ATE306475T1 - Phenethyl-5-bromopyridylthioharnstoff (pbt) derivative mit spermizider wirkung - Google Patents

Phenethyl-5-bromopyridylthioharnstoff (pbt) derivative mit spermizider wirkung

Info

Publication number
ATE306475T1
ATE306475T1 AT99967737T AT99967737T ATE306475T1 AT E306475 T1 ATE306475 T1 AT E306475T1 AT 99967737 T AT99967737 T AT 99967737T AT 99967737 T AT99967737 T AT 99967737T AT E306475 T1 ATE306475 T1 AT E306475T1
Authority
AT
Austria
Prior art keywords
bromopyridylthiourea
pbt
phenethyl
derivative
spermicidal
Prior art date
Application number
AT99967737T
Other languages
English (en)
Inventor
Fatih M Uckun
Cruz Osmond D
Original Assignee
Parker Hughes Inst
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 Parker Hughes Inst filed Critical Parker Hughes Inst
Application granted granted Critical
Publication of ATE306475T1 publication Critical patent/ATE306475T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06—Antiabortive agents; Labour repressants
    • 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
    • A61P15/16—Masculine contraceptives
    • 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
    • A61P15/18—Feminine contraceptives
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/61—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/38—One sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/56—One oxygen atom and one sulfur atom
    • 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
    • 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
    • A61K9/0036—Devices retained in the vagina or cervix for a prolonged period, e.g. intravaginal rings, medicated tampons, medicated diaphragms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Reproductive Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Orthopedics, Nursing, And Contraception (AREA)
  • Saccharide Compounds (AREA)
AT99967737T 1998-12-31 1999-12-29 Phenethyl-5-bromopyridylthioharnstoff (pbt) derivative mit spermizider wirkung ATE306475T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/224,677 US6136335A (en) 1998-12-31 1998-12-31 Phenethyl-5-bromopyridylthiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DABO) derivatives exhibiting spermicidal activity
PCT/US1999/031160 WO2000039095A2 (en) 1998-12-31 1999-12-29 Phenethyl-5-bromopyridylthiourea (pbt) and dihydroalkoxybenzyloxopyrimidine (dabo) derivatives exhibiting spermicidal activity

Publications (1)

Publication Number Publication Date
ATE306475T1 true ATE306475T1 (de) 2005-10-15

Family

ID=22841684

Family Applications (1)

Application Number Title Priority Date Filing Date
AT99967737T ATE306475T1 (de) 1998-12-31 1999-12-29 Phenethyl-5-bromopyridylthioharnstoff (pbt) derivative mit spermizider wirkung

Country Status (15)

Country Link
US (2) US6136335A (de)
EP (2) EP1557197A1 (de)
JP (1) JP2002533444A (de)
KR (1) KR20010082772A (de)
CN (1) CN1371367A (de)
AT (1) ATE306475T1 (de)
AU (1) AU2396800A (de)
BR (1) BR9916620A (de)
CA (1) CA2362492A1 (de)
DE (1) DE69927710T2 (de)
HU (1) HUP0104904A2 (de)
IL (1) IL143508A0 (de)
MX (1) MXPA01006746A (de)
NO (1) NO20012817L (de)
WO (1) WO2000039095A2 (de)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1305313B1 (it) 1998-07-17 2001-05-04 Colla Paolo 3,4 - diidro- 6- benzil-4-oxopirimidine sostituite e relativo processodi produzione e impiego nella terapia delle infezioni da hiv-1.
US6136335A (en) * 1998-12-31 2000-10-24 Hughes Institute Phenethyl-5-bromopyridylthiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DABO) derivatives exhibiting spermicidal activity
US7064114B2 (en) * 1999-03-19 2006-06-20 Parker Hughes Institute Gel-microemulsion formulations
CA2428753C (en) * 2000-11-17 2013-05-21 Universita Degli Studi Di Cagliari Methods for inhibiting the transmission of hiv using topically applied substituted 6-benzyl-4-oxopyrimidines
SE0100733D0 (sv) 2001-03-05 2001-03-05 Medivir Ab Non-nucleoside reverse transcriptase inhibitors
SE0102867D0 (sv) 2001-08-28 2001-08-28 Medivir Ab Non-nucleoside reverse transcriptase inhibitors
US6929945B2 (en) * 2002-12-09 2005-08-16 Advanced Fluidix Laboratories Llc Male fertility assay method and device
TW200600492A (en) 2004-05-18 2006-01-01 Achillion Pharmaceuticals Inc Substituted aryl acylthioureas and related compounds; inhibitors of viral replication
WO2009102736A1 (en) 2008-02-12 2009-08-20 Dow Agrosciences Llc Pesticidal compositions
CN101628996B (zh) * 2008-07-18 2012-05-30 绿神(北京)乳胶业有限公司 一种乳胶避孕套的制备方法
WO2012109292A1 (en) 2011-02-09 2012-08-16 Dow Agrosciences Llc Pesticidal compositions and processes related thereto
KR20140045542A (ko) 2011-07-12 2014-04-16 다우 아그로사이언시즈 엘엘씨 살충 조성물 및 그에 관한 방법
CN103193771B (zh) * 2013-03-29 2015-08-05 中国人民解放军军事医学科学院生物工程研究所 链状酰胺类ccr5受体抑制剂的药物新用途

