AR107032A1 - Inhibidores bicíclicos de pad4 - Google Patents
Inhibidores bicíclicos de pad4Info
- Publication number
- AR107032A1 AR107032A1 ARP160103778A ARP160103778A AR107032A1 AR 107032 A1 AR107032 A1 AR 107032A1 AR P160103778 A ARP160103778 A AR P160103778A AR P160103778 A ARP160103778 A AR P160103778A AR 107032 A1 AR107032 A1 AR 107032A1
- Authority
- AR
- Argentina
- Prior art keywords
- formulas
- optionally substituted
- group
- aliphatic
- pad4
- Prior art date
Links
- 101100406797 Arabidopsis thaliana PAD4 gene Proteins 0.000 title abstract 3
- 101150094373 Padi4 gene Proteins 0.000 title abstract 3
- 102100035731 Protein-arginine deiminase type-4 Human genes 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 125000001931 aliphatic group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 3
- 229910052731 fluorine Inorganic materials 0.000 abstract 3
- 239000011737 fluorine Substances 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- -1 PAD4 inhibitors Chemical class 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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- A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract
Compuestos útiles como inhibidores de PAD4, composiciones de estos y métodos para tratar trastornos relacionados con PAD4. Reivindicación 1: Un compuesto caracterizado por la fórmula (1), o una sal de este aceptable desde el punto de vista farmacéutico, en donde: El anillo A es seleccionado del grupo de fórmulas (2), en donde el anillo A se sustituye opcionalmente con 1 - 4 grupos seleccionados de flúor, -CN, -OR, o C₁₋₆ alifático opcionalmente sustituido con 1 - 3 átomos de flúor; el anillo B es seleccionado del grupo de fórmulas (3); R¹ es hidrógeno, -CN, -OR, un resto del grupo de fórmulas (4) o C₁₋₆ alifático opcionalmente sustituido con 1 - 4 grupos seleccionados de flúor, -CN o -OR; R² es hidrógeno o C₁₋₁₀ alifático opcionalmente sustituido con 1 - 5 grupos seleccionados de flúor, -CN o -OR; cada uno de X¹ y X² se selecciona independientemente de N o C(R⁴); R³ es halógeno, -CN, -R, un resto del grupo de fórmulas (5) o -OR; cada R⁴ es independientemente halógeno, -CN, -R, un resto seleccionado del grupo de fórmulas (6) o -OR; R⁵ es hidrógeno o halógeno; n es 0 - 4; y cada R es independientemente hidrógeno o C₁₋₆ alifático opcionalmente sustituido con 1 - 3 átomos de flúor.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562264925P | 2015-12-09 | 2015-12-09 |
Publications (1)
| Publication Number | Publication Date |
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| AR107032A1 true AR107032A1 (es) | 2018-03-14 |
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ID=59013640
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160103778A AR107032A1 (es) | 2015-12-09 | 2016-12-07 | Inhibidores bicíclicos de pad4 |
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| TW (1) | TW201726674A (es) |
| UY (1) | UY37018A (es) |
| WO (1) | WO2017100594A1 (es) |
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| BR112017024678A2 (pt) * | 2015-05-21 | 2018-07-31 | Glaxosmithkline Intellectual Property Development Limited | derivados de benzoimidazol como inibidores de pad4 |
| CN109071497B (zh) | 2016-02-23 | 2021-10-22 | 帕德罗科治疗公司 | Pad4杂芳基抑制剂 |
| KR102398941B1 (ko) | 2016-07-27 | 2022-05-17 | 패들락 테라퓨틱스, 인코포레이티드 | Pad4의 공유결합성 억제제 |
| WO2018049296A1 (en) | 2016-09-12 | 2018-03-15 | Padlock Therapeutics, Inc. | Heteroaryl inhibitors of pad4 |
| TWI762769B (zh) * | 2018-02-26 | 2022-05-01 | 大陸商藥捷安康(南京)科技股份有限公司 | 肽醯精胺酸脫亞胺酶抑制劑及其用途 |
| CN112566916B (zh) * | 2018-08-08 | 2023-10-20 | 百时美施贵宝公司 | 作为pad4抑制剂的经取代的噻吩并吡咯 |
