ES2573497T3 - Pirrolopirazin-amidas de piperidina espirocíclicas como moduladores de canales iónicos - Google Patents

Pirrolopirazin-amidas de piperidina espirocíclicas como moduladores de canales iónicos Download PDF

Info

Publication number
ES2573497T3
ES2573497T3 ES12704985.6T ES12704985T ES2573497T3 ES 2573497 T3 ES2573497 T3 ES 2573497T3 ES 12704985 T ES12704985 T ES 12704985T ES 2573497 T3 ES2573497 T3 ES 2573497T3
Authority
ES
Spain
Prior art keywords
piperidine
pyrazine
dihydropyrrolo
spiro
methyl
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES12704985.6T
Other languages
English (en)
Spanish (es)
Inventor
Sara S. Hadida Ruah
Edward Adam Kallel
Mark Thomas Miller
Vijayalaksmi Arumugam
Jason Mccartney
Corey Anderson
Peter Diederik Jan Grootenhuis
Licong JIANG
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex 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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Application granted granted Critical
Publication of ES2573497T3 publication Critical patent/ES2573497T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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 three 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
    • A61K31/495Heterocyclic 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
    • A61K31/499Spiro-condensed pyrazines or piperazines
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary 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
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • 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
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • 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
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • 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
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
ES12704985.6T 2011-02-02 2012-02-02 Pirrolopirazin-amidas de piperidina espirocíclicas como moduladores de canales iónicos Active ES2573497T3 (es)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201161438685P 2011-02-02 2011-02-02
US201161438685P 2011-02-02
US201161440987P 2011-02-09 2011-02-09
US201161440987P 2011-02-09
US201161495538P 2011-06-10 2011-06-10
US201161495538P 2011-06-10
PCT/US2012/023593 WO2012106499A1 (en) 2011-02-02 2012-02-02 Pyrrolopyrazine-spirocyclic piperidine amides as modulators of ion channels

Publications (1)

Publication Number Publication Date
ES2573497T3 true ES2573497T3 (es) 2016-06-08

Family

ID=45689011

Family Applications (1)

Application Number Title Priority Date Filing Date
ES12704985.6T Active ES2573497T3 (es) 2011-02-02 2012-02-02 Pirrolopirazin-amidas de piperidina espirocíclicas como moduladores de canales iónicos

Country Status (27)

Country Link
US (3) US8916565B2 (enExample)
EP (2) EP2670752B1 (enExample)
JP (2) JP6021824B2 (enExample)
KR (1) KR101923367B1 (enExample)
CN (2) CN103403004B (enExample)
AR (1) AR085893A1 (enExample)
AU (1) AU2012212196B2 (enExample)
BR (1) BR112013019211A2 (enExample)
CA (1) CA2825204C (enExample)
CY (1) CY1117471T1 (enExample)
DK (1) DK2670752T3 (enExample)
ES (1) ES2573497T3 (enExample)
HR (1) HRP20160382T8 (enExample)
HU (1) HUE028789T2 (enExample)
IL (1) IL227815B (enExample)
MX (1) MX355907B (enExample)
NZ (1) NZ613028A (enExample)
PL (1) PL2670752T3 (enExample)
PT (1) PT2670752E (enExample)
RS (1) RS54785B1 (enExample)
RU (1) RU2634900C2 (enExample)
SG (1) SG192248A1 (enExample)
SI (1) SI2670752T1 (enExample)
SM (1) SMT201600162B (enExample)
TW (2) TWI520964B (enExample)
WO (1) WO2012106499A1 (enExample)
ZA (1) ZA201305152B (enExample)

Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5389030B2 (ja) 2007-08-24 2014-01-15 バーテックス ファーマシューティカルズ インコーポレイテッド (特に)嚢胞性線維症の処置に有用なイソチアゾロピリジノン
WO2011140425A1 (en) 2010-05-06 2011-11-10 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
ES2573497T3 (es) 2011-02-02 2016-06-08 Vertex Pharmaceuticals Incorporated Pirrolopirazin-amidas de piperidina espirocíclicas como moduladores de canales iónicos
CA2827311A1 (en) 2011-02-18 2012-08-23 Vertex Pharmaceuticals Incorporated Chroman-spirocyclic piperidine amides as modulators of ion channels
CA2829803A1 (en) 2011-03-14 2012-09-20 Vertex Pharmaceuticals Incorporated Morpholine-spirocyclic piperidine amides as modulators of ion channels
EP2773641B1 (en) 2011-10-31 2017-09-27 Xenon Pharmaceuticals Inc. Biaryl ether sulfonamides and their use as therapeutic agents
ES2586213T3 (es) 2011-10-31 2016-10-13 Xenon Pharmaceuticals Inc. Compuestos de bencenosulfonamida y su uso como agentes terapéuticos
PE20150400A1 (es) 2012-05-22 2015-03-27 Genentech Inc Benzamidas n-sustituidas y su uso en el tratamiento del dolor
US10071957B2 (en) 2012-07-06 2018-09-11 Genentech, Inc. N-substituted benzamides and methods of use thereof
WO2014022639A1 (en) 2012-08-01 2014-02-06 Vertex Pharmaceuticals Incorporated Solid forms of (4-isopropoxy-3-methoxyphenyl)(2'-methyl-6'-(trifluoromethyl)-3',4'-dihydro-2'h-spiro[piperidine-4,1'-pyrrolo[1,2-a]pyrazine]-1-yl)methanone
EP3239134B1 (en) 2013-01-31 2020-12-23 Vertex Pharmaceuticals Incorporated Pyridone amides as modulators of sodium channels
AR095192A1 (es) 2013-01-31 2015-09-30 Vertex Pharma Quinolina y quinazolinamidas como modulares de canales de sodio
TW201444798A (zh) 2013-02-28 2014-12-01 必治妥美雅史谷比公司 作爲強效rock1及rock2抑制劑之苯基吡唑衍生物
WO2014134391A1 (en) 2013-02-28 2014-09-04 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors
RU2015143906A (ru) 2013-03-14 2017-04-18 Дженентек, Инк. Замещенные триазолопиридины и способы их применения
WO2014144545A2 (en) 2013-03-15 2014-09-18 Genentech, Inc. Substituted benzoxazoles and methods of use thereof
AU2014287471C1 (en) * 2013-07-10 2019-11-28 Vertex Pharmaceuticals Incorporated Fused piperidine amides as modulators of ion channels
EP3022175B1 (en) 2013-07-19 2017-11-08 Vertex Pharmaceuticals Incorporated Sulfonamides as modulators of sodium channels
CA2931732A1 (en) 2013-11-27 2015-06-04 Genentech, Inc. Substituted benzamides and methods of use thereof
KR102435145B1 (ko) 2013-12-13 2022-08-24 버텍스 파마슈티칼스 인코포레이티드 나트륨 채널의 조절제로서의 피리돈 아미드의 프로드럭
JP2017525677A (ja) 2014-07-07 2017-09-07 ジェネンテック, インコーポレイテッド 治療用化合物及びその使用方法
MA42118A (fr) 2015-05-22 2018-03-28 Genentech Inc Benzamides substitués et leurs méthodes d'utilisation
MA42683A (fr) 2015-08-27 2018-07-04 Genentech Inc Composés thérapeutiques et leurs méthodes utilisation
SG10202007787RA (en) 2015-09-28 2020-09-29 Genentech Inc Therapeutic compounds and methods of use thereof
WO2017091592A1 (en) 2015-11-25 2017-06-01 Genentech, Inc. Substituted benzamides useful as sodium channel blockers
EP3436432B1 (en) 2016-03-30 2021-01-27 Genentech, Inc. Substituted benzamides and methods of use thereof
WO2018072602A1 (en) 2016-10-17 2018-04-26 Genentech, Inc. Therapeutic compounds and methods of use thereof
CN106749330A (zh) * 2016-12-29 2017-05-31 长春海谱润斯科技有限公司 一种杂环衍生物及使用该杂环衍生物的有机发光器件
EP3601273B1 (en) 2017-03-24 2021-12-01 Genentech, Inc. 4-piperidin-n-(pyrimidin-4-yl)chroman-7-sulfonamide derivatives as sodium channel inhibitors
CA3063901A1 (en) 2017-05-16 2018-11-22 Vertex Pharmaceuticals Incorporated Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels
JP7277431B2 (ja) 2017-07-11 2023-05-19 バーテックス ファーマシューティカルズ インコーポレイテッド ナトリウムチャネルのモジュレーターとしてのカルボキサミド
EP3752152A1 (en) 2018-02-12 2020-12-23 Vertex Pharmaceuticals Incorporated A method of treating pain
