BRPI0410158A - pró-drogas para hiv cliváveis por cd26 - Google Patents

pró-drogas para hiv cliváveis por cd26

Info

Publication number
BRPI0410158A
BRPI0410158A BRPI0410158-8A BRPI0410158A BRPI0410158A BR PI0410158 A BRPI0410158 A BR PI0410158A BR PI0410158 A BRPI0410158 A BR PI0410158A BR PI0410158 A BRPI0410158 A BR PI0410158A
Authority
BR
Brazil
Prior art keywords
prodrugs
alkyl
acid
cleavable
present
Prior art date
Application number
BRPI0410158-8A
Other languages
English (en)
Inventor
Herman Augustinus De Kock
Piet Tom Bert Paul Wigerinck
Jan Balzarini
Original Assignee
Tibotec Pharm Ltd
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Filing date
Publication date
Application filed by Tibotec Pharm Ltd filed Critical Tibotec Pharm Ltd
Publication of BRPI0410158A publication Critical patent/BRPI0410158A/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • 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
    • 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
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/08—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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/17—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/24—Condensed ring systems having three or more rings
    • C07H15/252—Naphthacene radicals, e.g. daunomycins, adriamycins
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • C07K5/06113—Asp- or Asn-amino acid
    • 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
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • 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
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1008—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • 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
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/101—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
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    • 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
    • C07K5/10—Tetrapeptides
    • C07K5/1019—Tetrapeptides with the first amino acid being basic
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    • C07—ORGANIC CHEMISTRY
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    • 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
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    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
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    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K9/00—Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequence; Derivatives thereof
    • C07K9/001—Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequence; Derivatives thereof the peptide sequence having less than 12 amino acids and not being part of a ring structure
    • C07K9/003—Peptides being substituted by heterocyclic radicals, e.g. bleomycin, phleomycin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
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  • Hematology (AREA)
  • Obesity (AREA)
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  • Child & Adolescent Psychology (AREA)
  • Cardiology (AREA)
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Abstract

"PRó-DROGAS PARA HIV CLIVáVEIS POR CD26". A presente invenção refere-se a novas pró-drogas que são conjugadas de um composto terapêutico e um peptídeo em que o conjugado é clivável por dipeptidil-peptidases, mais preferivelmente pela CD26, também conhecida como DPPIV (dipeptidil aminopeptidase IV). As presentes pró-drogas têm a fórmula (I), as formas estereoisoméricas e sais das mesmas, em que n é de 1 a 5; Y é prolina, alanina, hidroxiprolina, dihidroxiprolina, ácido tiazolidinacarboxílico (tioprolina), desidroprolina, ácido pipecólico (L-homoprolina), ácido azetidinacarboxílico, ácido aziridinacarboxílico, glicina, serina, valina, leucina, isoleucina e treonina; X é selecionado de qualquer aminoácido na configuração D ou L; X e Y, em cada repetição de ¢Y-X!, são escolhidos independentemente um do outro e independentemente de outras repetições; Z é uma ligação direta ou um grupo hidrocarboneto saturado linear ou ramificado bivalente tendo de 1 a 4 átomos de carbono; R¬ 1¬ é uma arila, heteroarila, arilóxi, heteroarilóxi, arilóxi C~ 1-4~alquila, heterocicloalquilóxi, heterocicloalquil C~ 1-4~ alquilóxi, heteroarilóxi C~ 1-4~alquila, heteroaril C~ 1-4~alquilóxi; R¬ 2¬ é aril C~ 1-4~alquila; R¬ 3¬ é C~ 1-10~aloalquila, C~ 2-6~alquenila ou C~ 3-7~cicloalquil C~ 1-4~alquila; R~ 4¬ é hidrogênio ou C~ 1-4~alquila. A presente invenção, além disso, refere-se ao uso das referidas pró-drogas como medicamentos, bem como um método de produção das referidas pró-drogas.
BRPI0410158-8A 2003-05-08 2004-05-10 pró-drogas para hiv cliváveis por cd26 BRPI0410158A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0310593.9A GB0310593D0 (en) 2003-05-08 2003-05-08 Peptidic prodrugs
PCT/EP2004/050753 WO2004099135A2 (en) 2003-05-08 2004-05-10 Hiv prodrugs cleavable by cd26

Publications (1)

Publication Number Publication Date
BRPI0410158A true BRPI0410158A (pt) 2006-05-16

Family

ID=9957688

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0410158-8A BRPI0410158A (pt) 2003-05-08 2004-05-10 pró-drogas para hiv cliváveis por cd26

Country Status (22)

