AR095707A1 - Derivados de piperazina como inhibidores de fasn - Google Patents
Derivados de piperazina como inhibidores de fasnInfo
- Publication number
- AR095707A1 AR095707A1 ARP140101320A ARP140101320A AR095707A1 AR 095707 A1 AR095707 A1 AR 095707A1 AR P140101320 A ARP140101320 A AR P140101320A AR P140101320 A ARP140101320 A AR P140101320A AR 095707 A1 AR095707 A1 AR 095707A1
- Authority
- AR
- Argentina
- Prior art keywords
- denotes
- atoms
- hal
- branched
- alkyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 102100022089 Acyl-[acyl-carrier-protein] hydrolase Human genes 0.000 title 1
- 101000824278 Homo sapiens Acyl-[acyl-carrier-protein] hydrolase Proteins 0.000 title 1
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical class C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 title 1
- 229940066771 systemic antihistamines piperazine derivative Drugs 0.000 title 1
- -1 [1,8] naphthyridinyl Chemical group 0.000 abstract 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 102000015303 Fatty Acid Synthases Human genes 0.000 abstract 1
- 108010039731 Fatty Acid Synthases Proteins 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000001738 Nervous System Trauma Diseases 0.000 abstract 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 abstract 1
- 125000005874 benzothiadiazolyl group Chemical group 0.000 abstract 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 abstract 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 abstract 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 125000005956 isoquinolyl group Chemical group 0.000 abstract 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 208000028412 nervous system injury Diseases 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000005493 quinolyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
-
- 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
- A61K31/495—Heterocyclic 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
- C07D217/08—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with a hetero atom directly attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
- C07D217/24—Oxygen atoms
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Son inhibidores de sintasa de ácidos grasos y se pueden emplear, inter alia, para el tratamiento de enfermedades tales como cáncer, enfermedades cardiovasculares, lesión del sistema nervioso central y diferentes formas de inflamación. Reivindicación 1: Compuestos de la fórmula (1), en donde R denota naftilo, [1,8]naftiridinilo, benzoxazolilo, benzotiazolilo, bencimidazolilo, benzotriazolilo, indolilo, benzo-1,3-dioxolilo, benzodioxanilo, benzotia diazolilo, indazolilo, benzofuranilo, quinolilo, isoquinolilo, oxazolo[5,4-b]piridilo u oxazolo[5,4-c]piridilo, cada uno de los cuales no está sustituido o está mono- o disustituido con Hal, A y/o [C(R³)₂]ₙOA, y/o en donde un átomo de nitrógeno puede estar oxidado; R¹ denota A o [C(R³)₂]ₙCyc; R² denota F, Cl, Br, OH, CN, NO₂, A, OA, SA, SO₂Me, COA, CONH₂, CONHA o CONA₂; X¹, X², X³, X⁴ cada uno denota, de modo independiente entre sí, CH o N; A denota alquilo no ramificado o ramificado C₁₋₁₀, en donde dos átomos de carbono adyacentes pueden formar un enlace doble y/o uno o dos grupos CH y/o CH₂ no adyacentes pueden estar reemplazados por átomos de N, O y/o S y en donde 1 - 7 átomos de H pueden estar reemplazados por R⁵; Cyc denota cicloalquilo C₃₋₇, que no está sustituido o que está monosustituido con OH, Hal o A; A denota alquilo no ramificado o ramificado C₁₋₆, en donde 1 - 5 átomos de H pueden estar reemplazados por F; R³ denota H o alquilo no ramificado o ramificado C₁₋₆; R⁵ denota F, Cl u OH; Hal denota F, Cl, Br o I; n denota 0, 1 ó 2; q denota 0, 1, 2 ó 3; siempre que sólo uno o dos de X¹, X², X³, X⁴ denoten N; y sus sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13001462 | 2013-03-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR095707A1 true AR095707A1 (es) | 2015-11-04 |