AR114263A1 (es) 2018-02-26 2020-08-12 Genentech Inc Compuestos terapéuticos y métodos para utilizarlos
JP2021519788A (ja) * 2018-03-30 2021-08-12 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft ナトリウムチャネル阻害剤としての縮合環ヒドロピリド化合物
TW202003490A (zh) 2018-05-22 2020-01-16 瑞士商赫孚孟拉羅股份公司 治療性化合物及其使用方法
AU2019301628C1 (en) 2018-07-09 2025-02-06 Lieber Institute, Inc. Pyridine carboxamide compounds for inhibiting NaV1.8
AU2019302534B2 (en) 2018-07-09 2024-10-03 Lieber Institute, Inc. Pyridazine compounds for inhibiting NaV1.8
US11414431B2 (en) * 2018-10-15 2022-08-16 Nimbus Lakshmi, Inc. Substituted pyrazolo[1,5-a]pyrimidines as TYK2 inhibitors
US12440481B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
WO2020146682A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
WO2020176763A1 (en) 2019-02-27 2020-09-03 Vertex Pharmaceuticals Incorporated Dosage form comprising prodrug of na 1.8 sodium channel inhibitor
WO2020185915A1 (en) 2019-03-11 2020-09-17 Nocion Therapeutics, Inc. Ester substituted ion channel blockers and methods for use
AU2020237474C1 (en) 2019-03-11 2025-09-18 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US10828287B2 (en) 2019-03-11 2020-11-10 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
CA3129111A1 (en) 2019-03-11 2020-09-17 Bridget M. Cole Charged ion channel blockers and methods for use
WO2020219867A1 (en) 2019-04-25 2020-10-29 Vertex Pharmaceuticals Incorporated Pyridone amide co-crystal compositions for the treatment of pain
KR102890953B1 (ko) 2019-11-06 2025-11-24 녹시온 테라퓨틱스 인코포레이티드 하전된 이온 채널 차단제 및 사용 방법
US10933055B1 (en) 2019-11-06 2021-03-02 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
PH12022551379A1 (en) 2019-12-06 2023-05-03 Vertex Pharma Substituted tetrahydrofurans as modulators of sodium channels
US12162851B2 (en) 2020-03-11 2024-12-10 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
WO2021183639A1 (en) 2020-03-11 2021-09-16 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US20240294512A1 (en) 2021-06-04 2024-09-05 Vertex Pharmaceuticals Incorporated Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels
WO2022256702A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels
DK4347031T3 (da) 2021-06-04 2025-12-01 Vertex Pharma N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler
KR20240031299A (ko) 2021-06-04 2024-03-07 버텍스 파마슈티칼스 인코포레이티드 (2r,3s,4s,5r)-4-[[3-(3,4-디플루오로-2-메톡시-페닐)-4,5-디메틸-5-(트리플루오로메틸)테트라하이드로푸란-2-카르보닐]아미노]피리딘-2-카르복사미드를 포함하는 고체 투여 형태 및 투여 요법
AU2022286438A1 (en) 2021-06-04 2023-11-30 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels
CA3221938A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran analogs as modulators of sodium channels
CA3257285A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated HETEROARYL COMPOUNDS FOR PAIN RELIEF
US20250388543A1 (en) 2022-04-22 2025-12-25 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
CA3256604A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated HETEROARYL COMPOUNDS FOR PAIN RELIEF
CR20240513A (es) 2022-04-22 2025-04-30 Vertex Pharma Compuestos de heteroarilo para el tratamiento del dolor
CN120603815A (zh) 2022-12-06 2025-09-05 沃泰克斯药物股份有限公司 钠通道的取代四氢呋喃调节剂的合成方法
CN117385378B (zh) * 2023-10-13 2024-09-24 厦门大学 一种缺电子芳香缩醛的电氧化制备方法和应用
WO2025090516A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Methods of preparing compounds for treating pain and solid forms thereof
WO2025090480A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
TW202535867A (zh) 2023-10-23 2025-09-16 美商維泰克斯製藥公司 用於治療疼痛之鈉通道調節劑及其固體形式的製備方法
TW202523313A (zh) 2023-10-23 2025-06-16 美商維泰克斯製藥公司 用於治療疼痛之雜芳基化合物
US20250186419A1 (en) 2023-12-07 2025-06-12 Vertex Pharmaceuticals Incorporated Dosing regimens for treating pain
EP4648759A1 (en) * 2024-03-22 2025-11-19 Queen, Aaric Magnesium and lidocaine composition
US20260001877A1 (en) 2024-06-28 2026-01-01 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain

Family Cites Families (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3939159A (en) 1974-05-29 1976-02-17 American Hoechst Corporation Spiro(pyrrolo (1,2-A)quinoxalines)
PT67194B (en) 1976-11-02 1979-03-23 Lilly Co Eli Process for preparing 4a-aryl-octahydro-1h-2-pyrindines
NZ189230A (en) 1977-12-27 1981-05-15 Lilly Co Eli Trans-4a-aryl-2-substituted-octahydro-1h-2-pyrindines
US4353901A (en) 1981-10-19 1982-10-12 Syntex (U.S.A.) Inc. 9-(1,4-Benzodioxan-2-ylalkyl and hydroxyalkyl)-1-oxa-4,9-diazaspiro[5.5]undecan-3-ones
GB8827479D0 (en) 1988-11-24 1988-12-29 Zambeletti Spa L Novel compounds
US5206240A (en) 1989-12-08 1993-04-27 Merck & Co., Inc. Nitrogen-containing spirocycles
IL96507A0 (en) 1989-12-08 1991-08-16 Merck & Co Inc Nitrogen-containing spirocycles and pharmaceutical compositions containing them
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
JPH04297458A (ja) 1991-03-27 1992-10-21 Toray Ind Inc イソキノリン誘導体およびその製造方法
GB9104656D0 (en) 1991-03-05 1991-04-17 Zambeletti Spa L Pharmaceuticals
US5994341A (en) 1993-07-19 1999-11-30 Angiogenesis Technologies, Inc. Anti-angiogenic Compositions and methods for the treatment of arthritis
DE4341403A1 (de) 1993-12-04 1995-06-08 Basf Ag N-substituierte 3-Azabicycloalkan-Derivate, ihre Herstellung und Verwendung
US6017768A (en) 1994-05-06 2000-01-25 Pharmacopeia, Inc. Combinatorial dihydrobenzopyran library
EP0758313A4 (en) 1994-05-06 1999-09-15 Pharmacopeia Inc COMBINATORIAL LIBRARY OF DIHYDROBENZOPYRANES
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
IT1276462B1 (it) 1995-07-03 1997-10-31 Rotta Research Lab Diamidi aromatiche acide ad attivita' antigastrinica, procedimento per la loro preparazione e loro uso farmaceutico
JPH11512723A (ja) 1995-09-29 1999-11-02 イーライ リリー アンド カンパニー フィブリノゲン依存血小板凝集抑制物質としてのスピロ化合物
IL146755A0 (en) * 1999-06-07 2002-07-25 Warner Lambert Co Tricyclic analgesics
US20040266802A1 (en) 1999-06-07 2004-12-30 Alain Calvet Tricyclic analgesics
US20020151712A1 (en) 1999-09-14 2002-10-17 Nan-Horng Lin 3-pyrrolidinyloxy-3'-pyridyl ether compounds useful for controlling chemical synaptic transmission
WO2002020509A2 (de) 2000-09-06 2002-03-14 Bayer Aktiengesellschaft Arzneimittel gegen virale erkrankungen
US20040014744A1 (en) 2002-04-05 2004-01-22 Fortuna Haviv Substituted pyridines having antiangiogenic activity
AU2003235912A1 (en) 2002-05-10 2003-11-11 Taisho Pharmaceutical Co., Ltd. Spiro-ring compound
AU2003242092A1 (en) 2002-06-11 2003-12-22 Sankyo Company, Limited Process for producing cyclic thioether and synthetic intermediate thereof
