BR112013017296A2 - Composto e composição compreendendo oxicodona, método para reduzir o abuso potencial da referida composição, unidade de dose e método para a sua preparação, e método para identificar um composto e um inibidor de tripsina - Google Patents

Composto e composição compreendendo oxicodona, método para reduzir o abuso potencial da referida composição, unidade de dose e método para a sua preparação, e método para identificar um composto e um inibidor de tripsina

Info

Publication number
BR112013017296A2
BR112013017296A2 BR112013017296A BR112013017296A BR112013017296A2 BR 112013017296 A2 BR112013017296 A2 BR 112013017296A2 BR 112013017296 A BR112013017296 A BR 112013017296A BR 112013017296 A BR112013017296 A BR 112013017296A BR 112013017296 A2 BR112013017296 A2 BR 112013017296A2
Authority
BR
Brazil
Prior art keywords
compound
composition
trypsin
oxicodone
inhibtor
Prior art date
Application number
BR112013017296A
Other languages
English (en)
Other versions
BR112013017296B1 (pt
Inventor
E Jenkins Thomas
O Husfeld Craig
Original Assignee
Signature Therapeutics 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 Signature Therapeutics Inc filed Critical Signature Therapeutics Inc
Publication of BR112013017296A2 publication Critical patent/BR112013017296A2/pt
Publication of BR112013017296B1 publication Critical patent/BR112013017296B1/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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
    • A61K31/245—Amino benzoic acid types, e.g. procaine, novocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05—Dipeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/06—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
    • C07D489/08—Oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0815—Tripeptides with the first amino acid being basic
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/37—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Wood Science & Technology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

COMPOSTO E COMPOSIÇÃO COMPREENDENDO OXICODONA, MÉTODO PARA REDUZIR O ABUSO POTENCIAL DA REFERIDA COMPOSIÇÃO, UNIDADE DE DOSE E MÉTODO PARA A SUA PREPARAÇÃO, E MÉTODO PARA IDENTIFICAR UM COMPOSTO E UM INIBIDOR DE TRIPSINA. A presente invenção refere-se às modalidades que proveem o Composto KC-8, ácido N-1 -[3-(oxicodona-6-enol-carbonil-metil-amino)-2,2-dimetil-propilamina]-arginina-glicina malônico, ou sais, solvatos, e hidratos aceitáveis dos mesmos. A presente divulgação provê também composições, e seus métodos de utilização, em que as composições compreendem um profármaco, o Composto KC-8, que fornece liberação controlada de oxicodona. Essas composições podem opcionalmente prover um inibidor da tripsina que interage com a enzima que medeia a liberação controlada de oxicodona do profármaco de modo a atenuar a clivagem enzimática do profármaco.
BR112013017296-7A 2011-01-11 2012-01-09 composto e composição compreendendo oxicodona, método para reduzir o abuso potencial da referida composição, unidade de dose e método para a sua preparação, e método para identificar um composto e um inibidor de tripsina BR112013017296B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161431781P 2011-01-11 2011-01-11
US61/431,781 2011-01-11
PCT/US2012/020649 WO2012096887A2 (en) 2011-01-11 2012-01-09 Compositions comprising enzyme-cleavable oxycodone prodrug

Publications (2)

Publication Number Publication Date
BR112013017296A2 true BR112013017296A2 (pt) 2017-09-05
BR112013017296B1 BR112013017296B1 (pt) 2021-02-17

Family

ID=46455749

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112013017296-7A BR112013017296B1 (pt) 2011-01-11 2012-01-09 composto e composição compreendendo oxicodona, método para reduzir o abuso potencial da referida composição, unidade de dose e método para a sua preparação, e método para identificar um composto e um inibidor de tripsina

Country Status (14)

