AR091310A1 - Antibioticos de peptidos lineales - Google Patents

Antibioticos de peptidos lineales

Info

Publication number
AR091310A1
AR091310A1 ARP130100482A AR091310A1 AR 091310 A1 AR091310 A1 AR 091310A1 AR P130100482 A ARP130100482 A AR P130100482A AR 091310 A1 AR091310 A1 AR 091310A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
alkyl
independently
formula
ch2ch2c
Prior art date
Application number
Other languages
English (en)
Inventor
Curran Roberts Tucker
Paraselli Prasuna
Andrew Smith Peter
Campbell David
I Higuchi Robert
Original Assignee
Rqx Pharmaceuticals Inc
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 Rqx Pharmaceuticals Inc filed Critical Rqx Pharmaceuticals Inc
Publication of AR091310A1 publication Critical patent/AR091310A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • 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
    • A61P31/08—Antibacterial agents for leprosy
    • 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
    • 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
    • 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
    • C07K5/1013—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • 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
    • C07K5/1019—Tetrapeptides with the first amino acid being basic
    • 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
    • C07K5/1021—Tetrapeptides with the first amino acid being acidic
    • 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
    • C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Compuestos antibacterianos que en algunas formas de realización tienen un amplio espectro de bioactividad. En otras formas de realización pueden vencer la resistencia conferida por mutaciones de un solo aminoácido en posiciones determinadas de Peptidasas Señal (SPasas) bacterianas y en otras formas de realización proveen una actividad antibiótica de mayor amplitud de espectro. También se proveen composiciones farmacéuticas y métodos de tratamiento en los que se usan los compuestos. Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de fórmula (1) donde: R¹ se selecciona entre: los compuestos de fórmula (2) a (9); R², R⁴, R¹⁰, R¹¹, R¹², y R¹³ son en forma independiente entre sí -H, -CH₃, -CH(CH₃)₂, -C(CH₃)₃, -CH(CH₃)(CH₂CH₃), -CH₂CH(CH₃)₂, -CH₂OH, -CH(OH)(CH₃), -CH₂CF₃, -CH₂C(O)OH, -CH₂C(O)OR²⁵, -CH₂CH₂C(O)OH, -CH₂CH₂C(O)OR²⁵, -CH₂C(O)NH₂, -CH₂CH₂C(O)NH₂, -CH₂CH₂C(O)N(H)C(H)(CH₃)CO₂H, -CH₂CH₂C(O)N(H)C(H)(CO₂H)CH₂CO₂H, -CH₂NR²¹R²², -(CH₂)₂NR²¹R²², -(CH₂)₃NR²¹R²², -(CH₂)₄NR²¹R²², -(CH₂)₄N(R²⁵)₃, -(CH₂)₄N(H)C(O)(2,3-dihidroxibenceno), alquilo C₁₋₈ opcionalmente sustituido, heteroalquilo C₁₋₈ opcionalmente sustituido, cicloalquilo C₃₋₈ opcionalmente sustituido, -CH₂-cicloalquilo C₃₋₈ opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, o un resto de fórmula (10) a (14); R³ es metilo, etilo, isopropilo, o ciclopropilo; R⁵ es H, metilo, etilo, o -CH₂OH; o R⁵ y R²⁴ junto con el átomo de boro forman un anillo que contiene boro de 5 ó 6 miembros; R⁶ es -C(=O)H, -CH₂C(=O)H, -C(=O)NHCH₂C(=O)H, -C(=O)C(=O)N(R¹⁴)₂, -B(OR²³)(OR²⁴), o un resto de formula (15); o R⁵ y R⁶ junto con el átomo de carbono forman el resto de fórmula (16); Rˣ es H, alquilo C₁₋₆ opcionalmente sustituido, heteroalquilo C₁₋₆ opcionalmente sustituido, o cicloalquilo C₃₋₈ opcionalmente sustituido; o Rˣ y R² junto con el átomo de nitrógeno forman un anillo que contiene nitrógeno opcionalmente sustituido; Rʸ es H o metilo; o Rʸ y R⁵ junto con el átomo de nitrógeno forman un anillo que contiene nitrógeno opcionalmente sustituido; Rᶻ es -NR¹⁵R¹⁶, -CH₂-NR¹⁵R¹⁶, o -(CH₂)₂-NR¹⁵R¹⁶; R⁷ es arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, alquenilo opcionalmente sustituido, o una cadena alquilo lineal o ramificada de aproximadamente 1 - 22 átomos de carbono, que opcionalmente comprende dentro de la cadena alquilo o en el extremo de una cadena alquilo un arilo opcionalmente sustituido, un heteroarilo opcionalmente sustituido, un heterocicloalquilo opcionalmente sustituido, o un resto de fórmula (17) opcionalmente sustituido, donde Z es una unión, O, S, NH, CH₂, NHCH₂, o CºC; R⁸ es una unión, -O-, o -N(R¹⁷)-, arilo opcionalmente sustituido, o heteroarilo opcionalmente sustituido; R⁹ es -CH₂OH, -CH₂CH(CH₃)₂, o restos de fórmula (10), (11) y (14); R¹⁴, R¹⁵, y R¹⁶ son en forma independiente entre sí H, o alquilo C₁₋₄; R¹⁷ es H, metilo, etilo, isopropilo, o ciclopropilo; R¹⁸, R¹⁹, y R²⁰ son en forma independiente entre sí H, o metilo; cada R²¹ es en forma independiente H, o alquilo C₁₋₄; cada R²² es en forma independiente H, alquilo C₁₋₄, -C(=NH)(NH₂), o -CH(=NH); R²³ y R²⁴ son en forma independiente entre sí H, o alquilo C₁₋₄; o R²³ y R²⁴ junto con el átomo de boro forman un anillo que contiene boro de 5 ó 6 miembros opcionalmente sustituido; cada R²⁵ es en forma independiente alquilo C₁₋₆; R²⁶ es H, alquilo C₁₋₄, alcoxi C₁₋₄, -CH₂C(O)OR²⁵, o -OCH₂C(O)OR²⁵; n es 0 ó 1; p es 0 ó 1; y q es 0 ó 1; o una sal farmacéuticamente aceptable, solvato, o prodroga del mismo.
ARP130100482 2012-02-16 2013-02-15 Antibioticos de peptidos lineales AR091310A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261599851P 2012-02-16 2012-02-16
US201261730928P 2012-11-28 2012-11-28

