EA201490653A1 - Производные эстра-1,3,5(10),16-тетраен-3-карбоксамида, способ их получения, содержащие их фармацевтические препараты, а также их применение для получения лекарственных средств - Google Patents

Производные эстра-1,3,5(10),16-тетраен-3-карбоксамида, способ их получения, содержащие их фармацевтические препараты, а также их применение для получения лекарственных средств

Info

Publication number
EA201490653A1
EA201490653A1 EA201490653A EA201490653A EA201490653A1 EA 201490653 A1 EA201490653 A1 EA 201490653A1 EA 201490653 A EA201490653 A EA 201490653A EA 201490653 A EA201490653 A EA 201490653A EA 201490653 A1 EA201490653 A1 EA 201490653A1
Authority
EA
Eurasian Patent Office
Prior art keywords
tetraen
estra
carboxamide
derivatives
pharmaceutical preparations
Prior art date
Application number
EA201490653A
Other languages
English (en)
Other versions
EA025518B1 (ru
EA025518B9 (ru
Inventor
Ульрих Ботэ
Наоми Барак
Маттиас Буземанн
Оливер Мартин Фишер
Андреа Ротгери
Изабелла Гашав
Инго Хартунг
Тобиас Марквардт
Original Assignee
Байер Интеллектуэль Проперти Гмбх
Байер Фарма Акциенгезельшафт
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46963705&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201490653(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Байер Интеллектуэль Проперти Гмбх, Байер Фарма Акциенгезельшафт filed Critical Байер Интеллектуэль Проперти Гмбх
Publication of EA201490653A1 publication Critical patent/EA201490653A1/ru
Publication of EA025518B1 publication Critical patent/EA025518B1/ru
Publication of EA025518B9 publication Critical patent/EA025518B9/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • 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
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61P11/00—Drugs for disorders of the respiratory 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
    • 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
    • A61P17/10—Anti-acne agents
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • 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
    • A61P5/32—Antioestrogens

Abstract

Заявка касается ингибиторов AKR1C3 и способа их получения, их применения для лечения и/или предупреждения заболеваний, а также их применения для изготовления лекарственных средств для лечения и/или предупреждения заболеваний, в частности для лечения и/или предупреждения маточных кровотечений и эндометриоза.
EA201490653A 2011-09-29 2012-09-24 Производные эстра-1,3,5(10),16-тетраен-3-карбоксамида, способ их получения, содержащие их фармацевтические препараты, а также их применение для получения лекарственных средств EA025518B9 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102011083725A DE102011083725A1 (de) 2011-09-29 2011-09-29 Estra-1,3,5(10),16-tetraen-3-carboxamid-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln
PCT/EP2012/068803 WO2013045407A1 (de) 2011-09-29 2012-09-24 Estra-1,3,5(10),16-tetraen-3-carboxamid-derivate, verfahren zu ihrer herstellung, pharmazeutische präparate, die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln

Publications (3)

Publication Number Publication Date
EA201490653A1 true EA201490653A1 (ru) 2014-09-30
EA025518B1 EA025518B1 (ru) 2016-12-30
EA025518B9 EA025518B9 (ru) 2017-10-31

Family

ID=46963705

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201490653A EA025518B9 (ru) 2011-09-29 2012-09-24 Производные эстра-1,3,5(10),16-тетраен-3-карбоксамида, способ их получения, содержащие их фармацевтические препараты, а также их применение для получения лекарственных средств

Country Status (42)