Country Link
US (3) US8569228B2 (pt)
EP (1) EP2663187B1 (pt)
JP (1) JP6016810B2 (pt)
CN (1) CN103384472B (pt)
AU (1) AU2012205733B2 (pt)
BR (1) BR112013017296B1 (pt)
CA (1) CA2814763C (pt)
DK (1) DK2663187T3 (pt)
ES (1) ES2584634T3 (pt)
HK (1) HK1189763A1 (pt)
IL (1) IL225904B (pt)
RU (1) RU2609412C2 (pt)
TW (1) TWI526209B (pt)
WO (1) WO2012096887A2 (pt)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI1765292T1 (en) 2004-06-12 2018-04-30 Collegium Pharmaceutical, Inc. Formulations of medicines to discourage abuse
UA102916C2 (uk) 2009-07-02 2013-08-27 Кемфарм, Інк. Композиція на основі кон'югату гідрокодону з бензойною кислотою, похідними бензойної кислоти або гетероарилкарбоновою кислотою, проліки, спосіб лікування від зловживань
CA2773340C (en) 2009-09-08 2019-07-23 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof
US10668060B2 (en) 2009-12-10 2020-06-02 Collegium Pharmaceutical, Inc. Tamper-resistant pharmaceutical compositions of opioids and other drugs
US20110262355A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
US20110262359A1 (en) * 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable prodrugs of active agents and inhibitors thereof
ES2710617T3 (es) 2010-04-21 2019-04-26 Signature Therapeutics Inc Composiciones que comprenden profármacos de anfetamina escindibles enzimáticamente e inhibidores de los mismos
RU2609412C2 (ru) * 2011-01-11 2017-02-01 Сигничер Терапьютикс, Инк. Композиции, содержащие расщепляемое ферментами пролекарство оксикодона
WO2012122420A2 (en) 2011-03-09 2012-09-13 Pharmacofore, Inc. Opioid prodrugs with heterocyclic linkers
EP2683394B1 (en) 2011-03-09 2021-01-06 Signature Therapeutics, Inc. Active agent prodrugs with heterocyclic linkers
WO2015081891A1 (en) 2013-12-06 2015-06-11 Baikang (Suzhou) Co., Ltd Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs
JP6400848B2 (ja) 2014-11-25 2018-10-03 ケムファーム・インコーポレーテッド オキシコドンの安息香酸、安息香酸誘導体及びヘテロアリールカルボン酸結合体
US11634384B2 (en) 2014-11-25 2023-04-25 Concentric Analgesics, Inc. Prodrugs of phenolic TRPV1 agonists
US10335406B2 (en) 2015-10-01 2019-07-02 Elysium Therapeutics, Inc. Opioid compositions resistant to overdose and abuse
JP2018534269A (ja) 2015-10-01 2018-11-22 エリージウム セラピューティクス， インコーポレイテッド 過剰摂取および乱用に抵抗性のポリサブユニットオピオイドプロドラッグ
EP3210630A1 (en) 2016-02-29 2017-08-30 G.L. Pharma GmbH Abuse-deterrent pharmaceutical compositions
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
WO2017222575A1 (en) 2016-06-23 2017-12-28 Collegium Pharmaceutical, Inc. Process of making more stable abuse-deterrent oral formulations
US11541125B2 (en) 2016-12-19 2023-01-03 The Regents Of The University Of California Noncrushable pill formulations
WO2018118902A1 (en) 2016-12-19 2018-06-28 The Regents Of The University Of California Dual-enzyme responsive peptides
AU2018234911B2 (en) * 2017-03-17 2024-04-18 Elysium Therapeutics, Inc. Polysubunit opioid prodrugs resistant to overdose and abuse
EP3749697A4 (en) 2018-02-05 2021-11-03 Bio-Rad Laboratories, Inc. CHROMATOGRAPHIC RESIN WITH A LIGAND WITH ANION EXCHANGE-HYDROPHOBIC MIXED MODE
CN113166051A (zh) 2018-07-27 2021-07-23 同心镇痛药物公司 酚类trpv1激动剂的聚乙二醇化前药

