[go: up one dir, main page]

PE20171105A1 - Formas solidas de un inhibidor ask1 - Google Patents

Formas solidas de un inhibidor ask1

Info

Publication number
PE20171105A1
PE20171105A1 PE2017001098A PE2017001098A PE20171105A1 PE 20171105 A1 PE20171105 A1 PE 20171105A1 PE 2017001098 A PE2017001098 A PE 2017001098A PE 2017001098 A PE2017001098 A PE 2017001098A PE 20171105 A1 PE20171105 A1 PE 20171105A1
Authority
PE
Peru
Prior art keywords
theta
crystalline form
solid forms
refers
compound
Prior art date
Application number
PE2017001098A
Other languages
English (en)
Inventor
Mark Andres
Ernest A Carra
Brenda J Burke Chan
Anna Chiu
Olga Viktorovna Lapina
Stephen P Lathrop
Valeriya Smolenskaya
Lok Him Yu
Gregory Notte
Original Assignee
Gilead Sciences Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of PE20171105A1 publication Critical patent/PE20171105A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02Dicarboxylic acids
    • C07C55/06Oxalic acid
    • C07C55/07Salts thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13Dicarboxylic acids
    • C07C57/145Maleic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13Dicarboxylic acids
    • C07C57/15Fumaric acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/01Saturated compounds having only one carboxyl group and containing hydroxy or O-metal groups
    • C07C59/06Glycolic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se refiere a las formas cristalinas I, II, III, entre otras del compuesto 5-(4-ciclopropil-1H-imidazol-1-il)-N-(6-(4-isopropil-4H-1,2,4-triazol-3-il)piridin-2-il)2-fluoro-4-metilbenzamida (Compuesto I), caracterizada por un difractograma de rayos X en polvo que comprende los siguientes picos: 16,7; 21,3 y 22,8 ± 0,2° (2-theta) para la forma cristalina I; 11,2; 16,6 y 17,4 ± 0,2° (2-theta) para la forma cristalina II; y 5,1; 10,2 y 25,3 ± 0,2° (2-theta) para la forma cristalina III. Tambien se refiere a una composicion farmaceutica. Dichas formas cristalinas son inhibidores de la quinasa reguladora de la senal de apoptosis 1 (ASK1), siendo utiles en el tratamiento diabetes, nefropatia diabetica, entre otros.
PE2017001098A 2014-12-23 2015-12-22 Formas solidas de un inhibidor ask1 PE20171105A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462096406P 2014-12-23 2014-12-23
US201562269066P 2015-12-17 2015-12-17

Publications (1)

Publication Number Publication Date
PE20171105A1 true PE20171105A1 (es) 2017-08-07

Family

ID=55168336

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017001098A PE20171105A1 (es) 2014-12-23 2015-12-22 Formas solidas de un inhibidor ask1

Country Status (28)

