DK2683694T3 - Androgenreceptorantagonister og anvendelser deraf - Google Patents

Androgenreceptorantagonister og anvendelser deraf Download PDF

Info

Publication number
DK2683694T3
DK2683694T3 DK12755126.5T DK12755126T DK2683694T3 DK 2683694 T3 DK2683694 T3 DK 2683694T3 DK 12755126 T DK12755126 T DK 12755126T DK 2683694 T3 DK2683694 T3 DK 2683694T3
Authority
DK
Denmark
Prior art keywords
cyano
compound
hydroxyl
alkyl
optionally substituted
Prior art date
Application number
DK12755126.5T
Other languages
English (en)
Inventor
Youzhi Tong
Original Assignee
Suzhou Kintor Pharmaceuticals Inc
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 Suzhou Kintor Pharmaceuticals Inc filed Critical Suzhou Kintor Pharmaceuticals Inc
Application granted granted Critical
Publication of DK2683694T3 publication Critical patent/DK2683694T3/da

Links

Classifications

    • 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
    • C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/86—Oxygen and sulfur atoms, e.g. thiohydantoin
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • 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
    • A61P17/08—Antiseborrheics
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/42—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (14)

1. Forbindelse ifølge formel (I):
eller et farmaceutisk acceptabelt salt, solvat eller hydrat deraf, hvor Z er valgt blandt CF3, Ci-C3-alkoxy, CF3O, halogen, cyano og C1-C4-alkyl eventuelt substitueret med ét eller flere halogener, Y er valgt blandt halogen, Ci-C3-alkoxy, hydroxyl, CF3O og cyano, W er valgt blandt oxygen-, svovl- og to hydrogenatomer, R3 og R4 er valgt uafhængigt af hinanden blandt Ci-C4-alkyl, eventuelt substitueret med en eller flere fluor- eller hydroxylgrupper, eller R3 og R4 og det carbon, hvortil de er bundet, tilsammen danner en 3-6-leddet cycloalkylring, hvor ét eller flere carbonatomer eventuelt kan være substitueret med en eller flere fluor- eller hydroxylgrupper, og hvor ét af carbonatomerne eventuelt er et oxygen- eller nitrogenatom, Ai er en arylgruppe eller heteroarylgruppe, eventuelt substitueret med en eller flere Ci-C4-alkyl, cyano, hydroxyl, methoxy, ethoxyl, halogen eller en 5-6-leddet heteroarylgruppe, A2 er (CF2)a(CH2)mYi(CH2)nQ, hvor a, m og n er uafhængigt valgte heltal fra 0 til 4, og hvor mindst én af a eller m eller n ikke er nul, eller A2 er (CH2)mYi(CH2)nQ, hvor m og n er uafhængigt valgte heltal fra 0 til 4, og hvor mindst én af m eller n ikke er nul, Q er valgt blandt C(0)NHR", C(RxRy)C(0)NR"Ri", S02R", S02NR"Ri", cyano, hydroxyl, CrC3-alkoxy, C(S)NR"Ri", C(0)0R", 0C(0)NR''Ri'', C(0)NR''Ri'', 5-6-leddet heteroaryl eventuelt substitueret med hydroxyl, Ci-C3-alkoxy, Ci-C6-alkyl, halogen eller cyano, og en 4-6-leddet heterocyklisk gruppe eventuelt substitueret med hydroxyl, Ci-C3-alkoxy, CpCe-alkyl, halogen eller cyano, og Yi er valgt blandt direkte binding, -O-, -S- og NR"-, R" og Ri" er uafhængigt valgt blandt hydrogen, Ci-C6-alkyl, Ci-C6-cycloalkyl og Ci-C6-alkenyl, eller NR"Ri" tilsammen danner en 3-7-leddet heterocyklisk ring, hvor ét eller flere carbonatomer eventuelt kan være substitueret med en eller flere hydroxyl-, amino-, cyano- eller fluorgrupper, Rx og Ry er valgt uafhængigt blandt hydrogen eller methyl, eller C(RxRy) tilsammen udgør en 3-5-leddet cyklisk alkylring eventuelt substitueret med en eller flere hydroxyl-, amino-, cyano-eller fluorgrupper eller en 3-5-leddet cyklisk ring, hvor ét carbonatom er udskiftet med et oxygenatom eller en amin.