Country Link
US (1) US9487554B2 (ru)
EP (1) EP2760878B1 (ru)
JP (1) JP5791810B2 (ru)
KR (1) KR20140069013A (ru)
CN (1) CN103827133B (ru)
AP (1) AP2014007598A0 (ru)
AR (1) AR088180A1 (ru)
AU (1) AU2012314627B2 (ru)
BR (1) BR112014007223A2 (ru)
CA (1) CA2850047C (ru)
CL (1) CL2014000775A1 (ru)
CO (1) CO6920294A2 (ru)
CR (1) CR20140144A (ru)
CU (1) CU20140037A7 (ru)
CY (1) CY1117123T1 (ru)
DE (1) DE102011083725A1 (ru)
DK (1) DK2760878T3 (ru)
DO (1) DOP2014000059A (ru)
EA (1) EA025518B9 (ru)
EC (1) ECSP14013275A (ru)
ES (1) ES2560257T3 (ru)
GT (1) GT201400059A (ru)
HK (1) HK1197414A1 (ru)
HR (1) HRP20160050T1 (ru)
HU (1) HUE026645T2 (ru)
IL (1) IL231755A (ru)
JO (1) JO3122B1 (ru)
MA (1) MA35455B1 (ru)
MX (1) MX2014003823A (ru)
MY (1) MY175804A (ru)
PE (1) PE20141554A1 (ru)
PL (1) PL2760878T3 (ru)
PT (1) PT2760878E (ru)
RS (1) RS54521B1 (ru)
SG (1) SG11201400144SA (ru)
SI (1) SI2760878T1 (ru)
TN (1) TN2014000131A1 (ru)
TW (1) TWI537284B (ru)
UA (1) UA107550C2 (ru)
UY (1) UY34356A (ru)
WO (1) WO2013045407A1 (ru)
ZA (1) ZA201401568B (ru)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112015000443A2 (pt) 2012-07-10 2017-06-27 Bayer Pharma AG derivados de estra-1,3,5(10),16-tetraeno 3-substituídos, processo para a sua produção, preparações farmacêuticas que contêm os mesmos, bem como seu uso para a produção de medicamentos
CN105008382B (zh) 2013-02-21 2018-01-30 拜耳医药股份公司 用于抑制17β‑羟类固醇脱氢酶(AKR1 C3)的雌甾‑1,3,5(10),16‑四烯‑3‑羧酰胺
JP6407415B2 (ja) * 2014-09-11 2018-10-17 バイエル・ファルマ・アクティエンゲゼルシャフト ３−窒素または硫黄置換エストラ−１，３，５（１０），１６−テトラエンａｋｒ１ｃ３阻害剤
US10167293B2 (en) 2016-05-26 2019-01-01 Bayer Pharma Aktiengesellschaft [8-(phenylsulfonyl)-3,8-diazabicyclo[3.2.1]oct-3-yl](1H-1,2,3-triazol-4-yl)methanones
CZ307437B6 (cs) 2016-06-07 2018-08-22 Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v.v.i. 15β-substituované deriváty estronu jako selektivní inhibitory 17β-hydroxysteoiddehydrogenáz
EP3269373A1 (en) * 2016-07-11 2018-01-17 Bayer Pharma Aktiengesellschaft Low-dosed oral dosage form of an akr1c3 inhibitor for treatment of diseases
US20200087284A1 (en) 2016-12-19 2020-03-19 Bayer Pharma Aktiengesellschaft [4-(phenylsulfonyl)piperazin-1-yl](1h-1, 2, 3-triazol-4-yl)methanones
TW201825478A (zh) 2016-12-19 2018-07-16 德商拜耳製藥公司 ［４－（苯基磺醯基）哌嗪－１－-基］（１ｈ－１，２，３－三唑－４-基）甲酮
CA3047196A1 (en) 2016-12-19 2018-06-28 Bayer Pharma Aktiengesellschaft [(phenylsulfonyl)octahydro-epiminoisoindol-yl](1h-1,2,3-triazol-5-yl)methanones
EP3421483A1 (en) 2017-06-29 2019-01-02 Bayer Pharma Aktiengesellschaft Novel steroidal 17-beta heteroaryl compounds as inhibitors of akr1c3
CN108503695B (zh) * 2018-03-09 2021-06-08 南方医科大学南方医院 基于GnRH多肽衍生物的示踪剂及其制备方法和应用
CN110693892A (zh) * 2018-07-09 2020-01-17 深圳艾欣达伟医药科技有限公司 化合物用于制备预防、治疗或改善疼痛的药物的用途
CN113683648A (zh) * 2021-08-26 2021-11-23 上海皓鸿生物医药科技有限公司 一种2’-氟-2’-脱氧尿苷的合成方法及其中间体

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4632003A (en) 1985-07-15 1986-12-30 Kopp William L Musical instrument sound quality enhancement device
ES2138618T3 (es) * 1992-03-31 2000-01-16 Btg Int Ltd Esteroides 17-sustituidos utiles en el tratamiento del cancer.
US5604213A (en) 1992-03-31 1997-02-18 British Technology Group Limited 17-substituted steroids useful in cancer treatment
CA2323089A1 (en) * 1998-03-11 1999-09-16 Endorecherche, Inc. Inhibitors of type 5 and type 3 17.beta.-hydroxysteroid dehydrogenase and methods for their use
CA2558014A1 (en) 2004-03-12 2005-09-29 Entremed, Inc. Antiangiogenic agents
WO2008065100A1 (en) * 2006-11-30 2008-06-05 Solvay Pharmaceuticals Gmbh Substituted estratrien derivatives as 17beta hsd inhibitors
US20110118219A1 (en) 2008-03-25 2011-05-19 University Of Maryland, Baltimore Novel prodrugs of c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity
US20110312916A1 (en) 2009-02-05 2011-12-22 Tokai Pharmaceuticals, Inc. Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
CN102947322B (zh) 2010-04-27 2016-09-07 法马马有限公司 在7（8）位不饱和的抗癌甾体内酯

