EA201201201A1 - Новые ингибиторы rock - Google Patents

Новые ингибиторы rock

Info

Publication number
EA201201201A1
EA201201201A1 EA201201201A EA201201201A EA201201201A1 EA 201201201 A1 EA201201201 A1 EA 201201201A1 EA 201201201 A EA201201201 A EA 201201201A EA 201201201 A EA201201201 A EA 201201201A EA 201201201 A1 EA201201201 A1 EA 201201201A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
diseases
treatment
drugs
relates
Prior art date
Application number
EA201201201A
Other languages
English (en)
Other versions
EA031616B1 (ru
Inventor
Дирк Лейсен
Оливер Деферт
Надежда Каваль
Петра Блум
Сандро Боланд
Original Assignee
Амакем Нв
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
Priority claimed from GB201003395A external-priority patent/GB201003395D0/en
Priority claimed from GB201018996A external-priority patent/GB201018996D0/en
Application filed by Амакем Нв filed Critical Амакем Нв
Publication of EA201201201A1 publication Critical patent/EA201201201A1/ru
Publication of EA031616B1 publication Critical patent/EA031616B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems

Abstract

Изобретение относится к новым ингибиторам киназы, а именно к ингибиторам ROCK, композициям, в частности лекарственным препаратам, включающим такие ингибиторы, и использованию таких ингибиторов в лечении и профилактике заболеваний. В частности, настоящее изобретение относится к новым ингибиторам ROCK, композициям, а именно лекарственным препаратам, включающим такие ингибиторы, и использованию таких ингибиторов в лечении и профилактике заболеваний. Также изобретение относится к способам лечения и использованию указанных соединений при производстве лекарственных средств для применения при различных показаниях, включая сексуальную дисфункцию, воспалительные заболевания, офтальмологические заболевания и респираторные заболевания.
EA201201201A 2010-03-02 2011-03-04 Новые ингибиторы rock EA031616B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB201003395A GB201003395D0 (en) 2010-03-02 2010-03-02 Novel rock inhibitors
GB201018996A GB201018996D0 (en) 2010-11-10 2010-11-10 Novel ROCK inhibitors
PCT/EP2011/053343 WO2011107608A1 (en) 2010-03-02 2011-03-04 Heterocyclic amides as rock inhibitors

Publications (2)

Publication Number Publication Date
EA201201201A1 true EA201201201A1 (ru) 2013-05-30
EA031616B1 EA031616B1 (ru) 2019-01-31

Family

ID=43903856

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201201201A EA031616B1 (ru) 2010-03-02 2011-03-04 Новые ингибиторы rock

Country Status (17)

Country Link
US (2) US8815873B2 (ru)
EP (2) EP2626348A1 (ru)
KR (1) KR101794009B1 (ru)
AU (1) AU2011222900B2 (ru)
BR (1) BR112012021889B1 (ru)
CA (1) CA2791338C (ru)
DK (1) DK2542528T3 (ru)
EA (1) EA031616B1 (ru)
ES (1) ES2426410T3 (ru)
IL (1) IL221676A (ru)
MX (1) MX2012010174A (ru)
NZ (1) NZ602191A (ru)
PL (1) PL2542528T3 (ru)
PT (1) PT2542528E (ru)
SG (1) SG183285A1 (ru)
WO (1) WO2011107608A1 (ru)
ZA (1) ZA201206450B (ru)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112771025A (zh) * 2018-03-23 2021-05-07 重庆复创医药研究有限公司 作为rock抑制剂的氘代化合物

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201114854D0 (en) 2011-08-29 2011-10-12 Amakem Nv Novel rock inhibitors
CN103874682A (zh) 2011-08-31 2014-06-18 阿玛克姆股份有限公司 作为rock激酶抑制剂的联苯基羧酰胺
KR20150008406A (ko) 2012-05-15 2015-01-22 노파르티스 아게 Abl1, abl2 및 bcr-abl1의 활성을 억제하기 위한 벤즈아미드 유도체
EP4116293A3 (en) 2012-10-05 2023-03-29 Kadmon Corporation, LLC Rho kinase inhibitors
US9682963B2 (en) * 2013-01-29 2017-06-20 Redx Pharma Plc Pyridine derivatives as soft rock inhibitors
WO2015041533A1 (en) 2013-09-20 2015-03-26 Stichting Het Nederlands Kanker Instituut Rock in combination with mapk-pathway
EP4088719A1 (en) 2015-10-13 2022-11-16 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods and pharmaceutical compositions for the treatment of retinal capillary non-perfusion
US20180296474A1 (en) 2015-10-13 2018-10-18 INSERM (Institut National de la Santé et de la Recherche Médicale Methods and pharmaceutical compositions for the treatment of retinal capillary non-perfusion
JP2020532551A (ja) 2017-09-03 2020-11-12 アンジオン バイオメディカ コーポレーション Ｒｈｏ関連コイルドコイルキナーゼ（ＲＯＣＫ）阻害剤としてのビニルヘテロ環
US10696638B2 (en) 2017-12-26 2020-06-30 Industrial Technology Research Institute Compounds for inhibiting AGC kinase and pharmaceutical compositions comprising the same
US20210292766A1 (en) 2018-08-29 2021-09-23 University Of Massachusetts Inhibition of Protein Kinases to Treat Friedreich Ataxia