2. Forbindelse ifølge krav 1, hvor Αχ er en phenyl gruppe eller pyridylgruppe, eventuelt substitueret med en eller flere Ci-C4-alkyl, cyano, hydroxyl, methoxy, ethoxyl, halogen eller en 5-6-leddet heteroarylgruppe.
3. Forbindelse ifølge krav 1, hvor Q er en 5-6-leddet heteroarylgruppe, eventuelt substitueret med hydroxyl, Ci-C3-alkoxy, Ci-C6-alkyl, halogen eller cyano.
4. Forbindelse ifølge krav 1, hvor Q er valgt blandt
5. Forbindelse ifølge krav 1, hvor m+n er 2 eller 3.
6. Forbindelse ifølge krav 1, hvor Q er valgt blandt C(RxRy)C(0)NR"Ri", 0C(0)N"Ri", en 5-6-leddet heteroaryl eventuelt substitueret med hydroxyl, C1-C3-alkoxy, Ci-C6-alkyl, halogen eller cyano, og en 4-6-leddet heterocyklisk gruppe, eventueltsubstitueret med hydroxyl, Ci-C3-alkoxy, Ci-C6-alkyl, halogen eller cyano, og R" og Ri" er uafhængigt valgt blandt hydrogen, Ci-C6-alkyl, Ci-C6-cycloalkyl og Ci-C6-alkenyl, eller NR"Ri" tilsammen danner en 3-7-leddet heterocyklisk ring, hvor ét eller flere carbonatomer eventuelt kan være substitueret med en eller flere hydroxyl-, amino-, cyano- eller fluorgrupper, Rx og Ry er uafhængigt valgt blandt hydrogen eller methyl, eller C(RxRy) tilsammen udgør en 3-5-leddet cyklisk alkylring, eventuelt substitueret med en eller flere hydroxyl-, amino-, cyano- eller fluorgrupper eller en 3-5-leddet cyklisk ring, hvor ét carbonatom er udskiftet med et oxygenatom eller en amin.
7. Forbindelse ifølge krav 1, hvor Q er en 4-6-leddet heterocyklisk gruppe eventuelt substitueret med hydroxyl, Ci-C3-alkoxy, Ci-C6-alkyl, halogen eller cyano.
8. Forbindelse ifølge krav 1, valgt blandt
9. Farmaceutisk præparat, der omfatteren forbindelse ifølge krav 1 og en farmaceutisk acceptabel bærer, fortyndingsmiddel eller excipiens.
10. Topisk farmaceutisk formulering, der omfatter en forbindelse ifølge krav 1 til anvendelse i dermal brug.
11. Forbindelse ifølge krav 1 eller præparat ifølge krav 9 til anvendelse i behandling.
12. Forbindelse ifølge krav 1 eller præparat ifølge krav 9 til anvendelse til forebyggelse, reduktion af progrediering, behandling eller regression af en sygdom eller lidelse valgt blandt hormonsensitiv prostatakræft eller hormonresistent prostatakræft, godartet prostatahyperplasi, acne, hirsutisme, overskydende talgproduktion, alopeci, hyperseksualitet, seksuel afvigelse og maskulinisering i tilfældet af trans seksuelle kvinder, der gennemgår kønsskiftebehandling.
13. Forbindelse ifølge krav 1 eller præparat ifølge krav 9 til anvendelse som mandlig prævention.
14. Forbindelse ifølge krav 1 eller præparat ifølge krav 9 til anvendelse til reduktion af forekomsten, standsning eller forårsagelse af regression af prostatakræft.
DK12755126.5T 2011-03-10 2012-03-08 Androgenreceptorantagonister og anvendelser deraf DK2683694T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161451120P 2011-03-10 2011-03-10
PCT/CN2012/072091 WO2012119559A1 (en) 2011-03-10 2012-03-08 Androgen receptor antagonists and uses thereof

Publications (1)

Publication Number Publication Date
DK2683694T3 true DK2683694T3 (da) 2016-07-18

Family

ID=46797504

Family Applications (1)

