AR074676A1 - Derivados de isooxazol como antagonistas de receptores de acido lisofosfatidico, composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades mediadas por la actividad fisiologica de lpa. - Google Patents

Derivados de isooxazol como antagonistas de receptores de acido lisofosfatidico, composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades mediadas por la actividad fisiologica de lpa.

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Publication number
AR074676A1
AR074676A1 ARP090104891A ARP090104891A AR074676A1 AR 074676 A1 AR074676 A1 AR 074676A1 AR P090104891 A ARP090104891 A AR P090104891A AR P090104891 A ARP090104891 A AR P090104891A AR 074676 A1 AR074676 A1 AR 074676A1
Authority
AR
Argentina
Prior art keywords
alkyl
antagonists
lpa
fluoroalkyl
lisophosphytidic
Prior art date
Application number
ARP090104891A
Other languages
English (en)
Inventor
Thomas Jon Seiders
Timothy Parr
John Howard Hutchinson
Bowei Wang
Jeannie M Arruda
Jeffrey Roger Roppe
Original Assignee
Amira Pharmaceuticals 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 Amira Pharmaceuticals Inc filed Critical Amira Pharmaceuticals Inc
Publication of AR074676A1 publication Critical patent/AR074676A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/14—Nitrogen atoms
    • 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
    • A61K31/41—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
    • A61K31/42—Oxazoles
    • 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
    • A61K31/41—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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P1/04—Drugs 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
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    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D413/02—Heterocyclic 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
    • C07D413/10—Heterocyclic 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 carbon chain containing aromatic rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

En este documento se describen compuestos que son antagonistas de receptor(es) lisofosfatídico(s). También se describen composiciones farmacéuticas y medicamentos que incluyen los compuestos que se describen en este documento, así como el uso de tales antagonistas, solos y en combinación con otros compuestos, para tratar condiciones o enfermedades dependientes de LPA o mediadas por LPA. Reivindicación 1: Un compuesto que tiene la estructura de la fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde R1 es -CO2H, -CO2RD, -CN, tetrazolilo, o -C(=O)NHSO2R10; RD es H o alquilo C1-4; L1 está ausente o es alquileno C1-6; R3 es H, alquilo C1-4, cicloalquilo C3-6, o fluoroalquilo C1-4; R7 es H o alquilo C1-4; R8 es H, alquilo C1-4 o fluoroalquilo C1-4; R10 es un alquilo C1-6, fluoroalquilo C1-6, cicloalquilo C3-6 o un fenilo sustituido o no sustituido; cada uno de RA, RB, y RC se seleccionan independientemente de H, F, CI, Br, I, -CN, -OH, alquilo C1-4, fluoroalquilo C1-4, fluoroalcoxi C1-4, alcoxi C1-4, y heteroalquilo C1-4; m es 0, 1, o 2; n es 0, 1, o 2; p es 0, 1, o 2.
ARP090104891A 2008-12-15 2009-12-15 Derivados de isooxazol como antagonistas de receptores de acido lisofosfatidico, composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades mediadas por la actividad fisiologica de lpa. AR074676A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US12256808P 2008-12-15 2008-12-15

Publications (1)

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AR074676A1 true AR074676A1 (es) 2011-02-02

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ARP090104891A AR074676A1 (es) 2008-12-15 2009-12-15 Derivados de isooxazol como antagonistas de receptores de acido lisofosfatidico, composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades mediadas por la actividad fisiologica de lpa.

Country Status (18)

