WO2002003976A3 - Combinations of bisphosphonates, estrogenic agents and optionally estrogens - Google Patents

Combinations of bisphosphonates, estrogenic agents and optionally estrogens Download PDF

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Publication number
WO2002003976A3
WO2002003976A3 PCT/US2001/020970 US0120970W WO0203976A3 WO 2002003976 A3 WO2002003976 A3 WO 2002003976A3 US 0120970 W US0120970 W US 0120970W WO 0203976 A3 WO0203976 A3 WO 0203976A3
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
ethers
optionally
bisphosphonates
combinations
Prior art date
Application number
PCT/US2001/020970
Other languages
French (fr)
Other versions
WO2002003976A2 (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 JP2002508431A priority Critical patent/JP2004502730A/en
Priority to AU2001273125A priority patent/AU2001273125A1/en
Priority to CA002415052A priority patent/CA2415052A1/en
Priority to EP01952365A priority patent/EP1299093A2/en
Priority to BR0112364-5A priority patent/BR0112364A/en
Priority to MXPA02012897A priority patent/MXPA02012897A/en
Publication of WO2002003976A2 publication Critical patent/WO2002003976A2/en
Publication of WO2002003976A3 publication Critical patent/WO2002003976A3/en

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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
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A61K31/663—Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
    • 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
    • A61K31/40—Heterocyclic 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
    • 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
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/454—Non 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds 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
    • 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
    • A61K31/66—Phosphorus compounds
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Abstract

This invention comprises methods of treating bone disorders and lowering blood LDL levels comprising administration of a bisphosphonate, and compound of the formula (I) or (II), wherein Z is a moiety selected from the group of (a), (b), or (c); wherein: R1 is selected from H, OH or the 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 H, R2 is not OH; Y is the moiety (1); R7 and R8 are alkyl or concatenated together to form an optionally substituted, nitrogen-containing ring; or a pharmaceutically acceptable salt thereof, and optionally an estrogen.
PCT/US2001/020970 2000-07-06 2001-06-29 Combinations of bisphosphonates, estrogenic agents and optionally estrogens WO2002003976A2 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
JP2002508431A JP2004502730A (en) 2000-07-06 2001-06-29 Combinations of bisphosphonates, estrogenic agents and optional estrogens
AU2001273125A AU2001273125A1 (en) 2000-07-06 2001-06-29 Combinations of bisphosphonates, estrogenic agents and optionally estrogens
CA002415052A CA2415052A1 (en) 2000-07-06 2001-06-29 Combinations of bisphosphonates, estrogenic agents and optionally estrogens
EP01952365A EP1299093A2 (en) 2000-07-06 2001-06-29 Combinations of bisphosphonates, estrogenic agents and optionally estrogens
BR0112364-5A BR0112364A (en) 2000-07-06 2001-06-29 Combinations of bisphosphonates, estrogens and optionally estrogens
MXPA02012897A MXPA02012897A (en) 2000-07-06 2001-06-29 Combinations of bisphosphonates, estrogenic agents and optionally estrogens.

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US21618800P 2000-07-06 2000-07-06
US21606900P 2000-07-06 2000-07-06
US60/216,188 2000-07-06
US60/216,069 2000-07-06

Publications (2)

Publication Number Publication Date
WO2002003976A2 WO2002003976A2 (en) 2002-01-17
WO2002003976A3 true WO2002003976A3 (en) 2003-01-03

Family

ID=26910620

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/020970 WO2002003976A2 (en) 2000-07-06 2001-06-29 Combinations of bisphosphonates, estrogenic agents and optionally estrogens

Country Status (8)