Family Cites Families (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU527371B2 (en) 1980-09-16 1983-03-03 Torii & Co., Ltd. Amidine
US5109118A (en) 1989-07-06 1992-04-28 Yutaka Mizushima Modified biologically active proteins
US5217987A (en) 1989-10-30 1993-06-08 Berger Stephen P Dopamine uptake inhibitors in reducing substance abuse and/or craving
CA2032420A1 (en) 1989-12-22 1991-06-23 Akira Okuyama Guanidinobenzene derivatives
US6692766B1 (en) 1994-06-15 2004-02-17 Yissum Research Development Company Of The Hebrew University Of Jerusalem Controlled release oral drug delivery system
US6388122B1 (en) 1996-04-10 2002-05-14 Ono Pharmaceutical Co., Ltd. Tryptase inhibitor and novel guanidino derivatives
ATE234090T1 (de) 1998-11-13 2003-03-15 Lilly Co Eli Kombination von duloxetin mit nichtsteroid- entzündungshemmern für die behandlung von schmerz
WO2000036098A1 (en) 1998-12-15 2000-06-22 Tropix, Inc. Multiple enzyme assays
US6849263B2 (en) 1998-12-21 2005-02-01 Generex Pharmaceutical Incorporated Pharmaceutical compositions for buccal delivery of pain relief medications
DE60011053T2 (de) 1999-02-18 2005-05-25 SuperGen, Inc., Dublin An phosphocholin gebundene prodrug-derivate
US7060708B2 (en) 1999-03-10 2006-06-13 New River Pharmaceuticals Inc. Active agent delivery systems and methods for protecting and administering active agents
CN1407884B (zh) * 1999-10-29 2012-06-20 欧罗赛铁克股份有限公司 控释氢可酮制剂
US20030180352A1 (en) 1999-11-23 2003-09-25 Patel Mahesh V. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
US6673574B2 (en) 2000-11-30 2004-01-06 Unigene Laboratories Inc. Oral delivery of peptides using enzyme-cleavable membrane translocators
DE60239679D1 (de) 2001-06-11 2011-05-19 Medarex Inc Methode für die ausarbeitung von cd10-aktivierten prodrug-verbindungen
US7169752B2 (en) 2003-09-30 2007-01-30 New River Pharmaceuticals Inc. Compounds and compositions for prevention of overdose of oxycodone
US7375082B2 (en) 2002-02-22 2008-05-20 Shire Llc Abuse-resistant hydrocodone compounds
EP1531844B1 (en) 2002-02-22 2014-08-20 Shire LLC Novel sustained release pharmaceutical compounds to prevent abuse of controlled substances
US20100092562A1 (en) 2002-11-26 2010-04-15 Hollenbeck R Gary Sustained-release drug delivery compositions and methods
US7230005B2 (en) * 2003-03-13 2007-06-12 Controlled Chemicals, Inc. Compounds and methods for lowering the abuse potential and extending the duration of action of a drug
EP1782834A3 (en) * 2003-03-13 2007-08-01 Controlled Chemicals, Inc. Oxycodone conjugates with lower abuse potential and extended duration of action
ATE545427T2 (de) 2003-05-29 2012-03-15 Shire Llc Gegen missbrauch geschützte amphetamin- verbindungen
KR100915284B1 (ko) 2003-09-30 2009-09-03 샤이어 엘엘씨 과용 또는 남용을 예방하기 위한 제약 조성물
AU2004286238A1 (en) 2003-10-24 2005-05-12 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds
US8163701B2 (en) * 2005-08-19 2012-04-24 Signature Therapeutics, Inc. Prodrugs of active agents
JP5276982B2 (ja) 2005-08-26 2013-08-28 ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティ オキシトシンの投与による頭痛の処置のための方法
BRPI0617987A2 (pt) 2005-10-06 2011-08-16 Auspex Pharmaceuticals Inc composição, composição farmacêutica, forma de dosagem efervescente, composição farmacêutica oral de comprimidos unitários múltiplos, forma de dosagem farmacêutica de liberação prolongada, forma de dosagem farmacêutica revestida entérica, forma de dosagem farmacêutica estável para administração oral a sujeitos mamìferos, método para tratamento de doenças relacionadas a ácido gástrico pela inibição de secreção de ácido gástrico, método para tratamento de uma infecção bacteriana provocada ou mediada por helicobacter pylori, processo para preparar um composto da fórmula 3, processo para preparar um composto da fórmula 5, uso de um composto da fórmula 1 para a preparação de um medicamento para tratamento de doenças relacionadas a ácido gástrico, pela inibição de secreção de ácido gástrico, uso de um composto da fórmula 1 para a preparação de um medicamento para tratamento de uma infecção bacteriana provocada ou mediada por helicobacter pylori uso de um composto da fórmula 1 para a preparação de um medicamento para tratamento de doenças relecionadas a ácido gástrico pela inibição de secreção de ácido gástrico