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR950006713B1 (ko) 1988-03-31 1995-06-21 미쓰비시 가세이 가부시끼가이샤 6-치환 비환식 피리미딘뉴클레오시드 유도체 및 그 유도체를 유효성분으로 하는 항 비루스제
US5686428A (en) * 1989-04-07 1997-11-11 Aktiebolaget Astra Pharmaceutical composition
HU205917B (en) * 1989-09-29 1992-07-28 Mitsubishi Chem Ind Process for producing 6-substituted pyrimidine derivatives and antiviral pharmaceutical compositions containing them as active components
US5503978A (en) * 1990-06-11 1996-04-02 University Research Corporation Method for identification of high affinity DNA ligands of HIV-1 reverse transcriptase
US5593993A (en) * 1991-08-02 1997-01-14 Medivir Ab Method for inhibition of HIV related viruses
IL102548A (en) * 1991-08-02 1998-08-16 Medivir Ab Thiourea derivatives for use in the preparation of medicaments for the inhibition of hiv and the treatment of aids and some such novel compounds
JPH0725770A (ja) * 1993-07-09 1995-01-27 Mitsubishi Chem Corp 経皮吸収性抗ウイルス剤
DE69414708T2 (de) * 1993-08-24 1999-04-15 Medivir Ab, Huddinge Verbindungen und methoden zur inhibition von hiv und verwandten viren
US5998411A (en) * 1998-03-17 1999-12-07 Hughes Institute Heterocyclic nonnucleoside inhibitors of reverse transcriptase
IT1305313B1 (it) * 1998-07-17 2001-05-04 Colla Paolo 3,4 - diidro- 6- benzil-4-oxopirimidine sostituite e relativo processodi produzione e impiego nella terapia delle infezioni da hiv-1.
US6136335A (en) * 1998-12-31 2000-10-24 Hughes Institute Phenethyl-5-bromopyridylthiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DABO) derivatives exhibiting spermicidal activity

Also Published As

Publication number Publication date
WO2000039095A3 (en) 2000-11-09
WO2000039095B1 (en) 2001-06-21
HUP0104904A2 (hu) 2002-04-29
MXPA01006746A (es) 2002-04-24
NO20012817D0 (no) 2001-06-07
EP1557197A1 (de) 2005-07-27
EP1140848B1 (de) 2005-10-12
KR20010082772A (ko) 2001-08-30
CA2362492A1 (en) 2000-07-06
AU2396800A (en) 2000-07-31
NO20012817L (no) 2001-08-29
BR9916620A (pt) 2001-09-25
US6376504B1 (en) 2002-04-23
JP2002533444A (ja) 2002-10-08
EP1140848A2 (de) 2001-10-10
DE69927710T2 (de) 2006-07-20
DE69927710D1 (de) 2006-02-23
WO2000039095A2 (en) 2000-07-06
IL143508A0 (en) 2002-04-21
CN1371367A (zh) 2002-09-25
US6136335A (en) 2000-10-24

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