| KR102825194B1 (ko) * | 2018-08-08 | 2025-06-24 | 브리스톨-마이어스 스큅 컴퍼니 | Pad4 억제제로서의 치환된 벤즈이미다졸 |
| EP3833439B1 (en) * | 2018-08-08 | 2023-07-12 | Bristol-Myers Squibb Company | Benzimidazole inhibitors of pad enzymes |
| SG11202101174RA (en) | 2018-08-08 | 2021-03-30 | Bristol Myers Squibb Co | Indole and azaindole inhibitors of pad enzymes |
| KR20210146370A (ko) | 2019-03-28 | 2021-12-03 | 루핀 리미티드 | Sting 효능제로서의 매크로사이클릭 화합물 |
| CN112574230B (zh) * | 2019-09-27 | 2022-10-28 | 药捷安康(南京)科技股份有限公司 | 肽酰精氨酸脱亚胺酶抑制剂及其用途 |
| WO2021158840A1 (en) * | 2020-02-06 | 2021-08-12 | Bristol-Myers Squibb Company | Macrocyclic pad4 inhibitors useful as immunosuppressant |
| TW202140477A (zh) | 2020-02-12 | 2021-11-01 | 美商必治妥美雅史谷比公司 | 雜環pad4抑制劑 |
| WO2021222353A1 (en) * | 2020-04-30 | 2021-11-04 | Gilead Sciences, Inc. | Macrocyclic inhibitors of peptidylarginine deiminases |
| TW202233174A (zh) | 2020-12-22 | 2022-09-01 | 美商基利科學股份有限公司 | 肽基精胺酸去亞胺酶之抑制劑 |
| US11878965B2 (en) | 2020-12-22 | 2024-01-23 | Gilead Sciences, Inc. | Inhibitors of peptidylarginine deiminases |
| CN112618546B (zh) * | 2020-12-22 | 2022-03-01 | 陈昊 | Pad4抑制剂在制备放射治疗增敏药物方面的应用 |
| AU2023387505A1 (en) * | 2022-11-24 | 2025-07-10 | Helios Huaming Biopharma Co., Ltd. | Selenium containing heterocycle compounds and use thereof |
| WO2025024265A1 (en) | 2023-07-21 | 2025-01-30 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad4 modulators |
| WO2025181830A2 (en) * | 2024-03-01 | 2025-09-04 | Jubilant Epipad LLC | Polyheterocyclic compounds as peptidyl arginine deiminase 4 (pad4) inhibitors |
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| ITMI20012060A1 (it) * | 2001-10-05 | 2003-04-05 | Recordati Chem Pharm | Nuovi eterocilcli n-acilati |
| US6897208B2 (en) | 2001-10-26 | 2005-05-24 | Aventis Pharmaceuticals Inc. | Benzimidazoles |
| WO2004041277A1 (en) | 2002-11-01 | 2004-05-21 | Merck & Co., Inc. | Carbonylamino-benzimidazole derivatives as androgen receptor modulators |
| EP2234486A4 (en) | 2007-12-19 | 2011-09-14 | Scripps Research Inst | BENZIMIDAZOLES AND ANALOGS AS INHIBITORS OF RHO-KINASE |
| US8710039B2 (en) * | 2010-11-01 | 2014-04-29 | The Penn State Research Foundation | Therapeutic compositions and methods |
| JP5721484B2 (ja) | 2011-03-17 | 2015-05-20 | 富士フイルム株式会社 | 重合性液晶組成物、それを用いた高分子材料および光学異方性フィルム、並びに重合性液晶化合物 |
| WO2013052263A2 (en) | 2011-09-16 | 2013-04-11 | Microbiotix, Inc. | Antifungal compounds |
| WO2013157021A1 (en) | 2012-04-20 | 2013-10-24 | Advinus Therapeutics Limited | Bicyclic compounds, compositions and medicinal applications thereof |
| CA2874303C (en) | 2012-06-11 | 2020-10-13 | Ucb Biopharma Sprl | Tnf -alpha modulating benz imidazoles |
| EP3255049A1 (en) | 2012-06-29 | 2017-12-13 | Pfizer Inc | Novel 4-(substituted-amino)-7h-pyrrolo[2,3-d]pyrimidines as lrrk2 inhibitors |
| PL2877467T3 (pl) * | 2012-07-26 | 2017-08-31 | Glaxo Group Limited | 2-(azaindolo-2-ylo)benzoimidazole jako inhibitory pad4 |
| BR112017024678A2 (pt) | 2015-05-21 | 2018-07-31 | Glaxosmithkline Intellectual Property Development Limited | derivados de benzoimidazol como inibidores de pad4 |
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| US9963448B2 (en) | 2018-05-08 |
| CA3007639A1 (en) | 2017-06-15 |
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| BR112018011709A2 (pt) | 2018-12-04 |
| SG11201804668UA (en) | 2018-06-28 |
| US20170166565A1 (en) | 2017-06-15 |
| EP3885342A1 (en) | 2021-09-29 |
| EP3386590A1 (en) | 2018-10-17 |
| JP6932136B2 (ja) | 2021-09-08 |
| KR102729670B1 (ko) | 2024-11-12 |
| CN109069869B (zh) | 2022-09-13 |
| UY37018A (es) | 2017-06-30 |
| TW201726674A (zh) | 2017-08-01 |
| CN109069869A (zh) | 2018-12-21 |
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