BR112016012465A8 - sal, método de preparação do sal e composição farmacêutica - Google Patents

sal, método de preparação do sal e composição farmacêutica Download PDF

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Publication number
BR112016012465A8
BR112016012465A8 BR112016012465A BR112016012465A BR112016012465A8 BR 112016012465 A8 BR112016012465 A8 BR 112016012465A8 BR 112016012465 A BR112016012465 A BR 112016012465A BR 112016012465 A BR112016012465 A BR 112016012465A BR 112016012465 A8 BR112016012465 A8 BR 112016012465A8
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Brazil
Prior art keywords
salt
pharmaceutical composition
preparation
methods
aramchol
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BR112016012465A
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English (en)
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BR112016012465B1 (pt
Inventor
Baharaff Allen
Eshkar-Oren Idit
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Galmed Res & Development Ltd
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Publication date
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Publication of BR112016012465A8 publication Critical patent/BR112016012465A8/pt
Publication of BR112016012465B1 publication Critical patent/BR112016012465B1/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/68—Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/02—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C211/03—Monoamines
    • C07C211/05—Mono-, di- or tri-ethylamine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/08—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
    • C07C215/08—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with only one hydroxy group and one amino group bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/10—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
    • C07C229/12—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of acyclic carbon skeletons
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/26—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C277/00—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/14—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

a presente invenção refere-se aos sais de ácido colanóico amido araquidílico (aramchol), as composições farmacêuticas que compreendem sais de aramchol, métodos para a sua preparação e métodos de uso dos mesmos em tratamento médico.
BR112016012465-0A 2013-12-04 2014-12-04 Sal, método de preparação do sal e composição farmacêutica BR112016012465B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361911478P 2013-12-04 2013-12-04
US61/911,478 2013-12-04
PCT/IL2014/051052 WO2015083164A1 (en) 2013-12-04 2014-12-04 Aramchol salts

Publications (2)

Publication Number Publication Date
BR112016012465A8 true BR112016012465A8 (pt) 2020-05-05
BR112016012465B1 BR112016012465B1 (pt) 2023-04-18

Family

ID=53272986

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112016012465-0A BR112016012465B1 (pt) 2013-12-04 2014-12-04 Sal, método de preparação do sal e composição farmacêutica

Country Status (21)

Country Link
US (1) US20160304553A1 (pt)
EP (1) EP3077047B1 (pt)
JP (2) JP6675310B2 (pt)
KR (1) KR102320191B1 (pt)
CN (2) CN105848718B (pt)
AU (2) AU2014358668B2 (pt)
BR (1) BR112016012465B1 (pt)
CA (1) CA2930232C (pt)
CY (1) CY1121736T1 (pt)
DK (1) DK3077047T3 (pt)
ES (1) ES2732845T3 (pt)
HK (1) HK1226347A1 (pt)
HR (1) HRP20191023T1 (pt)
HU (1) HUE045209T2 (pt)
LT (1) LT3077047T (pt)
PL (1) PL3077047T3 (pt)
PT (1) PT3077047T (pt)
RS (1) RS59067B1 (pt)
SI (1) SI3077047T1 (pt)
TR (1) TR201909447T4 (pt)
WO (1) WO2015083164A1 (pt)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL227890A0 (en) * 2013-08-08 2014-01-30 Galderm Therapeutics Ltd Antiaging compounds containing bile acid and fatty acid conjugates
RS59067B1 (sr) * 2013-12-04 2019-09-30 Galmed Res & Development Ltd Soli aramchol-a
US10849911B2 (en) 2015-06-10 2020-12-01 Galmed Research And Development Ltd. Low dose compositions of Aramachol salts
DK3328390T3 (da) * 2015-07-12 2022-01-10 Cfso Gmbh Lysinsalte af cholecalciferolsulfat og deres anvendelse til behandling af vitamin d3-mangel
WO2017017677A1 (en) * 2015-07-27 2017-02-02 Galmed Research And Development Ltd. Combination treatment for liver disease
IL243707A0 (en) 2016-01-20 2016-05-01 Galmed Res And Dev Ltd Treatment to regulate the microbiota in the intestine
FR3050112B1 (fr) 2016-04-15 2020-09-04 Soc Civ Immobiliere Gecinq Utilisation de l'acide fenofibrique dans le traitement des maladies hepatiques
EP3518918A4 (en) * 2016-09-28 2020-04-22 Eiger Biopharmaceuticals, Inc. METHOD AND PHARMACEUTICAL COMPOSITIONS FOR TREATING NON-ALCOHOLIC STEATOHEPATITIS
US11197870B2 (en) 2016-11-10 2021-12-14 Galmed Research And Development Ltd Treatment for hepatic fibrosis
JP2019537607A (ja) * 2016-11-10 2019-12-26 ガルメド リサーチ アンド ディベロップメント リミテッド 非アルコール性脂肪性肝疾患の患者における線維化の抑制
EP3636655A4 (en) * 2017-06-07 2020-08-26 Crystal Pharmaceutical (Suzhou) Co., Ltd. CRYSTALLINE FORM OF A FATTY ACID - BILIARY ACID CONJUGATE, PROCESS OF PREPARATION AND APPLICATION
WO2019125913A1 (en) * 2017-12-20 2019-06-27 Michael Guarnieri Nutritional bolus for animals
WO2020026471A1 (ja) * 2018-07-31 2020-02-06 株式会社親広産業 グルコース消費促進剤および解糖系促進剤
JP6612004B1 (ja) * 2018-07-31 2019-11-27 株式会社親広産業 グルコース消費促進剤および解糖系促進剤