Country Link
US (4) US9643956B2 (es)
EP (2) EP3237402B1 (es)
JP (3) JP2017538774A (es)
KR (1) KR101971387B1 (es)
CN (1) CN107108574A (es)
AU (2) AU2015371629B2 (es)
BR (1) BR102015032466A2 (es)
CA (1) CA2972012C (es)
CL (1) CL2017001617A1 (es)
CO (1) CO2017006099A2 (es)
CR (1) CR20170266A (es)
CU (1) CU20170087A7 (es)
DO (1) DOP2017000145A (es)
EA (1) EA201791066A1 (es)
EC (1) ECSP17038512A (es)
ES (1) ES2955208T3 (es)
GT (1) GT201700136A (es)
IL (1) IL252756A0 (es)
MA (1) MA41252A (es)
MX (1) MX2017008416A (es)
MY (1) MY194953A (es)
NZ (1) NZ732441A (es)
PE (1) PE20171105A1 (es)
PH (1) PH12017550028A1 (es)
SG (1) SG11201704834UA (es)
SV (1) SV2017005467A (es)
TW (2) TWI689504B (es)
WO (1) WO2016105453A1 (es)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI598347B (zh) 2009-07-13 2017-09-11 基利科學股份有限公司 調節細胞凋亡信號之激酶的抑制劑
UY34573A (es) 2012-01-27 2013-06-28 Gilead Sciences Inc Inhibidor de la quinasa que regula la señal de la apoptosis
EP3099304B1 (en) 2014-01-31 2024-07-17 Mayo Foundation for Medical Education and Research Chroman derivatives and their use in the treatment of glaucoma
EP3034499A1 (en) * 2014-12-17 2016-06-22 Gilead Sciences, Inc. Novel FXR (NR1H4) modulating compounds
SG11201704738UA (en) 2014-12-23 2017-07-28 Gilead Sciences Inc Processes for preparing ask1 inhibitors
MA41252A (fr) 2014-12-23 2017-10-31 Gilead Sciences Inc Formes solides d'un inhibiteur d'ask 1
PL3896064T3 (pl) 2015-07-06 2025-09-08 Gilead Sciences, Inc. Pochodne 4,6-diamino-chinolino-3-karbonitrylu jako modulatory cot w leczeniu choroby leśniowskiego-crohna i wrzodziejącego zapalenia jelita grubego
US20170174788A1 (en) * 2015-12-17 2017-06-22 Gilead Sciences, Inc. Combination of a jak inhibitor and an mmp9 binding protein for treating inflammatory disorders
CA3042398A1 (en) * 2016-11-11 2018-05-17 Gilead Sciences, Inc. Methods of treating liver disease
US11136324B2 (en) 2017-03-03 2021-10-05 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Substituted imidazoles as apoptosis signal regulating kinase 1 inhibitors
JOP20180017A1 (ar) * 2017-03-14 2019-01-30 Gilead Sciences Inc مثبط كيناز منظم لإشارة تلاشي خلايا
AU2018266911C1 (en) 2017-05-12 2022-10-20 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2018218042A1 (en) 2017-05-25 2018-11-29 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2018218044A2 (en) 2017-05-25 2018-11-29 Enanta Pharmaceuticals Inc Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US10450301B2 (en) 2017-05-25 2019-10-22 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US10597382B2 (en) 2017-08-28 2020-03-24 Enanta Pharmaceuticals, Inc. Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
CN109232538B (zh) * 2017-10-12 2020-07-24 深圳市塔吉瑞生物医药有限公司 一种1,2,4-三氮唑类化合物
US11008304B2 (en) 2018-05-02 2021-05-18 Enanta Pharmaceuticals, Inc. Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US10683289B2 (en) 2018-05-02 2020-06-16 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2020015721A1 (zh) * 2018-07-20 2020-01-23 福建广生堂药业股份有限公司 作为ask1抑制剂的晶型及其制备方法和应用
TW202021967A (zh) * 2018-08-14 2020-06-16 大陸商江蘇豪森藥業集團有限公司 凋亡信號調節激酶1抑制劑的鹽及其晶型
US10968199B2 (en) 2018-08-22 2021-04-06 Enanta Pharmaceuticals, Inc. Cycloalkyl-containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US11345699B2 (en) 2018-11-19 2022-05-31 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2020177705A1 (zh) * 2019-03-05 2020-09-10 苏州科睿思制药有限公司 Filgotinib的马来酸盐晶型CSI及其制备方法和用途
WO2020198214A1 (en) 2019-03-25 2020-10-01 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2020202096A1 (en) * 2019-04-05 2020-10-08 Dr. Reddy’S Laboratories Limited Amorphous filgotinib maleate, its solid dispersion and processes thereof
TWI770527B (zh) 2019-06-14 2022-07-11 美商基利科學股份有限公司 Cot 調節劑及其使用方法
CN115443132A (zh) 2019-12-12 2022-12-06 奎拉里斯生物公司 色满卡林前药的受控递送
US20230105984A1 (en) 2019-12-23 2023-04-06 Svetlana Marukian Compositions and methods for the treatment of liver diseases and disorders
WO2021158992A1 (en) * 2020-02-07 2021-08-12 Qlaris Bio, Inc. Improved methods and compositions for cromakalim prodrug therapy
CA3175541A1 (en) 2020-03-30 2021-10-07 Gilead Sciences, Inc. Solid forms of (s)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1h-1,2,3-triazol-4-yl)2-methyl-1-oxo-1,2- dihydroisoquinolin-5-yl)methyl)))amino)8-chloro-(neopentylamino)quinoline-3-carb onitrile a cot inhibitor compound
EP4613745A3 (en) 2020-04-02 2025-11-26 Gilead Sciences, Inc. Process for preparing a cot inhibitor compound
CN114470217B (zh) * 2020-11-24 2023-06-20 深圳微芯生物科技股份有限公司 预防和治疗代谢异常或炎症引起的组织损伤的药物组合物
US12091404B2 (en) 2021-03-11 2024-09-17 Gilead Sciences, Inc. GLP-1R modulating compounds
EP4313967B1 (en) 2021-03-29 2025-11-12 Gilead Sciences, Inc. Khk inhibitors
TW202345826A (zh) 2021-06-04 2023-12-01 美商基利科學股份有限公司 治療nash之方法
TW202311256A (zh) 2021-06-18 2023-03-16 美商基利科學股份有限公司 用於治療fxr誘發之搔癢之il-31調節劑