Publications (1)

Publication Number Publication Date
AR091310A1 true AR091310A1 (es) 2015-01-28

Family

ID=48982724

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130100482 AR091310A1 (es) 2012-02-16 2013-02-15 Antibioticos de peptidos lineales

Country Status (12)

Country Link
US (3) US8999922B2 (es)
EP (1) EP2814807A4 (es)
JP (2) JP2015509942A (es)
KR (1) KR20140132367A (es)
CN (1) CN104254518A (es)
AR (1) AR091310A1 (es)
CA (1) CA2864669A1 (es)
EA (1) EA201491511A1 (es)
HK (1) HK1205736A1 (es)
MX (1) MX357561B (es)
TW (1) TWI601746B (es)
WO (1) WO2013123456A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8999922B2 (en) * 2012-02-16 2015-04-07 Rqx Pharmaceuticals, Inc. Linear peptide antibiotics
CN105431447A (zh) * 2013-03-15 2016-03-23 阿达拉塔合伙有限公司 Pcsk9的小分子调节剂和其使用方法
CN105636978A (zh) * 2013-08-14 2016-06-01 阿奇克斯制药公司 线性肽抗生素
US10344043B2 (en) 2015-04-14 2019-07-09 B-Organic Films Corp Antiviral and antibacteria agents based on quaternary ammonium compound complexed with boric acid and its derivatives
PL3464336T3 (pl) 2016-06-01 2022-05-16 Athira Pharma, Inc. Związki
KR102595723B1 (ko) 2016-06-21 2023-10-27 오리온 옵탈몰로지 엘엘씨 헤테로시클릭 프롤린아미드 유도체
EP3472151A4 (en) 2016-06-21 2020-03-04 Orion Ophthalmology LLC CARBOCYCLIC PROLINAMIDE DERIVATIVES
KR102042600B1 (ko) * 2018-02-13 2019-11-08 전북대학교산학협력단 항산화 및 항염증 활성을 갖는 홍갯지렁이 유래 신규 펩타이드 및 이의 이용

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SI0932617T1 (en) * 1996-10-18 2002-06-30 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
ZA979327B (en) * 1996-10-18 1998-05-11 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis C virus NS3 protease.
GB9623908D0 (en) * 1996-11-18 1997-01-08 Hoffmann La Roche Amino acid derivatives
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AR029851A1 (es) * 2000-07-21 2003-07-16 Dendreon Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c
SV2003000617A (es) * 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
KR20040004642A (ko) * 2001-05-23 2004-01-13 덴드레온 샌 디에고 엘엘씨 세포 표면 프로테아제에 의해 활성화되는 접합체 및 이의치료학적 용도
US7244815B2 (en) * 2001-05-23 2007-07-17 The Curators Of The University Of Missouri Attachment and elaboration strategies for inverse peptide synthesis
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US8999922B2 (en) 2012-02-16 2015-04-07 Rqx Pharmaceuticals, Inc. Linear peptide antibiotics

Also Published As

Publication number Publication date
JP2015509942A (ja) 2015-04-02
WO2013123456A1 (en) 2013-08-22
US9708368B2 (en) 2017-07-18
EP2814807A4 (en) 2015-10-07
US20150166605A1 (en) 2015-06-18
EA201491511A1 (ru) 2014-12-30
CN104254518A (zh) 2014-12-31
KR20140132367A (ko) 2014-11-17
MX2014009899A (es) 2015-03-09
MX357561B (es) 2018-07-13
US8999922B2 (en) 2015-04-07
US20170275334A1 (en) 2017-09-28
HK1205736A1 (en) 2015-12-24
TW201341403A (zh) 2013-10-16
US20130217619A1 (en) 2013-08-22
CA2864669A1 (en) 2013-08-22
TWI601746B (zh) 2017-10-11
JP2018135334A (ja) 2018-08-30
EP2814807A1 (en) 2014-12-24

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