CA3170070A1 - Charged ion channel blockers and methods for use - Google Patents

Charged ion channel blockers and methods for use Download PDF

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Publication number
CA3170070A1
CA3170070A1 CA3170070A CA3170070A CA3170070A1 CA 3170070 A1 CA3170070 A1 CA 3170070A1 CA 3170070 A CA3170070 A CA 3170070A CA 3170070 A CA3170070 A CA 3170070A CA 3170070 A1 CA3170070 A1 CA 3170070A1
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CA
Canada
Prior art keywords
compound
substituted
unsubstituted
hydrogen
methyl
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CA3170070A
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English (en)
French (fr)
Inventor
Bridget Mccarthy Cole
James Lamond ELLIS
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Nocion Therapeutics Inc
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Individual
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Filing date
Publication date
Priority claimed from US16/815,426 external-priority patent/US10968179B2/en
Application filed by Individual filed Critical Individual
Publication of CA3170070A1 publication Critical patent/CA3170070A1/en
Pending legal-status Critical Current

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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
    • C07D295/04—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P17/04—Antipruritics
    • 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
    • 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
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/14—Ectoparasiticides, e.g. scabicides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • C07D207/06—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 radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • 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
    • C07D211/10—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 radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/14—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 radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/06—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
    • C07D213/16—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom containing only one pyridine ring
    • C07D213/20—Quaternary compounds thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/04—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with only hydrogen atoms, halogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D225/00—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom
    • C07D225/02—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
    • C07D245/02—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/10—Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/22—Eight-membered rings
    • 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
    • C07D295/04—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Medicinal Preparation (AREA)
CA3170070A 2020-03-11 2021-03-10 Charged ion channel blockers and methods for use Pending CA3170070A1 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US16/815,426 2020-03-11
US16/815,426 US10968179B2 (en) 2019-03-11 2020-03-11 Charged ion channel blockers and methods for use
US17/197,508 US11332446B2 (en) 2020-03-11 2021-03-10 Charged ion channel blockers and methods for use
PCT/US2021/021697 WO2021183639A1 (en) 2020-03-11 2021-03-10 Charged ion channel blockers and methods for use

Publications (1)

Publication Number Publication Date
CA3170070A1 true CA3170070A1 (en) 2021-09-16

Family

ID=77664473

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3170070A Pending CA3170070A1 (en) 2020-03-11 2021-03-10 Charged ion channel blockers and methods for use

Country Status (11)

Country Link
US (1) US11332446B2 (https=)
EP (1) EP4118070A4 (https=)
JP (1) JP7708777B2 (https=)
KR (1) KR20230022830A (https=)
CN (2) CN119118953A (https=)
AU (1) AU2021236130A1 (https=)
BR (1) BR112022017801A2 (https=)
CA (1) CA3170070A1 (https=)
IL (1) IL295950A (https=)
MX (1) MX2022011194A (https=)
WO (1) WO2021183639A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2020235888A1 (en) 2019-03-11 2021-09-30 Nocion Therapeutics, Inc. Charged ION channel blockers and methods for use
US10933055B1 (en) * 2019-11-06 2021-03-02 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US12162851B2 (en) * 2020-03-11 2024-12-10 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
CN119487002A (zh) * 2022-05-03 2025-02-18 诺西恩医疗公司 用于治疗炎症性肠病的组合物和方法
US20260060989A1 (en) * 2024-03-06 2026-03-05 Nocion Therapeutics, Inc. Charged Ion Channel Blockers And Methods For Use

Family Cites Families (205)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE150423C (https=)
DE151036C (https=)
US1889645A (en) 1930-12-22 1932-11-29 Winthrop Chem Co Inc Beta-dimethylaminoethyl ester of para-butylamino-benzoic acid
US2441498A (en) 1943-07-15 1948-05-11 Astra Apotekarnes Kem Fab Alkyl glycinanilides
US2689248A (en) 1950-06-17 1954-09-14 Sterling Drug Inc Tertiary-aminoalkyl 4-amino-2-alkoxybenzoates and their synth esis
GB692332A (en) 1950-07-18 1953-06-03 Geigy Ag J R Improvements relating to quaternary ammonium compounds, and their uses
US2774770A (en) 1951-09-20 1956-12-18 Smith Kline French Lab Sulfur-containing amines
CH311610A (de) 1952-02-25 1955-11-30 Cilag Ag Verfahren zur Herstellung eines neuen basisch substituierten Fettsäure-(2-halogen-6-methyl-anilids).