DK1959948T3 (da) 2005-12-05 2012-08-20 Xenoport Inc Levodopa prodrug-mesylat, sammensætninger deraf og anvendelser deraf
AU2007238858A1 (en) 2006-04-10 2007-10-25 Shire Llc Mono and di-substituted oxycodone compounds and compositions
WO2007120864A2 (en) 2006-04-14 2007-10-25 Shire Llc Compositions and methods for enhancing analgesic potency of covalently bound compounds, attenuating its adverse side effects, and preventing their abuse
JP5371746B2 (ja) 2006-05-26 2013-12-18 ファーマコフォア， インコーポレイテッド フェノール性オピオイドの制御放出
TWI401237B (zh) 2006-07-24 2013-07-11 ３-〔（１ｒ，２ｒ）-３-（二甲基氨基）-１-乙基-２-甲基丙基〕酚之製備
EP2086986A4 (en) 2006-09-14 2011-05-04 Starfire Systems Inc SYNTHETIC PROCESS FOR CYCLIC ORGANOSILANES
US20120142718A1 (en) 2007-02-16 2012-06-07 Jenkins Thomas E N-17-Alkylated Prodrugs of Opioids
US20110105381A2 (en) * 2007-02-16 2011-05-05 Pharmacofore, Inc. Prodrugs of Peripheral Phenolic Opioid Antagonists
RS55769B1 (sr) 2007-11-23 2017-07-31 Gruenenthal Gmbh Kompozicije tapentadola
US9023860B2 (en) 2007-11-26 2015-05-05 Signature Therapeutics, Inc. Pro-drugs for controlled release of biologically active compounds
WO2009080030A1 (en) 2007-12-21 2009-07-02 Lifecycle Pharma A/S Treatment of autoimmune hepatitis with a once daily oral dosage form comprising tacrolimus
WO2009092073A2 (en) 2008-01-18 2009-07-23 Shire Llc Amino acid and peptide prodrugs of opioid analgesics with reduced gi side-effects
TR201809734T4 (tr) 2008-02-14 2018-07-23 Alkermes Inc Seçici opioid bileşikler.
BRPI0908292B1 (pt) 2008-05-05 2022-09-20 Oramed Ltd Métodos e composições para administração oral de exenatida
CN102186467B (zh) 2008-10-17 2014-06-04 特色疗法股份有限公司 具有减弱释放酚类阿片样物质的药用组合物
WO2010100477A2 (en) 2009-03-03 2010-09-10 Shire Llc Amino acid and peptide carbamate prodrugs of tapentadol and uses thereof
AU2010231126A1 (en) * 2009-04-02 2011-10-13 Shire Llc Novel dicarboxylic acid linked amino acid and peptide prodrugs of opioids and uses thereof
CA2767987A1 (en) 2009-07-17 2011-01-20 Shire Llc Novel carbamate amino acid and peptide prodrugs of opioids and uses thereof
CA2773340C (en) * 2009-09-08 2019-07-23 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof
WO2011133178A1 (en) 2010-04-21 2011-10-27 Pharmacofore, Inc Compositions comprising enzyme-cleavable phenol-modified tapentadol prodrug
US20110262359A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable prodrugs of active agents and inhibitors thereof
US20130079364A1 (en) * 2010-04-21 2013-03-28 Signature Therapeutics, Inc. Peripheral Opioid Agonists and Peripheral Opioid Antagonists
US20110262360A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions Comprising Enzyme-Cleavable Phenol-Modified Opioid Prodrugs and Inhibitors Thereof
JP2013525348A (ja) * 2010-04-21 2013-06-20 シグネーチャー セラピューティクス，インク． 酵素切断可能なオピオイドプロドラッグとそのインヒビターとを含んでなる組成物
ES2710617T3 (es) 2010-04-21 2019-04-26 Signature Therapeutics Inc Composiciones que comprenden profármacos de anfetamina escindibles enzimáticamente e inhibidores de los mismos
US20110262355A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
WO2011133150A1 (en) * 2010-04-21 2011-10-27 Pharmacofore, Inc. Compositions comprising enzyme-cleavable prodrugs of active agents and inhibitors thereof
WO2012096886A1 (en) 2011-01-11 2012-07-19 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable oxycodone prodrug
RU2609412C2 (ru) 2011-01-11 2017-02-01 Сигничер Терапьютикс, Инк. Композиции, содержащие расщепляемое ферментами пролекарство оксикодона
EP2683394B1 (en) 2011-03-09 2021-01-06 Signature Therapeutics, Inc. Active agent prodrugs with heterocyclic linkers
WO2012122420A2 (en) 2011-03-09 2012-09-13 Pharmacofore, Inc. Opioid prodrugs with heterocyclic linkers

