IL238409A - Pde4 antitumor inhibitors - Google Patents

Pde4 antitumor inhibitors

Info

Publication number
IL238409A
IL238409A IL238409A IL23840915A IL238409A IL 238409 A IL238409 A IL 238409A IL 238409 A IL238409 A IL 238409A IL 23840915 A IL23840915 A IL 23840915A IL 238409 A IL238409 A IL 238409A
Authority
IL
Israel
Prior art keywords
pde4
heteroaryl inhibitors
heteroaryl
inhibitors
Prior art date
Application number
IL238409A
Other languages
English (en)
Hebrew (he)
Other versions
IL238409A0 (en
Inventor
E Gurney Mark
J Hagen Timothy
Mo Xuesheng
Vellekoop A
L Romero Donna
F Campbell Robert
r walker Joel
Zhu Lei
Original Assignee
Tetra Discovery Partners Llc
E Gurney Mark
J Hagen Timothy
Mo Xuesheng
Vellekoop A
L Romero Donna
F Campbell Robert
r walker Joel
Zhu Lei
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 Tetra Discovery Partners Llc, E Gurney Mark, J Hagen Timothy, Mo Xuesheng, Vellekoop A, L Romero Donna, F Campbell Robert, r walker Joel, Zhu Lei filed Critical Tetra Discovery Partners Llc
Publication of IL238409A0 publication Critical patent/IL238409A0/en
Publication of IL238409A publication Critical patent/IL238409A/en

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    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/027Organoboranes and organoborohydrides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • C07D213/04Heterocyclic 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
    • C07D213/24Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon atoms
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
IL238409A 2012-10-25 2015-04-21 Pde4 antitumor inhibitors IL238409A (en)

Applications Claiming Priority (4)

