CL2022001439A1 - Combinación de antagonista del receptor lpa1 de azetidina con pirfenidona y, o nintedanib. - Google Patents
Combinación de antagonista del receptor lpa1 de azetidina con pirfenidona y, o nintedanib.Info
- Publication number
- CL2022001439A1 CL2022001439A1 CL2022001439A CL2022001439A CL2022001439A1 CL 2022001439 A1 CL2022001439 A1 CL 2022001439A1 CL 2022001439 A CL2022001439 A CL 2022001439A CL 2022001439 A CL2022001439 A CL 2022001439A CL 2022001439 A1 CL2022001439 A1 CL 2022001439A1
- Authority
- CL
- Chile
- Prior art keywords
- nintedanib
- pirfenidone
- combination
- azetidine
- receptor antagonist
- Prior art date
Links
- XZXHXSATPCNXJR-ZIADKAODSA-N nintedanib Chemical compound O=C1NC2=CC(C(=O)OC)=CC=C2\C1=C(C=1C=CC=CC=1)\NC(C=C1)=CC=C1N(C)C(=O)CN1CCN(C)CC1 XZXHXSATPCNXJR-ZIADKAODSA-N 0.000 title abstract 3
- 229960004378 nintedanib Drugs 0.000 title abstract 3
- ISWRGOKTTBVCFA-UHFFFAOYSA-N pirfenidone Chemical compound C1=C(C)C=CC(=O)N1C1=CC=CC=C1 ISWRGOKTTBVCFA-UHFFFAOYSA-N 0.000 title abstract 3
- 229960003073 pirfenidone Drugs 0.000 title abstract 3
- 102000004137 Lysophosphatidic Acid Receptors Human genes 0.000 title abstract 2
- 108090000642 Lysophosphatidic Acid Receptors Proteins 0.000 title abstract 2
- 239000002464 receptor antagonist Substances 0.000 title abstract 2
- 229940044551 receptor antagonist Drugs 0.000 title abstract 2
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 title 1
- 230000003510 anti-fibrotic effect Effects 0.000 abstract 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000004480 active ingredient Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000003176 fibrotic effect Effects 0.000 abstract 1
- 239000004615 ingredient Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
-
- 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
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención se refiere a un compuesto de fórmula (I), en donde R1, R2, R3, X e Y son como se describe en la descripción, y su uso como antagonistas del receptor de LPA1, en combinación con uno o más ingredientes terapéuticamente activos que actúan como agentes antifibróticos; tal como especialmente pirfenidona y/o nintedanib, en la prevención y/o tratamiento de enfermedades fibróticas. La invención se refiere además a composiciones farmacéuticas que comprenden los compuestos de la fórmula (I) en combinación con uno o más ingredientes terapéuticamente activos que actúan tal como agentes antifibróticos tales como pirfenidona o nintedanib.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP2019083757 | 2019-12-04 |
Publications (1)
Publication Number | Publication Date |
---|---|
CL2022001439A1 true CL2022001439A1 (es) | 2023-01-27 |
Family
ID=76221504
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CL2022001439A CL2022001439A1 (es) | 2019-12-04 | 2022-06-01 | Combinación de antagonista del receptor lpa1 de azetidina con pirfenidona y, o nintedanib. |
Country Status (13)
Country | Link |
---|---|
US (1) | US20230000846A1 (es) |
EP (1) | EP4069227A1 (es) |
JP (1) | JP2023504415A (es) |
KR (1) | KR20220109439A (es) |
CN (1) | CN114761001A (es) |
AU (1) | AU2020397207A1 (es) |
BR (1) | BR112022010891A2 (es) |
CA (1) | CA3160410A1 (es) |
CL (1) | CL2022001439A1 (es) |
IL (1) | IL293474A (es) |
MX (1) | MX2022006736A (es) |
TW (1) | TW202133844A (es) |
WO (1) | WO2021110805A1 (es) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2020384883B2 (en) | 2019-11-15 | 2023-11-16 | Gilead Sciences, Inc. | Triazole carbamate pyridyl sulfonamides as LPA receptor antagonists and uses thereof |
JP2023529369A (ja) | 2020-06-03 | 2023-07-10 | ギリアード サイエンシーズ, インコーポレイテッド | Lpa受容体アンタゴニスト及びそれらの使用 |
CR20220609A (es) | 2020-06-03 | 2023-05-04 | Gilead Sciences Inc | Antagonistas del receptor de lpa y usos de los mismos |
US11980609B2 (en) | 2021-05-11 | 2024-05-14 | Gilead Sciences, Inc. | LPA receptor antagonists and uses thereof |
US11939318B2 (en) | 2021-12-08 | 2024-03-26 | Gilead Sciences, Inc. | LPA receptor antagonists and uses thereof |
WO2023192648A1 (en) * | 2022-03-31 | 2023-10-05 | Puretech Lyt 100, Inc. | Methods of treating interstitial lung diseases and other fibrotic-mediated pulmonary diseases and disorders with deupirfenidone |
Family Cites Families (23)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6762180B1 (en) | 1999-10-13 | 2004-07-13 | Boehringer Ingelheim Pharma Kg | Substituted indolines which inhibit receptor tyrosine kinases |
DE10233500A1 (de) | 2002-07-24 | 2004-02-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 3-Z-[1-(4-(N-((4-Methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylen]-6-methoxycarbonyl-2-indolinon-Monoethansulfonat und dessen Verwendung als Arzneimittel |
US20040204458A1 (en) | 2002-08-16 | 2004-10-14 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Use of Lck inhibitors for treatment of immunologic diseases |
PE20060777A1 (es) | 2004-12-24 | 2006-10-06 | Boehringer Ingelheim Int | Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas |
NZ591443A (en) | 2005-09-22 | 2013-04-26 | Intermune Inc | Granule formation of pirfenidone and pharmaceutically acceptable excipients |
DE602007014113D1 (de) | 2006-12-18 | 2011-06-01 | Intermune Inc | Verfahren zur bereitstellung einer pirfenidontherapie an einem patienten |
US20170065529A1 (en) | 2015-09-09 | 2017-03-09 | Boehringer Ingelheim International Gmbh | Pharmaceutical dosage form for immediate release of an indolinone derivative |
EP2299987B1 (en) | 2008-06-06 | 2018-02-21 | Boehringer Ingelheim International GmbH | Capsule pharmaceutical dosage form comprising a suspension formulation of an indolinone derivative |
US7566729B1 (en) | 2008-11-10 | 2009-07-28 | Intermune, Inc. | Modifying pirfenidone treatment for patients with atypical liver function |
US7635707B1 (en) | 2008-11-10 | 2009-12-22 | Intermune, Inc. | Pirfenidone treatment for patients with atypical liver function |
GB2470833B (en) | 2009-06-03 | 2011-06-01 | Amira Pharmaceuticals Inc | Polycyclic antagonists of lysophosphatidic acid receptors |
US7816383B1 (en) | 2009-12-04 | 2010-10-19 | Intermune, Inc. | Methods of administering pirfenidone therapy |
US8084475B2 (en) | 2009-12-04 | 2011-12-27 | Intermune, Inc. | Pirfenidone therapy and inducers of cytochrome P450 |
EP2648726B1 (en) | 2010-12-07 | 2018-04-04 | Amira Pharmaceuticals, Inc. | Polycyclic lpa1 antagonist and uses thereof |
EP2713732A4 (en) | 2011-05-25 | 2014-12-03 | Intermune Inc | PIRFENIDONE AND ANTIFIBROTIC TREATMENT IN SELECTED PATIENTS |
SG2014011555A (en) * | 2011-08-15 | 2014-08-28 | Intermune Inc | Lysophosphatidic acid receptor antagonists |
CA2819967C (en) | 2012-08-31 | 2016-03-22 | Intermune, Inc. | Use of pirfenidone concomitantly with ciprofloxacin |
AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
EP3126362B1 (en) | 2014-04-02 | 2022-01-12 | Intermune, Inc. | Anti-fibrotic pyridinones |
US20190275033A1 (en) * | 2016-06-01 | 2019-09-12 | Boehringer Ingelheim International Gmbh | Use of ecm biomarkers for determining the treatment onset with nintedanib and pirfenidone |
WO2019152863A1 (en) | 2018-02-02 | 2019-08-08 | Genentech, Inc. | Pharmaceutical compound, salts thereof, formulations thereof, and methods of making and using same |
LT3802517T (lt) | 2018-06-07 | 2023-03-10 | Idorsia Pharmaceuticals Ltd | Alkoksi-pakeistieji piridinilo dariniai kaip lpa1 receptoriaus antagonistai ir jų panaudojimas fibrozės gydymui |
AR119162A1 (es) * | 2019-06-18 | 2021-12-01 | Idorsia Pharmaceuticals Ltd | Derivados de piridin-3-ilo |
-
2020
- 2020-12-03 JP JP2022531534A patent/JP2023504415A/ja active Pending
- 2020-12-03 EP EP20816188.5A patent/EP4069227A1/en active Pending
- 2020-12-03 AU AU2020397207A patent/AU2020397207A1/en active Pending
- 2020-12-03 WO PCT/EP2020/084401 patent/WO2021110805A1/en unknown
- 2020-12-03 KR KR1020227022458A patent/KR20220109439A/ko unknown
- 2020-12-03 MX MX2022006736A patent/MX2022006736A/es unknown
- 2020-12-03 CN CN202080083930.1A patent/CN114761001A/zh active Pending
- 2020-12-03 BR BR112022010891A patent/BR112022010891A2/pt unknown
- 2020-12-03 CA CA3160410A patent/CA3160410A1/en active Pending
- 2020-12-03 TW TW109142607A patent/TW202133844A/zh unknown
- 2020-12-03 US US17/782,530 patent/US20230000846A1/en active Pending
- 2020-12-03 IL IL293474A patent/IL293474A/en unknown
-
2022
- 2022-06-01 CL CL2022001439A patent/CL2022001439A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
AU2020397207A1 (en) | 2022-07-21 |
IL293474A (en) | 2022-08-01 |
EP4069227A1 (en) | 2022-10-12 |
TW202133844A (zh) | 2021-09-16 |
CN114761001A (zh) | 2022-07-15 |
BR112022010891A2 (pt) | 2022-08-16 |
MX2022006736A (es) | 2022-07-11 |
JP2023504415A (ja) | 2023-02-03 |
US20230000846A1 (en) | 2023-01-05 |
KR20220109439A (ko) | 2022-08-04 |
WO2021110805A1 (en) | 2021-06-10 |
CA3160410A1 (en) | 2021-06-10 |
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