Also Published As

Publication number Publication date
DK2663187T3 (en) 2016-08-29
BR112013017296B1 (pt) 2021-02-17
US8569228B2 (en) 2013-10-29
WO2012096887A2 (en) 2012-07-19
CN103384472B (zh) 2016-01-20
CA2814763C (en) 2019-05-28
CN103384472A (zh) 2013-11-06
US8962547B2 (en) 2015-02-24
AU2012205733A1 (en) 2013-05-09
ES2584634T3 (es) 2016-09-28
EP2663187B1 (en) 2016-06-01
CA2814763A1 (en) 2012-07-19
WO2012096887A3 (en) 2012-10-04
EP2663187A4 (en) 2014-09-10
JP6016810B2 (ja) 2016-10-26
US20150197544A1 (en) 2015-07-16
TW201309297A (zh) 2013-03-01
US20120178772A1 (en) 2012-07-12
EP2663187A2 (en) 2013-11-20
JP2014502972A (ja) 2014-02-06
AU2012205733B2 (en) 2015-10-08
RU2609412C2 (ru) 2017-02-01
HK1189763A1 (zh) 2014-06-20
US20140162935A1 (en) 2014-06-12
US9499581B2 (en) 2016-11-22
IL225904B (en) 2020-03-31
TWI526209B (zh) 2016-03-21
RU2013137452A (ru) 2015-02-20

Similar Documents

Publication Publication Date Title
BR112013017296A2 (pt) Composto e composição compreendendo oxicodona, método para reduzir o abuso potencial da referida composição, unidade de dose e método para a sua preparação, e método para identificar um composto e um inibidor de tripsina
WO2012142498A3 (en) Mif inhibitors and their uses
BR112012021659A2 (pt) composto, composição farmacêutica, método para tratar e/ou prevenir distúrbios e doenças.
EP3520793A3 (en) Substances and compostions for use in methods of inhibiting muscle atrophy
TN2013000348A1 (en) Compounds and compositions as trk inhibitors
CL2014000314A1 (es) Compuestos derivados de ciclopropanamina, inhibidores de desmetilasa especifica de lisina 1 (lsd1); medicamento que los comprende; metodo para profilaxis o tratamiento; metodo para inhibir lsd1; y su uso en la profilaxis o tratamiento de esquizofrenia, enfermedad de alzheimer, enfermedad de parkinson o corea de huntington.
BR112014003590A2 (pt) processo para preparação de ternesite
BR112013002484A2 (pt) composto, composição farmacêutica, métodos para tratar esclerose múltipla e artrite reumatoide, e, uso de um composto.
WO2015011284A3 (en) Inhibitors of fapp2 and uses thereof
BR112012004453A8 (pt) composto inibidor de proteína quinase, sua composição farmacêutica e seu uso
BR112014030655A2 (pt) inibidores de pirimidinil tirosina quinase
UY33597A (es) Compuestos y composiciones como inhibidores de la trk
BR112014027236A2 (pt) pirrolidinas substituídas como um fator inibidor de xia para o tratamento de doenças tromboembolíticas
BRPI0814348A2 (pt) sais de ésteres saporíferos de ácidos policarboxílicos e métodos para distribuir compostos saporíferos que contêm grupos hiroxila.
BR112013017988A2 (pt) inibidores de bace-2 para o tratamento de distúrbios metabólicos
BR112013011441A2 (pt) composto, composição farmacêutica, e, uso de um composto
BR112012021656A2 (pt) composto, uso do mesmo, e, composição farmacêutica
BR112013026280A2 (pt) Derivados de cicloalquenil arila para inibidor da cetp
BR112013017845A2 (pt) agente antidiabético de abaixamento de lipídio
BR112013008211A8 (pt) Cocristais e sais de inibidores de ccr3, seu uso e composição que os compreende
BR112014004319A2 (pt) compostos e composições como inibidores de c-kit cinase
BR112014028991A2 (pt) triazóis como inibidores de kv3
CR20150390A (es) Inhibidores de la yodoproteina basada en 2,3-dihidroimidazol[1,2-c]pirimidin-5(1-h)-ona-asociada a la fosfolipasa a2 (lp-pla2)
CL2016001362A1 (es) Composiciones y métodos para reducir eventos adversos cardiovasculares graves
BR112013020975A2 (pt) compostos contendo fósforo como inibidores de proteína quinases

Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
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]
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 09/01/2012, OBSERVADAS AS CONDICOES LEGAIS.