Country Link
US (4) US20110301211A1 (es)
EP (1) EP2358688B1 (es)
JP (1) JP2012512178A (es)
KR (1) KR101323054B1 (es)
CN (1) CN102245584A (es)
AR (1) AR074676A1 (es)
AU (1) AU2009333275B2 (es)
BR (1) BRPI0923512A2 (es)
CA (1) CA2744221C (es)
EA (1) EA201100691A1 (es)
GB (1) GB2466121B (es)
IL (1) IL212779A (es)
MX (1) MX2011006407A (es)
SG (1) SG172163A1 (es)
TW (1) TWI415841B (es)
UY (1) UY32327A (es)
WO (2) WO2010077883A2 (es)
ZA (1) ZA201103945B (es)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2324852B1 (en) 2008-08-07 2015-07-08 Nagasaki University Therapeutic or prophylactic agent for generalized pain syndrome
US8455499B2 (en) 2008-12-11 2013-06-04 Amira Pharmaceuticals, Inc. Alkyne antagonists of lysophosphatidic acid receptors
GB2466121B (en) 2008-12-15 2010-12-08 Amira Pharmaceuticals Inc Antagonists of lysophosphatidic acid receptors
GB2470833B (en) * 2009-06-03 2011-06-01 Amira Pharmaceuticals Inc Polycyclic antagonists of lysophosphatidic acid receptors
EP2462128B1 (en) 2009-08-04 2016-09-21 Amira Pharmaceuticals, Inc. Compounds as lysophosphatidic acid receptor antagonists
GB2474748B (en) 2009-10-01 2011-10-12 Amira Pharmaceuticals Inc Polycyclic compounds as lysophosphatidic acid receptor antagonists
GB2474120B (en) * 2009-10-01 2011-12-21 Amira Pharmaceuticals Inc Compounds as Lysophosphatidic acid receptor antagonists
CA2809892C (en) 2010-09-02 2019-05-28 Merck Patent Gmbh Pyrazolopyridinone derivatives as lpa receptor antagonists
EA024967B1 (ru) * 2010-12-07 2016-11-30 Амира Фармасьютикалс, Инк. Полициклический lpaантагонист и его применение
MX2013006040A (es) * 2010-12-07 2013-08-26 Amira Pharmaceuticals Inc Antagonistas del receptor de acido lisofosfatidico y su uso en el tratamiento de fibrosis.
US8785442B2 (en) 2011-01-30 2014-07-22 Curegenix, Inc. Compound as antagonist of lysophosphatidic acid receptor, composition, and use thereof
JP2014513077A (ja) 2011-04-05 2014-05-29 アミラ ファーマシューティカルス，インコーポレーテッド 線維症、疼痛、癌、ならびに呼吸器、アレルギー性、神経系または心血管疾患の治療に有用な３−または５−ビフェニル−４−イルイソキサゾールに基づく化合物
KR20140067048A (ko) 2011-08-15 2014-06-03 인터뮨, 인크. 라이소포스파티드산 수용체 길항제
WO2013070879A1 (en) * 2011-11-10 2013-05-16 Bristol-Myers Squibb Company Methods for treating spinal cord injury with lpa receptor antagonists
US20130150426A1 (en) 2011-11-22 2013-06-13 Intermune, Inc. Methods of diagnosing and treating idiopathic pulmonary fibrosis
WO2013085824A1 (en) * 2011-12-04 2013-06-13 Angion Biomedica Corp. Small molecule anti-fibrotic compounds and uses thereof
KR20150011003A (ko) * 2012-06-20 2015-01-29 에프. 호프만-라 로슈 아게 Lpar 길항제로서 치환된 피라졸 화합물
AU2013279512A1 (en) * 2012-06-20 2014-10-16 F. Hoffmann-La Roche Ag N-alkyltriazole compounds as LPAR antagonists
EP2940013B1 (en) 2012-12-28 2018-02-21 Ube Industries, Ltd. Halogen-substituted heterocyclic compound
CA2906931C (en) 2013-03-15 2023-03-14 Epigen Biosciences, Inc. Heterocyclic compounds useful in the treatment of disease
KR102588702B1 (ko) 2013-03-15 2023-10-16 더 보드 오브 리젠츠 오브 더 유니버시티 오브 텍사스 시스템 누트린-3a 및 펩티드에 의한 폐 섬유증의 저해
US9567288B2 (en) 2013-12-30 2017-02-14 Rxbio, Inc. Crystalline salts of (Z)-O-octadec-9-en-1-yl O,O-dihydrogen phosphorothioate
MX370408B (es) 2014-06-27 2019-12-11 Ube Industries Sal de compuesto heterociclico sustituido con halogeno.
WO2016197009A1 (en) 2015-06-05 2016-12-08 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
CA3005811A1 (en) * 2015-11-20 2017-05-26 Ube Industries, Ltd. Pharmaceutical composition for treatment or prevention of nash
WO2018106643A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Heterocyclic azoles for the treatment of demyelinating diseases
WO2018106641A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Pyrazoles for the treatment of demyelinating diseases
WO2018106646A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Aminotriazoles for the treatment of demyelinating diseases
WO2019041340A1 (en) 2017-09-04 2019-03-07 Eli Lilly And Company LYSOPHOSPHATIDE ACID RECEPTOR 1 RECEPTOR INHIBITORS (LPAR1)
US11447475B2 (en) 2017-12-19 2022-09-20 Bristol-Myers Squibb Company Isoxazole N-linked carbamoyl cyclohexyl acids as LPA antagonists
JP7496826B2 (ja) 2018-09-10 2024-06-07 ラング セラピューティクス，エルエルシー Ｃａｖ－１タンパク質の修飾ペプチドフラグメント及び線維症の治療におけるその使用
CA3158743A1 (en) 2019-11-15 2021-05-20 Gilead Sciences, Inc. Triazole carbamate pyridyl sulfonamides as lpa receptor antagonists and uses thereof
US11702407B2 (en) 2020-06-03 2023-07-18 Gilead Sciences, Inc. LPA receptor antagonists and uses thereof
TWI843503B (zh) 2020-06-03 2024-05-21 美商基利科學股份有限公司 Lpa受體拮抗劑及其用途
US11980609B2 (en) 2021-05-11 2024-05-14 Gilead Sciences, Inc. LPA receptor antagonists and uses thereof
WO2023107938A1 (en) 2021-12-08 2023-06-15 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
AR128613A1 (es) 2022-02-25 2024-05-29 Lhotse Bio Inc Compuestos y composiciones para el tratamiento de afecciones asociadas con la actividad del receptor de lpa
CN115181069B (zh) * 2022-07-15 2023-04-11 天津医科大学眼科医院 一种防治近视的化合物
CN116236486B (zh) * 2023-03-30 2024-03-22 复旦大学附属中山医院 髓过氧化物酶抑制剂在制备心脏保护药物中的应用
CN117562896B (zh) * 2023-11-23 2024-04-26 中国人民解放军海军军医大学第二附属医院 Lpar拮抗剂在制备多发性骨髓瘤car t细胞联合治疗药物中的应用