Family Cites Families (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US4326525A (en) 1980-10-14 1982-04-27 Alza Corporation Osmotic device that improves delivery properties of agent in situ
US5364620A (en) 1983-12-22 1994-11-15 Elan Corporation, Plc Controlled absorption diltiazem formulation for once daily administration
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US4902514A (en) 1988-07-21 1990-02-20 Alza Corporation Dosage form for administering nilvadipine for treating cardiovascular symptoms
WO1998034946A1 (en) 1997-02-12 1998-08-13 Massachusetts Institute Of Technology Daxx, a novel fas-binding protein that activates jnk and apoptosis
US6881555B2 (en) 1999-03-19 2005-04-19 Aventis Pharmaceuticals Inc. AKT nucleic acids, polypeptides, and uses thereof
DK1144600T3 (da) 1999-03-19 2008-11-24 Aventis Pharma Inc Akt-3-nukleinsyre, polypeptider og anvendelser deraf
US20070237770A1 (en) 2001-11-30 2007-10-11 Albert Lai Novel compositions and methods in cancer
JPWO2005009470A1 (ja) 2003-07-28 2006-09-28 財団法人大阪産業振興機構 Ask1阻害剤を有効成分とする心不全治療薬およびそのスクリーニング方法
JP2008514635A (ja) 2004-09-27 2008-05-08 コーザン バイオサイエンシス インコーポレイテッド 特異的キナーゼ阻害剤
AU2005304393B2 (en) 2004-11-10 2012-09-27 Synta Pharmaceuticals Corp. IL-12 modulatory compounds
EP1677113A1 (en) 2004-12-29 2006-07-05 Max-Delbrück-Centrum für Molekulare Medizin (MDC) Method for the identification of protein-protein interactions in disease related protein networks
US20070276050A1 (en) 2006-02-27 2007-11-29 Gilead Sciences, Inc. Methods for identifying ASK1 inhibitors useful for preventing and/or treating cardiovascular diseases
EP2058309A4 (en) 2006-08-04 2010-12-22 Takeda Pharmaceutical CONDENSED HETEROCYCLIC COMPOUND
WO2008042867A2 (en) 2006-09-29 2008-04-10 Emiliem Inc. Modulators of multiple kinases
AU2007333106A1 (en) 2006-12-08 2008-06-19 Asuragen, Inc. miR-20 regulated genes and pathways as targets for therapeutic intervention
WO2009011850A2 (en) 2007-07-16 2009-01-22 Abbott Laboratories Novel therapeutic compounds
JP5659014B2 (ja) 2007-08-02 2015-01-28 ジリード バイオロジクス,インク. 線維症、腫瘍浸潤、血管新生及び転移の治療及び診断のための方法及び組成物
MX2010002312A (es) 2007-08-31 2010-03-18 Merck Serono Sa Compuestos de triazolopiridina y su uso como inhibidores de cinasa reguladora de señal de apoptosis.
WO2009123986A1 (en) 2008-03-31 2009-10-08 Takeda Pharmaceutical Company Limited Apoptosis signal-regulating kinase 1 inhibitors
US8178555B2 (en) 2008-06-24 2012-05-15 Takeda Pharmaceutical Company Limited Apoptosis signal-regulating kinase 1 inhibitors
WO2010045470A2 (en) 2008-10-15 2010-04-22 Dana-Farber Cancer Institute, Inc. Compositions, kits, and methods for identification, assessment, prevention, and therapy of hepatic disorders
US20110294693A1 (en) 2008-11-17 2011-12-01 The George Washington University Compositions and Methods for Identifying Autism Spectrum Disorders
PA8854101A1 (es) 2008-12-18 2010-07-27 Ortho Mcneil Janssen Pharm Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa
JP2012521760A (ja) 2009-03-27 2012-09-20 メルク・シャープ・エンド・ドーム・コーポレイション 低分子干渉核酸(siNA)を用いたアポトーシスシグナル調節キナーゼ1(ASK1)遺伝子発現のRNA干渉媒介性阻害
TWI462920B (zh) 2009-06-26 2014-12-01 葛萊伯格有限公司 用於治療退化性及發炎疾病之新穎化合物
TWI598347B (zh) 2009-07-13 2017-09-11 基利科學股份有限公司 調節細胞凋亡信號之激酶的抑制劑
WO2011022670A1 (en) 2009-08-21 2011-02-24 Arresto Biosciences, Inc In vivo screening assays
WO2011041293A1 (en) 2009-09-30 2011-04-07 Takeda Pharmaceutical Company Limited Pyrazolo [1, 5-a] pyrimidine derivatives as apoptosis signal-regulating kinase 1 inhibitors
CN102834393B (zh) 2010-02-03 2015-07-22 武田药品工业株式会社 细胞凋亡信号调节激酶1抑制剂
EP2534145A4 (en) 2010-02-08 2013-09-11 Kinagen Inc THERAPEUTIC METHODS AND COMPOSITIONS INVOLVING THE INHIBITION OF ALLOSTERIC KINASE
WO2011119894A2 (en) 2010-03-24 2011-09-29 Kinagen, Inc Heterocyclic compounds useful for kinase inhibition
MX2012015105A (es) 2010-07-02 2013-05-28 Gilead Sciences Inc Inhibidores de cinasa de regulacion mediante señal de apoptosis.
US20130236441A1 (en) 2010-11-18 2013-09-12 University Of Delaware Methods of treating and preventing thrombotic diseases using ask1 inhibitors
US9045485B2 (en) 2010-12-16 2015-06-02 Convergence Pharmaceuticals Limited ASK 1 inhibiting pyrrolopyrimidine derivatives
CN103492590A (zh) 2011-02-22 2014-01-01 卡里斯生命科学卢森堡控股有限责任公司 循环生物标志物
AR086657A1 (es) 2011-06-01 2014-01-15 Gilead Biologics Inc Ensayo de la lisil oxidasa-like 2 y sus metodos de empleo
JP2014526032A (ja) 2011-06-07 2014-10-02 カリス ライフ サイエンシズ ルクセンブルク ホールディングス エス.アー.エール.エル. 癌に対する循環バイオマーカー
TW201837023A (zh) 2011-07-01 2018-10-16 美商基利科學股份有限公司 作為離子通道調節劑之稠合雜環化合物
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
UY34573A (es) 2012-01-27 2013-06-28 Gilead Sciences Inc Inhibidor de la quinasa que regula la señal de la apoptosis
UY35212A (es) 2012-12-21 2014-06-30 Gilead Sciences Inc Inhibidores de la quinasa que regula la señal de la apoptosis
WO2015187499A1 (en) 2014-06-03 2015-12-10 Gilead Sciences, Inc. Use of an ask1 inhibitor for the treatment of liver disease, optionally in combination with a loxl2 inhibitor
SG11201704738UA (en) 2014-12-23 2017-07-28 Gilead Sciences Inc Processes for preparing ask1 inhibitors
MA41252A (fr) 2014-12-23 2017-10-31 Gilead Sciences Inc Formes solides d'un inhibiteur d'ask 1