CH311609A (de) 1952-02-25 1955-11-30 Cilag Ag Verfahren zur Herstellung eines neuen basisch substituierten Fettsäure-(2-halogen-6-methyl-anilids).
CH311612A (de) 1952-02-25 1955-11-30 Cilag Ag Verfahren zur Herstellung eines neuen basisch substituierten Fettsäure-(2-halogen-6-methyl-anilids).
CH311608A (de) 1952-02-25 1955-11-30 Cilag Ag Verfahren zur Herstellung eines neuen basisch substituierten Fettsäure-(2-halogen-6-methyl-anilids).
CH311611A (de) 1952-02-25 1955-11-30 Cilag Ag Verfahren zur Herstellung eines neuen basisch substituierten Fettsäure-(2-halogen-6-methyl-anilids).
CH311614A (de) 1952-02-25 1955-11-30 Cilag Ag Verfahren zur Herstellung eines neuen basisch substituierten Fettsäure-(2-halogen-6-methyl-anilids).
CH311606A (de) 1952-02-25 1955-11-30 Cilag Ag Verfahren zur Herstellung eines neuen basisch substituierten Fettsäure-(2-halogen-6-methyl-anilids).
CH311613A (de) 1952-02-25 1955-11-30 Cilag Ag Verfahren zur Herstellung eines neuen basisch substituierten Fettsäure-(2-halogen-6-methyl-anilids).
CH311607A (de) 1952-02-25 1955-11-30 Cilag Ag Verfahren zur Herstellung eines neuen basisch substituierten Fettsäure-(2-halogen-6-methyl-anilids).
CH311615A (de) 1952-02-25 1955-11-30 Cilag Ag Verfahren zur Herstellung eines neuen basisch substituierten Fettsäure-(2-halogen-6-methyl-anilids).
US2759975A (en) 1952-05-28 1956-08-21 Gen Aniline & Film Corp Mixed alkyl-benzyl-alkylol quaternary ammonium salts
US2783230A (en) 1953-03-16 1957-02-26 Hoffmann La Roche Derivatives of meta hydroxy aniline
GB751522A (en) 1953-03-16 1956-06-27 Roche Products Ltd Novel derivatives of úÝ-hydroxy-aniline and the manufacture thereof
GB756538A (en) 1953-12-24 1956-09-05 Bayer Ag Alkylation of aromatic amines
US2799679A (en) 1955-04-28 1957-07-16 Bofors Ab Process of preparing amides of heterocyclic carboxylic acids
US2955111A (en) 1957-01-28 1960-10-04 Bofors Ab Synthesis of n-alkyl-piperidine and n-alkyl-pyrrolidine-alpha-carboxylic acid amides
US3160662A (en) 1957-06-26 1964-12-08 Astra Apotekarnes Kem Fab Lower alkylaminoacyl amide anesthetics
GB895601A (en) 1957-11-20 1962-05-02 Sterling Drug Inc N[n-(monocarbocyclic aryl) carbamyl-lower-alkyl] amines and their preparation
DE1146872B (de) 1959-01-29 1963-04-11 Bayer Ag Verfahren zur Herstellung von organischen Isocyanaten
US3049546A (en) 1959-03-05 1962-08-14 Geigy Chem Corp Process for the decarbalkoxylation of alkyl esters of unsaturated, nitrogencontaining carboxylic acids
BE588558A (https=) * 1959-03-13 1960-09-12
US3264309A (en) 1959-08-24 1966-08-02 Sterling Drug Inc N' [nu-(monocarbocyclic aryl) carbamyllower-alkyl]-1, 5-iminocycloalkanes, -iminocycloalkenes and related compounds
US3080327A (en) 1959-11-20 1963-03-05 T & H Smith Ltd Quaternary salts as denaturants for organic substances
FR1549152A (https=) * 1961-06-09 1968-12-13
NL281394A (https=) 1961-07-25
DE1251764B (de) 1965-08-18 1967-10-12 C H Boehnnger Sohn Ingelheim/ Rhein Verfahren zur Herstellung von antimikrobiell wirksamen 12 3,4-Tetra hydro 9 -ammo acridmiumverbmdungen
GB1221061A (en) 1967-01-18 1971-02-03 May & Baker Ltd Quaternary ammonium derivatives, their use as anthelmintics and methods for their preparation
US3574216A (en) 1968-04-12 1971-04-06 American Home Prod Quaternary 3-pyridinium-2-quinolones
US3812147A (en) 1970-12-22 1974-05-21 Astra Pharma Prod Acylxylidide local anaesthetics
US3931195A (en) 1971-03-03 1976-01-06 Mead Johnson & Company Substituted piperidines
BE786875A (fr) 1971-07-28 1973-01-29 Astra Pharma Prod Amide, methode pour sa preparation et ses compositions therapeutiques
US3773939A (en) 1971-11-24 1973-11-20 Janssen Pharmaceutica Nv N-arallyl-n'-aralkyl piperazine pharmaceutical compositions