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2252863A (en) * 1941-02-03 1941-08-19 Searle & Co Quaternary ammonium salts
GB1532413A (en) * 1974-12-23 1978-11-15 Union International Co Ltd Chenodeoxycholic acid
IL123998A (en) * 1998-04-08 2004-09-27 Galmed Int Ltd Conjugates of bile salts and pharmaceutical preparations containing them
IL142650A (en) * 1998-04-08 2007-06-03 Galmed Int Ltd Use of bile acid conjugates or bile salts and fatty acids or fatty acids in the preparation of pharmaceuticals for lowering cholesterol, for the treatment of fatty liver and for the treatment of hyperglycemia and diabetes
US8975246B2 (en) * 2001-04-17 2015-03-10 Galmed Research And Development Ltd. Bile acid or bile salt fatty acid conjugates
ITMI20061735A1 (it) * 2006-09-12 2008-03-13 Dipharma Spa Procedimento per la preparazione di acidi colanici
DE102007032507A1 (de) * 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
WO2010086864A1 (en) * 2009-02-02 2010-08-05 Galmed International Ltd. Methods and compositions for treating alzheimer's disease
CN102115486B (zh) * 2009-12-30 2015-06-03 上海特化医药科技有限公司 一种3-β-花生酰胺基-7α,12α,5β-胆烷-24-羧酸的制备方法
JP2013518110A (ja) * 2010-01-28 2013-05-20 メルク・シャープ・エンド・ドーム・コーポレイション 疼痛および他の適応症の治療用の医薬組成物
US8802695B2 (en) * 2010-02-03 2014-08-12 Takeda Pharmaceutical Company Limited Apoptosis signal-regulating kinase 1 inhibitors
JP6030567B2 (ja) * 2010-12-07 2016-11-24 アミラ ファーマシューティカルス，インコーポレーテッド 多環式ｌｐａ１アンタゴニストおよびその使用
RS59067B1 (sr) * 2013-12-04 2019-09-30 Galmed Res & Development Ltd Soli aramchol-a

Also Published As

Publication number Publication date
JP2020111584A (ja) 2020-07-27
EP3077047B1 (en) 2019-04-24
DK3077047T3 (da) 2019-07-15
HRP20191023T1 (hr) 2019-09-06
ES2732845T3 (es) 2019-11-26
CN105848718B (zh) 2019-07-30
HUE045209T2 (hu) 2019-12-30
CA2930232A1 (en) 2015-06-11
BR112016012465B1 (pt) 2023-04-18
CY1121736T1 (el) 2020-07-31
EP3077047A4 (en) 2017-05-03
US20160304553A1 (en) 2016-10-20
LT3077047T (lt) 2019-08-26
RS59067B1 (sr) 2019-09-30
PL3077047T3 (pl) 2019-10-31
WO2015083164A1 (en) 2015-06-11
EP3077047A1 (en) 2016-10-12
HK1226347A1 (zh) 2017-09-29
TR201909447T4 (tr) 2019-07-22
AU2014358668A1 (en) 2016-06-02
JP6675310B2 (ja) 2020-04-01
CN110437298A (zh) 2019-11-12
PT3077047T (pt) 2019-07-11
KR20160093051A (ko) 2016-08-05
AU2019275638A1 (en) 2020-01-23
CN105848718A (zh) 2016-08-10
AU2014358668B2 (en) 2019-10-24
CA2930232C (en) 2020-09-15
KR102320191B1 (ko) 2021-11-03
SI3077047T1 (sl) 2019-09-30
JP2016539131A (ja) 2016-12-15
AU2019275638B2 (en) 2021-05-06

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
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]
B154 Notification of filing of divisional application [chapter 15.50 patent gazette]

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