Also Published As

Publication number Publication date
EP3237402C0 (en) 2023-06-07
JP2019011371A (ja) 2019-01-24
ECSP17038512A (es) 2017-07-31
EA201791066A1 (ru) 2017-12-29
CO2017006099A2 (es) 2017-10-20
WO2016105453A1 (en) 2016-06-30
ES2955208T3 (es) 2023-11-29
AU2015371629B2 (en) 2019-01-31
TW201629042A (zh) 2016-08-16
AU2019200333B2 (en) 2020-10-29
CN107108574A (zh) 2017-08-29
CA2972012C (en) 2021-01-26
GT201700136A (es) 2019-04-18
NZ732441A (en) 2018-11-30
CR20170266A (es) 2017-09-12
PH12017550028A1 (en) 2017-10-18
TWI731591B (zh) 2021-06-21
US20170209423A1 (en) 2017-07-27
SG11201704834UA (en) 2017-07-28
MA41252A (fr) 2017-10-31
HK1246277A1 (en) 2018-09-07
EP4265250A2 (en) 2023-10-25
JP6790183B2 (ja) 2020-11-25
US20200061042A1 (en) 2020-02-27
KR20170096036A (ko) 2017-08-23
CL2017001617A1 (es) 2018-02-16
IL252756A0 (en) 2017-08-31
TWI689504B (zh) 2020-04-01
AU2015371629A1 (en) 2017-06-22
EP3237402B1 (en) 2023-06-07
EP3237402A1 (en) 2017-11-01
EP4265250A3 (en) 2024-01-10
US9907790B2 (en) 2018-03-06
US20180243281A1 (en) 2018-08-30
CU20170087A7 (es) 2017-11-07
AU2019200333A1 (en) 2019-02-07
SV2017005467A (es) 2017-10-17
KR101971387B1 (ko) 2019-04-22
JP6650008B2 (ja) 2020-02-19
TW202019912A (zh) 2020-06-01
JP2019156852A (ja) 2019-09-19
US9643956B2 (en) 2017-05-09
CA2972012A1 (en) 2016-06-30
US10946004B2 (en) 2021-03-16
BR102015032466A2 (pt) 2016-07-05
MY194953A (en) 2022-12-28
JP2017538774A (ja) 2017-12-28
US20160280683A1 (en) 2016-09-29
DOP2017000145A (es) 2017-08-15
MX2017008416A (es) 2017-10-19