WO2004037800A1 (en) 2002-10-22 2004-05-06 Glaxo Group Limited Aryloxyalkylamine derivates as h3 receptor ligands
CA2503520A1 (en) 2002-10-24 2004-05-06 Sankyo Company Limited Process for producing optically active sulfoxide
AU2003300902A1 (en) 2002-12-13 2004-07-09 Smithkline Beecham Corporation Piperidine derivatives as CCR5 antagonists
CA2512886A1 (en) 2003-02-28 2004-09-10 Galderma Research & Development, S.N.C. Ligands that modulate lxr-type receptors
WO2004092179A1 (ja) 2003-04-14 2004-10-28 Nippon Soda Co. Ltd. スピロ誘導体、製造法および抗酸化薬
FR2856685B1 (fr) 2003-06-25 2005-09-23 Merck Sante Sas Derives de thiazolylpiperidine, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent
JP4976134B2 (ja) 2003-10-01 2012-07-18 アドラー コーポレーション スピロ環複素環誘導体及びそれらを使用する方法
EP1679069A4 (en) 2003-10-21 2009-05-13 Dainippon Sumitomo Pharma Co NEW PIPERIDINE DERIVATIVE
TWI350168B (en) 2004-05-07 2011-10-11 Incyte Corp Amido compounds and their use as pharmaceuticals
WO2005121090A1 (en) 2004-06-02 2005-12-22 Abbott Laboratories Substituted piperidines that have antiangiogenic activity
US7598261B2 (en) 2005-03-31 2009-10-06 Adolor Corporation Spirocyclic heterocyclic derivatives and methods of their use
EP1879863A1 (en) 2005-05-03 2008-01-23 Pfizer, Inc. Amide resorcinol compounds
WO2007050124A1 (en) 2005-05-19 2007-05-03 Xenon Pharmaceuticals Inc. Fused piperidine derivatives and their uses as therapeutic agents
EP1910375B1 (en) 2005-07-19 2011-05-11 Merck Sharp & Dohme Corp. Spirochromanone derivatives as acetyl coenzyme a carboxylase (acc) inhibitors
JP2009508963A (ja) 2005-09-21 2009-03-05 インサイト・コーポレイション アミド化合物および医薬組成物としてのその使用
PL1961744T3 (pl) 2005-11-18 2013-09-30 Ono Pharmaceutical Co Związek zawierający grupę zasadową oraz jego zastosowanie
CN101360750A (zh) * 2005-11-23 2009-02-04 英特芒尼公司 应激活化蛋白激酶系统的调节方法
AR057579A1 (es) 2005-11-23 2007-12-05 Merck & Co Inc Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac)
US20080027072A1 (en) 2006-04-20 2008-01-31 Ampla Pharmaceuticals, Inc. Potentiation of MC4 receptor activity
EP2024370A1 (en) 2006-05-05 2009-02-18 Boehringer Ingelheim International GmbH Spiro- (tho) benzopyran-2, 4' -piperidine-and cyclohexane derivatives as inhibitors of specific cell cycle enzymes
JP5257068B2 (ja) 2006-05-16 2013-08-07 小野薬品工業株式会社 保護されていてもよい酸性基を含有する化合物およびその用途
AU2007254359A1 (en) 2006-05-18 2007-11-29 Merck Sharp & Dohme Corp. Aryl-fused spirocyclic compounds
WO2008016006A1 (fr) 2006-07-31 2008-02-07 Ono Pharmaceutical Co., Ltd. Composé auquel un groupe cyclique est lié par une liaison spiro et son utilisation
