AR106798A1 - Inhibidores pirazol de acc y usos de los mismos - Google Patents
Inhibidores pirazol de acc y usos de los mismosInfo
- Publication number
- AR106798A1 AR106798A1 ARP160103590A ARP160103590A AR106798A1 AR 106798 A1 AR106798 A1 AR 106798A1 AR P160103590 A ARP160103590 A AR P160103590A AR P160103590 A ARP160103590 A AR P160103590A AR 106798 A1 AR106798 A1 AR 106798A1
- Authority
- AR
- Argentina
- Prior art keywords
- independently selected
- sulfur
- nitrogen
- membered
- oxygen
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/93—Ligases (6)
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Y—ENZYMES
- C12Y604/00—Ligases forming carbon-carbon bonds (6.4)
- C12Y604/01—Ligases forming carbon-carbon bonds (6.4.1)
- C12Y604/01002—Acetyl-CoA carboxylase (6.4.1.2)
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Biochemistry (AREA)
- General Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Plant Pathology (AREA)
- Pest Control & Pesticides (AREA)
- Environmental Sciences (AREA)
- Dentistry (AREA)
- Molecular Biology (AREA)
- Microbiology (AREA)
- Biotechnology (AREA)
- Biomedical Technology (AREA)
- Agronomy & Crop Science (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
La presente proporciona compuestos de pirazol útiles como inhibidores de la Acetil-CoA carboxilasa (ACC), composiciones de los mismos, y métodos de uso de la misma. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable o una sal agrícolamente aceptable del mismo, donde: X es -O-, -S-, o -NR-; R¹ es hidrógeno o alifático C₁₋₄ opcionalmente sustituido con 1 - 4 grupos seleccionados independientemente entre halógeno, -OR, -SR, -N(R)₂, -N(R)C(O)R, -C(O)N(R)₂, -N(R)C(O)N(R)₂, -N(R)C(O)OR, -OC(O)N(R)₂, -N(R)S(O)₂R, -S(O)₂N(R)₂, -C(O)R, -C(O)OR, -OC(O)R, -S(O)R, o -S(O)₂R; cada R², R⁶, R⁷, y R⁸ es independientemente oxo, halógeno, -CN, -Rᵃ, -OR, -SR, -N(R)₂, -N(R)C(O)R, -C(O)N(R)₂, -N(R)C(O)N(R)₂, -N(R)C(O)OR, -OC(O)N(R)₂, -N(R)S(O)₂R, -S(O)₂N(R)₂, -C(O)R, -C(O)OR, -OC(O)R, -S(O)R, o -S(O)₂R; cada R es independientemente hidrógeno, o Rᵃ; cada Rᵃ es independientemente un grupo opcionalmente sustituido seleccionado entre alifático C₁₋₆, un anillo carbocíclico monocíclico saturado o parcialmente insaturado de 3 - 8 miembros, fenilo, un anillo carbocíclico aromático bicíclico de 8 - 10 miembros, un anillo heterocíclico monocíclico saturado o parcialmente insaturado de 4 - 8 miembros que tiene 1 - 2 heteroátomos seleccionados independientemente de nitrógeno, oxígeno o azufre, un anillo heteroaromático monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno o azufre, o un anillo heteroaromático bicíclico de 8 - 10 miembros que tiene 1 - 5 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno o azufre; L¹ es un enlace covalente, una cadena hidrocarbonada bivalente lineal o ramificada de 1 - 6 miembros, ciclopropilenilo, ciclobutilenilo u oxetanilenilo; L² es un enlace covalente o una cadena hidrocarbonada bivalente lineal o ramificada de 1 - 6 miembros, en la que L² está sustituido por n instancias de R⁹; R³ es -OR, -C(O)OR, -N(R)C(O)OR, -OC(O)N(R)₂, -C(O)N(R)OR, -C(O)NH₂, -C(O)NHRᵃ, -C(O)N(Rᵃ)₂, o -C(O)Hy; Hy es un anillo heterocíclico monocíclico saturado o parcialmente insaturado de 3 - 8 miembros que tiene 1 - 2 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno o azufre, un anillo heteroaromático monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente de