019436A1 (en) 2002-12-18 2005-01-27 Algorx Injectable capsaicin
US20040202735A1 (en) * 2003-04-08 2004-10-14 Moore Bob M. Method and kit for controlling bleeding
US20080193481A1 (en) 2005-03-14 2008-08-14 Governors Of The University Of Alberta Synthetic Anti-Candida Albicans Oligosaccharide Based Vaccines
ZA200709821B (en) * 2005-04-25 2009-10-28 Neurogesx Inc TRPV1 agonist compounds and methods for making and using the same
US7943666B2 (en) 2006-07-24 2011-05-17 Trinity Laboratories, Inc. Esters of capsaicin for treating pain
JP2010529039A (ja) 2007-05-30 2010-08-26 ブリガム・ヤング・ユニバーシティ タンパク質キナーゼ結合ヌクレオシドおよび関連の方法
US8535655B2 (en) 2008-10-10 2013-09-17 Polyactiva Pty Ltd. Biodegradable polymer—bioactive moiety conjugates
NZ592139A (en) * 2008-10-10 2013-03-28 Bionic Ear Inst Biodegradable polymer - bioactive moiety conjugates
CN101774938B (zh) * 2010-01-20 2014-04-30 中国药科大学 一类辣椒碱衍生物、其制备方法及其制备新型镇痛药物的用途
US9492409B2 (en) 2012-05-23 2016-11-15 Cellix Bio Private Limited Compositions and methods for the treatment of local pain
KR101478520B1 (ko) * 2014-01-24 2015-01-02 동신대학교산학협력단 피부 안전성이 향상된 캡사이신-펩타이드 및 이를 이용한 피부 외용제 조성물
CN104447777B (zh) * 2014-11-26 2016-09-14 浙江大学 一种辣椒碱-喜树碱类抗癌药物偶联物及其制备方法和应用

Also Published As

Publication number Publication date
KR102562571B1 (ko) 2023-08-01
KR20170095896A (ko) 2017-08-23
PT3223805T (pt) 2021-05-28
CA2968061C (en) 2023-08-22
JP7026152B2 (ja) 2022-02-25
TWI692465B (zh) 2020-05-01
BR112017010950A2 (pt) 2018-07-03
PH12017500974A1 (en) 2018-01-08
EA033619B1 (ru) 2019-11-11
US20160145225A1 (en) 2016-05-26
MX2017006818A (es) 2018-01-30
JP6670841B2 (ja) 2020-03-25
EA201790896A1 (ru) 2017-12-29
LT3223805T (lt) 2021-06-10
IL252307B (en) 2021-02-28
EP3872063A1 (en) 2021-09-01
ES2871095T3 (es) 2021-10-28
DK3223805T3 (da) 2021-05-25
JP2020114813A (ja) 2020-07-30
AU2015353532A1 (en) 2017-06-15
US9359316B1 (en) 2016-06-07
JP2017536416A (ja) 2017-12-07
CN107205961B (zh) 2021-03-16
WO2016086063A1 (en) 2016-06-02
SG11201704290VA (en) 2017-06-29
AU2015353532B2 (en) 2021-03-18
CN107205961A (zh) 2017-09-26
HUE054449T2 (hu) 2021-09-28
EP3223805A1 (en) 2017-10-04
CA2968061A1 (en) 2016-06-02
PH12017500974B1 (en) 2018-01-08
RS61875B1 (sr) 2021-06-30
AR102799A1 (es) 2017-03-22
PL3223805T3 (pl) 2021-10-11
ZA201703409B (en) 2023-10-25
SI3223805T1 (sl) 2021-09-30
EP3223805A4 (en) 2018-07-25
IL252307A0 (en) 2017-07-31
CY1124811T1 (el) 2022-11-25
SMT202100308T1 (it) 2021-07-12
HK1244672A1 (zh) 2018-08-17
MX382872B (es) 2025-03-13
HRP20210775T1 (hr) 2021-06-25
TW201629004A (zh) 2016-08-16
EP3223805B1 (en) 2021-02-24

Similar Documents

Publication Publication Date Title
BR112017010950B1 (pt) Composto, composição farmacêutica de pró-fármacos de agonistas fenólicos de trpv1 e uso do composto
US10851123B2 (en) Prodrugs of phenolic TRPV1 agonists
US20230219901A1 (en) Pegylated prodrugs of phenolic trpv1 agonists
US11634384B2 (en) Prodrugs of phenolic TRPV1 agonists
US20170260131A1 (en) Prodrugs of phenolic trpv1 agonists
WO2020023793A1 (en) Pegylated prodrugs of phenolic trpv1 agonists
US20250388533A1 (en) Prodrugs of phenolic trpv1 agonists
HK1244672B (zh) 酚类trpv1激动剂的前药
HK40059345A (en) Pegylated prodrugs of phenolic trpv1 agonists

Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B25G Requested change of headquarter approved

Owner name: CONCENTRIC ANALGESICS, INC. (US)

B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 24/11/2015, OBSERVADAS AS CONDICOES LEGAIS