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WO2002003977A3 - Combinations of statins, estrogenic agents and optionally estrogens - Google Patents

Combinations of statins, estrogenic agents and optionally estrogens Download PDF

Info

Publication number
WO2002003977A3
WO2002003977A3 PCT/US2001/021085 US0121085W WO0203977A3 WO 2002003977 A3 WO2002003977 A3 WO 2002003977A3 US 0121085 W US0121085 W US 0121085W WO 0203977 A3 WO0203977 A3 WO 0203977A3
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
ethers
statins
combinations
esters
Prior art date
Application number
PCT/US2001/021085
Other languages
French (fr)
Other versions
WO2002003977A2 (en
Inventor
Simon Nicholas Jenkins
Barry Samuel Komm
Christopher Paul Miller
Original Assignee
Wyeth Corp
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 Wyeth Corp filed Critical Wyeth Corp
Priority to EP01950826A priority Critical patent/EP1359940A2/en
Priority to BR0112365-3A priority patent/BR0112365A/en
Priority to AU2001271785A priority patent/AU2001271785A1/en
Priority to MXPA02012896A priority patent/MXPA02012896A/en
Priority to CA002414060A priority patent/CA2414060A1/en
Priority to JP2002508432A priority patent/JP2004502731A/en
Publication of WO2002003977A2 publication Critical patent/WO2002003977A2/en
Publication of WO2002003977A3 publication Critical patent/WO2002003977A3/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

This invention comprises methods of treating cardiovascular disorders and lowering blood LDL levels comprising administration of a statin, an estrogen and compound of the formulae (I or II): wherein Z is a moiety selected from the group of: (III) wherein: R1 is selected from H, OH or the C1-C12 esters or C1-C12 alkyl ethers thereof, benzyloxy, or halogen; or C1-C4 halogenated ethers including trifluoromethyl ether and trichloromethyl ether; R2, R3, R4, R5, and R6 are H, OH or C1-C12 esters or C1-C12 alkyl ethers thereof, halogens, or C1-C4 halogenated ethers, cyano, C1-C6 alkyl, or trifluoromethyl, with the proviso that, when R1 is H1, R2 is not OH; Y is the moiety: (IV) R7 and R8 are alkyl or concatenated together to form an optionally substituted, nitrogen-containing ring; or a pharmaceutically acceptable salt thereof.
PCT/US2001/021085 2000-07-06 2001-06-29 Combinations of statins, estrogenic agents and optionally estrogens WO2002003977A2 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
EP01950826A EP1359940A2 (en) 2000-07-06 2001-06-29 Combinations of statins, estrogenic agents and optionally estrogens
BR0112365-3A BR0112365A (en) 2000-07-06 2001-06-29 Combinations of statins, estrogens and optionally estrogens
AU2001271785A AU2001271785A1 (en) 2000-07-06 2001-06-29 Combinations of statins, estrogenic agents and optionally estrogens
MXPA02012896A MXPA02012896A (en) 2000-07-06 2001-06-29 Combinations of statins, estrogenic agents and optionally estrogens.
CA002414060A CA2414060A1 (en) 2000-07-06 2001-06-29 Combinations of statins, estrogenic agents and optionally estrogens
JP2002508432A JP2004502731A (en) 2000-07-06 2001-06-29 Combinations of statins, estrogens and optional estrogens

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US21609600P 2000-07-06 2000-07-06
US21618400P 2000-07-06 2000-07-06
US60/216,184 2000-07-06
US60/216,096 2000-07-06

Publications (2)

Publication Number Publication Date
WO2002003977A2 WO2002003977A2 (en) 2002-01-17
WO2002003977A3 true WO2002003977A3 (en) 2003-09-04

Family

ID=26910656

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/021085 WO2002003977A2 (en) 2000-07-06 2001-06-29 Combinations of statins, estrogenic agents and optionally estrogens

Country Status (8)