Application Number Title Priority Date Filing Date
DK12755126.5T DK2683694T3 (da) 2011-03-10 2012-03-08 Androgenreceptorantagonister og anvendelser deraf

Country Status (13)

Country Link
US (1) US9216957B2 (da)
EP (1) EP2683694B1 (da)
JP (1) JP5833681B2 (da)
KR (1) KR101567958B1 (da)
CN (1) CN103608333B (da)
AU (1) AU2012225038B2 (da)
BR (1) BR112013023028B1 (da)
CA (1) CA2829322C (da)
DK (1) DK2683694T3 (da)
PL (1) PL2683694T3 (da)
RU (1) RU2598854C2 (da)
WO (1) WO2012119559A1 (da)
ZA (1) ZA201307115B (da)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2835248T3 (es) 2012-09-04 2021-06-22 Jiangsu Hengrui Medicine Co Derivados de imidazolina, métodos de preparación de los mismos y sus aplicaciones en medicina
WO2015042029A1 (en) * 2013-09-19 2015-03-26 Glaxosmithkline Llc Combination drug therapy
IL252843B1 (en) * 2014-12-19 2024-10-01 Aragon Pharmaceuticals Inc A process for preparing a diarylthiohydantoin compound
CN106810542B (zh) * 2015-11-30 2021-03-09 苏州开拓药业股份有限公司 一种硫代咪唑烷酮化合物的晶型、盐型及其制备方法
TWI726969B (zh) 2016-01-11 2021-05-11 比利時商健生藥品公司 用作雄性激素受體拮抗劑之經取代之硫尿囊素衍生物
KR102125661B1 (ko) * 2017-02-13 2020-06-22 강푸 바이오파마슈티칼즈 리미티드 전립선암 치료용 조합, 약학 조성물 및 치료 방법
WO2019025250A1 (en) 2017-08-04 2019-02-07 Basf Se SUBSTITUTED TRIFLUOROMETHYLOXADIAZOLES FOR COMBATING PHYTOPATHOGENIC FUNGI
JP2022509917A (ja) 2018-11-05 2022-01-25 ファイザー・インク がんを処置するための組合せ
AU2019387367A1 (en) 2018-11-30 2021-06-10 Nuvation Bio Inc. Diarylhydantoin compounds and methods of use thereof
MX2021007475A (es) 2018-12-19 2021-08-05 Celgene Corp Compuestos de 3-((3-aminofenil)amino)piperidina-2,6-diona sustituida, composiciones de estos y metodos de tratamiento con estos.
CN113453681B (zh) 2018-12-19 2024-10-11 细胞基因公司 经取代的3-((3-氨基苯基)氨基)哌啶-2，6-二酮化合物、其组合物及使用它们的治疗方法
CN113143924B (zh) * 2020-12-31 2023-04-14 苏州开拓药业股份有限公司 硫代咪唑烷酮药物在治疗covid-19疾病中的用途
CN114805327A (zh) * 2021-01-29 2022-07-29 苏州开拓药业股份有限公司 一种硫代乙内酰脲药物用中间体及其制备方法与用途
EP4288051A1 (en) * 2021-02-04 2023-12-13 Suzhou Kintor Pharmaceuticals, Inc. Compositions and methods for treatment of hidradenitis suppurativa
CN113717166B (zh) * 2021-03-12 2024-04-05 杭州科巢生物科技有限公司 一种普克鲁胺的合成方法
CN117642410A (zh) * 2021-06-18 2024-03-01 苏州春海生物医药有限公司 N4-羟基胞苷的酯衍生物及其用途
CN114014850A (zh) * 2021-12-17 2022-02-08 山东汇海医药化工有限公司 一种普克鲁胺中间体及其合成方法及由该中间体合成普克鲁胺的方法
CN114181138B (zh) * 2021-12-23 2023-09-05 大连万福制药有限公司 一种硝基吡啶丁酰胺的衍生物制备普克鲁胺中间体的方法
CN115286623B (zh) * 2022-07-15 2024-09-10 深圳湾实验室 普克鲁胺的合成方法和其中间体
CN115181043B (zh) * 2022-07-27 2024-05-07 爱斯特（成都）生物制药股份有限公司 一种连续流制备4-异硫氰基-2-(三氟甲基)苯甲腈的方法
WO2024022483A1 (en) * 2022-07-28 2024-02-01 Suzhou Kintor Pharmaceuticals, Inc. A bifunctional pharmaceutical intermediate and its preparation method and use
WO2024022475A1 (en) * 2022-07-28 2024-02-01 Suzhou Kintor Pharmaceuticals, Inc. A pyridinyl substituted thiohydantoin pharmaceutical intermediate and its preparation method and use
CN115819303B (zh) * 2022-11-15 2024-10-01 江苏睿实生物科技有限公司 一种化合物3-氟-4-异硫氰基-2-三氟甲基苄腈的制备方法
WO2024121163A1 (en) 2022-12-06 2024-06-13 Cancer Research Technology Limited Combination of 10d1f and an androgen inhibitor for treatment and prevention of cancers