Also Published As

Publication number Publication date
HK1197414A1 (zh) 2015-01-16
KR20140069013A (ko) 2014-06-09
TN2014000131A1 (en) 2015-07-01
DOP2014000059A (es) 2014-06-15
ES2560257T3 (es) 2016-02-18
DE102011083725A1 (de) 2013-04-04
MX2014003823A (es) 2014-06-04
SI2760878T1 (sl) 2016-02-29
CL2014000775A1 (es) 2014-08-18
HRP20160050T1 (hr) 2016-02-12
MA35455B1 (fr) 2014-09-01
JP2014527994A (ja) 2014-10-23
CR20140144A (es) 2014-05-16
AU2012314627B2 (en) 2016-08-18
EA025518B1 (ru) 2016-12-30
CU20140037A7 (es) 2014-07-30
IL231755A (en) 2016-06-30
HUE026645T2 (en) 2016-07-28
JP5791810B2 (ja) 2015-10-07
JO3122B1 (ar) 2017-09-20
PE20141554A1 (es) 2014-10-24
TWI537284B (zh) 2016-06-11
AU2012314627A1 (en) 2014-04-10
NZ622081A (en) 2015-10-30
TW201317253A (zh) 2013-05-01
WO2013045407A1 (de) 2013-04-04
PT2760878E (pt) 2016-02-26
MY175804A (en) 2020-07-09
AP2014007598A0 (en) 2014-04-30
CO6920294A2 (es) 2014-04-10
BR112014007223A2 (pt) 2017-04-04
CA2850047A1 (en) 2013-04-04
UA107550C2 (ru) 2015-01-12
RS54521B1 (en) 2016-06-30
CN103827133B (zh) 2015-11-25
ECSP14013275A (es) 2014-04-30
ZA201401568B (en) 2016-11-30
SG11201400144SA (en) 2014-05-29
UY34356A (es) 2013-04-30
CY1117123T1 (el) 2017-04-05
CA2850047C (en) 2016-03-29
AR088180A1 (es) 2014-05-14
GT201400059A (es) 2015-02-17
DK2760878T3 (en) 2016-01-25
US20140249119A1 (en) 2014-09-04
CN103827133A (zh) 2014-05-28
EP2760878A1 (de) 2014-08-06
EA025518B9 (ru) 2017-10-31
EP2760878B1 (de) 2015-10-28
US9487554B2 (en) 2016-11-08
PL2760878T3 (pl) 2016-04-29

Similar Documents

Publication Publication Date Title
EA201490653A1 (ru) Производные эстра-1,3,5(10),16-тетраен-3-карбоксамида, способ их получения, содержащие их фармацевтические препараты, а также их применение для получения лекарственных средств
EA201591166A1 (ru) Ингибиторы аутотаксина
PH12015502002B1 (en) Tripeptide epoxy ketone protease inhibitors
EA201590343A1 (ru) Алкилпиримидиновые производные для лечения вирусных инфекций и дальнейших заболеваний
EA201200551A1 (ru) Фармацевтическая композиция, фармацевтическая дозированная форма, способы их получения и применения для лечения
UY33370A (es) Composiciones farmacéuticas comprendiendo un fármaco inhibidor de la DPP4 y de la pioglitazona, procedimientos de preparación y utilización
EA201290980A1 (ru) Производные 1-амино-2-циклопропилэтилбороновой кислоты
EA201591371A1 (ru) Пиридиновые производные в качестве легкоразлагаемых ингибиторов rock
EA201590667A1 (ru) Ациламинопиримидиновые производные для лечения вирусных инфекций и других заболеваний
EA201391719A1 (ru) Хиназолиновые производные для лечения вирусных инфекций и дальнейших заболеваний
EA201270780A1 (ru) С-3 модифицированные производные бетулиновой кислоты в качестве ингибиторов созревания вич
EA201300669A1 (ru) Замещенные 1-бензилциклоалкилкарбоновые кислоты и их применение
EA201001577A1 (ru) Ингибитор дпп-4 в комбинации с дополнительным противодиабетическим агентом, таблетки, включающие указанные композиции, их применение и способ их получения
PH12015502539A1 (en) Cenicriviroc compositions and methods of making and using the same
EA201500112A1 (ru) 3-замещенные производные эстра-1,3,5(10),16-тетраена, способы их получения, фармацевтические средства, которые их содержат, и их использование для получения лекарственных средств
EA201500851A1 (ru) ЭСТРА-1,3,5(10),16-ТЕТРАЕН-3-КАРБОКСАМИДЫ ДЛЯ ИНГИБИРОВАНИЯ 17β-ГИДРОКСИСТЕРОИД-ДЕГИДРОГЕНАЗЫ (AKR1C3)
EA200801580A1 (ru) Новые производные пирониндола и способ их получения
JO3326B1 (ar) مثبطات إيبوكسي كيتون بروتياز ثلاثي الببتيد
EA201592254A1 (ru) Производные пиразолопирролидин-4-она и их применение при лечении заболевания
TR201905218T4 (tr) Nörodejenerati̇f hastaliklarin tedavi̇si̇ i̇çi̇n yararli vi̇tanoli̇dler.
EA201592242A1 (ru) Производные пиридона для лечения вирусных инфекций и других заболеваний
BR112016007031A8 (pt) composição farmacêutica oral sólida, processo para preparar a composição farmacêutica oral sólida, e uso de uma composição farcêutica oral sólida
EA201400444A1 (ru) Производные 2-оксопиперидинила
EA201200799A1 (ru) Гепатопротекторное средство

Legal Events

Date Code Title Description
TH4A Publication of the corrected specification to eurasian patent
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AZ KG TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM BY KZ RU