BR112012032813B1 - Composto heterocíclico de benzodioxol ou benzodioxepina, composição farmacêutica, e, uso do composto - Google Patents

Composto heterocíclico de benzodioxol ou benzodioxepina, composição farmacêutica, e, uso do composto Download PDF

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Publication number
BR112012032813B1
BR112012032813B1 BR112012032813-1A BR112012032813A BR112012032813B1 BR 112012032813 B1 BR112012032813 B1 BR 112012032813B1 BR 112012032813 A BR112012032813 A BR 112012032813A BR 112012032813 B1 BR112012032813 B1 BR 112012032813B1
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BR
Brazil
Prior art keywords
compound
difluoromethoxy
ethanone
oxide
dichloro
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BR112012032813-1A
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English (en)
Portuguese (pt)
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BR112012032813A2 (pt
Inventor
Simon Hldbaek Nielsen
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UNION therapeutics A/S
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Publication date
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Publication of BR112012032813A2 publication Critical patent/BR112012032813A2/pt
Publication of BR112012032813B1 publication Critical patent/BR112012032813B1/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
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    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/06Antipsoriatics
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    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
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    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
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    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Otolaryngology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
BR112012032813-1A 2010-06-24 2011-06-24 Composto heterocíclico de benzodioxol ou benzodioxepina, composição farmacêutica, e, uso do composto BR112012032813B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US35820910P 2010-06-24 2010-06-24
US61/358,209 2010-06-24
PCT/DK2011/000069 WO2011160632A1 (en) 2010-06-24 2011-06-24 Benzodioxole or benzodioxepine heterocyclic compounds phosphodiesterase inhibitors

Publications (2)

Publication Number Publication Date
BR112012032813A2 BR112012032813A2 (pt) 2016-11-08
BR112012032813B1 true BR112012032813B1 (pt) 2022-02-01

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BR112012032813-1A BR112012032813B1 (pt) 2010-06-24 2011-06-24 Composto heterocíclico de benzodioxol ou benzodioxepina, composição farmacêutica, e, uso do composto

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US (3) US8980905B2 (enExample)
EP (2) EP2585469B1 (enExample)
JP (2) JP6174997B2 (enExample)
KR (1) KR101864578B1 (enExample)
CN (1) CN102958937B (enExample)
AU (1) AU2011269429B2 (enExample)
BR (1) BR112012032813B1 (enExample)
CA (1) CA2802895C (enExample)
CY (2) CY1117862T1 (enExample)
DK (2) DK2585469T3 (enExample)
ES (2) ES2584055T3 (enExample)
HR (2) HRP20160919T1 (enExample)
HU (2) HUE044301T2 (enExample)
IL (1) IL223329A (enExample)
LT (2) LT3070091T (enExample)
MX (1) MX2012014131A (enExample)
MY (1) MY157481A (enExample)
NZ (1) NZ603895A (enExample)
PL (2) PL2585469T3 (enExample)
PT (2) PT2585469T (enExample)
RS (2) RS58945B1 (enExample)
RU (1) RU2583787C2 (enExample)
SG (1) SG186140A1 (enExample)
SI (2) SI3070091T1 (enExample)
TR (1) TR201909709T4 (enExample)
TW (1) TWI507410B (enExample)
UA (1) UA109140C2 (enExample)
WO (1) WO2011160632A1 (enExample)
ZA (1) ZA201209031B (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104822392B (zh) * 2012-11-30 2017-09-08 利奥制药有限公司 抑制活化的t‑细胞中il‑22表达的方法
CA2953284A1 (en) * 2014-06-23 2015-12-30 Leo Pharma A/S Methods for the preparation of 1,3-benzodioxole heterocyclic compounds
WO2017089347A1 (en) 2015-11-25 2017-06-01 Inserm (Institut National De La Sante Et De La Recherche Medicale) Methods and pharmaceutical compositions for the treatment of braf inhibitor resistant melanomas
CA3007432A1 (en) * 2015-12-18 2017-06-22 Leo Pharma A/S Methods for the preparation of 1,3-benzodioxole heterocyclic compounds
IL271399B (en) * 2017-06-20 2022-07-01 Leo Pharma As Methods for the preparation of 1,3-benzodioxole heterocyclic compounds
US11384096B2 (en) 2017-12-15 2022-07-12 UNION therapeutics A/S Substituted azetidine dihydrothienopyridines and their use as phosphodiesterase inhibitors
CA3100977A1 (en) 2018-05-21 2019-11-28 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
LT3911304T (lt) * 2019-01-15 2023-11-10 UNION therapeutics A/S Modifikuoto atpalaidavimo tablečių vaisto formos, kurių sudėtyje yra fosfodiesterazės inhibitorių
WO2021016409A1 (en) * 2019-07-24 2021-01-28 Constellation Pharmaceuticals, Inc. Ezh2 inhibition in combination therapies for the treatment of cancers
CN112552276B (zh) * 2019-09-25 2023-03-21 中国科学院上海药物研究所 苯并氧杂卓-5-酮类化合物及其制备方法和用途
WO2022200339A1 (en) 2021-03-22 2022-09-29 UNION therapeutics A/S Treatment of hidradenitis suppurativa with orismilast
GB202205715D0 (en) 2022-04-19 2022-06-01 Union Therapeutics As Treatment of neutrophilic dermatoses
GB202306662D0 (en) 2023-05-05 2023-06-21 Union Therapeutics As Dosage regimen
GB202306663D0 (en) 2023-05-05 2023-06-21 Union Therapeutics As Combination therapy