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US201261718285P 2012-10-25 2012-10-25
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Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI633087B (zh) 2012-06-13 2018-08-21 赫孚孟拉羅股份公司 新穎二氮雜螺環烷及氮雜螺環烷
RS59512B1 (sr) 2012-09-25 2019-12-31 Hoffmann La Roche Derivati heksahidropirolo[3,4−c]pirola i srodna jedinjenja kao inhibitori autotaksina (atx) i kao inhibitori proizvodnje lizofosfatidne kiseline (lpa) za lečenje npr. bubrežnih bolesti
US9221843B2 (en) 2012-10-25 2015-12-29 Tetra Discovery Partners, LLC Heteroaryl inhibitors of PDE4
EP2951173B1 (en) * 2013-02-04 2017-05-17 Grünenthal GmbH Novel substituted condensed pyrimidine compounds
WO2014117947A1 (en) * 2013-02-04 2014-08-07 Grünenthal GmbH 4-amino substituted condensed pyrimidine compounds as pde4 inhibitors
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
WO2015078803A1 (en) 2013-11-26 2015-06-04 F. Hoffmann-La Roche Ag NEW OCTAHYDRO-CYCLOBUTA [1,2-c;3,4-c']DIPYRROL-2-YL
CN106103446B (zh) 2014-03-26 2019-07-30 豪夫迈·罗氏有限公司 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的二环化合物
KR20160128428A (ko) 2014-03-26 2016-11-07 에프. 호프만-라 로슈 아게 오토탁신(atx) 및 리소포스파티드산(lpa) 생성 억제제로서의 축합형 [1,4]다이아제핀 화합물
WO2016161268A1 (en) 2015-04-01 2016-10-06 Enanta Pharmaceuticals, Inc. Hepatitis b antviral agents
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
US10738035B2 (en) 2015-05-13 2020-08-11 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
WO2017011552A1 (en) 2015-07-13 2017-01-19 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
US10301255B2 (en) 2015-07-22 2019-05-28 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
CN108026077B (zh) 2015-09-04 2021-11-05 豪夫迈·罗氏有限公司 苯氧基甲基衍生物
KR20180054635A (ko) 2015-09-24 2018-05-24 에프. 호프만-라 로슈 아게 오토탁신(atx) 억제제로서 이환형 화합물
PE20180461A1 (es) 2015-09-24 2018-03-06 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores de la atx
EP3353178B1 (en) 2015-09-24 2021-07-14 F. Hoffmann-La Roche AG Bicyclic compounds as dual atx/ca inhibitors
CR20180143A (es) 2015-09-24 2018-05-03 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de atx/ca
WO2017136403A1 (en) 2016-02-02 2017-08-10 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
CN109069488B (zh) 2016-03-07 2021-09-07 英安塔制药有限公司 乙型肝炎抗病毒剂
KR20190027814A (ko) * 2016-06-10 2019-03-15 이난타 파마슈티칼스, 인코포레이티드 B형 간염 항바이러스제
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
CN110382484B (zh) 2017-03-16 2022-12-06 豪夫迈·罗氏有限公司 新的作为atx抑制剂的二环化合物
TWI811236B (zh) 2017-08-28 2023-08-11 美商因那塔製藥公司 B型肝炎抗病毒試劑
US11365204B2 (en) 2017-09-20 2022-06-21 UNION therapeutics A/S Substituted dihydrothienopyrimidines and their use as phosphodiesterase inhibitors
TW201927789A (zh) 2017-12-06 2019-07-16 美商因那塔製藥公司 B型肝炎抗病毒試劑
WO2019113175A1 (en) 2017-12-06 2019-06-13 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
US11292799B2 (en) 2017-12-15 2022-04-05 UNION therapeutics A/S Substituted azetidine dihydrothienopyrimidines and their use as phosphodiesterase inhibitors
JP7203846B2 (ja) 2017-12-15 2023-01-13 ユニオン・セラピューティクス・アクティエセルスカブ 置換アゼチジンジヒドロチエノピリジンおよびホスホジエステラーゼ阻害剤としてのそれらの使用
WO2019143902A2 (en) 2018-01-22 2019-07-25 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
WO2019191166A1 (en) 2018-03-29 2019-10-03 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
EP3773562A1 (en) 2018-04-05 2021-02-17 Universiteit Hasselt Selective pde4d inhibitors against demyelinating diseases
CN108997394A (zh) * 2018-06-12 2018-12-14 广州百霆医药科技有限公司 苯并氧杂硼杂环戊烷类化合物及其制备方法
US10865211B2 (en) 2018-09-21 2020-12-15 Enanta Pharmaceuticals, Inc. Functionalized heterocycles as antiviral agents
PE20211546A1 (es) * 2018-10-05 2021-08-16 Pfizer Inhibidores de pde4 que contienen boro
US11198693B2 (en) 2018-11-21 2021-12-14 Enanta Pharmaceuticals, Inc. Functionalized heterocycles as antiviral agents
CN111635400A (zh) 2019-03-02 2020-09-08 察略盛医药科技(上海)有限公司 吡唑并[1,5-a]吡啶类衍生物、及其制备方法和用途
US11028050B2 (en) 2019-04-18 2021-06-08 Tetra Discovery Partners, Inc. Salts and polymorphs of a PDE4 inhibitor
EP3969458A4 (en) 2019-05-13 2023-05-17 Borah, Inc. CHEMICAL COMPOUNDS
US11236111B2 (en) 2019-06-03 2022-02-01 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
US11472808B2 (en) 2019-06-04 2022-10-18 Enanta Pharmaceuticals, Inc. Substituted pyrrolo[1,2-c]pyrimidines as hepatitis B antiviral agents
WO2020247561A1 (en) 2019-06-04 2020-12-10 Enanta Pharmaceuticals, Inc, Hepatitis b antiviral agents
AU2020300689B2 (en) * 2019-07-03 2025-09-18 Borah, Inc. Chemical compounds
US11738019B2 (en) 2019-07-11 2023-08-29 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
US11236108B2 (en) 2019-09-17 2022-02-01 Enanta Pharmaceuticals, Inc. Functionalized heterocycles as antiviral agents
US11802125B2 (en) 2020-03-16 2023-10-31 Enanta Pharmaceuticals, Inc. Functionalized heterocyclic compounds as antiviral agents
CN114149410B (zh) * 2020-09-07 2025-02-25 四川科伦博泰生物医药股份有限公司 吡啶并环类化合物及其制备方法和用途
WO2022099284A1 (en) * 2020-11-05 2022-05-12 Young Biopharma, Llc Novel capsaicin analogs and uses thereof
AU2021408311A1 (en) * 2020-12-25 2023-06-29 Reistone Biopharma Company Limited Borate derivative and uses thereof
CN115521946B (zh) * 2022-10-14 2024-06-21 浙江玖世生物科技有限公司 一种TiOx基光酶催化剂合成(R)-1-[3,5-二(三氟甲基)]苯乙醇的方法
JPWO2024135840A1 (enExample) * 2022-12-23 2024-06-27
WO2024179493A1 (zh) * 2023-02-28 2024-09-06 上海翊石医药科技有限公司 二氢噻吩并嘧啶衍生物的制备方法和用途
GB202306663D0 (en) 2023-05-05 2023-06-21 Union Therapeutics As Combination therapy
WO2025080415A1 (en) 2023-10-12 2025-04-17 Alto Neuroscience, Inc. Treatment of neuropsychiatric disorders with tilivapram
WO2025161532A1 (zh) * 2024-02-01 2025-08-07 艾派克斯生物科技有限公司 Pde4b抑制剂及其药物组合物和用途
WO2025221488A1 (en) 2024-04-16 2025-10-23 Alto Neuroscience, Inc. Transdermal administration of pde4 inhibitors for reduction in adverse events