MX2009002715A (es) 2006-09-12 2009-08-12 Adolor Corp Metodos para mejorar la funcion cognoscitiva.
US20100210633A1 (en) 2006-10-12 2010-08-19 Epix Delaware, Inc. Carboxamide compounds and their use
WO2008065508A1 (en) 2006-11-29 2008-06-05 Pfizer Products Inc. Spiroketone acetyl-coa carboxylase inhibitors
KR101122969B1 (ko) * 2006-12-22 2012-03-22 에프. 호프만-라 로슈 아게 스피로-피페리딘 유도체
JP5271917B2 (ja) 2007-01-12 2013-08-21 メルク・シャープ・アンド・ドーム・コーポレーション スピロクロマノン誘導体
PE20081559A1 (es) 2007-01-12 2008-11-20 Merck & Co Inc DERIVADOS DE ESPIROCROMANONA SUSTITUIDOS COMO INHIBIDORES DE ACETIL CoA CARBOXILASA
US20100113418A1 (en) 2007-02-20 2010-05-06 Takeda Pharmaceutical Company Limited Heterocyclic compound
EP2110377A1 (en) 2008-04-15 2009-10-21 DAC S.r.l. Spirocyclic derivatives as histone deacetylase inhibitors
US8318762B2 (en) 2008-05-28 2012-11-27 Pfizer Inc. Pyrazolospiroketone acetyl-CoA carboxylase inhibitors
EP2307422B1 (en) 2008-07-04 2014-03-26 Msd K.K. Novel spirochromanone carboxylic acids
EP2318404B1 (en) 2008-07-16 2013-08-21 Merck Sharp & Dohme Corp. Bicyclic heterocycle derivatives and use thereof as gpr119 modulators
US20110166124A1 (en) 2008-07-23 2011-07-07 Mccormick Kevin D Tricyclic spirocycle derivatives and methods of use
CA2779261C (en) 2008-10-31 2015-03-24 Pain Therapeutics, Inc. Filamin a binding anti-inflammatory and analgesic
CA2779252C (en) 2008-10-31 2015-05-05 Pain Therapeutics, Inc. Filamin a-binding anti-inflammatory analgesic
WO2010114957A1 (en) 2009-04-03 2010-10-07 Schering Corporation Bicyclic piperidine and piperazine derivatives as gpcr modulators for the treatment of obesity, diabetes and other metabolic disorders
WO2010151597A1 (en) * 2009-06-26 2010-12-29 Schering Corporation Methods for using pyrrolo-benzo-1,4-diazines as sodium channel blockers
EP2470021B1 (en) 2009-08-27 2014-10-22 Merck Sharp & Dohme Corp. Novel pyrrolidine derived beta 3 adrenergic receptor agonists
UY33199A (es) 2010-01-26 2011-08-31 Boehringer Ingelheim Int 5-alquinil-pirimidinas.
WO2011140425A1 (en) 2010-05-06 2011-11-10 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
ES2573497T3 (es) * 2011-02-02 2016-06-08 Vertex Pharmaceuticals Incorporated Pirrolopirazin-amidas de piperidina espirocíclicas como moduladores de canales iónicos
CA2827311A1 (en) 2011-02-18 2012-08-23 Vertex Pharmaceuticals Incorporated Chroman-spirocyclic piperidine amides as modulators of ion channels
CA2829803A1 (en) 2011-03-14 2012-09-20 Vertex Pharmaceuticals Incorporated Morpholine-spirocyclic piperidine amides as modulators of ion channels

