BR0010564A - Compostos antitumor ativados por fap - Google Patents

Compostos antitumor ativados por fap

Info

Publication number
BR0010564A
BR0010564A BR0010564-3A BR0010564A BR0010564A BR 0010564 A BR0010564 A BR 0010564A BR 0010564 A BR0010564 A BR 0010564A BR 0010564 A BR0010564 A BR 0010564A
Authority
BR
Brazil
Prior art keywords
fap
antitumor compounds
activated antitumor
prodrug
drug
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
BR0010564-3A
Other languages
English (en)
Inventor
Pilar Garin-Chesa
Martin Lenter
John Edward Park
Stefan Peters
Wolfgang J Rettig
Raymond Armand Firestone
Dietmar Leipert
Juergen Mack
Leila A Telan
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim Pharma GmbH Co KG
Original Assignee
Boehringer Ingelheim Pharma GmbH Co KG
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 Boehringer Ingelheim Pharma GmbH Co KG filed Critical Boehringer Ingelheim Pharma GmbH Co KG
Publication of BR0010564A publication Critical patent/BR0010564A/pt
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B82NANOTECHNOLOGY
    • B82YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • 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
    • A61K47/62Medicinal 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
    • A61K47/65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • A61K47/62Medicinal 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
    • A61K47/66Medicinal 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 the modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells
    • A61K47/67Enzyme prodrug therapy, e.g. gene directed enzyme drug therapy [GDEPT] or VDEPT
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20Carbocyclic rings
    • C07H15/24Condensed ring systems having three or more rings
    • C07H15/252Naphthacene radicals, e.g. daunomycins, adriamycins
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1019Tetrapeptides with the first amino acid being basic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1024Tetrapeptides with the first amino acid being heterocyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biotechnology (AREA)
  • Epidemiology (AREA)
  • Nanotechnology (AREA)
  • Cell Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Engineering & Computer Science (AREA)
  • Medical Informatics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Patente de Invenção: "COMPOSTOS ANTITUMOR ATIVADOS POR FAP". A invenção refere-se a uma pró-droga que é capaz de ser convertida em uma droga por ação catalítica de proteína de ativação de fibroblasto humana (FAP <244>), a pró-droga possuindo um sítio de clivagem que é reconhecido por FAP<244>), e a dita droga sendo citotóxica ou citostática sob condições fisiológicas.
BR0010564-3A 1999-05-14 2000-05-11 Compostos antitumor ativados por fap Expired - Fee Related BR0010564A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13413699P 1999-05-14 1999-05-14
PCT/EP2000/004261 WO2000071571A2 (en) 1999-05-14 2000-05-11 Fap-activated anti-tumor compounds

Publications (1)

Publication Number Publication Date
BR0010564A true BR0010564A (pt) 2002-02-19

Family

ID=22461925

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0010564-3A Expired - Fee Related BR0010564A (pt) 1999-05-14 2000-05-11 Compostos antitumor ativados por fap

Country Status (28)

Country Link
US (1) US6613879B1 (pt)
EP (1) EP1180116A2 (pt)
JP (1) JP3607201B2 (pt)
KR (1) KR20020030270A (pt)
CN (1) CN1213058C (pt)
AR (1) AR033792A1 (pt)
AU (1) AU777521B2 (pt)
BG (1) BG106096A (pt)
BR (1) BR0010564A (pt)
CA (1) CA2369933A1 (pt)
CO (1) CO5170516A1 (pt)
CZ (1) CZ20014097A3 (pt)
EA (1) EA005204B1 (pt)
EE (1) EE200100600A (pt)
HK (1) HK1048642B (pt)
HU (1) HUP0202367A3 (pt)
IL (1) IL145798A0 (pt)
MX (1) MXPA01011401A (pt)
MY (1) MY125939A (pt)
NO (1) NO20015536L (pt)
NZ (1) NZ516075A (pt)
PL (1) PL351680A1 (pt)
SK (1) SK16452001A3 (pt)
TW (1) TWI248444B (pt)
UA (1) UA73506C2 (pt)
WO (1) WO2000071571A2 (pt)
YU (1) YU80901A (pt)
ZA (1) ZA200109151B (pt)

