CA2716838C - Ccr5 antagonists as prophylactics for preventing hiv infection and methods of inhibiting transmission of same - Google Patents

Ccr5 antagonists as prophylactics for preventing hiv infection and methods of inhibiting transmission of same Download PDF

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Publication number
CA2716838C
CA2716838C CA2716838A CA2716838A CA2716838C CA 2716838 C CA2716838 C CA 2716838C CA 2716838 A CA2716838 A CA 2716838A CA 2716838 A CA2716838 A CA 2716838A CA 2716838 C CA2716838 C CA 2716838C
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CA
Canada
Prior art keywords
alkyl
group
hiv
hydrogen
vaginal
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
CA2716838A
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English (en)
French (fr)
Other versions
CA2716838A1 (en
Inventor
Julie M. Strizki
Rahul Rajan Gandhi
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.)
Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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Filing date
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Publication of CA2716838A1 publication Critical patent/CA2716838A1/en
Application granted granted Critical
Publication of CA2716838C publication Critical patent/CA2716838C/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/15—Oximes (>C=N—O—); Hydrazines (>N—N<); Hydrazones (>N—N=) ; Imines (C—N=C)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4425—Pyridinium derivatives, e.g. pralidoxime, pyridostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Organic Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Cosmetics (AREA)
CA2716838A 2008-02-29 2009-02-24 Ccr5 antagonists as prophylactics for preventing hiv infection and methods of inhibiting transmission of same Expired - Fee Related CA2716838C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US3253908P 2008-02-29 2008-02-29
US61/032,539 2008-02-29
PCT/US2009/034990 WO2009111218A2 (en) 2008-02-29 2009-02-24 Ccr5 antagonists as prophylactics for preventing hiv infection and methods of inhibiting transmission of same

Publications (2)

Publication Number Publication Date
CA2716838A1 CA2716838A1 (en) 2009-09-11
CA2716838C true CA2716838C (en) 2014-01-07

Family

ID=40627290

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2716838A Expired - Fee Related CA2716838C (en) 2008-02-29 2009-02-24 Ccr5 antagonists as prophylactics for preventing hiv infection and methods of inhibiting transmission of same

Country Status (6)

Country Link
US (1) US20110059154A1 (https=)
EP (1) EP2259772A2 (https=)
JP (1) JP2011513317A (https=)
AU (1) AU2009220462A1 (https=)
CA (1) CA2716838C (https=)
WO (1) WO2009111218A2 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8580294B2 (en) 2010-10-19 2013-11-12 International Partnership For Microbicides Platinum-catalyzed intravaginal rings
DE102012209008B4 (de) 2012-05-29 2015-02-05 Wellcomet Gmbh Vorrichtung zum Erzeugen von Behandlungswellen
US10137031B2 (en) 2013-11-14 2018-11-27 International Partnership For Microbicides, Inc. Combination therapy intravaginal rings
CN104997725B (zh) * 2015-07-13 2017-10-20 山西锦波生物医药股份有限公司 抗hiv病毒的马来酸b07凝胶制剂配方及制备方法
EP3370701A1 (en) 2015-11-06 2018-09-12 INEB-Instituto Nacional De Engenharia Biomédica A composition for use in a method for prevention or treatment of human immunodeficiency virus infections
JP7512010B2 (ja) * 2018-09-20 2024-07-08 株式会社ヤクルト本社 経皮吸収用組成物及び経皮吸収性向上方法
US11629196B2 (en) 2020-04-27 2023-04-18 Incelldx, Inc. Method of treating SARS-CoV-2-associated hypercytokinemia by administering a human monoclonal antibody (PRO-140) that inhibits CCR5/CCL5 binding interactions

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050276836A1 (en) * 1997-06-11 2005-12-15 Michelle Wilson Coated vaginal devices for vaginal delivery of therapeutically effective and/or health-promoting agents
CA2371583C (en) * 1999-05-04 2005-09-13 Schering Corporation Piperazine derivatives useful as ccr5 antagonists
US6387930B1 (en) * 1999-05-04 2002-05-14 Schering Corporation Piperidine derivatives useful as CCR5 antagonists
HK1039330B (en) * 1999-05-04 2005-12-09 Schering Corporation Piperidine derivatives useful as ccr5 antagonists
US6391865B1 (en) * 1999-05-04 2002-05-21 Schering Corporation Piperazine derivatives useful as CCR5 antagonists
RS50904B (sr) * 2000-05-26 2010-08-31 Pfizer Inc. Derivati tropana i njihova primena
PL364560A1 (en) * 2001-03-29 2004-12-13 Schering Corporation Ccr5 antagonists useful for treating aids
US8178123B2 (en) * 2001-08-29 2012-05-15 Femina Pharma Incorporated Method for augmentation of intraepithelial and systemic exposure of therapeutic agents having substrate activity for cytochrome P450 enzymes and membrane efflux systems following vaginal and oral cavity administration
UA93354C2 (ru) * 2004-07-09 2011-02-10 Гилиад Сайенсиз, Инк. Местный противовирусный препарат
AR052865A1 (es) * 2005-01-06 2007-04-11 Schering Corp Preparacion de compuestos farmaceuticos derivados de sales de piperazina
WO2007033208A2 (en) * 2005-09-12 2007-03-22 University Of Maryland Biotechnology Institute Off. Of Research Admin/Tech. Dev. Use of indirubin and its derivatives in the treatments of hiv infection and heart failure
EP1948103A2 (en) * 2005-09-15 2008-07-30 UMD, Inc. A method of intraepithelial and systemic exposure of therapeutic agents following vaginal and oral cavity administration
TW200745087A (en) * 2006-02-24 2007-12-16 Schering Corp CCR5 antagonists useful for treating HIV

Also Published As

Publication number Publication date
WO2009111218A3 (en) 2009-11-05
WO2009111218A2 (en) 2009-09-11
CA2716838A1 (en) 2009-09-11
EP2259772A2 (en) 2010-12-15
AU2009220462A1 (en) 2009-09-11
US20110059154A1 (en) 2011-03-10
JP2011513317A (ja) 2011-04-28

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