US4069309A (en) 1972-09-19 1978-01-17 Avon Products, Inc. Cationic skin substantive sunscreen composition and method
US3900481A (en) 1974-04-01 1975-08-19 Riker Laboratories Inc Derivatives of pyrrolidine and piperidine
US4005038A (en) 1974-04-15 1977-01-25 Peerless Paint And Varnish Corporation Paint composition containing denatonium benzoate or lignocaine benzyl octanoate with a latex resin binder for application over old paint films to prevent ingestion of poisons therefrom
CS195321B2 (en) 1975-12-23 1980-01-31 Ciba Geigy Ag Plant growth suppressing agents
BE849723A (fr) 1975-12-23 1977-06-22 Nouveaux regulateurs de la croissance des plantes, a base d'anilides d'acides ammonium quaternaire-alcanoiques
US4070347A (en) 1976-08-16 1978-01-24 Alza Corporation Poly(orthoester) co- and homopolymers and poly(orthocarbonate) co- and homopolymers having carbonyloxy functionality
US4147792A (en) 1977-02-04 1979-04-03 Ciba-Geigy Corporation Fungicidal compositions
DE2913523A1 (de) * 1979-04-04 1980-10-23 Basf Ag Substituierte alkylammoniumsalze, ihre herstellung und verwendung zur regulierung des pflanzenwachstums
DE2915250A1 (de) 1979-04-14 1980-10-30 Basf Ag Salze von alpha -aminoacetaniliden
US4293539A (en) 1979-09-12 1981-10-06 Eli Lilly And Company Controlled release formulations and method of treatment
DE2940765A1 (de) * 1979-10-08 1981-04-23 Basf Ag, 6700 Ludwigshafen Substituierte alkylammoniumsalze, ihre herstellung, ihre verwendung zur regulierung des pflanzenwachstums und mittel dafuer
US4877805A (en) 1985-07-26 1989-10-31 Kligman Albert M Methods for treatment of sundamaged human skin with retinoids
US5212183A (en) * 1981-11-14 1993-05-18 Basf Aktiengesellschaft 4-(p-tert.-butylphenyl)-3-methylpiperidines substituted at the nitrogen, their quaternary salts and their use as fungicides
US4757128A (en) 1986-08-01 1988-07-12 Massachusetts Institute Of Technology High molecular weight polyanhydride and preparation thereof
US5169637A (en) 1983-03-24 1992-12-08 The Liposome Company, Inc. Stable plurilamellar vesicles
DE3379266D1 (en) 1983-08-01 1989-04-06 Astra Laekemedel Ab L-n-n-propylpipecolic acid-2,6-xylidide and method for preparing the same
CA1237671A (en) 1983-08-01 1988-06-07 Michael W. Fountain Enhancement of pharmaceutical activity
US4975282A (en) 1985-06-26 1990-12-04 The Liposome Company, Inc. Multilamellar liposomes having improved trapping efficiencies
US5409704A (en) 1985-06-26 1995-04-25 The Liposome Company, Inc. Liposomes comprising aminoglycoside phosphates and methods of production and use
US5023087A (en) 1986-02-10 1991-06-11 Liposome Technology, Inc. Efficient method for preparation of prolonged release liposome-based drug delivery system
IE60901B1 (en) 1986-08-21 1994-08-24 Vestar Inc Improved treatment of systemic fungal infections with phospholipid particles encapsulating polyene antifungal antibiotics
US5049388A (en) 1986-11-06 1991-09-17 Research Development Foundation Small particle aerosol liposome and liposome-drug combinations for medical use
US5032582A (en) 1987-02-27 1991-07-16 Liposome Technology, Inc. Method for treating fungal infections with amphotericin B/cholesterol sulfate composition
GB8727504D0 (en) 1987-11-24 1987-12-23 Glaxo Group Ltd Chemical compositions
US4994213A (en) 1988-05-17 1991-02-19 Liposome Technology, Inc. Method of preparing lipid structures
US5082866A (en) 1988-06-01 1992-01-21 Odontex, Inc. Biodegradable absorption enhancers
US4980378A (en) 1988-06-01 1990-12-25 Odontex, Inc. Biodegradable absorption enhancers
US5194581A (en) 1989-03-09 1993-03-16 Leong Kam W Biodegradable poly(phosphoesters)
US5194266A (en) 1989-08-08 1993-03-16 Liposome Technology, Inc. Amphotericin B/cholesterol sulfate composition and method
