BR0208924A - Uso de conjugados de ácido graxo de sal biliar ou de ácido biliar - Google Patents

Uso de conjugados de ácido graxo de sal biliar ou de ácido biliar

Info

Publication number
BR0208924A
BR0208924A BR0208924-6A BR0208924A BR0208924A BR 0208924 A BR0208924 A BR 0208924A BR 0208924 A BR0208924 A BR 0208924A BR 0208924 A BR0208924 A BR 0208924A
Authority
BR
Brazil
Prior art keywords
bile
acid
salt
fatty acid
conjugates
Prior art date
Application number
BR0208924-6A
Other languages
English (en)
Inventor
Tuvia Gilat
Original Assignee
Galmed Int Ltd
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 Galmed Int Ltd filed Critical Galmed Int Ltd
Publication of BR0208924A publication Critical patent/BR0208924A/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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 an organic compound
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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 an organic compound
    • A61K47/542Carboxylic acids, e.g. a fatty acid or an amino acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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 an organic compound
    • A61K47/543Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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 an organic compound
    • A61K47/554Medicinal 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 an organic compound the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Botany (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

"USO DE CONJUGADOS DE áCIDO GRAXO DE SAL BILIAR OU DE áCIDO BILIAR". A presente invenção refere-se ao uso de um conjugado de ácido graxo biliar ou de ácido biliar da fórmula geral II W-X-G, em que G é um radical de sal biliar ou de ácido biliar, que, se desejado, é conjugado na posição 24 com um aminoácido adequado, W significa um ou dois radicais de ácido graxo tendo de 14-22 átomos de carbono e X significa um membro de ligação adequado ou para uma ligação de C=C direta entre o dito radical de sal biliar ou de ácido biliar e o(s) ácido(s) graxo(s) ou de uma composição farmacêutica compreendendo o mesmo para a redução de colesterol no sangue, para o tratamento de fígado graxo, hiperglicemia e diabetes.
BR0208924-6A 2001-04-17 2002-04-15 Uso de conjugados de ácido graxo de sal biliar ou de ácido biliar BR0208924A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IL142650A IL142650A (en) 1998-04-08 2001-04-17 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
PCT/IL2002/000303 WO2002083147A1 (en) 2001-04-17 2002-04-15 Use of bile acid or bile salt fatty acid conjugates

Publications (1)

Publication Number Publication Date
BR0208924A true BR0208924A (pt) 2004-04-20

Family

ID=11075322

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0208924-6A BR0208924A (pt) 2001-04-17 2002-04-15 Uso de conjugados de ácido graxo de sal biliar ou de ácido biliar

Country Status (24)

Country Link
US (2) US7501403B2 (pt)
EP (2) EP1379254B1 (pt)
JP (1) JP4324706B2 (pt)
KR (1) KR100883080B1 (pt)
CN (1) CN1259918C (pt)
AT (2) ATE432705T1 (pt)
AU (2) AU2002307771B2 (pt)
BR (1) BR0208924A (pt)
CA (2) CA2703688C (pt)
CY (1) CY1106853T1 (pt)
CZ (2) CZ309042B6 (pt)
DE (2) DE60220775T2 (pt)
DK (2) DK1790346T3 (pt)
EA (1) EA007565B1 (pt)
ES (2) ES2289137T3 (pt)
HU (1) HU230548B1 (pt)
IL (1) IL142650A (pt)
MX (1) MXPA03009553A (pt)
NO (2) NO333910B1 (pt)
NZ (1) NZ528868A (pt)
PL (2) PL205057B1 (pt)
PT (2) PT1790346E (pt)
UA (1) UA78699C2 (pt)
WO (1) WO2002083147A1 (pt)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
TR201901012T4 (tr) * 2007-07-25 2019-02-21 Univ Graz Medizinische Arteriosklerozun tedavisinde nor-safra asitlerinin kullanımı.
US9314444B2 (en) 2009-01-12 2016-04-19 Biokier, Inc. Composition and method for treatment of NASH
US9006288B2 (en) 2009-01-12 2015-04-14 Biokier, Inc. Composition and method for treatment of diabetes
SI2376077T1 (sl) 2009-01-12 2017-09-29 Biokier Inc. Sestavek in metoda za zdravljenje diabetesa
EP2391370B1 (en) 2009-02-02 2015-06-03 Galmed Research and Development Ltd. Methods and compositions for treating alzheimer's disease
US20120202890A1 (en) 2011-02-08 2012-08-09 Nian Wu Polymer-carbohydrate-lipid conjugates
WO2013166176A1 (en) * 2012-05-01 2013-11-07 Catabasis Pharmaceuticals, Inc. Fatty acid conjugates of statin and fxr agonists; compositions and method of uses
CN103571617A (zh) * 2012-07-26 2014-02-12 丰益(上海)生物技术研发中心有限公司 改进的动物油脂加工工艺
WO2014084421A1 (en) * 2012-11-29 2014-06-05 Mediplex Corp. Bile acid oligomer conjugate for novel vesicular transport and use thereof
IL227890A0 (en) * 2013-08-08 2014-01-30 Galderm Therapeutics Ltd Antiaging compounds containing bile acid and fatty acid conjugates
US11571431B2 (en) 2013-12-04 2023-02-07 Galmed Research And Development Ltd Aramchol salts
CN105848718B (zh) * 2013-12-04 2019-07-30 盖尔梅德研究与发展有限公司 Aramchol盐
JP2017519726A (ja) * 2014-06-01 2017-07-20 ガルメッド リサーチ アンド ディベロップメント リミテッド. リポジストロフィー治療用脂肪酸胆汁酸複合体
US10849911B2 (en) 2015-06-10 2020-12-01 Galmed Research And Development Ltd. Low dose compositions of Aramachol salts
IL243707A0 (en) 2016-01-20 2016-05-01 Galmed Res And Dev Ltd Treatment to regulate the microbiota in the intestine
US11197870B2 (en) 2016-11-10 2021-12-14 Galmed Research And Development Ltd Treatment for hepatic fibrosis
CN116687850A (zh) 2022-02-24 2023-09-05 甘莱制药有限公司 包含环状膦酸酯化合物的药物组合物及其制备方法与用途