Country Link
EP (1) EP1359940A2 (en)
JP (1) JP2004502731A (en)
CN (1) CN1468110A (en)
AU (1) AU2001271785A1 (en)
BR (1) BR0112365A (en)
CA (1) CA2414060A1 (en)
MX (1) MXPA02012896A (en)
WO (1) WO2002003977A2 (en)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1545206B1 (en) 2002-07-24 2020-03-04 Children's Hospital Medical Center Compositions and products containing enantiomeric equol, and methods for their making
US8668914B2 (en) 2002-07-24 2014-03-11 Brigham Young University Use of equol for treating skin diseases
JP4889944B2 (en) 2002-10-29 2012-03-07 コロラド ステート ユニバーシティー リサーチ ファウンデーション Use of equol to treat androgen-mediated diseases
US8580846B2 (en) 2002-10-29 2013-11-12 Brigham Young University Use of equol for ameliorating or preventing neuropsychiatric and neurodegenerative diseases or disorders
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
NZ779654A (en) 2015-10-01 2024-12-20 Olema Pharmaceuticals Inc Tetrahydro-1h-pyrido[3,4-b]indole anti-estrogenic drugs
HRP20221462T1 (en) 2015-12-09 2023-01-20 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective estrogen receptor downregulators
ES2990061T3 (en) 2016-05-10 2024-11-28 C4 Therapeutics Inc Spirocyclic degronimers for the degradation of target proteins
WO2017197051A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Amine-linked c3-glutarimide degronimers for target protein degradation
ES2989988T3 (en) 2016-05-10 2024-11-28 C4 Therapeutics Inc Heterocyclic degronimers for the degradation of target proteins
CN109641874A (en) 2016-05-10 2019-04-16 C4医药公司 C for target protein degradation3The glutarimide degron body of carbon connection
CN109789143A (en) 2016-07-01 2019-05-21 G1治疗公司 Antiproliferative based on pyrimidine
WO2018081168A2 (en) 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
CN110177554B (en) 2017-01-06 2023-06-02 G1治疗公司 Combination Therapies Used to Treat Cancer
CA3052810A1 (en) 2017-02-10 2018-08-16 G1 Therapeutics, Inc. Benzothiophene estrogen receptor modulators
BR112019027967A2 (en) 2017-06-29 2020-07-14 G1 Therapeutics, Inc. isolated crystalline form b, pharmaceutical composition, method for treating a disorder, method of a compound or composition, and, process for producing crystalline form b.
CN113453679A (en) 2018-12-20 2021-09-28 C4医药公司 Targeted protein degradation
CN118344370A (en) 2019-12-20 2024-07-16 C4医药公司 Isoindolinone and indazole compounds for EGFR degradation
CN115279370B (en) 2020-03-05 2025-01-10 C4医药公司 Compounds for targeted degradation of BRD9
EP4192458A4 (en) 2020-08-05 2024-09-04 C4 Therapeutics, Inc. COMPOUNDS FOR TARGETED RET DEGRADATION
CN119998285A (en) 2022-08-03 2025-05-13 百时美施贵宝公司 Compounds for modulating RET proteins
WO2024097980A1 (en) 2022-11-04 2024-05-10 Bristol-Myers Squibb Company Ret-ldd protein inhibitors
WO2024097989A1 (en) 2022-11-04 2024-05-10 Bristol-Myers Squibb Company Ret-ldd protein degraders
WO2025006753A2 (en) 2023-06-30 2025-01-02 Merck Patent Gmbh Heterobifunctional compounds for the degradation of kras protein

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999059581A1 (en) * 1998-05-15 1999-11-25 American Home Products Corporation 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole in combination with estrogens
WO1999059969A1 (en) * 1998-05-15 1999-11-25 American Home Products Corporation Compositions comprising 2-phenyl-indole compounds and estrogen formulations

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999059581A1 (en) * 1998-05-15 1999-11-25 American Home Products Corporation 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole in combination with estrogens
WO1999059969A1 (en) * 1998-05-15 1999-11-25 American Home Products Corporation Compositions comprising 2-phenyl-indole compounds and estrogen formulations

Also Published As

Publication number Publication date
EP1359940A2 (en) 2003-11-12
CN1468110A (en) 2004-01-14
JP2004502731A (en) 2004-01-29
WO2002003977A2 (en) 2002-01-17
BR0112365A (en) 2003-05-13
MXPA02012896A (en) 2003-10-24
CA2414060A1 (en) 2002-01-17
AU2001271785A1 (en) 2002-01-21

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