US5356633A (en) 1989-10-20 1994-10-18 Liposome Technology, Inc. Method of treatment of inflamed tissues
AU657961B2 (en) 1991-04-19 1995-03-30 Nexstar Pharmaceuticals, Inc. Pharmaceutical formulation and process
US5176907A (en) 1991-08-13 1993-01-05 The Johns Hopkins University School Of Medicine Biocompatible and biodegradable poly (phosphoester-urethanes)
GR1002207B (en) 1992-08-06 1996-03-27 Johnson & Johnson Consumer Skin care compositions containing imidazoles.
US5552155A (en) 1992-12-04 1996-09-03 The Liposome Company, Inc. Fusogenic lipsomes and methods for making and using same
US5480971A (en) 1993-06-17 1996-01-02 Houghten Pharmaceuticals, Inc. Peralkylated oligopeptide mixtures
US5409805A (en) 1993-07-29 1995-04-25 Konica Corporation Solid processing agent for silver halide photographic light-sensitive materials
US6051576A (en) 1994-01-28 2000-04-18 University Of Kentucky Research Foundation Means to achieve sustained release of synergistic drugs by conjugation
US5591317A (en) 1994-02-16 1997-01-07 Pitts, Jr.; M. Michael Electrostatic device for water treatment
US5716622A (en) 1995-01-06 1998-02-10 The Rockefeller University Functionally active regions of signal transducer and activators of transcription
US5783683A (en) 1995-01-10 1998-07-21 Genta Inc. Antisense oligonucleotides which reduce expression of the FGFRI gene
AU5938996A (en) 1995-06-07 1996-12-30 Nexstar Pharmaceuticals, Inc. Method for encapsulating pharmaceutical materials
US5747470A (en) 1995-06-07 1998-05-05 Gen-Probe Incorporated Method for inhibiting cellular proliferation using antisense oligonucleotides to gp130 mRNA
WO1997004770A1 (en) 1995-07-31 1997-02-13 Merck & Co., Inc. 2-(fluorenonyl)-carbapenems, compositions and methods of use
US6413961B1 (en) 1995-12-12 2002-07-02 Omeros Medical Systems, Inc. Irrigation solution and method for inhibition of pain and inflammation
SE508357C2 (sv) 1996-01-02 1998-09-28 Kay Laserow Mätinstrument för mätning av smärta jämte ett förfarande för att med ett mätinstrument mäta smärta
WO1998024428A1 (en) 1996-12-02 1998-06-11 Brigham & Women's Hospital, Inc. Long-acting local anesthetics
SE9604751D0 (sv) 1996-12-20 1996-12-20 Astra Ab New therapy
US5837713A (en) 1997-02-26 1998-11-17 Mayo Foundation For Medical Education And Research Treatment of eosinophil-associated pathologies by administration of topical anesthetics and glucocorticoids
US6008318A (en) 1997-06-18 1999-12-28 Guilford Pharmaceuticals Inc. Two-stage solution polymerization of high molecular weight poly(phosphoesters)
RU2105554C1 (ru) 1997-06-24 1998-02-27 Всероссийский научный центр по безопасности биологически активных веществ N-(2,4,6-триметилфенилкарбамоилметил)-n-аллилморфолиний бромид, проявляющий противоишемическое и антиаритмическое действие при ишемической болезни сердца и способ его получения
US6028163A (en) 1997-06-27 2000-02-22 Guilford Pharmaceuticals Inc. Solution polymerization of high molecular weight poly(phosphoesters) in toluene
AU7937298A (en) 1997-07-08 1999-02-08 Ono Pharmaceutical Co. Ltd. Amino acid derivatives
US6623040B1 (en) 1997-09-03 2003-09-23 Recot, Inc. Method for determining forced choice consumer preferences by hedonic testing
TW536401B (en) 1997-09-03 2003-06-11 Cardiome Pharma Corp A pharmaceutical composition of N,N-bis(phenylcarbamoylmethyl)dimethylammomum chloride and derivatives for the treatment of pain
US5891919A (en) 1997-09-19 1999-04-06 Burlington Bio-Medical & Scientific Corp. Denatonium capsaicinate and methods of producing the same
US6083996A (en) 1997-11-05 2000-07-04 Nexmed Holdings, Inc. Topical compositions for NSAI drug delivery