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5612359A (en) * 1994-08-26 1997-03-18 Bristol-Myers Squibb Company Substituted biphenyl isoxazole sulfonamides
US5861359A (en) * 1995-07-25 1999-01-19 Fmc Corporation Herbicidal phenylmethoxphenyl heterocycles
EP0923579A1 (en) * 1996-08-27 1999-06-23 Novartis AG Herbicidal s-substituted 1,2,4,6-thiatriazines
WO1998028282A2 (en) 1996-12-23 1998-07-02 Du Pont Pharmaceuticals Company OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS
JP3237608B2 (ja) * 1997-04-21 2001-12-10 住友製薬株式会社 イソキサゾール誘導体
US20050119332A1 (en) 1998-03-12 2005-06-02 Lone Jeppesen Substituted thiophene compounds as modulators of protein tyrosine phosphatases (PTPases)
ES2249920T3 (es) * 1998-10-23 2006-04-01 Dow Agrosciences Llc Compuestos de 3.(fenilo sustituido)-5-(heterociclilo sustituidoi-1,2,4-triazol.
EP1175419B1 (en) 1999-04-02 2003-05-28 Bristol-Myers Squibb Pharma Company Aryl sulfonyls as factor xa inhibitors
DK1258484T3 (da) * 2000-02-18 2009-04-20 Kyowa Hakko Kirin Co Ltd Nye isoxazol- og thiazolforbindelser og anvendelse deraf som lægemidler
AU2001273040A1 (en) 2000-06-27 2002-01-08 Du Pont Pharmaceuticals Company Factor xa inhibitors
WO2002062389A1 (fr) * 2001-02-08 2002-08-15 Ono Pharmaceutical Co., Ltd. Remedes pour des maladies urinaires contenant des agents de regulation du recepteur de lpa
US7521192B2 (en) 2001-04-18 2009-04-21 Rigel Pharmaceuticals, Inc. EDG: modulators of lymphocyte activation and migration
US20040171582A1 (en) * 2001-07-17 2004-09-02 Shinji Nakade Pancreatic juice secretion regulators comprising lpa receptor controller
MY151199A (en) * 2001-11-02 2014-04-30 Rigel Pharmaceuticals Inc Substituted diphenyl heterocycles useful for treating hcv infection
EP1466602A4 (en) * 2001-12-25 2006-03-01 Ajinomoto Kk ORGAN FIBROSIS INHIBITORS
US20050101518A1 (en) * 2002-01-18 2005-05-12 David Solow-Cordero Methods of treating conditions associated with an EDG-2 receptor
US20050261298A1 (en) * 2002-01-18 2005-11-24 David Solow-Cordero Methods of treating conditions associated with an Edg-7 receptor
US20050113283A1 (en) * 2002-01-18 2005-05-26 David Solow-Cordero Methods of treating conditions associated with an EDG-4 receptor
JP2005519915A (ja) 2002-01-18 2005-07-07 セレテック・リミテッド・ライアビリティ・カンパニー Ｅｄｇ受容体に関連する症状の処置方法
WO2003094965A2 (en) * 2002-05-08 2003-11-20 Neuronova Ab Modulation of neural stem cells with s1p or lpa receptor agonists
WO2003097047A1 (en) 2002-05-13 2003-11-27 Eli Lilly And Company Multicyclic compounds for use as melanin concentrating hormone antagonists in the treatment of obesity and diabetes
WO2003099765A1 (fr) * 2002-05-28 2003-12-04 Ono Pharmaceutical Co., Ltd. Derive de $g(b)-alanine et utilisation correspondante
EP1550461A1 (en) * 2002-06-26 2005-07-06 Ono Pharmaceutical Co., Ltd. Remedy for chronic disease
TW200408393A (en) * 2002-10-03 2004-06-01 Ono Pharmaceutical Co Antagonist of lysophosphatidine acid receptor
CA2506243A1 (en) * 2002-11-19 2004-06-03 Amgen Inc. Amplified genes involved in cancer
US20050065194A1 (en) * 2003-01-16 2005-03-24 Geetha Shankar Methods of treating conditions associated with an Edg-2 receptor
US20040192739A1 (en) * 2003-01-16 2004-09-30 David Solow-Cordero Methods of treating conditions associated with an Edg-2 receptor