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2694290B1 (fr) 1992-07-08 1994-09-02 Roussel Uclaf Nouvelles phénylimidazolidines éventuellement substituées, leur procédé de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant.
FR2715402B1 (fr) * 1994-01-05 1996-10-04 Roussel Uclaf Nouvelles phénylimidazolines éventuellement substituées, leur procédé et des intermédiaires de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant.
TW521073B (en) 1994-01-05 2003-02-21 Hoechst Marion Roussel Inc New optionally substituted phenylimidazolidines, their preparation process, their use as anti-androgenic agent and the pharmaceutical compositions containing them
FR2725206B1 (fr) 1994-09-29 1996-12-06 Roussel Uclaf Nouvelles imidazolidines substituees par un heterocycle, leur procede et des intermediaires de preparation, leur application comme medicaments et les compositions pharmaceutiques les renfermant
FR2741342B1 (fr) 1995-11-22 1998-02-06 Roussel Uclaf Nouvelles phenylimidazolidines fluorees ou hydroxylees, procede, intermediaires de preparation, application comme medicaments, nouvelle utilisation et compositions pharmaceutiques
FR2742749B1 (fr) 1995-12-22 1998-02-06 Roussel Uclaf Nouvelles phenylimidazolidines comportant notamment un radical nitrooxy ou carbonyloxy, procede et intermediaires de preparation, application comme medicaments, nouvelles utilisations et compositions pharmaceutiques
US6982265B1 (en) 1999-05-21 2006-01-03 Bristol Myers Squibb Company Pyrrolotriazine inhibitors of kinases
JP2006510600A (ja) 2002-10-04 2006-03-30 ラボラトワール フルニエ エス・アー ２−チオヒダントインに由来する化合物及び治療におけるその使用
EP1634874A4 (en) 2003-06-12 2008-04-02 Chugai Pharmaceutical Co Ltd imidazolidine
JP4912148B2 (ja) 2004-08-03 2012-04-11 中外製薬株式会社 新規イミダゾリジン誘導体
TW200621723A (en) 2004-09-09 2006-07-01 Chugai Pharmaceutical Co Ltd Novel imidazolidine derivative and use thereof
US7709517B2 (en) 2005-05-13 2010-05-04 The Regents Of The University Of California Diarylhydantoin compounds
EP1893196B2 (en) 2005-05-13 2015-07-29 The Regents of The University of California Diarylhydantoin compound
US7709516B2 (en) 2005-06-17 2010-05-04 Endorecherche, Inc. Helix 12 directed non-steroidal antiandrogens
MX2008012492A (es) * 2006-03-29 2008-12-12 Univ California Compuestos de diariltiohidantoina.
GB0610765D0 (en) 2006-05-31 2006-07-12 Proskelia Sas Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such
TW200846338A (en) * 2007-02-01 2008-12-01 Chugai Pharmaceutical Co Ltd Pyridyl imidazolidine derivative having sulfamoyl group, and pharmaceutical use thereof
JP5535925B2 (ja) 2007-10-26 2014-07-02 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア アンドロゲン受容体調節物質としてのジアリールヒダントイン化合物
GB2463514C (en) 2008-09-11 2018-09-26 Galapagos Nv Imidazolidine compounds and uses therefor
CN101817787B (zh) * 2009-02-26 2013-07-24 童友之 抗前列腺癌的雄性激素受体拮抗剂
WO2010118354A1 (en) 2009-04-09 2010-10-14 Medivation Prostate Therapeutics, Inc. Substituted di-arylhydantoin and di-arylthiohydantoin compounds and methods for use thereof
US8809550B2 (en) 2009-09-10 2014-08-19 Youzhi Tong Androgen receptor antagonists and uses thereof
CN201520005U (zh) 2009-09-14 2010-07-07 三一重工股份有限公司 混凝土搅拌站上的收尘装置及带收尘装置的混凝土搅拌系统
DK3124481T3 (da) 2010-02-16 2018-05-07 Aragon Pharmaceuticals Inc Androgen-receptormodulatorer og anvendelser deraf
DK2538785T3 (da) 2010-02-24 2018-05-22 Medivation Prostate Therapeutics Llc Fremgangsmåder til syntese af diarylthiohydantoin- og diarylhydantoinforbindelser
RU2434851C1 (ru) * 2010-07-22 2011-11-27 Александр Васильевич Иващенко Циклические n, n'-диарилтиомочевины или n, n'-диарилмочевины - антагонисты андрогенных рецепторов, противораковое средство, способ получения и применения