US6140351A (en) 1997-12-19 2000-10-31 Berlex Laboratories, Inc. Ortho-anthranilamide derivatives as anti-coagulants
US6207290B1 (en) 1998-04-07 2001-03-27 Burlington Bio-Medical & Scientific Corp. Antifoulant compositions and methods of treating wood
BR9911094A (pt) 1998-06-09 2001-10-30 Nortran Pharmaceuticals Inc Composições e métodos para o tratamento detosse
JP2000143635A (ja) 1998-06-10 2000-05-26 Takeda Chem Ind Ltd 血管新生阻害剤
US6153212A (en) 1998-10-02 2000-11-28 Guilford Pharmaceuticals Inc. Biodegradable terephthalate polyester-poly (phosphonate) compositions, articles, and methods of using the same
US7507545B2 (en) 1999-03-31 2009-03-24 Cardiome Pharma Corp. Ion channel modulating activity method
US6103255A (en) 1999-04-16 2000-08-15 Rutgers, The State University Porous polymer scaffolds for tissue engineering
US6118020A (en) 1999-05-19 2000-09-12 Nexmed Holdings, Inc. Crystalline salts of dodecyl 2-(N,N-dimethylamino)-propionate
US6355637B1 (en) 1999-10-01 2002-03-12 Advanced Medicine, Inc. Local anesthetic compounds
HUP0204014A3 (en) 1999-12-15 2005-04-28 Ucb Farchim Sa Quaternary salts of-n-substituted cyclic or acyclic amines and their use as pharmaceutical compositions
CZ20022095A3 (cs) 1999-12-15 2003-02-12 Ucb Farchim S. A. Cyklická kvarterní amoniová sloučenina pro použití při léčbě a/nebo prevenci kašle u teplokrevného živočicha a farmaceutický prostředek ji obsahující
WO2001045678A2 (de) 1999-12-21 2001-06-28 Id Pharma Gmbh Arzneimittel, verfahren zu dessen herstellung und dessen verwendung
WO2001083828A1 (en) 2000-05-04 2001-11-08 Dzgenes, Llc TGFβ-RII PROMOTER POLYMORPHISMS
IL153574A0 (en) 2000-06-23 2003-07-06 Mayo Foundation Methods of treating neutrophil-related diseases with topical anesthetics
DE10039449A1 (de) 2000-08-11 2003-07-24 Id Pharma Gmbh I Ins Verwendung einer lokalanästhetikumhaltigen Zusammensetzung zur Behandlung von Hyperalgesien
US20040067938A1 (en) 2000-09-29 2004-04-08 Penglie Zhang Quaternary amines and related inhibitors of factor xa
US6766319B1 (en) 2000-10-31 2004-07-20 Robert J. Might Method and apparatus for gathering and evaluating information
US6884782B2 (en) 2000-11-08 2005-04-26 Amgen Inc. STAT modulators
US20030152637A1 (en) 2001-01-25 2003-08-14 Mark Chasin Local anesthetic, and method of use
US20040146590A1 (en) 2001-03-22 2004-07-29 Iadarola Michael J Molecular neurochirurgie for pain control administering locally capsaicin or resinferatoxin
CA2446060A1 (en) 2001-05-07 2002-11-14 Corium International Compositions and delivery systems for administration of a local anesthetic agent
CA2450769A1 (en) 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
US7157103B2 (en) 2001-08-06 2007-01-02 Euro-Celtique S.A. Pharmaceutical formulation containing irritant
US20030068276A1 (en) 2001-09-17 2003-04-10 Lyn Hughes Dosage forms
ITMI20012025A1 (it) 2001-09-28 2003-03-28 Dompe Spa Sali di ammonio quaternari di omega-amminoalchilammidi di acidi r 2-aril-propionici e composizioni farmaceutiche che li contengono
US7585511B2 (en) 2002-08-02 2009-09-08 Universite Libre De Bruxelles Apolipoprotein L-I and/or derivated polypeptide for the treatment of and/or the prevention of diseases induced by trypanosoma
US7622592B2 (en) 2002-11-01 2009-11-24 Merck & Co., Inc. Carbonylamino-benzimidazole derivatives as androgen receptor modulators
ES2535045T3 (es) 2003-04-10 2015-05-04 Vanderbilt Royalty Sub L.P. Usos y composiciones para administración de capsaicina
US20040220187A1 (en) 2003-04-22 2004-11-04 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a sodium ion channel blocker for the treatment of pain, inflammation or inflammation mediated disorders
ES2223277B1 (es) 2003-06-19 2006-03-01 Fernando Bouffard Fita Composicion anestesica para administracion topica.
