HRP20210775T1 - Predlijekovi fenolnih agonista trpv1 - Google Patents

Predlijekovi fenolnih agonista trpv1 Download PDF

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HRP20210775T1
HRP20210775T1 HRP20210775TT HRP20210775T HRP20210775T1 HR P20210775 T1 HRP20210775 T1 HR P20210775T1 HR P20210775T T HRP20210775T T HR P20210775TT HR P20210775 T HRP20210775 T HR P20210775T HR P20210775 T1 HRP20210775 T1 HR P20210775T1
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pharmaceutically acceptable
substituted
image
unsubstituted
compound according
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HRP20210775TT
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Craig Husfeld
John F. Donovan
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Concentric Analgesics, Inc.
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Publication of HRP20210775T1 publication Critical patent/HRP20210775T1/hr

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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/40Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings
    • C07C271/42Esters 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
    • C07C271/52Esters 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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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    • A61P19/00Drugs for skeletal disorders
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00Anaesthetics
    • A61P23/02Local anaesthetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/08Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/26Heterocyclic 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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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/16Heterocyclic 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
    • C07D295/18Heterocyclic 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
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/185Radicals derived from carboxylic acids from aliphatic carboxylic acids
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/16Heterocyclic 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
    • C07D295/18Heterocyclic 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
    • C07D295/195Radicals derived from nitrogen analogues of carboxylic acids

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Claims (15)

1. Spoj koji ima strukturu Formule (I): [image] naznačen time što: Y je: [image] [image] [image] X je -N(R5)-; n je cijeli broj od 1 do 10; Z je -NR3R4 ili -CO2H; R5 je vodik, supstituiran ili nesupstituiran alkil, ili supstituiran ili nesupstituiran aril, i svaki R1 i R2 je svaki neovisno vodik, supstituiran ili nesupstituiran alkil, supstituiran ili nesupstituiran aril, ili supstituiran ili nesupstituiran acil, ili dvije R1 ili R2 skupine na susjednim ugljikovim atomima, zajedno s atomima ugljika na koje su oni vezani, tvore supstituiranu ili nesupstituiranu cikloalkilnu skupinu, ili R1 i R5 skupine na susjednim atomima, zajedno s atomima na koje su oni vezani, tvore supstituiranu ili nesupstituiranu heterocikloalkilnu skupinu; i R3 i R4 je svaki neovisno vodik, supstituirani ili nesupstituirani alkil ili supstituirani ili nesupstituirani aril; ili njegova farmaceutski prihvatljiva sol, farmaceutski prihvatljiv solvat ili hidrat; pri čemu je supstituirana skupina supstituirana s jednom ili više skupina neovisno odabranih iz niza koji sadrži alkil, cikloalkil, aril, heteroaril, heterocikloalkil, -OH, alkoksi, ariloksi, alkiltio, ariltio, alkilsulfoksid, arilsulfoksid, alkilsulfon, arilsulfon, -CN, alkin, C1-C6alkilalkin, halo, acil, aciloksi, -CO2H, -CO2-alkil, nitro, haloalkil, fluoroalkil, fluoroalkoksi, i amino.
2. Spoj prema patentnom zahtjevu 1, naznačen time što Z je -NR3R4.
3. Spoj prema bilo kojem od patentnih zahtjeva 1-2, naznačen time što R3 je vodik i R4 je vodik ili supstituirani ili nesupstituirani alkil.
4. Spoj prema bilo kojem od patentnih zahtjeva 1-3, naznačen time što R1 i R5 skupine na susjednim atomima, zajedno s atomima na koje su one vezane, tvore supstituiranu ili nesupstituiranu heterocikloalkilnu skupinu.
5. Spoj prema patentnom zahtjevu 4, naznačen time što je heterocikloalkilna skupina supstituirani ili nesupstituirani pirolidinski prsten, supstituirani ili nesupstituirani piperidinski prsten, ili supstituirani ili nesupstituirani piperazinski prsten.
6. Spoj prema patentnom zahtjevu 4, naznačen time što je heterocikloalkilna skupina nesupstituirani pirolidinski prsten, nesupstituirani piperidinski prsten ili nesupstituirani piperazinski prsten.
7. Spoj prema patentnom zahtjevu 4, ili njegova farmaceutski prihvatljiva sol, farmaceutski prihvatljiv solvat ili hidrat, naznačen time što ima strukturu: [image]
8. Spoj prema patentnom zahtjevu 4, ili njegova farmaceutski prihvatljiva sol, farmaceutski prihvatljiv solvat ili hidrat, naznačen time što ima strukturu: [image]
9. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, farmaceutski prihvatljiv solvat ili hidrat, naznačen time što ima strukturu: [image]
10. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, farmaceutski prihvatljiv solvat ili hidrat, naznačen time što ima strukturu: [image]
11. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, farmaceutski prihvatljiv solvat ili hidrat, naznačen time što ima strukturu: [image]
12. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, farmaceutski prihvatljiv solvat ili hidrat, naznačen time što ima strukturu: [image] [image] [image] [image] [image] [image] ili [image]
13. Farmaceutski pripravak naznačen time što sadrži spoj, ili njegovu farmaceutski prihvatljivu sol, farmaceutski prihvatljiv solvat ili hidrat, prema bilo kojem od zahtjeva 1-12, i farmaceutski prihvatljiv razrjeđivač, pomoćnu tvar ili vezivo.
14. Spoj prema bilo kojem od patentnih zahtjeva 1-12, ili njegova farmaceutski prihvatljiva sol, farmaceutski prihvatljiv solvat ili hidrat, naznačen time što je za uporabu u postupku terapije.
15. Spoj prema bilo kojem od patentnih zahtjeva 1-12, ili njegova farmaceutski prihvatljiva sol, farmaceutski prihvatljiv solvat ili hidrat, naznačen time što je za uporabu u postupku liječenja boli.
HRP20210775TT 2014-11-25 2021-05-14 Predlijekovi fenolnih agonista trpv1 HRP20210775T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201462084515P 2014-11-25 2014-11-25
US14/743,375 US9359316B1 (en) 2014-11-25 2015-06-18 Prodrugs of phenolic TRPV1 agonists
PCT/US2015/062531 WO2016086063A1 (en) 2014-11-25 2015-11-24 Prodrugs of phenolic trpv1 agonists
EP15863380.0A EP3223805B1 (en) 2014-11-25 2015-11-24 Prodrugs of phenolic trpv1 agonists