Also Published As

Publication number Publication date
EP2683694A4 (en) 2014-08-27
CN103608333B (zh) 2016-01-06
AU2012225038B2 (en) 2016-03-10
KR20130131462A (ko) 2013-12-03
US20140066425A1 (en) 2014-03-06
BR112013023028A2 (pt) 2016-12-13
JP5833681B2 (ja) 2015-12-16
ZA201307115B (en) 2014-05-28
CA2829322A1 (en) 2012-09-13
PL2683694T3 (pl) 2016-10-31
CA2829322C (en) 2017-01-10
RU2598854C2 (ru) 2016-09-27
EP2683694B1 (en) 2016-04-27
EP2683694A1 (en) 2014-01-15
JP2014510074A (ja) 2014-04-24
AU2012225038A1 (en) 2013-10-03
CN103608333A (zh) 2014-02-26
BR112013023028B1 (pt) 2021-09-21
KR101567958B1 (ko) 2015-11-10
WO2012119559A1 (en) 2012-09-13
RU2014138827A (ru) 2016-04-10
US9216957B2 (en) 2015-12-22

Similar Documents

Publication Publication Date Title
DK2683694T3 (da) Androgenreceptorantagonister og anvendelser deraf
CA2772579C (en) Thioimidazolidinone androgen receptor antagonists and uses thereof
CN100482659C (zh) 具有5-ht4受体激动活性的苯并咪唑酮化合物
CN113474335A (zh) 新型化合物及其作为甲状腺激素受体激动剂的用途
TWI338685B (en) N3 alkylated benzimid azole derivatives as mek inhibitors
CN105452226A (zh) 四氢-和二氢-异喹啉prmt5抑制剂及其用途
KR20080073337A (ko) 옥사졸 화합물 및 제약 조성물
JP2007536366A (ja) 置換メチルアリール又はヘテロアリールアミド化合物
PT2089367E (pt) Compostos de pirazolina como antagonistas dos receptores mineralcorticóides
JPH10510281A (ja) イミダゾール誘導体
KR20160006207A (ko) 사이클로알킬산 유도체, 그의 제조 방법, 및 그의 약학적 용도
JP2013532657A (ja) 環式ｎ，ｎ’−ジアリールチオ尿素及びｎ，ｎ’−ジアリール尿素−アンドロゲン受容体アンタゴニスト、抗癌剤、その調製のための方法及び使用
US20100216823A1 (en) Spirocyclic Derivatives
JP4174068B1 (ja) アンドロゲンモジュレーター
MXPA02006723A (es) Sulfonil-heteroaril-triazoles como agentes anti-inflamatorios/analgesicos.
MXPA02006722A (es) Sulfonilaril triazoles como agentes antiinflamatorios / analgesicos.
TW202434591A (zh) 具有apj受體活性之化合物之鹽及固體形式
KR20110106312A (ko) 인다닐 화합물