PE20050231A1 (es) 2003-06-24 2005-05-20 Novartis Ag Derivados de piperidinium y pirrolidinium como antagonistas del receptor muscarinico m3
WO2005014849A2 (en) 2003-07-03 2005-02-17 Euro-Celtique, S.A. Genes associated with responses to neuropathic pain
US8361467B2 (en) 2003-07-30 2013-01-29 Depuy Spine, Inc. Trans-capsular administration of high specificity cytokine inhibitors into orthopedic joints
NO20034069L (no) 2003-09-12 2005-03-14 Aximed As Fremstilling og bruk av capsaicinderivater
US20070149469A1 (en) 2003-10-02 2007-06-28 Christian Korherr Medical use of tbk-1 or of inhibitors thereof
US20050142596A1 (en) 2003-11-14 2005-06-30 Krolewski Andrzej S. Methods of diagnosing renal and cardiovascular disease
MXPA06006460A (es) 2003-12-11 2006-08-23 Univ Texas Compuestos para el tratamiento de enfermedades proliferativas celulares.
WO2005089206A2 (en) 2004-03-13 2005-09-29 Irm Llc Modulators of ion channel trpa1
US7161034B2 (en) 2004-04-20 2007-01-09 Dade Behring Inc. Lidocaine analogs and methods of making and using same
US20060106020A1 (en) 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
JP5148271B2 (ja) 2004-06-02 2013-02-20 ニューロジズエックス，インコーポレーテッド 疼痛処置のためのカプサイシノイド、局所麻酔薬および／または鎮痒薬を含有する処方物
RU2258700C1 (ru) 2004-06-28 2005-08-20 Государственное образовательное учреждение высшего профессионального образования "Мордовский государственный университет им. Н.П. Огарева" Четвертичное аммониевое производное лидокаина, обладающее противоаритмической активностью и способ его получения
ES2651021T3 (es) 2004-07-24 2018-01-23 Laboratorios Del Dr. Esteve, S.A. Uso de compuestos activos sobre el receptor sigma para el tratamiento de alodinia mecánica
ITMI20041566A1 (it) 2004-07-30 2004-10-30 Indena Spa "trpv1 agonisti, formulazioni che li contengono e loro usi"
JP2008513445A (ja) 2004-09-20 2008-05-01 コラス ファーマ インコーポレイテッド 吸入による送達で治療効果のある薬剤の許容性の改善方法
US7947682B2 (en) 2004-12-29 2011-05-24 University Of Southern California Substituted N′-pyrrolo[1,2-a]quinoxalin-4-yl-hydrazides as anti-cancer agents
US20090306429A1 (en) 2004-12-06 2009-12-10 Henk Pluim Preparation of a quaternary ammonium hydroxide and use thereof for the preparation of a quaternary ammonium salt
US20060134008A1 (en) 2004-12-16 2006-06-22 Daniel Deaver Compositions and methods for pulmonary conditions
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
GB0428418D0 (en) * 2004-12-24 2005-02-02 Novartis Ag Organic compounds
WO2006133588A1 (en) 2005-06-13 2006-12-21 Oncalis Ag ARYL UREA COMPOUNDS AS β-SECRETASE INHIBITORS
GB0516313D0 (en) * 2005-08-08 2005-09-14 Argenta Discovery Ltd Azole derivatives and their uses
GB0517966D0 (en) 2005-09-02 2005-10-12 Novartis Ag Organic compounds
CA2621261C (en) 2005-09-22 2014-05-20 Incyte Corporation Azepine inhibitors of janus kinases
EP2982679A1 (en) 2005-10-12 2016-02-10 Idera Pharmaceuticals, Inc. Immune regulatory oligonucleotide (iro) compounds to modulate toll-like receptor based immune response
SG10202003901UA (en) 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
KR20080089416A (ko) 2005-12-21 2008-10-06 페인셉터 파마 코포레이션 개폐 이온 통로를 조절하기 위한 조성물 및 방법
