WO2002047722A1 - Medicinal compositions of nonpeptidyl gonadotropin-releasing hormone agonist or antagonist, process for producing the same and use thereof - Google Patents

Medicinal compositions of nonpeptidyl gonadotropin-releasing hormone agonist or antagonist, process for producing the same and use thereof Download PDF

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Publication number
WO2002047722A1
WO2002047722A1 PCT/JP2001/010956 JP0110956W WO0247722A1 WO 2002047722 A1 WO2002047722 A1 WO 2002047722A1 JP 0110956 W JP0110956 W JP 0110956W WO 0247722 A1 WO0247722 A1 WO 0247722A1
Authority
WO
WIPO (PCT)
Prior art keywords
nonpeptidyl
antagonist
gonadotropin
releasing hormone
medicinal compositions
Prior art date
Application number
PCT/JP2001/010956
Other languages
French (fr)
Japanese (ja)
Inventor
Hiroshi Suzuki
Yoshio Hata
Original Assignee
Takeda Chemical Industries, Ltd.
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 Takeda Chemical Industries, Ltd. filed Critical Takeda Chemical Industries, Ltd.
Priority to AU2002221139A priority Critical patent/AU2002221139A1/en
Publication of WO2002047722A1 publication Critical patent/WO2002047722A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Abstract

Medicinal compositions comprising: (i) a nonpeptidyl gonadotropin-releasing hormone agonist or antagonist; (ii) an organic acid or its salt; and (iii) a biodegradable polymer or its salt. These compositions can be efficiently produced, suffer from no trouble in quality control and can achieve a stable releasing speed over a long period of time, even in case where the nonpeptidyl GnRH agonist or antagonist is contained in a large amount regardless of the solubility, melting point or crystallinity thereof.
PCT/JP2001/010956 2000-12-15 2001-12-14 Medicinal compositions of nonpeptidyl gonadotropin-releasing hormone agonist or antagonist, process for producing the same and use thereof WO2002047722A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002221139A AU2002221139A1 (en) 2000-12-15 2001-12-14 Medicinal compositions of nonpeptidyl gonadotropin-releasing hormone agonist or antagonist, process for producing the same and use thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2000382431 2000-12-15
JP2000-382431 2000-12-15

Publications (1)

Publication Number Publication Date
WO2002047722A1 true WO2002047722A1 (en) 2002-06-20

Family

ID=18850254

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2001/010956 WO2002047722A1 (en) 2000-12-15 2001-12-14 Medicinal compositions of nonpeptidyl gonadotropin-releasing hormone agonist or antagonist, process for producing the same and use thereof

Country Status (2)

Country Link
AU (1) AU2002221139A1 (en)
WO (1) WO2002047722A1 (en)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003002092A3 (en) * 2001-06-29 2003-04-10 Takeda Chemical Industries Ltd Controlled release composition comprising lactic acid polymer and hydroxynaphthoic acid, and method of producing the same
WO2004067535A1 (en) * 2003-01-29 2004-08-12 Takeda Pharmaceutical Company Limited Thienopyrimidine compounds and use thereof
US8921326B2 (en) 2006-12-18 2014-12-30 Takeda Pharmaceutical Company Limited Sustained-release composition and method for producing the same

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0626170A2 (en) * 1993-05-10 1994-11-30 Sandoz Ltd. Stabilisation of pharmacologically active compounds in sustained release compositions
WO1995015767A1 (en) * 1993-12-09 1995-06-15 Asta Medica Aktiengesellschaft Long-acting injection suspensions and a process for their preparation
WO1995028405A1 (en) * 1994-04-19 1995-10-26 Takeda Chemical Industries, Ltd. Bicyclic thiophene derivatives and use as gonadotropin releasing hormone antagonists
WO1996024597A1 (en) * 1995-02-08 1996-08-15 Takeda Chemical Industries, Ltd. Thienopyrimidine derivatives, their production and use
WO1998032423A1 (en) * 1997-01-29 1998-07-30 Takeda Chemical Industries, Ltd. Sustained-release microspheres, their production and use
WO1999036099A1 (en) * 1998-01-16 1999-07-22 Takeda Chemical Industries, Ltd. Sustained release compositions, process for producing the same and utilization thereof
WO2000056739A1 (en) * 1999-03-24 2000-09-28 Takeda Chemical Industries, Ltd. Thienopyrimidine compounds, their production and use
JP2001081043A (en) * 1999-07-15 2001-03-27 Takeda Chem Ind Ltd Sustained release composition, its production and use