Country Link
EP (1) EP1299093A2 (en)
JP (1) JP2004502730A (en)
CN (1) CN1450913A (en)
AU (1) AU2001273125A1 (en)
BR (1) BR0112364A (en)
CA (1) CA2415052A1 (en)
MX (1) MXPA02012897A (en)
WO (1) WO2002003976A2 (en)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001271781A1 (en) * 2000-07-06 2002-01-21 Wyeth Use of substituted indole compounds for treating sphincter incontinence
US6455568B2 (en) 2000-07-06 2002-09-24 Wyeth Combination therapy for inhibiting sphincter incontinence
US6376486B1 (en) 2000-07-06 2002-04-23 American Home Products Corporation Methods of inhibiting sphincter incontinence
US8668914B2 (en) 2002-07-24 2014-03-11 Brigham Young University Use of equol for treating skin diseases
JP2006504409A (en) 2002-07-24 2006-02-09 チルドレンズ　ホスピタル　メディカル　センター Compositions and products containing enantiomeric equol and methods for their production
US8580846B2 (en) 2002-10-29 2013-11-12 Brigham Young University Use of equol for ameliorating or preventing neuropsychiatric and neurodegenerative diseases or disorders
AU2003286781B2 (en) 2002-10-29 2009-05-21 Brigham Young University Use of equol for treating androgen mediated diseases
JP4427453B2 (en) † 2002-12-20 2010-03-10 エフ．ホフマン−ラ ロシュ アーゲー High-dose ibandronate formulation
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
HUE055321T2 (en) 2015-10-01 2021-11-29 Olema Pharmaceuticals Inc Tetrahydro-1h-pyrido[3,4-b]indole anti-estrogenic drugs
MX2018007079A (en) 2015-12-09 2018-11-12 The Board Of Trustees Of Univ Of Illinois Benzothiophene-based selective estrogen receptor downregulators.
CN109562113A (en) 2016-05-10 2019-04-02 C4医药公司 Loop coil degron body for target protein degradation
CN109641874A (en) 2016-05-10 2019-04-16 C4医药公司 C for target protein degradation3The glutarimide degron body of carbon connection
WO2017197055A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
EA201990187A1 (en) 2016-07-01 2019-07-31 Г1 Терапьютикс, Инк. PYRIMIDINE ANTIPROLIFERATION AGENTS
WO2018081168A2 (en) 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
AU2018205262A1 (en) 2017-01-06 2019-07-11 G1 Therapeutics, Inc. Combination therapy for the treatment of cancer
CA3052810A1 (en) 2017-02-10 2018-08-16 G1 Therapeutics, Inc. Benzothiophene estrogen receptor modulators
AU2018291026B2 (en) 2017-06-29 2022-09-01 G1 Therapeutics, Inc. Morphic forms of GIT38 and methods of manufacture thereof
CN113453679A (en) 2018-12-20 2021-09-28 C4医药公司 Targeted protein degradation
WO2024030968A1 (en) 2022-08-03 2024-02-08 Brystol-Myers Squibb Company Compounds for modulating ret protein

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999059969A1 (en) * 1998-05-15 1999-11-25 American Home Products Corporation Compositions comprising 2-phenyl-indole compounds and estrogen formulations
WO1999059581A1 (en) * 1998-05-15 1999-11-25 American Home Products Corporation 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole in combination with estrogens
WO1999063974A2 (en) * 1998-06-11 1999-12-16 Endorecherche, Inc. Selective estrogen receptor modulator in combination with denydroepiandrosterone (dhea) or analogues

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999059969A1 (en) * 1998-05-15 1999-11-25 American Home Products Corporation Compositions comprising 2-phenyl-indole compounds and estrogen formulations
WO1999059581A1 (en) * 1998-05-15 1999-11-25 American Home Products Corporation 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole in combination with estrogens
WO1999063974A2 (en) * 1998-06-11 1999-12-16 Endorecherche, Inc. Selective estrogen receptor modulator in combination with denydroepiandrosterone (dhea) or analogues

Also Published As

Publication number Publication date
MXPA02012897A (en) 2003-10-24
CA2415052A1 (en) 2002-01-17
WO2002003976A2 (en) 2002-01-17
EP1299093A2 (en) 2003-04-09
CN1450913A (en) 2003-10-22
JP2004502730A (en) 2004-01-29
BR0112364A (en) 2003-07-29
AU2001273125A1 (en) 2002-01-21

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