GB0526244D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
EP1867338A1 (en) 2006-05-30 2007-12-19 Université Libre De Bruxelles Pharmaceutical composition comprising apolipoproteins for the treatment of human diseases
AU2007322033B2 (en) 2006-11-20 2013-07-11 President And Fellows Of Harvard College Methods, compositions, and kits for treating pain and pruritis
CA2673038C (en) 2006-12-22 2015-12-15 Incyte Corporation Substituted tricyclic heteroaryl compounds as janus kinase inhibitors
GB0702382D0 (en) 2007-02-07 2007-03-21 Argenta Discovery Ltd New salt
EP1995241B1 (en) 2007-03-23 2010-03-17 ICAgen, Inc. Inhibitors of ion channels
ES2609912T3 (es) 2007-06-22 2017-04-25 Hydra Biosciences, Inc. Compuestos de 2,6-dioxo, -2,3-dihidro-1h-purina útiles para el tratamiento de trastornos relacionados con la actividad del canal trpa1
WO2009026107A1 (en) 2007-08-17 2009-02-26 Portola Pharmaceuticals, Inc. Protein kinase inhibitors
CN101156851A (zh) 2007-09-27 2008-04-09 刘全胜 盐酸尼卡地平分散片及其制备方法
EP2271329A4 (en) 2008-03-11 2013-01-09 Harvard College METHOD, COMPOSITIONS AND SETS FOR TREATING PAIN AND PRURITIS
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
AU2009238590A1 (en) 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
US20120108614A1 (en) 2008-05-14 2012-05-03 Chong Jayhong A Compounds and compositions for treating chemical warfare agent-induced injuries
AU2009268841B2 (en) 2008-07-08 2014-02-06 Board Of Regents, The University Of Texas System Novel inhibitors of proliferation and activation of signal transducer and activator of transcription (STATS)
DE102008037682A1 (de) 2008-08-14 2010-04-08 Strackharn, Klaus, Dr.med. Verwendung äquipotenter Dosierungen von Lokalanästetika oder Derivaten davon zur Therapie chronischer Schmerzen
CN101347427A (zh) 2008-09-22 2009-01-21 北京理工大学 一种沙坦化合物或其可药用盐和钙通道阻断剂或可药用盐的复方
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
WO2010042543A2 (en) 2008-10-06 2010-04-15 Idera Pharmaceuticals, Inc. Use of inhibitors of toll-like receptors in the prevention and treatment of hypercholesterolemia and hyperlipidemia and diseases related thereto
WO2010111471A2 (en) 2009-03-27 2010-09-30 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF SIGNAL TRANSDUCER AND ACTIVATOR OF TRANSCRIPTION 1 (STAT1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
JP6205133B2 (ja) * 2009-07-10 2017-09-27 プレジデント アンド フェローズ オブ ハーバード カレッジ 抗炎症剤としての恒久的に荷電したナトリウムおよびカルシウムチャンネルブロッカー
US9023355B2 (en) 2010-04-13 2015-05-05 Beth Israel Deaconess Medical Center, Inc. Compositions and methods for treating renal disease
WO2011133474A2 (en) 2010-04-18 2011-10-27 Beth Israel Deaconess Medical Center Methods of predicting predisposition to or risk of kidney disease
EP2611448A1 (en) 2010-09-01 2013-07-10 Ambit Biosciences Corporation 7-cyclylquinazoline derivatives and methods of use thereof
KR101923367B1 (ko) 2011-02-02 2018-12-04 버텍스 파마슈티칼스 인코포레이티드 이온 채널의 조절제로서의 피롤로피라진―스피로사이클릭 피페리딘 아미드
WO2013064884A1 (en) 2011-10-31 2013-05-10 Purdue Pharma L.P. Quaternized amines as sodium channel blockers
WO2013130808A1 (en) 2012-02-29 2013-09-06 D.E. Shaw Research, Llc Methods for screening voltage gated proteins