Family
ID=47912880
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140101320A AR095707A1 (es) | 2013-03-21 | 2014-03-21 | Derivados de piperazina como inhibidores de fasn |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9809552B2 (es) |
| EP (1) | EP2976328B2 (es) |
| JP (2) | JP6412553B2 (es) |
| CN (1) | CN105008329B (es) |
| AR (1) | AR095707A1 (es) |
| AU (1) | AU2014234721A1 (es) |
| CA (1) | CA2907657A1 (es) |
| ES (1) | ES2634875T3 (es) |
| IL (1) | IL241513A0 (es) |
| WO (1) | WO2014146747A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014164767A1 (en) | 2013-03-13 | 2014-10-09 | Forma Therapeutics, Inc. | Novel compounds and compositions for inhibition of fasn |
| JP6986972B2 (ja) | 2015-06-18 | 2021-12-22 | エイティナイン バイオ リミテッド | 置換４−ベンジル及び４−ベンゾイルピペリジン誘導体 |
| ES2821049T3 (es) | 2015-06-18 | 2021-04-23 | 89Bio Ltd | Derivados de piperidina 1,4 sustituidos |
| EP3458448B1 (en) | 2016-04-25 | 2021-06-23 | Forma Therapeutics, Inc. | Fasn inhibitors for use in treating non-alcoholic steatohepatitis |
| TWI767148B (zh) | 2018-10-10 | 2022-06-11 | 美商弗瑪治療公司 | 抑制脂肪酸合成酶(fasn) |
| US10793554B2 (en) | 2018-10-29 | 2020-10-06 | Forma Therapeutics, Inc. | Solid forms of 4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19743435A1 (de) | 1997-10-01 | 1999-04-08 | Merck Patent Gmbh | Benzamidinderivate |
| DE102007007751A1 (de) * | 2007-02-16 | 2008-08-21 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue substituierte Arylsulfonylglycine, deren Herstellung und deren Verwendung als Arzneimittel |
| EP2247600A4 (en) | 2008-02-06 | 2011-09-14 | Biomarin Pharm Inc | BENZOXAZOLEBOXYLIC ACID AMIDE AS INHIBITORS OF POLY (ADP-RIBOSE) POLYMERASE (PARP) |
| US8614238B2 (en) | 2009-10-19 | 2013-12-24 | Boehringer Ingelheim International Gmbh | Cyclopentanecarboxamide derivatives, medicaments containing such compounds and their use |
| KR101261702B1 (ko) * | 2011-01-07 | 2013-05-06 | 이화여자대학교 산학협력단 | 신규한 2-페닐퀴나졸린-4(3ｈ)-온 유도체, 그 제조방법 및 그 약학적 조성물 |
| CN102627610B (zh) | 2012-04-11 | 2014-06-25 | 江苏先声药物研究有限公司 | 一类苯并咪唑类衍生物及其应用 |
| WO2014164767A1 (en) * | 2013-03-13 | 2014-10-09 | Forma Therapeutics, Inc. | Novel compounds and compositions for inhibition of fasn |
-
2014
- 2014-02-24 CN CN201480016107.3A patent/CN105008329B/zh not_active Expired - Fee Related
- 2014-02-24 AU AU2014234721A patent/AU2014234721A1/en not_active Abandoned
- 2014-02-24 JP JP2016504506A patent/JP6412553B2/ja not_active Expired - Fee Related
- 2014-02-24 EP EP14708800.9A patent/EP2976328B2/en not_active Not-in-force
- 2014-02-24 CA CA2907657A patent/CA2907657A1/en not_active Abandoned
- 2014-02-24 US US14/778,253 patent/US9809552B2/en not_active Expired - Fee Related
- 2014-02-24 ES ES14708800.9T patent/ES2634875T3/es active Active
- 2014-02-24 WO PCT/EP2014/000478 patent/WO2014146747A1/en active Application Filing
- 2014-03-21 AR ARP140101320A patent/AR095707A1/es unknown
-
2015
- 2015-09-10 IL IL241513A patent/IL241513A0/en unknown
-
2018
- 2018-07-09 JP JP2018129665A patent/JP2018188452A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP2976328B1 (en) | 2017-05-03 |
| US9809552B2 (en) | 2017-11-07 |
| EP2976328B2 (en) | 2019-07-03 |
| WO2014146747A1 (en) | 2014-09-25 |
| US20160280655A1 (en) | 2016-09-29 |
| ES2634875T3 (es) | 2017-09-29 |
| CN105008329B (zh) | 2018-01-05 |
| JP2018188452A (ja) | 2018-11-29 |
| JP2016515550A (ja) | 2016-05-30 |
| JP6412553B2 (ja) | 2018-10-24 |
| AU2014234721A1 (en) | 2015-11-05 |
| CN105008329A (zh) | 2015-10-28 |
| IL241513A0 (en) | 2015-11-30 |
| EP2976328A1 (en) | 2016-01-27 |
| CA2907657A1 (en) | 2014-09-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |