PE20211068A1 - Inhibidores tipo indol y azaindol de enzimas pad - Google Patents
Inhibidores tipo indol y azaindol de enzimas padInfo
- Publication number
- PE20211068A1 PE20211068A1 PE2021000171A PE2021000171A PE20211068A1 PE 20211068 A1 PE20211068 A1 PE 20211068A1 PE 2021000171 A PE2021000171 A PE 2021000171A PE 2021000171 A PE2021000171 A PE 2021000171A PE 20211068 A1 PE20211068 A1 PE 20211068A1
- Authority
- PE
- Peru
- Prior art keywords
- substituted
- alkyl
- inhibitors
- alkyl substituted
- pad4
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 102000004190 Enzymes Human genes 0.000 title 1
- 108090000790 Enzymes Proteins 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 101100406797 Arabidopsis thaliana PAD4 gene Proteins 0.000 abstract 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 abstract 2
- 101150094373 Padi4 gene Proteins 0.000 abstract 2
- 102100035731 Protein-arginine deiminase type-4 Human genes 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 abstract 1
- -1 2- (5 - ((1R, 4R, 7R) -7 -amino-2-azabicyclo [2.2.1] heptane-2-carbonyl) -1-methyl-1H-benzo [d] imidazol-2-yl) -1- (cyclopropylmethyl) -1H-pyrrolo [2,3-b ] pyridin-6-yl Chemical group 0.000 abstract 1
- 206010009900 Colitis ulcerative Diseases 0.000 abstract 1
- 201000003883 Cystic fibrosis Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 101150105130 RORB gene Proteins 0.000 abstract 1
- 201000006704 Ulcerative Colitis Diseases 0.000 abstract 1
- 206010047115 Vasculitis Diseases 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 abstract 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 abstract 1
- 206010025135 lupus erythematosus Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000001235 protein arginine deiminase Human genes 0.000 abstract 1
- 108060006632 protein arginine deiminase Proteins 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 abstract 1
Classifications
-
- 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
- C07D471/08—Bridged systems
-
- 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
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- 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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862715850P | 2018-08-08 | 2018-08-08 | |
| PCT/US2019/045466 WO2020033520A1 (en) | 2018-08-08 | 2019-08-07 | Indole and azaindole inhibitors of pad enzymes |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20211068A1 true PE20211068A1 (es) | 2021-06-09 |
Family
ID=67766306
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021000171A PE20211068A1 (es) | 2018-08-08 | 2019-08-07 | Inhibidores tipo indol y azaindol de enzimas pad |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US11524959B1 (https=) |
| EP (1) | EP3833440A1 (https=) |
| JP (1) | JP7651451B2 (https=) |
| KR (1) | KR102885181B1 (https=) |
| CN (1) | CN112805067B (https=) |
| AR (1) | AR115920A1 (https=) |
| AU (1) | AU2019319835A1 (https=) |
| BR (1) | BR112021002091A2 (https=) |
| CA (1) | CA3108791A1 (https=) |
| CL (1) | CL2021000296A1 (https=) |
| CO (1) | CO2021001217A2 (https=) |
| EA (1) | EA202190462A1 (https=) |
| IL (1) | IL280650A (https=) |
| MX (1) | MX2021001565A (https=) |
| PE (1) | PE20211068A1 (https=) |
| SG (1) | SG11202101174RA (https=) |
| TW (1) | TW202019415A (https=) |
| WO (1) | WO2020033520A1 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3833671B1 (en) | 2018-08-08 | 2022-08-24 | Bristol-Myers Squibb Company | Substituted thienopyrroles as pad4 inhibitors |
| AU2019319835A1 (en) | 2018-08-08 | 2021-03-25 | Bristol-Myers Squibb Company | Indole and azaindole inhibitors of PAD enzymes |
| EP4100405A1 (en) | 2020-02-06 | 2022-12-14 | 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 |
| EP4143189A1 (en) * | 2020-04-30 | 2023-03-08 | Gilead Sciences, Inc. | Macrocyclic inhibitors of peptidylarginine deiminases |
| CN111943947B (zh) * | 2020-07-24 | 2021-04-30 | 重庆文理学院 | 1H-吡咯[2,3-b]吡啶衍生物及其合成方法与应用 |
| CN116075510A (zh) | 2020-08-19 | 2023-05-05 | 百时美施贵宝公司 | 1H-苯并[d]咪唑衍生物作为TLR9抑制剂用于治疗纤维化 |
| WO2022040267A1 (en) | 2020-08-19 | 2022-02-24 | Bristol-Myers Squibb Company | 1h-pyrrolo[3,2-c]pyridine and 1h-pyrrolo[2,3-c]pyridine derivatives as tlr9 inhibitors for the treatment of fibrosis |
| TW202241884A (zh) * | 2020-12-22 | 2022-11-01 | 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 |
| WO2022140428A2 (en) * | 2020-12-22 | 2022-06-30 | Gilead Sciences, Inc. | Inhibitors of peptidylarginine deiminases |
| WO2025024265A1 (en) | 2023-07-21 | 2025-01-30 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad4 modulators |
| CN117427074A (zh) * | 2023-11-13 | 2024-01-23 | 山东第一医科大学(山东省医学科学院) | 四氢喹啉醇作为铁死亡抑制剂在制备急性肾损伤药物中的应用 |
| WO2026020127A2 (en) | 2024-07-19 | 2026-01-22 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad2 modulators |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS55684B1 (sr) | 2012-07-26 | 2017-07-31 | Glaxo Group Ltd | 2-(azaindol-2-il)benzimidazoli kao pad4 inhibitori |
| US10407407B2 (en) | 2015-05-21 | 2019-09-10 | Glaxosmithkline Intellectual Property Development Limited | Benzoimidazole derivatives as PAD4 inhibitors |
| AR107030A1 (es) | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores aza-bencimidazol de pad4 |
| AR107032A1 (es) | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores bicíclicos de pad4 |
| RU2747431C2 (ru) | 2015-12-22 | 2021-05-05 | Кансера Аб | Бициклические гидроксамовые кислоты, полезные в качестве ингибиторов активности деацетилазы гистонов млекопитающих |
| JP6926126B2 (ja) | 2016-02-23 | 2021-08-25 | パドロック・セラピューティクス・インコーポレイテッドＰａｄｌｏｃｋ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． | Ｐａｄ４のヘテロアリール阻害剤 |
| KR102398941B1 (ko) | 2016-07-27 | 2022-05-17 | 패들락 테라퓨틱스, 인코포레이티드 | Pad4의 공유결합성 억제제 |
| JP7118951B2 (ja) | 2016-09-12 | 2022-08-16 | パドロック・セラピューティクス・インコーポレイテッド | Ｐａｄ４のヘテロアリール阻害剤 |
| CN110582489B (zh) | 2017-06-30 | 2023-10-27 | 北京泰德制药股份有限公司 | Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途 |
| AU2018352142B2 (en) | 2017-10-18 | 2022-08-25 | Jubilant Epipad LLC | Imidazo-pyridine compounds as PAD inhibitors |
| CN112789087B (zh) | 2018-08-08 | 2024-08-13 | 百时美施贵宝公司 | Pad酶的苯并咪唑抑制剂 |
| AU2019319835A1 (en) | 2018-08-08 | 2021-03-25 | Bristol-Myers Squibb Company | Indole and azaindole inhibitors of PAD enzymes |
| WO2020033488A1 (en) | 2018-08-08 | 2020-02-13 | Bristol-Myers Squibb Company | Substituted benzimidazoles as pad4 inhibitors |
| EP3833671B1 (en) | 2018-08-08 | 2022-08-24 | Bristol-Myers Squibb Company | Substituted thienopyrroles as pad4 inhibitors |
-
2019
- 2019-08-07 AU AU2019319835A patent/AU2019319835A1/en not_active Abandoned
- 2019-08-07 EA EA202190462A patent/EA202190462A1/ru unknown
- 2019-08-07 SG SG11202101174RA patent/SG11202101174RA/en unknown
- 2019-08-07 US US17/265,842 patent/US11524959B1/en active Active
- 2019-08-07 CA CA3108791A patent/CA3108791A1/en active Pending
- 2019-08-07 PE PE2021000171A patent/PE20211068A1/es unknown
- 2019-08-07 KR KR1020217006477A patent/KR102885181B1/ko active Active
- 2019-08-07 AR ARP190102237A patent/AR115920A1/es not_active Application Discontinuation
- 2019-08-07 TW TW108128155A patent/TW202019415A/zh unknown
- 2019-08-07 EP EP19759141.5A patent/EP3833440A1/en active Pending
- 2019-08-07 MX MX2021001565A patent/MX2021001565A/es unknown
- 2019-08-07 BR BR112021002091-8A patent/BR112021002091A2/pt not_active Application Discontinuation
- 2019-08-07 CN CN201980064963.9A patent/CN112805067B/zh active Active
- 2019-08-07 WO PCT/US2019/045466 patent/WO2020033520A1/en not_active Ceased
- 2019-08-07 JP JP2021506683A patent/JP7651451B2/ja active Active
-
2021
- 2021-02-03 CO CONC2021/0001217A patent/CO2021001217A2/es unknown
- 2021-02-03 CL CL2021000296A patent/CL2021000296A1/es unknown
- 2021-02-04 IL IL280650A patent/IL280650A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA3108791A1 (en) | 2020-02-13 |
| CN112805067A (zh) | 2021-05-14 |
| MX2021001565A (es) | 2021-04-19 |
| US11524959B1 (en) | 2022-12-13 |
| BR112021002091A2 (pt) | 2021-05-04 |
| AU2019319835A1 (en) | 2021-03-25 |
| SG11202101174RA (en) | 2021-03-30 |
| CO2021001217A2 (es) | 2021-02-26 |
| AR115920A1 (es) | 2021-03-10 |
| CL2021000296A1 (es) | 2021-06-25 |
| TW202019415A (zh) | 2020-06-01 |
| EP3833440A1 (en) | 2021-06-16 |
| KR102885181B1 (ko) | 2025-11-11 |
| JP2021534108A (ja) | 2021-12-09 |
| IL280650A (en) | 2021-03-25 |
| WO2020033520A1 (en) | 2020-02-13 |
| KR20210042934A (ko) | 2021-04-20 |
| EA202190462A1 (ru) | 2021-06-03 |
| CN112805067B (zh) | 2026-04-24 |
| JP7651451B2 (ja) | 2025-03-26 |
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