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HUP0300590A2 (hu) 2000-03-15 2003-07-28 Bristol-Myers Squibb Pharma Company Peptidázzal hasítható, célzott antineoplasztikus szerek és terápiás alkalmazásuk
GB0027552D0 (en) * 2000-11-10 2000-12-27 Boehringer Ingelheim Pharma Anti-tumor compounds
GB0027551D0 (en) * 2000-11-10 2000-12-27 Boehringer Ingelheim Pharma Anti-tumor compounds
EP1399467A4 (en) * 2001-05-09 2004-09-15 Newbiotics Inc PRODRUGS ACTIVATED BY PEPTIDDEFORMYLASE
US7091186B2 (en) * 2001-09-24 2006-08-15 Seattle Genetics, Inc. p-Amidobenzylethers in drug delivery agents
US20030211979A1 (en) * 2002-01-30 2003-11-13 Boehringer Ingelheim Pharma Gmbh & Co. Kg FAP-activated anti-tumor compounds
EP1333033A1 (en) * 2002-01-30 2003-08-06 Boehringer Ingelheim Pharma GmbH & Co.KG FAP-activated anti-tumor compounds
AU2003225047A1 (en) * 2002-04-18 2003-11-03 Celmed Oncology (Usa), Inc. Peptide deformylase activated prodrugs
WO2003094972A2 (en) * 2002-05-10 2003-11-20 Boehringer Ingelheim Pharma Gmbh & Co Kg Fap-activated anti-tumor prodrugs
US20040033957A1 (en) * 2002-05-10 2004-02-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg FAP-activated anti-tumor prodrugs
US20040001801A1 (en) * 2002-05-23 2004-01-01 Corvas International, Inc. Conjugates activated by cell surface proteases and therapeutic uses thereof
JP2006514009A (ja) * 2002-11-14 2006-04-27 セルメド オンコロジー (ユーエスエイ), インコーポレイテッド ペプチドデホルミラーゼ活性化プロドラッグ
GB0310593D0 (en) * 2003-05-08 2003-06-11 Leuven K U Res & Dev Peptidic prodrugs
EP1625122A1 (en) 2003-05-14 2006-02-15 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7678909B1 (en) 2003-08-13 2010-03-16 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2005118555A1 (en) 2004-06-04 2005-12-15 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2006073167A1 (ja) * 2005-01-07 2006-07-13 Ono Pharmaceutical Co., Ltd. ピロリジン誘導体
EP1943257A2 (en) 2005-05-19 2008-07-16 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods
US8067248B2 (en) * 2005-12-14 2011-11-29 Luwig Institute for Cancer Research Method for diagnosing rheumatoid arthritis via assaying myofibroblast-like synoviocytes for fibroblast activation protein
WO2007087131A2 (en) * 2006-01-05 2007-08-02 The Johns Hopkins University Peptide prodrugs
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2008005479A2 (en) * 2006-07-06 2008-01-10 University Of Wyoming Charge reversible polymers
WO2008116053A2 (en) * 2007-03-20 2008-09-25 Trustees Of Tufts College Fap-activated chemotherapeutic compounds, and methods of use thereof
AU2009290531B2 (en) * 2008-09-12 2014-08-21 Cadila Pharmaceuticals Ltd. Novel dipeptidyl peptidase (DP-IV) compounds
WO2011089215A1 (en) 2010-01-22 2011-07-28 Ascendis Pharma As Dipeptide-based prodrug linkers for aromatic amine-containing drugs
WO2011089216A1 (en) 2010-01-22 2011-07-28 Ascendis Pharma As Dipeptide-based prodrug linkers for aliphatic amine-containing drugs
US20150335761A1 (en) * 2012-02-16 2015-11-26 Raymond Firestone Compositions and methods for contraception
AU2013369261B2 (en) 2012-12-28 2018-08-09 Cobiores Nv Minimally toxic prodrugs
EP2987794B1 (en) * 2013-04-19 2018-05-30 Jinan University Vinblastine derivatives, preparation method therefor and application thereof
HUE045001T2 (hu) 2013-11-05 2019-12-30 Astrazeneca Ab NMDA antagonista prodrugok
CN106573073B (zh) 2014-06-13 2021-09-28 塔夫茨大学信托人 Fap激活的治疗剂以及其相关用途
US9737556B2 (en) 2014-06-13 2017-08-22 Trustees Of Tufts College FAP-activated therapeutic agents, and uses related thereto
CN105524141B (zh) * 2015-11-12 2019-11-26 中山大学 一种FAPa激活式肿瘤诊断多肽磁珠复合物的制备与应用
EP3222292A1 (en) 2016-03-03 2017-09-27 Heidelberg Pharma GmbH Amanitin conjugates
CN107043456B (zh) * 2017-04-19 2019-05-17 川北医学院 对氧环己酮与l-苯丙氨酸氮芥共聚物及其应用
CN110128501A (zh) * 2019-05-21 2019-08-16 北京海美源医药科技有限公司 一种靶向fap酶的喜树碱类化合物及其制备方法和应用
CN110128506B (zh) * 2019-05-22 2021-03-30 中国药科大学 一种寡肽及其应用

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Also Published As

Publication number Publication date
CN1374969A (zh) 2002-10-16
US6613879B1 (en) 2003-09-02
EP1180116A2 (en) 2002-02-20
IL145798A0 (en) 2002-07-25
EA005204B1 (ru) 2004-12-30
HK1048642B (zh) 2005-10-28
CN1213058C (zh) 2005-08-03
MY125939A (en) 2006-09-29
AR033792A1 (es) 2004-01-07
UA73506C2 (en) 2005-08-15
BG106096A (bg) 2002-05-31
ZA200109151B (en) 2002-12-17
WO2000071571A8 (en) 2002-03-07
CO5170516A1 (es) 2002-06-27
MXPA01011401A (es) 2002-06-04
JP3607201B2 (ja) 2005-01-05
HUP0202367A3 (en) 2003-10-28
WO2000071571A3 (en) 2001-09-07
JP2003500417A (ja) 2003-01-07
AU6559100A (en) 2000-12-12
NZ516075A (en) 2004-03-26
EA200101155A1 (ru) 2002-10-31
KR20020030270A (ko) 2002-04-24
SK16452001A3 (sk) 2002-03-05
AU777521B2 (en) 2004-10-21
HK1048642A1 (en) 2003-04-11
EE200100600A (et) 2003-02-17
CZ20014097A3 (cs) 2002-02-13
CA2369933A1 (en) 2000-11-30
NO20015536L (no) 2002-01-10
TWI248444B (en) 2006-02-01
YU80901A (sh) 2005-07-19
HUP0202367A2 (hu) 2002-11-28
NO20015536D0 (no) 2001-11-13
WO2000071571A2 (en) 2000-11-30
PL351680A1 (en) 2003-06-02

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Legal Events

Date Code Title Description
B25D Requested change of name of applicant approved
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 8A E 9A ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 NA RPI2003 DE 26/05/2009.