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK23392D0 (da) 1992-02-24 1992-02-24 Novo Nordisk As Heterocykliske forbindelser, deres anvendelse og fremstilling
FR2754260B1 (fr) 1996-10-04 1998-10-30 Adir Nouveaux derives substitues de biphenyle ou de phenylpyridine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
AU5648599A (en) * 1998-09-11 2000-04-03 Kyorin Pharmaceutical Co. Ltd. Phosphonic ester derivatives and process for producing the same
WO2003076398A2 (en) 2002-03-08 2003-09-18 Eli Lilly And Company Pyrrole-2, 5-dione derivatives and their use as gsk-3 inhibitors
WO2004066952A2 (en) 2003-01-29 2004-08-12 Incyte Corporation Benzoxazole, benzothiazole, and benzimidazole derivatives for the treatment of cancer and other diseases
JP2006123639A (ja) 2004-10-27 2006-05-18 Mitsubishi Electric Corp ホームドア状態認識システム
WO2006123639A1 (ja) * 2005-05-18 2006-11-23 Asahi Kasei Pharma Corporation ピリミジン誘導体
US20060293343A1 (en) * 2005-05-18 2006-12-28 Asahi Kasei Pharma Corporation Pyrimidine derivatives
US7919519B2 (en) 2005-11-23 2011-04-05 Epix Pharmaceuticals Inc. S1P receptor modulating compounds and use thereof
WO2009146388A1 (en) 2008-05-28 2009-12-03 The Trustees Of Columbia University In The City Of New York Voxel-based methods for assessing subjects using positron emission tomography
WO2010027975A1 (en) * 2008-09-04 2010-03-11 Anacor Pharmaceuticals, Inc. Boron-containing small molecules
RU2380890C1 (ru) 2008-10-17 2010-02-10 Государственное образовательное учреждение высшего профессионального образования Марийский государственный технический университет Способ испытания травяного покрова на прирусловой пойме реки
WO2010059838A2 (en) 2008-11-20 2010-05-27 Decode Genetics Ehf Pde4 inhibitors selective for the long form of pde4 for treating inflammation and avoiding side effects
WO2010097334A1 (de) * 2009-02-27 2010-09-02 Boehringer Ingelheim International Gmbh Arzneimittelkombinationen enthaltend pde4-inhibitoren und nsaids
EP2380890A1 (en) * 2010-04-23 2011-10-26 Almirall, S.A. New 7,8-dihydro-1,6-naphthyridin-5(6h)-one-derivatives as PDE4 inhibitors
US8889123B2 (en) * 2010-08-19 2014-11-18 Allergan, Inc. Compositions and soft tissue replacement methods
US9221843B2 (en) 2012-10-25 2015-12-29 Tetra Discovery Partners, LLC Heteroaryl inhibitors of PDE4
EP2951173B1 (en) * 2013-02-04 2017-05-17 Grünenthal GmbH Novel substituted condensed pyrimidine compounds
US20150086480A1 (en) 2013-09-26 2015-03-26 Tetra Discovery Partners, LLC Heteroaryl inhibitors of pde4
WO2016049595A1 (en) 2014-09-26 2016-03-31 Tetra Discovery Partners, LLC Heteroaryl inhibitors of pde4
US11028050B2 (en) * 2019-04-18 2021-06-08 Tetra Discovery Partners, Inc. Salts and polymorphs of a PDE4 inhibitor

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