nitrógeno, oxígeno o azufre, o un anillo heteroaromático bicíclico de 8 - 10 miembros que tiene 1 - 5 heteroátomos seleccionados independientemente de nitrógeno, oxígeno o azufre, en donde Hy está sustituido por p instancias de R⁶; R⁴ se selecciona de un anillo carbocíclico monocíclico saturado o parcialmente insaturado de 3 - 8 miembros, un anillo heterocíclico monocíclico saturado o parcialmente insaturado de 4 - 8 miembros que tiene 1 - 2 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno o azufre, fenilo, un anillo arilo bicíclico de 8 - 10 miembros, un anillo heteroarilo monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente de nitrógeno, oxígeno o azufre, y un anillo heteroarílico bicíclico de 8 - 10 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno o azufre, en el que R⁴ está sustituido por q instancias de R⁷; cada R⁵ se selecciona independientemente de hidrógeno, alifático C₁₋₄, un anillo carbocíclico monocíclico saturado o parcialmente insaturado de 3 - 8 miembros, un anillo heterocíclico monocíclico saturado o parcialmente insaturado de 4 - 8 miembros que tiene 1 - 2 heteroátomos seleccionados independientemente de nitrógeno, o azufre, fenilo, un anillo arilo bicíclico de 8 - 10 miembros, un anillo heteroarilo monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno o azufre, o un anillo heteroarílico bicíclico de 8 - 10 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente de nitrógeno, oxígeno o azufre, en donde cada R⁵ está sustituido con r instancias de R⁸; cada R⁹ es independientemente oxo o -OR⁵; m es 0, 1, 2, ó 3; n es 0, 1, ó 2; p es 0, 1, 2, 3, ó 4; q es 0, 1, 2, 3, 4, ó 5; r es 0, 1, 2, 3, ó 4.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562259973P | 2015-11-25 | 2015-11-25 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR106798A1 true AR106798A1 (es) | 2018-02-21 |
Family
ID=57543206
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP160103590A AR106798A1 (es) | 2015-11-25 | 2016-11-23 | Inhibidores pirazol de acc y usos de los mismos |
Country Status (18)
Country | Link |
---|---|
US (2) | US20170166582A1 (es) |
EP (1) | EP3380480B1 (es) |
JP (1) | JP2019502660A (es) |
KR (1) | KR20180082556A (es) |
CN (1) | CN108349995B (es) |
AR (1) | AR106798A1 (es) |
AU (1) | AU2016361412A1 (es) |
BR (1) | BR112018010113B1 (es) |
CA (1) | CA3004796C (es) |
CL (1) | CL2018001356A1 (es) |
CO (1) | CO2018005368A2 (es) |
EA (1) | EA201890913A1 (es) |
ES (1) | ES2939833T3 (es) |
MX (1) | MX2018006286A (es) |
PL (1) | PL3380480T3 (es) |
PT (1) | PT3380480T (es) |
SI (1) | SI3380480T1 (es) |
WO (1) | WO2017091600A1 (es) |
Families Citing this family (26)
Publication number | Priority date | Publication date | Assignee | Title |
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SI2776038T1 (en) | 2011-11-11 | 2018-06-29 | Gilead Apollo, Llc | ACC INHIBITORS AND THEIR USE |
EP3099693A4 (en) | 2014-01-31 | 2017-08-16 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
KR20160115953A (ko) | 2014-01-31 | 2016-10-06 | 다나-파버 캔서 인스티튜트 인크. | 디아미노피리미딘 벤젠술폰 유도체 및 그의 용도 |
JP2018526424A (ja) | 2015-09-11 | 2018-09-13 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | アセトアミドチエノトリアゾロジアゼピンおよびこれらの使用 |
MX2018003031A (es) | 2015-09-11 | 2018-08-01 | Dana Farber Cancer Inst Inc | Ciano tienotriazolpirazinas y usos de las mismas. |
AR106472A1 (es) | 2015-10-26 | 2018-01-17 | Gilead Apollo Llc | Inhibidores de acc y usos de los mismos |