Country Link
US (2) US20080214648A1 (pt)
EP (2) EP1620130A1 (pt)
JP (2) JP2006525235A (pt)
KR (1) KR20060008300A (pt)
CN (1) CN1784244A (pt)
AP (1) AP2005003465A0 (pt)
AT (1) ATE375172T1 (pt)
AU (2) AU2004236371B2 (pt)
BR (1) BRPI0410158A (pt)
CA (2) CA2517338A1 (pt)
DE (1) DE602004009435T2 (pt)
DK (1) DK1624897T3 (pt)
EA (1) EA009727B1 (pt)
ES (1) ES2295879T3 (pt)
GB (1) GB0310593D0 (pt)
MX (1) MXPA05012019A (pt)
NO (1) NO20055826L (pt)
NZ (1) NZ543946A (pt)
PT (1) PT1624897E (pt)
UA (1) UA82221C2 (pt)
WO (2) WO2004098644A1 (pt)
ZA (1) ZA200509940B (pt)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2005319578A1 (en) 2004-11-24 2006-06-29 Neopro Labs, Llc Methods and compositions for treating conditions
ES2381118T3 (es) * 2004-12-23 2012-05-23 Campina Nederland Holding B.V. Hidrolizado de proteínas enriquecido en péptidos de inhibición de DPP-IV y su uso
JP2009517464A (ja) 2005-11-30 2009-04-30 カンピーナ ネーダーランド ホールディング ビー．ブイ． グルカゴン様ペプチド１の活性を増強するタンパク質加水分解物の使用
EP2015765A4 (en) 2006-03-28 2011-11-23 Neopro Labs Llc METHODS AND COMPOSITIONS FOR TREATING CONDITIONS
CA2683288A1 (en) 2007-05-17 2008-11-27 Neopro Labs, Llc Crystalline and amorphous forms of peptide
EP2217701B9 (en) * 2007-10-30 2015-02-18 Indiana University Research and Technology Corporation Glucagon antagonists
EP2249853A4 (en) 2008-01-30 2012-12-26 Univ Indiana Res & Tech Corp ESTER BASED PEPTIDE PRODRUGS
EP2276479B1 (en) 2008-04-15 2014-07-02 SineVir Therapeutics LLC Prodrugs of neuraminidase inhibitors
AU2009290531B2 (en) * 2008-09-12 2014-08-21 Cadila Pharmaceuticals Ltd. Novel dipeptidyl peptidase (DP-IV) compounds
CN103396473A (zh) 2008-11-04 2013-11-20 安科治疗公司 Cxcr4受体化合物
RU2411248C2 (ru) * 2008-11-13 2011-02-10 Учреждение Российской академии наук Институт молекулярной генетики РАН (ИМГ РАН) Средство, обладающее антипсихотической активностью
AU2009327418A1 (en) 2008-12-19 2010-06-24 Indiana University Research And Technology Corporation Amide based glucagon superfamily peptide prodrugs
KR20110114568A (ko) * 2008-12-19 2011-10-19 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 디펩티드 링크된 약효 물질
WO2011061590A1 (en) 2009-11-17 2011-05-26 Hetero Research Foundation Novel carboxamide derivatives as hiv inhibitors
EP2566494B1 (en) * 2010-02-26 2017-11-29 Acer Therapeutics, Inc. Cxcr4 receptor compounds
US8946147B2 (en) 2010-06-24 2015-02-03 Indiana University Research And Technology Corporation Amide-based insulin prodrugs
US10426740B1 (en) 2010-08-18 2019-10-01 Avm Biotechnology, Llc Compositions and methods to inhibit stem cell and progenitor cell binding to lymphoid tissue and for regenerating germinal centers in lymphatic tissues
DK3066091T3 (da) * 2013-11-05 2019-07-15 Astrazeneca Ab Nmda-antagonist-prodrugs
WO2016039403A1 (ja) * 2014-09-11 2016-03-17 塩野義製薬株式会社 持続性ｈｉｖプロテアーゼ阻害剤
EP3197912B1 (en) * 2014-09-24 2023-01-04 Indiana University Research & Technology Corporation Lipidated amide-based insulin prodrugs
AU2016270597B2 (en) * 2015-05-29 2022-05-26 Arrowhead Pharmaceuticals, Inc. Biologically cleavable tetrapeptide linking agents
CA3054443A1 (en) 2017-04-01 2018-10-14 Avm Biotechnology, Llc Replacement of cytotoxic preconditioning before cellular immunotherapy
WO2019002945A2 (en) * 2017-06-29 2019-01-03 UREKA, Sarl PEPTIDE PRO-MEDICINE HAVING IMPROVED PHARMACEUTICAL PROPERTIES
EP3488851A1 (en) 2018-10-03 2019-05-29 AVM Biotechnology, LLC Immunoablative therapies
CN111233955B (zh) * 2020-02-28 2022-06-10 南京缘聚医药科技有限公司 一类噻唑酮甲酰胞嘧啶衍生物及其药物用途