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US3859437A (en) * 1972-06-02 1975-01-07 Intellectual Property Dev Corp Reducing cholesterol levels
US3856953A (en) * 1973-05-15 1974-12-24 Intellectual Property Dev Corp Method of treating fatty liver
IT1167478B (it) * 1981-07-24 1987-05-13 Carlo Scolastico Derivati dell'acido ursodesossicolico
IT1167479B (it) * 1981-07-24 1987-05-13 Carlo Scolastico Derivati dell'acido chenodesossicolico
JPS6164701A (ja) * 1984-09-06 1986-04-03 Meito Sangyo Kk カチオン化デキストラン誘導体とポリウロン酸の高分子電解質錯体及びその利用
DE3930696A1 (de) * 1989-09-14 1991-03-28 Hoechst Ag Gallensaeurederivate, verfahren zu ihrer herstellung, verwendung als arzneimittel
US5278320A (en) * 1992-09-11 1994-01-11 Merck & Co., Inc. Cholesterol lowering compounds produced by directed biosynthesis
DE4432708A1 (de) * 1994-09-14 1996-03-21 Hoechst Ag Modifizierte Gallensäuren, Verfahren zu ihrer Herstellung und ihre Verwendung
EP1027045A4 (en) * 1997-10-31 2004-12-08 Arch Dev Corp METHODS AND COMPOSITIONS FOR REGULATING 5-ALPHA-REDUCTASE ACTIVITY
US20030153541A1 (en) * 1997-10-31 2003-08-14 Robert Dudley Novel anticholesterol compositions and method for using same
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
IL123998A (en) * 1998-04-08 2004-09-27 Galmed Int Ltd Conjugates of bile salts and pharmaceutical preparations containing them
US6620821B2 (en) * 2000-06-15 2003-09-16 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
JP2006306800A (ja) * 2005-04-28 2006-11-09 Kirin Brewery Co Ltd ファルネソイドx受容体活性化剤

Also Published As

Publication number Publication date
PL205057B1 (pl) 2010-03-31
CA2444266C (en) 2010-07-27
US20090149537A1 (en) 2009-06-11
ATE432705T1 (de) 2009-06-15
KR100883080B1 (ko) 2009-02-10
EP1379254A1 (en) 2004-01-14
HU230548B1 (hu) 2016-11-28
JP2004525962A (ja) 2004-08-26
EP1790346B1 (en) 2009-06-03
DE60220775D1 (de) 2007-08-02
CN1529603A (zh) 2004-09-15
PT1790346E (pt) 2009-09-04
CN1259918C (zh) 2006-06-21
DK1790346T3 (da) 2009-10-12
EA200301017A1 (ru) 2005-04-28
ES2289137T3 (es) 2008-02-01
US20040121993A1 (en) 2004-06-24
AU2002307771B2 (en) 2006-10-19
NO335087B1 (no) 2014-09-08
HUP0400801A2 (hu) 2004-08-30
WO2002083147A1 (en) 2002-10-24
US8110564B2 (en) 2012-02-07
EP1790346A2 (en) 2007-05-30
IL142650A0 (en) 2002-03-10
DK1379254T3 (da) 2007-10-15
EP1379254B1 (en) 2007-06-20
NO20131219L (no) 2003-11-28
HUP0400801A3 (en) 2012-09-28
US7501403B2 (en) 2009-03-10
CA2703688A1 (en) 2002-10-24
AU2007200191B2 (en) 2008-09-04
ES2328966T3 (es) 2009-11-19
KR20030092063A (ko) 2003-12-03
PL211438B1 (pl) 2012-05-31
CZ2008296A3 (pt) 2004-04-14
NO20034609L (no) 2003-11-28
DE60232559D1 (de) 2009-07-16
CZ20032710A3 (cs) 2004-04-14
CA2703688C (en) 2012-07-31
EA007565B1 (ru) 2006-12-29
NO333910B1 (no) 2013-10-14
JP4324706B2 (ja) 2009-09-02
EP1790346A3 (en) 2007-08-22
CZ300489B6 (cs) 2009-06-03
NZ528868A (en) 2005-09-30
DE60220775T2 (de) 2008-03-06
CA2444266A1 (en) 2002-10-24
PL366585A1 (en) 2005-02-07
UA78699C2 (en) 2007-04-25
CZ309042B6 (cs) 2021-12-22
PT1379254E (pt) 2007-07-10
MXPA03009553A (es) 2004-05-24
CY1106853T1 (el) 2012-05-23
AU2007200191A1 (en) 2007-02-08
IL142650A (en) 2007-06-03
NO20034609D0 (no) 2003-10-15
ATE365044T1 (de) 2007-07-15

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Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B15K Others concerning applications: alteration of classification

Free format text: PARA.INT.CI.A61K 31/575, A61K 47/48, A61P 3/06

Ipc: A61K 31/575 (2011.01), A61K 47/48 (2011.01), A61P

B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]

Free format text: MANTIDO O INDEFERIMENTO UMA VEZ QUE NAO FOI APRESENTADO RECURSO DENTRO DO PRAZO LEGAL.

B15K Others concerning applications: alteration of classification

Ipc: C07J 9/00 (2006.01), A61K 31/575 (2006.01), A61K 4