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

Info

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
Authority
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
Other languages
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
Original Assignee
Merck Sharp and Dohme LLC
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 Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme LLC
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

Links

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)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Organic Chemistry (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (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
US6391865B1 (en) * 1999-05-04 2002-05-21 Schering Corporation Piperazine derivatives useful as CCR5 antagonists
KR100439357B1 (ko) * 1999-05-04 2004-07-07 쉐링 코포레이션 Ｃｃｒ５ 길항제로서 유용한 피페리딘 유도체
US6387930B1 (en) * 1999-05-04 2002-05-14 Schering Corporation Piperidine derivatives useful as CCR5 antagonists
SK287418B6 (sk) * 1999-05-04 2010-09-07 Schering Corporation Farmaceutický prípravok s obsahom CCR5 antagonistov a súprava s obsahom tohto prípravku
CN100355753C (zh) * 2000-05-26 2007-12-19 辉瑞大药厂 用于制备具有治疗作用的莨菪烷衍生物的中间体
AR033452A1 (es) * 2001-03-29 2003-12-17 Schering Corp Antagonistas de ccr5 utiles para el tratamiento del sida
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
JP2008526862A (ja) * 2005-01-06 2008-07-24 シェーリング コーポレイション ピペラジン化合物の薬学的な塩の調製
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
CA2716838A1 (en) 2009-09-11
WO2009111218A2 (en) 2009-09-11
EP2259772A2 (en) 2010-12-15
US20110059154A1 (en) 2011-03-10
JP2011513317A (ja) 2011-04-28
WO2009111218A3 (en) 2009-11-05
AU2009220462A1 (en) 2009-09-11

Similar Documents

Publication Publication Date Title
CA2716838C (en) Ccr5 antagonists as prophylactics for preventing hiv infection and methods of inhibiting transmission of same
EA032430B1 (ru) Конденсированные пиримидины для лечения вич
US8697662B2 (en) Methods for treating Kaposi sarcoma
TWI285200B (en) A61k 31/496 200601 a i vhtw a61p 31/12 200601 a i vhtw a61p 19/00 200601 a i vhtw
KR101743315B1 (ko) Ｂｃｒ-ａｂｌ, ｃ-ｋｉｔ, ｄｄｒ1, ｄｄｒ2 또는 ｐｄｇｆ-ｒ 키나제 활성에 의해 매개된 증식성 장애 및 다른 병적 상태의 치료 방법
CN108472245A (zh) 用于吲哚胺2,3-双加氧酶抑制及其适应症的药物组合物和方法
CN118084905A (zh) 苯甲酰胺化合物
ES2238277T3 (es) Terapia anti-vih con una combinacion de un interferon alfa-pegilado y un antagonista de ccr5.
CA3192145A1 (en) Bridged tricyclic carbamoylpyridone compounds and uses thereof
JP2021517116A (ja) 併用療法
CN103167881B (zh) 用于抑制hiv传播的方法和组合物
TW201006834A (en) Immunomodulation by IAP inhibitors
KR20030083014A (ko) Ａｉｄｓ 치료용 ｃｃｒ5 길항제
JP2007332141A (ja) 薬
JP2020521739A (ja) 併用療法
TW200534854A (en) Methods of treating HIV infection
JP2024503892A (ja) ピロロピリジン－アニリン化合物の結晶形
TW200533357A (en) 2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases
TW200536544A (en) Method of treating HIV infection
JP2024516353A5 (https=)
WO2021216814A1 (en) Btk inhibitors to treat pulmonary distress in covid-19 patients
JP2013237709A (ja) Ｐｇｄ２拮抗剤及びヒスタミン拮抗剤からなるアレルギー性鼻炎治療用医薬
CN109689048B (zh) 促进胚胎植入和预防流产的催产素拮抗剂给药方案
JP7759065B2 (ja) ペンドリン抑制活性を有する新規化合物およびその医薬用途
JP2021534114A (ja) 併用療法

Legal Events

Date Code Title Description
EEER Examination request
MKLA Lapsed

Effective date: 20160224