Similar Documents

Publication Publication Date Title
PE20171105A1 (es) Formas solidas de un inhibidor ask1
CU24605B1 (es) Pirimidin-2-il amino-1h-pirazoles útiles como inhibidores de lrrk2
CL2014002301A1 (es) Compuestos derivados de pirimidin piridinas sustituidas, inhibidores de serina/treonina cinasas; procedimiento de preparacion; compuestos intermediarios; composicion farmaceutica; combinacion farmaceutica; uso para el tratamiento de una enfermedad hiperproliferativa tal como melanoma, cancer, leucemias y una enfermedad inflamatoria como artritis y reumatismo entre otras.
CU24419B1 (es) 2-(morfolin-4-il)-1,7-naftiridinas útiles en el tratamiento o la profilaxis de enfermedades hiperproliferativas
SV2016005137A (es) Derivados de piperidinil-indol como inhibidores del factor de complemento b y usos de los mismos
CO2017004525A2 (es) Dihidropirrolopiridinas inhibidoras de ror-gamma
ECSP16076566A (es) Compuestos de heteroarilo o arilo biciclicos fusionados y su aplicación a inhibidores de irak4
DOP2017000109A (es) Derivados de feniltriazol sustituido con hidroxialquilo y sus usos
MX373318B (es) 5-bromo-2,6-di-(1h-pirazol-1-il) pirimidin-4-amina-para su uso en el tratamiento del cáncer.
CL2014001988A1 (es) Un compuesto 5-(4-ciclopropil-1h-imidazol-1-il)-n-(6-(4-isopropil-4h-1,2,4-triazol-3-il)piridin-2-il)-2-fluoro-4-metilbenzamida o sus sales, como inhibidores de la quinasa reguladora de la señal de apoptosis; compuestos intermediarios; composicion farmaceutica; y su uso para el tratamiento de la enfermedad renal cronica, nefropatia diabetica, fibrosis renal, entre otras.
CU20160192A7 (es) Derivados de indano e indolina útiles como activadores de la guanilato ciclasa soluble
JO3392B1 (ar) مركبات عطرية حلقية غير متجانسة كمركبات مضادة للالتهاب
UY35972A (es) Inhibidores macrocíclicos de fxia que tienen grupos heterocíclicos
NI201800042A (es) Nuevos derivados de pirrolo[2,3-d]pirimidina como inhibidores duales de dyrk1/clk1
MX2016005394A (es) Compuestos derivados de piridilo biciclicos fusionados a anillo como inhibidores de fgfr4.
SV2018005687A (es) Derivados de dihidroimidazopirazinona usados en el tratamiento del cancer
SV2017005405A (es) Compuestos y composiciones como inhibidores de quinasa raf
CL2015001377A1 (es) Inhbibidores de bmi-1 primidinas sustituidas inversas
CL2015002698A1 (es) Nuevos compuestos y composiciones para la inhibicion de fasn
ECSP13012596A (es) Proceso de elaboración para derivados de pirimidina
CL2015001279A1 (es) Compuestos derivados de piridina, inhibidores del transportador de uratos urat 1; composicion farmaceutica que los comprende; uso para el tratamiento o prevencion de enfermedades tales como gota, hiperuricemia, hipertensión, enfermedades renales, entre otras.
GT201700023A (es) Derivados de heterociclico opcionalmente condensados de piridimina útiles para el tratamiento de enfermedades inflamatorias, metabolicas, oncológicas y autoinmunitarias
CL2017000682A1 (es) Compuestos novedosos de imidazopiridazina y su uso.
AR095032A1 (es) Formulaciones de compuestos orgánicos, composición farmacéutica sólida comprimida por rodillo
CR20160016A (es) Pirazolpiridinas sustituidas