JP2019503338A (ja) | 2015-11-25 | 2019-02-07 | ギリアド アポロ, エルエルシー | 2,4−ジオキソ−1,4−ジヒドロチエノ[2,3−d]ピリミジンの誘導体を含む殺真菌組成物 |
MX2018006286A (es) | 2015-11-25 | 2018-09-07 | Gilead Apollo Llc | Inhibidores de acc pirazolicos y usos de los mismos. |
EA201890949A1 (ru) | 2015-11-25 | 2018-12-28 | Джилид Аполло, Ллс | СЛОЖНОЭФИРНЫЕ ИНГИБИТОРЫ АЦЕТИЛ-КоА-КАРБОКСИЛАЗЫ И ВАРИАНТЫ ИХ ПРИМЕНЕНИЯ |
BR112018009798A8 (pt) | 2015-11-25 | 2019-02-26 | Dana Farber Cancer Inst Inc | inibidores de bromodomínio bivalentes e usos dos mesmos |
KR20180082557A (ko) | 2015-11-25 | 2018-07-18 | 길리어드 아폴로, 엘엘씨 | 트리아졸 acc 억제제 및 그의 용도 |
KR20230035692A (ko) * | 2016-03-02 | 2023-03-14 | 길리어드 아폴로, 엘엘씨 | 티에노피리미딘디온 acc 억제제의 고체 형태 및 그의 제조 방법 |
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KR20190125359A (ko) | 2017-03-03 | 2019-11-06 | 길리어드 아폴로, 엘엘씨 | 살진균 화합물의 제조 방법 |
CN110431143B (zh) * | 2017-03-24 | 2022-08-12 | 浙江海正药业股份有限公司 | 杂芳基并嘧啶酮类衍生物及其制备方法和用途 |
US20180280394A1 (en) | 2017-03-28 | 2018-10-04 | Gilead Sciences, Inc. | Methods of treating liver disease |
CN110709402B (zh) * | 2017-06-15 | 2022-05-10 | 浙江海正药业股份有限公司 | 杂芳基并嘧啶酮类衍生物、其制备方法及其在医药上用途 |
WO2019015583A1 (en) | 2017-07-17 | 2019-01-24 | Nanjing Ruijie Pharmatech Co., Ltd. | NOVEL COMPOUNDS AND THEIR USES AS ACC INHIBITORS |
CN110950884B (zh) * | 2018-09-27 | 2024-03-26 | 上海翰森生物医药科技有限公司 | 含二并环类衍生物抑制剂、其制备方法和应用 |
WO2020092239A1 (en) | 2018-10-29 | 2020-05-07 | Gilead Apollo, Llc | Processes for the preparation of fungicidal compounds |
CN111484504B (zh) * | 2019-01-25 | 2024-05-10 | 南京圣和药业股份有限公司 | Acc抑制剂的光学异构体及其应用 |
AR119594A1 (es) | 2019-08-09 | 2021-12-29 | Gilead Sciences Inc | Derivados de tienopirimidina como inhibidores acc y usos de los mismos |
CN110746439B (zh) * | 2019-10-18 | 2020-10-30 | 南京瑞捷医药科技有限公司 | 一种噻吩并嘧啶二酮化合物的制备方法 |
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- 2016-11-22 ES ES16810189T patent/ES2939833T3/es active Active
- 2016-11-22 EP EP16810189.7A patent/EP3380480B1/en active Active
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- 2016-11-22 AU AU2016361412A patent/AU2016361412A1/en not_active Abandoned
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- 2016-11-22 US US15/358,627 patent/US20170166582A1/en not_active Abandoned
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- 2016-11-22 CN CN201680067509.5A patent/CN108349995B/zh active Active
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Also Published As
Publication number | Publication date |
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EA201890913A1 (ru) | 2018-11-30 |
AU2016361412A1 (en) | 2018-05-24 |
PT3380480T (pt) | 2023-03-14 |
JP2019502660A (ja) | 2019-01-31 |
SI3380480T1 (sl) | 2023-04-28 |
ES2939833T3 (es) | 2023-04-27 |
CA3004796C (en) | 2023-11-14 |
AU2016361412A9 (en) | 2018-12-06 |
EP3380480B1 (en) | 2022-12-14 |
CN108349995A (zh) | 2018-07-31 |
CA3004796A1 (en) | 2017-06-01 |
WO2017091600A9 (en) | 2018-07-19 |
US20170166582A1 (en) | 2017-06-15 |
BR112018010113A2 (pt) | 2018-11-21 |
US20190375759A1 (en) | 2019-12-12 |
CN108349995B (zh) | 2021-08-03 |
US10941158B2 (en) | 2021-03-09 |
BR112018010113B1 (pt) | 2022-06-14 |
MX2018006286A (es) | 2018-09-07 |
EP3380480A1 (en) | 2018-10-03 |
PL3380480T3 (pl) | 2023-05-08 |
WO2017091600A1 (en) | 2017-06-01 |
CO2018005368A2 (es) | 2018-05-31 |
KR20180082556A (ko) | 2018-07-18 |
CL2018001356A1 (es) | 2018-08-17 |
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