US20040167132A1 (en) * 2003-01-16 2004-08-26 Geetha Shankar Methods of treating conditions associted with an Edg-2 receptor
US7135469B2 (en) * 2003-03-18 2006-11-14 Bristol Myers Squibb, Co. Linear chain substituted monocyclic and bicyclic derivatives as factor Xa inhibitors
WO2004099164A1 (en) * 2003-05-02 2004-11-18 Rigel Pharmaceuticals, Inc. Substituted diphenyl isoxazoles, pyrazoles and oxadiazoles useful for treating hcv infection
JP4692281B2 (ja) 2003-08-05 2011-06-01 味の素株式会社 新規アゾール化合物
EP1695955B1 (en) * 2003-12-19 2011-10-12 Ono Pharmaceutical Co., Ltd. Compounds having lysophosphatidic acid receptor antagonism and uses thereof
DE10360369A1 (de) 2003-12-22 2005-07-14 Bayer Cropscience Ag Amide
JP5544503B2 (ja) * 2004-05-24 2014-07-09 独立行政法人物質・材料研究機構 マリモカーボン及びその製造方法並びにその製造装置
JP2006096712A (ja) 2004-09-30 2006-04-13 Senju Pharmaceut Co Ltd Ｌｐａ受容体拮抗剤を含有する角膜知覚改善剤
DE102005018389A1 (de) * 2005-04-20 2006-10-26 Sanofi-Aventis Deutschland Gmbh Azolderivate als Inhibitoren von Lipasen und Phospholipasen
BRPI0612028A2 (pt) 2005-06-08 2010-10-13 Novartis Ag oxadiazóis ou isodiazóis policìclicos e uso dos mesmos como ligantes de receptor s1p
WO2007007588A1 (ja) 2005-07-08 2007-01-18 Ono Pharmaceutical Co., Ltd. 平面性を有する環状基を母核とする化合物
CN101291908A (zh) 2005-08-23 2008-10-22 Irm责任有限公司 免疫抑制剂化合物和组合物
WO2007096647A2 (en) 2006-02-27 2007-08-30 Sterix Limited Diaryl compounds as non-steroidal inhibitors of 17-beta hydroxysteroid dehydrogenase and/or steroid sulphatase for the treatment of oestrogen-related diseases such as hormone dependent breast cancer
WO2007139946A2 (en) 2006-05-25 2007-12-06 University Of Tennessee Research Foundation Gpcr ligands identified by computational modeling
EP2054424A1 (en) * 2006-07-24 2009-05-06 University Of Virginia Patent Foundation Vinyl phosphonate lysophosphatidic acid receptor antagonists
US20080051372A1 (en) * 2006-08-24 2008-02-28 The Scripps Research Institute Methods utilizing cell-signaling lysophospholipids
WO2008024979A2 (en) 2006-08-24 2008-02-28 The Scripps Research Institute Methods utilizing cell-signaling lysophospholipids
US20100143381A1 (en) 2007-03-12 2010-06-10 Andrew Tager Lysophosphatidic acid receptor targeting for lung disease
WO2009011850A2 (en) 2007-07-16 2009-01-22 Abbott Laboratories Novel therapeutic compounds
NZ588807A (en) 2008-05-05 2011-07-29 Sanofi Aventis Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals
US8455499B2 (en) * 2008-12-11 2013-06-04 Amira Pharmaceuticals, Inc. Alkyne antagonists of lysophosphatidic acid receptors
GB2466121B (en) 2008-12-15 2010-12-08 Amira Pharmaceuticals Inc Antagonists of lysophosphatidic acid receptors
GB2470833B (en) 2009-06-03 2011-06-01 Amira Pharmaceuticals Inc Polycyclic antagonists of lysophosphatidic acid receptors
EP2462128B1 (en) 2009-08-04 2016-09-21 Amira Pharmaceuticals, Inc. Compounds as lysophosphatidic acid receptor antagonists
GB2474748B (en) 2009-10-01 2011-10-12 Amira Pharmaceuticals Inc Polycyclic compounds as lysophosphatidic acid receptor antagonists
GB2474120B (en) 2009-10-01 2011-12-21 Amira Pharmaceuticals Inc Compounds as Lysophosphatidic acid receptor antagonists

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