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL55431A (en) * 1978-08-24 1982-07-30 Yeda Res & Dev Anthracycline type antibiotics,their preparation and pharmaceutical compositions comprising them
WO1987007276A1 (fr) * 1986-05-30 1987-12-03 Fuji Kagaku Kogyo Kabushiki Kaisha Nouveaux composes de 5-fluorouridine et procede de preparation
US5627035A (en) * 1990-08-22 1997-05-06 Syntello Vaccine Development Ab Peptides that block human immunodeficiency virus and methods of use thereof
DK0810209T3 (da) * 1992-08-25 2002-08-12 Monsanto Co Alpha - and beta-aminosyre-hydroxyethylaminosulfonamider til anvendelse som inhibitorer af retrovirale proteaser
US5968942A (en) * 1992-08-25 1999-10-19 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US6046190A (en) * 1992-08-25 2000-04-04 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
US5830897A (en) * 1992-08-27 1998-11-03 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
WO1996005863A1 (fr) * 1994-08-19 1996-02-29 La Region Wallonne Composes, composition pharmaceutique et dispositif de diagnostic les comprenant et leur utilisation
US5939550A (en) * 1995-06-15 1999-08-17 Pfizer Inc. Process for preparing derivatives of azabicyclo naphthyridine carboxylic acid comprising a dipeptide
CA2256669A1 (en) * 1996-05-29 1997-12-04 Prototek, Inc. Prodrugs of thalidomide and methods for using same as modulators of t-cell function
US6177404B1 (en) * 1996-10-15 2001-01-23 Merck & Co., Inc. Conjugates useful in the treatment of benign prostatic hyperplasia
US5783689A (en) * 1996-11-12 1998-07-21 University Of Notre Dame Antibacterial and antifungal nucleosides
AU4828199A (en) * 1998-06-23 2000-01-10 Board Of Trustees Of The University Of Illinois, The Multi-drug resistant retroviral protease inhibitors and associated methods
DE19828113A1 (de) * 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV
US7425541B2 (en) * 1998-12-11 2008-09-16 Medarex, Inc. Enzyme-cleavable prodrug compounds
US6613879B1 (en) * 1999-05-14 2003-09-02 Boehringer Ingelheim Pharma Kg FAP-activated anti-tumour compounds
DE60135732D1 (de) * 2000-02-28 2008-10-23 Univ British Columbia Topoisomerasehemmern zur behandlung von chirurgischen verklebungen
AU2001275525B2 (en) * 2000-06-14 2007-04-26 Medarex, Inc. Tripeptide prodrug compounds
PT1325910E (pt) * 2000-10-06 2008-10-27 Mitsubishi Tanabe Pharma Corp Compostos de anel alifático de cinco membros contendo azoto
UA74912C2 (en) * 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
WO2003048190A2 (en) * 2001-12-04 2003-06-12 The Curators Of The University Of Missouri Acyclovir-peptide analogs
AU2003296601A1 (en) * 2002-12-10 2004-06-30 F. Hoffmann-La Roche Ag Antiviral nucleoside derivatives
CA2515679A1 (en) * 2003-02-21 2004-09-02 Tripep Ab Glycinamide derivative for inhibiting hiv replication

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EP1624897A2 (en) 2006-02-15
UA82221C2 (uk) 2008-03-25
EP1624897B1 (en) 2007-10-10
MXPA05012019A (es) 2006-02-03
WO2004098644A1 (en) 2004-11-18
CA2525191A1 (en) 2004-11-18
KR20060008300A (ko) 2006-01-26
DK1624897T3 (da) 2008-02-11
AU2004236371A1 (en) 2004-11-18
NO20055826L (no) 2006-02-08
WO2004099135A3 (en) 2005-02-17
CN1784244A (zh) 2006-06-07
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EA009727B1 (ru) 2008-02-28
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US8236756B2 (en) 2012-08-07
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ZA200509940B (en) 2007-04-25
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AU2004235988A1 (en) 2004-11-18
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AP2005003465A0 (en) 2005-12-31
JP2006525235A (ja) 2006-11-09
PT1624897E (pt) 2008-01-17
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DE602004009435T2 (de) 2008-07-24

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