Family Cites Families (11)

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Publication number Priority date Publication date Assignee Title
SI0706513T1 (en) * 1993-07-02 2002-10-31 Altana Pharma Ag Fluoroalkoxy-substituted benzamides and their use as cyclic nucleotide phosphodiesterase inhibitors
GB9507297D0 (en) 1995-04-07 1995-05-31 Rh Ne Poulenc Rorer Limited New composition of matter
AU705690B2 (en) 1995-05-19 1999-05-27 Kyowa Hakko Kogyo Co. Ltd. Oxygen-containing heterocyclic compounds
NZ332340A (en) * 1996-05-20 2000-04-28 Darwin Discovery Ltd 4-(aryl or heteroaryl) substituted benzofurancarboxamide derivatives and medicaments
CA2272327A1 (en) * 1996-11-19 1998-05-28 Kyowa Hakko Kogyo Co., Ltd. Oxygen-containing heterocyclic compounds
JP2005060375A (ja) * 2003-07-28 2005-03-10 Kyowa Hakko Kogyo Co Ltd 含酸素複素環化合物
DE10360792A1 (de) * 2003-12-23 2005-07-28 Grünenthal GmbH Spirocyclische Cyclohexan-Derivate
EP1831227B1 (en) * 2004-12-17 2013-06-19 Glenmark Pharmaceuticals S.A. Novel heterocyclic compounds useful for the treatment of inflammatory and allergic disorders
CN101631792B (zh) * 2007-02-28 2013-05-01 利奥制药有限公司 新的磷酸二酯酶抑制剂
KR101571654B1 (ko) * 2007-02-28 2015-11-25 레오 파마 에이/에스 신규한 포스포디에스테라제 억제제
ES2583478T3 (es) * 2011-12-21 2016-09-21 Leo Pharma A/S [1,2,4] triazolopiridinas y su uso como inhibidores de fosfodiesterasa

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US20160022657A1 (en) 2016-01-28
KR101864578B1 (ko) 2018-06-07
CA2802895A1 (en) 2011-12-29
JP2013529602A (ja) 2013-07-22
LT2585469T (lt) 2016-10-10
HRP20191136T1 (hr) 2019-09-20
MX2012014131A (es) 2013-01-29
US9273064B2 (en) 2016-03-01
CY1122201T1 (el) 2020-11-25
RS55104B1 (sr) 2016-12-30
CY1117862T1 (el) 2017-05-17
BR112012032813A2 (pt) 2016-11-08
CA2802895C (en) 2019-05-21
TR201909709T4 (tr) 2019-07-22
CN102958937B (zh) 2016-03-30
PT3070091T (pt) 2019-07-22
SI3070091T1 (sl) 2019-08-30
EP2585469B1 (en) 2016-05-25
NZ603895A (en) 2014-10-31
US8980905B2 (en) 2015-03-17
HUE030081T2 (en) 2017-04-28
EP3070091A1 (en) 2016-09-21
HUE044301T2 (hu) 2019-10-28
ES2733092T3 (es) 2019-11-27
SG186140A1 (en) 2013-01-30
RU2583787C2 (ru) 2016-05-10
DK2585469T3 (en) 2016-08-29
US9637499B2 (en) 2017-05-02
RU2013103079A (ru) 2014-07-27
JP6174997B2 (ja) 2017-08-02
IL223329A0 (en) 2013-02-03
TWI507410B (zh) 2015-11-11
EP2585469A1 (en) 2013-05-01
RS58945B1 (sr) 2019-08-30
MY157481A (en) 2016-06-15
KR20130038341A (ko) 2013-04-17
PL2585469T3 (pl) 2017-07-31
WO2011160632A1 (en) 2011-12-29
JP2016164168A (ja) 2016-09-08
LT3070091T (lt) 2019-07-25
EP3070091B1 (en) 2019-04-17
AU2011269429A1 (en) 2012-12-20
CN102958937A (zh) 2013-03-06
SI2585469T1 (sl) 2016-11-30
PT2585469T (pt) 2016-08-29
TW201206940A (en) 2012-02-16
PL3070091T3 (pl) 2019-09-30
US20130123291A1 (en) 2013-05-16
AU2011269429B2 (en) 2015-07-09
ZA201209031B (en) 2014-02-26
HRP20160919T1 (hr) 2016-10-07
DK3070091T3 (da) 2019-07-08
UA109140C2 (uk) 2015-07-27
ES2584055T3 (es) 2016-09-23
HK1182699A1 (zh) 2013-12-06
IL223329A (en) 2017-01-31
US20150111915A1 (en) 2015-04-23

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