CA3132310C (en) 2012-08-07 2024-01-09 Children's Medical Center Corporation Potassium channel openers for treating neurodegenerative diseases
WO2014044849A1 (en) 2012-09-24 2014-03-27 Boehringer Ingelheim International Gmbh Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof
US8822537B2 (en) 2012-09-27 2014-09-02 Achelios Therapeutics, Inc. Topical ketoprofen composition
LV15002B (lv) 2013-10-29 2015-07-20 Latvijas Organiskās Sintēzes Institūts Heterociklā aizvietoti [(2-karboksi vai -metoksikarbonil)fenilkarbamoil-metil (vai trimetilēn)] piridīnija vai izohinolīnija bromīdi kā hidroksikarbonskābju receptoru saimes (HCA2) jauna ligandu klase
CN105566148B (zh) 2014-10-14 2017-10-03 沈阳中化农药化工研发有限公司 一种季铵盐类化合物及其应用
CA2977387C (en) 2015-03-04 2020-04-28 The Procter & Gamble Company Fibrous elements, fibrous structures, and products comprising a deterrent agent and methods for making same
WO2016198472A1 (en) * 2015-06-09 2016-12-15 Hpf Ip Holding S.A. Topical delivery system
CN106310289B (zh) 2015-06-24 2020-10-13 天津键凯科技有限公司 一种聚乙二醇和麻醉药的结合物及其制备方法
KR20180069782A (ko) 2015-08-03 2018-06-25 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 하전 이온 채널 블록커 및 이용 방법
TWI721016B (zh) * 2015-09-15 2021-03-11 美商艾森伯利生物科學公司 B型肝炎核心蛋白質調節劑
US20170258774A1 (en) 2016-03-14 2017-09-14 Mississippi State University Novel oximes for reactivating butyrylcholinesterase
DE102016009766A1 (de) 2016-08-11 2018-02-15 Julius-Maximilians-Universität Würzburg Herstellung von Bitterstoffderivaten
CN109843286A (zh) * 2016-08-23 2019-06-04 纽里姆药物有限公司 治疗瘙痒和/或搔痒的方法
JOP20190245A1 (ar) 2017-04-20 2019-10-15 Novartis Ag أنظمة توصيل إطلاق مستدام تتضمن روابط بلا أثر لنقطة الربط
CN108929263B (zh) 2017-05-26 2022-07-22 中国医学科学院药物研究所 芳酰胺类Kv2.1抑制剂及其制备方法、药物组合物和用途
AU2019251359B2 (en) * 2018-04-10 2024-06-13 The Board Of Trustees Of The University Of Illinois FOXM1 inhibitor compositions and methods of using the same
US10835505B2 (en) 2018-06-11 2020-11-17 Aardvark Therapeutics, Inc. Oral pharmaceutical formulation for weight loss, diabetes and related disorders
WO2020064175A1 (en) * 2018-09-25 2020-04-02 Antabio Sas Indane derivatives for use in the treatment of bacterial infection
AU2020235888A1 (en) 2019-03-11 2021-09-30 Nocion Therapeutics, Inc. Charged ION channel blockers and methods for use
US10828287B2 (en) 2019-03-11 2020-11-10 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US10780083B1 (en) 2019-03-11 2020-09-22 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
MX2021010869A (es) 2019-03-11 2022-01-19 Nocion Therapeutics Inc Bloqueadores de canales iónicos sustituidos por éster y métodos para su uso.
US10934263B2 (en) 2019-03-11 2021-03-02 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US10933055B1 (en) 2019-11-06 2021-03-02 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
CN114828845A (zh) 2019-11-06 2022-07-29 诺西恩医疗公司 带电的离子通道阻滞剂及其使用方法
EP4054336A4 (en) 2019-11-06 2024-01-10 Nocion Therapeutics, Inc. PHOSPHONIUM ION CHANNEL BLOCKERS AND METHODS OF USE
CA3155578A1 (en) 2019-11-06 2021-05-14 Bridget Mccarthy Cole Phosphonium ion channel blockers and methods for use

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