EA201390008A1 - Новые ариламидные производные, обладающие антиандрогенными свойствами - Google Patents

Новые ариламидные производные, обладающие антиандрогенными свойствами

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Publication number
EA201390008A1
EA201390008A1 EA201390008A EA201390008A EA201390008A1 EA 201390008 A1 EA201390008 A1 EA 201390008A1 EA 201390008 A EA201390008 A EA 201390008A EA 201390008 A EA201390008 A EA 201390008A EA 201390008 A1 EA201390008 A1 EA 201390008A1
Authority
EA
Eurasian Patent Office
Prior art keywords
arylamide derivatives
new
androgenic properties
formula
derivatives
Prior art date
Application number
EA201390008A
Other languages
English (en)
Other versions
EA022619B1 (ru
Inventor
Яри Ратилайнен
Милла Койстинахо
Ану Муона
Original Assignee
Медея Терапьютикс Лтд.
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 Медея Терапьютикс Лтд. filed Critical Медея Терапьютикс Лтд.
Publication of EA201390008A1 publication Critical patent/EA201390008A1/ru
Publication of EA022619B1 publication Critical patent/EA022619B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/59—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
    • 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
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P5/28—Antiandrogens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/46—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Abstract

Изобретение относится к новым ариламидным производным, имеющим формулу (I), и к их стереоизомерам и фармацевтически приемлемым солям, где R1-R11, R', R'', z и X являются такими же, как они определены в формуле изобретения. Ариламидные производные формулы (I) обладают антиандрогенными свойствами. Также изобретение относится к соединениям формулы (I) для применения в качестве лекарственного средства и к фармацевтическим композициям, содержащим их, и к их получению.
EA201390008A 2010-07-15 2011-07-14 Ариламидные производные, обладающие антиандрогенными свойствами EA022619B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FI20105806A FI20105806A0 (fi) 2010-07-15 2010-07-15 Uudet aryyliamidijohdannaiset, joilla on antiandrogeenisia ominaisuuksia
PCT/FI2011/050655 WO2012007644A1 (en) 2010-07-15 2011-07-14 Novel arylamide derivatives having antiandrogenic properties

Publications (2)

Publication Number Publication Date
EA201390008A1 true EA201390008A1 (ru) 2013-05-30
EA022619B1 EA022619B1 (ru) 2016-02-29

Family

ID=42555499

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201390008A EA022619B1 (ru) 2010-07-15 2011-07-14 Ариламидные производные, обладающие антиандрогенными свойствами

Country Status (18)

Country Link
US (1) US8816119B2 (ru)
EP (1) EP2593424B1 (ru)
JP (1) JP5990833B2 (ru)
KR (1) KR101928375B1 (ru)
CN (1) CN102985403B (ru)
AR (1) AR082218A1 (ru)
AU (1) AU2011278201B2 (ru)
BR (1) BR112013000783B1 (ru)
CA (1) CA2804765C (ru)
EA (1) EA022619B1 (ru)
ES (1) ES2750309T3 (ru)
FI (1) FI20105806A0 (ru)
MX (1) MX2013000474A (ru)
NZ (1) NZ605636A (ru)
SG (1) SG187049A1 (ru)
TW (1) TWI542343B (ru)
WO (1) WO2012007644A1 (ru)
ZA (1) ZA201300300B (ru)

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WO2013104831A1 (en) * 2012-01-13 2013-07-18 Medeia Therapeutics Ltd Arylamide derivatives having antiandrogenic properties
WO2016079521A1 (en) * 2014-11-20 2016-05-26 University College Cardiff Consultants Limited Androgen receptor modulators and their use as anti-cancer agents
US10441570B2 (en) 2015-04-21 2019-10-15 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) Ligands and methods of use thereof
US9815776B2 (en) 2015-04-21 2017-11-14 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10806720B2 (en) 2015-04-21 2020-10-20 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10865184B2 (en) 2015-04-21 2020-12-15 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10654809B2 (en) 2016-06-10 2020-05-19 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10093613B2 (en) 2015-04-21 2018-10-09 Gtx, Inc. Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10017471B2 (en) 2015-04-21 2018-07-10 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10035763B2 (en) 2015-04-21 2018-07-31 Gtx, Inc. Selective androgen receptor degrader (SARD) ligands and methods of use thereof
EP3286164A4 (en) 2015-04-21 2018-12-05 Gtx, Inc. Selective androgen receptor degrader (sard) ligands and methods of use thereof
US9834507B2 (en) 2015-04-21 2017-12-05 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US11230523B2 (en) 2016-06-10 2022-01-25 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof

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EP0099165A1 (en) * 1982-03-23 1984-01-25 Imperial Chemical Industries Plc Triazole and imidazole compounds, process for their preparation and their use as fungicides and plant growth regulators, and intermediates for their synthesis
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US6160011A (en) * 1997-05-30 2000-12-12 The University Of Tennessee Research Corporation Non-steroidal agonist compounds and their use in male hormone therapy
US7741371B2 (en) 2002-06-17 2010-06-22 University Of Tennessee Research Foundation Selective androgen receptor modulators and methods of use thereof
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Also Published As

Publication number Publication date
EA022619B1 (ru) 2016-02-29
TWI542343B (zh) 2016-07-21
BR112013000783B1 (pt) 2022-01-25
JP2013532178A (ja) 2013-08-15
TW201208669A (en) 2012-03-01
MX2013000474A (es) 2013-05-17
US20130109750A1 (en) 2013-05-02
EP2593424B1 (en) 2019-08-28
AU2011278201A1 (en) 2013-01-31
ZA201300300B (en) 2013-09-25
CN102985403A (zh) 2013-03-20
BR112013000783A2 (pt) 2020-11-03
JP5990833B2 (ja) 2016-09-14
AR082218A1 (es) 2012-11-21
AU2011278201B2 (en) 2014-08-21
WO2012007644A1 (en) 2012-01-19
CA2804765A1 (en) 2012-01-19
NZ605636A (en) 2014-05-30
KR101928375B1 (ko) 2018-12-12
US8816119B2 (en) 2014-08-26
CA2804765C (en) 2018-08-07
ES2750309T3 (es) 2020-03-25
KR20130079479A (ko) 2013-07-10
SG187049A1 (en) 2013-02-28
CN102985403B (zh) 2016-03-23
EP2593424A1 (en) 2013-05-22
FI20105806A0 (fi) 2010-07-15

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Designated state(s): AM AZ KZ KG MD TJ TM