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US (1) US9359316B1 (hr)
EP (2) EP3872063A1 (hr)
JP (2) JP6670841B2 (hr)
KR (1) KR102562571B1 (hr)
CN (1) CN107205961B (hr)
AR (1) AR102799A1 (hr)
AU (1) AU2015353532B2 (hr)
BR (1) BR112017010950B1 (hr)
CA (1) CA2968061C (hr)
CY (1) CY1124811T1 (hr)
DK (1) DK3223805T3 (hr)
EA (1) EA033619B1 (hr)
ES (1) ES2871095T3 (hr)
HK (1) HK1244672A1 (hr)
HR (1) HRP20210775T1 (hr)
HU (1) HUE054449T2 (hr)
IL (1) IL252307B (hr)
LT (1) LT3223805T (hr)
MX (1) MX2017006818A (hr)
PH (1) PH12017500974B1 (hr)
PL (1) PL3223805T3 (hr)
PT (1) PT3223805T (hr)
RS (1) RS61875B1 (hr)
SG (1) SG11201704290VA (hr)
SI (1) SI3223805T1 (hr)
TW (1) TWI692465B (hr)
WO (1) WO2016086063A1 (hr)
ZA (1) ZA201703409B (hr)

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
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
JP7100635B2 (ja) 2016-11-02 2022-07-13 セントレクシオン セラピューティクス コーポレイション 安定な水性カプサイシン注射製剤およびその医学的使用
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
CA3069540A1 (en) 2017-07-20 2019-01-24 Centrexion Therapeutics Corporation Methods and compositions for treatment of pain using capsaicin
WO2020023793A1 (en) * 2018-07-27 2020-01-30 Concentric Analgesics, Inc. Pegylated prodrugs of phenolic trpv1 agonists
EP3830078A4 (en) 2018-07-27 2022-03-30 Concentric Analgesics, Inc. PEGYLATED PRODRUGS OF PHENOLIC TRPV1 AGONISTS
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
WO2021063373A1 (zh) * 2019-09-30 2021-04-08 南京清普生物科技有限公司 一种trpv1激动剂及其制备方法和用途
US20240058316A1 (en) * 2020-12-14 2024-02-22 Concentric Analgesics, Inc. Prodrug of a phenolic trpv1 agonist for the treatment of pain
AR124337A1 (es) * 2020-12-14 2023-03-15 Concentric Analgesics Inc Formulaciones farmacéuticas de un profármaco fenólico agonista del trpv1

Family Cites Families (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US3598122A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
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
US5116817A (en) 1982-12-10 1992-05-26 Syntex (U.S.A.) Inc. LHRH preparations for intranasal administration
US4476116A (en) 1982-12-10 1984-10-09 Syntex (U.S.A.) Inc. Polypeptides/chelating agent nasal compositions having enhanced peptide absorption
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 Hydrogel-operated release devices
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
WO1992018106A1 (en) 1991-04-16 1992-10-29 Nippon Shinyaku Co., Ltd. Method of manufacturing solid 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
ATE195075T1 (de) 1991-11-22 2000-08-15 Procter & Gamble Pharma Risedronat enthaltende arzneimittel mit verzögerter wirkstoffabgabe
US5229135A (en) 1991-11-22 1993-07-20 Prographarm Laboratories Sustained release diltiazem formulation
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
JP2616252B2 (ja) 1992-10-16 1997-06-04 日本新薬株式会社 ワックスマトリックスの製法
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
KR19990014865A (ko) 1995-05-17 1999-02-25 피터 이. 브래이브맨 소장에서의 소화 및 흡수를 증진시키기 위한, 지방산을 함유한조성물들
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
ATE400252T1 (de) 1999-02-10 2008-07-15 Pfizer Prod Inc Pharmazeutische feste dispersionen
US6395300B1 (en) 1999-05-27 2002-05-28 Acusphere, Inc. Porous drug matrices and methods of manufacture thereof
AU2002219783A1 (en) * 2000-10-10 2002-04-22 Ortho-Mcneil Pharmaceutical, Inc. Labeled resiniferatoxin derivatives for use in vanilloid receptor binding assay
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
US20050020690A1 (en) 2002-12-18 2005-01-27 Algorx Infiltration of capsaicin into surgical sites and open wounds
EP1587506B1 (en) 2002-12-18 2008-07-23 Algorx Administration of capsaicinoids
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
CN101208294A (zh) * 2005-04-25 2008-06-25 纽罗吉斯克斯公司 Trpv1激动剂化合物以及制备和使用它们的方法
US7943666B2 (en) 2006-07-24 2011-05-17 Trinity Laboratories, Inc. Esters of capsaicin for treating pain
CA2689310A1 (en) 2007-05-30 2008-12-11 Brigham Young University Protein kinase-binding nucleosides and associated methods
US8535655B2 (en) 2008-10-10 2013-09-17 Polyactiva Pty Ltd. Biodegradable polymer—bioactive moiety conjugates
CA2739078C (en) * 2008-10-10 2017-01-03 The Bionic Ear Institute 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

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