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0626170A2 (en) * 1993-05-10 1994-11-30 Sandoz Ltd. Stabilisation of pharmacologically active compounds in sustained release compositions
WO1995015767A1 (en) * 1993-12-09 1995-06-15 Asta Medica Aktiengesellschaft Long-acting injection suspensions and a process for their preparation
WO1995028405A1 (en) * 1994-04-19 1995-10-26 Takeda Chemical Industries, Ltd. Bicyclic thiophene derivatives and use as gonadotropin releasing hormone antagonists
WO1996024597A1 (en) * 1995-02-08 1996-08-15 Takeda Chemical Industries, Ltd. Thienopyrimidine derivatives, their production and use
WO1998032423A1 (en) * 1997-01-29 1998-07-30 Takeda Chemical Industries, Ltd. Sustained-release microspheres, their production and use
WO1999036099A1 (en) * 1998-01-16 1999-07-22 Takeda Chemical Industries, Ltd. Sustained release compositions, process for producing the same and utilization thereof
WO2000056739A1 (en) * 1999-03-24 2000-09-28 Takeda Chemical Industries, Ltd. Thienopyrimidine compounds, their production and use
JP2001081043A (en) * 1999-07-15 2001-03-27 Takeda Chem Ind Ltd Sustained release composition, its production and use

Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8067030B2 (en) 2001-06-29 2011-11-29 Takeda Pharmaceutical Company Limited Controlled release composition and method of producing the same
US8815801B2 (en) 2001-06-29 2014-08-26 Takeda Pharmaceutical Company Limited Controlled release composition and method of producing the same
EP1491236A1 (en) * 2001-06-29 2004-12-29 Takeda Chemical Industries, Ltd. Controlled release composition comprising lactic acid polymer and hydroxynaphthoic acid, and method of producing the same
US8246987B2 (en) 2001-06-29 2012-08-21 Takeda Pharmaceutical Company Limited Controlled release composition and method of producing the same
WO2003002092A3 (en) * 2001-06-29 2003-04-10 Takeda Chemical Industries Ltd Controlled release composition comprising lactic acid polymer and hydroxynaphthoic acid, and method of producing the same
US7429559B2 (en) 2001-06-29 2008-09-30 Takeda Pharmaceutical Company Limited Controlled release composition and method of producing the same
EP1949936A3 (en) * 2001-06-29 2008-10-08 Takeda Pharmaceutical Company Limited Controlled release composition and method of producing the same
CN100360538C (en) * 2003-01-29 2008-01-09 武田药品工业株式会社 Thienopyrimidine compound and use of the same
US8058280B2 (en) 2003-01-29 2011-11-15 Takeda Pharmaceutical Company Limited Substituted thieno[2,3-d]pyrimidin-2,4-dione compounds and uses thereof
US7300935B2 (en) 2003-01-29 2007-11-27 Takeda Pharmaceutical Company Thienopyrimidine compounds and use thereof
US8735401B2 (en) 2003-01-29 2014-05-27 Takeda Pharmaceutical Company Limited Thienopyrimidine compounds and use thereof
WO2004067535A1 (en) * 2003-01-29 2004-08-12 Takeda Pharmaceutical Company Limited Thienopyrimidine compounds and use thereof
US9346822B2 (en) 2003-01-29 2016-05-24 Takeda Pharmaceutical Company Limited Thienopyrimidine compounds and use thereof
US8921326B2 (en) 2006-12-18 2014-12-30 Takeda Pharmaceutical Company Limited Sustained-release composition and method for producing the same
US9617303B2 (en) 2006-12-18 2017-04-11 Takeda Pharmaceutical Company Limited Sustained-release composition and method for producing the same
US9713595B2 (en) 2006-12-18 2017-07-25 Takeda Pharmaceuticals Company Limited Sustained-release composition and method for producing the same

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Publication number Publication date
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