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990005723A1 (en) 1988-11-24 1990-05-31 Yoshitomi Pharmaceutical Industries, Ltd. Trans-4-amino(alkyl)-1-pyridylcarbamoyl-cyclohexane compounds and their medicinal use
IS2334B (is) 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
PT721331E (pt) 1993-10-01 2002-05-31 Astrazeneca Ab Processo i
US6043358A (en) 1995-11-01 2000-03-28 Merck & Co., Inc. Hexahydro-5-imino-1,4-heteroazepine derivatives as inhibitors of nitric oxide synthases
GB9718913D0 (en) 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
US6369087B1 (en) 1999-08-26 2002-04-09 Robert R. Whittle Alkoxy substituted benzimidazole compounds, pharmaceutical preparations containing the same, and methods of using the same
WO2007006547A1 (en) 2005-07-11 2007-01-18 Devgen N.V. Amide derivatives as kinase inhibitors
AU2006301458A1 (en) * 2005-10-13 2007-04-19 Devgen N.V. Kinase inhibitors

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112771025A (zh) * 2018-03-23 2021-05-07 重庆复创医药研究有限公司 作为rock抑制剂的氘代化合物
CN112771025B (zh) * 2018-03-23 2024-02-27 重庆复创医药研究有限公司 作为rock抑制剂的氘代化合物

Also Published As

Publication number Publication date
AU2011222900B2 (en) 2016-09-29
AU2011222900A1 (en) 2012-09-27
NZ602191A (en) 2014-07-25
MX2012010174A (es) 2012-11-30
EP2542528B1 (en) 2013-06-19
KR20130045851A (ko) 2013-05-06
KR101794009B1 (ko) 2017-11-07
PL2542528T3 (pl) 2013-11-29
PT2542528E (pt) 2013-09-09
WO2011107608A1 (en) 2011-09-09
CA2791338A1 (en) 2011-09-09
US20130252975A1 (en) 2013-09-26
US8815873B2 (en) 2014-08-26
BR112012021889B1 (pt) 2022-01-11
DK2542528T3 (da) 2013-09-23
CA2791338C (en) 2019-06-11
US20120322801A1 (en) 2012-12-20
EP2626348A1 (en) 2013-08-14
WO2011107608A8 (en) 2012-05-03
BR112012021889A2 (pt) 2017-07-18
ES2426410T3 (es) 2013-10-23
ZA201206450B (en) 2013-05-29
EP2542528A1 (en) 2013-01-09
US8912209B2 (en) 2014-12-16
EA031616B1 (ru) 2019-01-31
IL221676A (en) 2014-05-28
SG183285A1 (en) 2012-09-27

Similar Documents

Publication Publication Date Title
EA201201201A1 (ru) Новые ингибиторы rock
CY1124311T1 (el) Παρεμποδιστες dna-pk
EA201390803A1 (ru) Ингибиторы бромодомена и их применение
EA201492216A1 (ru) Ингибиторы бромодомена и их применение
EA201390711A1 (ru) Гидроксиамидные соединения пиримидина в качестве ингибиторов деацетилаз белков и способы их применения
EA201591591A1 (ru) Соединения карбазола, применяемые в качестве ингибиторов бромодомена
TR201901886T4 (tr) DNA-PK inhibitörleri.
EA202090291A3 (ru) Производные бипиразола в качестве ингибиторов jak
EA201500278A1 (ru) Пиразолилхиназолиновые ингибиторы киназы
MX362550B (es) Inhibidores ciclicos de glutaminasa.
EA201590850A1 (ru) Трициклические конденсированные производные тиофена как ингибиторы jak
EA201591166A1 (ru) Ингибиторы аутотаксина
EA201290980A1 (ru) Производные 1-амино-2-циклопропилэтилбороновой кислоты
EA201490042A1 (ru) Азетидинил-фенил-, пиридил- или пиразинилкарбоксамидные производные как ингибиторы jak
EA201291336A1 (ru) Замещенные 5-фтор-1н-пиразолопиридины и их применение
EA201590930A1 (ru) Лекарственные формы руксолитиниба с замедленным высвобождением
EA201391719A1 (ru) Хиназолиновые производные для лечения вирусных инфекций и дальнейших заболеваний
EA201300471A1 (ru) Замещенные 6-аминоникотинамиды в качестве модуляторов kcnq2/3
EA201691032A1 (ru) Производные изохромена в качестве ингибиторов фосфоинозитид-3-киназ
EA201400161A1 (ru) Замещенные гетероароматические пиразолсодержащие карбоксамидные и мочевинные производные в качестве лигандов ваниллоидных рецепторов
EA201490471A1 (ru) Пиридазиноновые соединения и их применение в качестве ингибиторов daao
EA201692313A1 (ru) Производные индолизина в качестве ингибиторов фосфоинозитид-3-киназ
EA201490515A1 (ru) Новые ингибиторы rock-киназ
UA114001C2 (xx) Оксазолідин-2-он-піримідинові похідні
EA201400623A1 (ru) Новые 2h-индазолы в качестве антагонистов рецептора ep