Also Published As

Publication number Publication date
CN106008504A (zh) 2016-10-12
RU2013140401A (ru) 2015-03-10
KR20140014162A (ko) 2014-02-05
WO2012106499A1 (en) 2012-08-09
SMT201600162B (it) 2016-07-01
BR112013019211A2 (pt) 2021-07-06
RS54785B1 (sr) 2016-10-31
IL227815A0 (en) 2013-09-30
SG192248A1 (en) 2013-09-30
KR101923367B1 (ko) 2018-12-04
TW201604196A (zh) 2016-02-01
US20170145011A1 (en) 2017-05-25
HRP20160382T1 (hr) 2016-06-17
EP2670752A1 (en) 2013-12-11
HUE028789T2 (en) 2017-01-30
CY1117471T1 (el) 2017-04-26
EP2670752B1 (en) 2016-03-16
TW201309699A (zh) 2013-03-01
US20150174127A1 (en) 2015-06-25
JP6261558B2 (ja) 2018-01-17
MX355907B (es) 2018-05-04
AU2012212196A1 (en) 2013-07-25
US9511067B2 (en) 2016-12-06
RU2634900C2 (ru) 2017-11-08
HRP20160382T8 (hr) 2016-10-21
JP2016041764A (ja) 2016-03-31
CN103403004A (zh) 2013-11-20
CA2825204A1 (en) 2012-08-09
CN103403004B (zh) 2016-06-01
PT2670752E (pt) 2016-06-14
CA2825204C (en) 2019-06-11
SI2670752T1 (sl) 2016-10-28
MX2013008902A (es) 2013-08-21
PL2670752T3 (pl) 2016-09-30
JP6021824B2 (ja) 2016-11-09
IL227815B (en) 2019-07-31
EP3056495A1 (en) 2016-08-17
AR085893A1 (es) 2013-11-06
US8916565B2 (en) 2014-12-23
TWI520964B (zh) 2016-02-11
JP2014504642A (ja) 2014-02-24
DK2670752T3 (en) 2016-07-04
AU2012212196B2 (en) 2016-10-13
NZ613028A (en) 2015-08-28
ZA201305152B (en) 2014-09-25
US20120196869A1 (en) 2012-08-02

Similar Documents

Publication Publication Date Title
ES2573497T3 (es) Pirrolopirazin-amidas de piperidina espirocíclicas como moduladores de canales iónicos
ES2539859T3 (es) Nuevo derivado de aminodihidrotiazina condensado
ES2606016T3 (es) Derivados de piperidina condensados en espiro para su uso como inhibidores del canal de potasio medular externo renal
ES2989888T3 (es) Derivados heterocíclicos novedosos útiles como inhibidores de SHP2
CN113614087B (zh) Wee1抑制剂及其制备和用途
ES2618421T3 (es) Moduladores espiro-lactama del receptor NMDA y usos de los mismos
ES2610360T3 (es) Compuestos de imidazotriazinona
RU2559881C2 (ru) Производные дигидроптеридинона, способ их получения и фармацевтическое применение
ES2625330T3 (es) Compuestos multicíclicos y métodos de uso de estos
EP3455226B1 (en) Spirocycle compounds and methods of making and using same
BR112020012084A2 (pt) compostos de indol substituído úteis como inibidores de tlr
BR112019014549A2 (pt) Compostos de fórmulas i, ig, ih, ie, compostos, composição farmacêutica, métodos de tratamento, de modulação da atividade de um alvo biológico, de inibição da ativação de um inflamassoma e utilização de um composto
JP2025528147A (ja) 複素環式化合物、その組成物、及びそれによる処置方法
BR112020011771A2 (pt) compostos 4-azaindol
EA031905B1 (ru) Спиролактамные модуляторы рецептора nmda и их применение
KR20230174210A (ko) 신경 및 정신 장애의 치료를 위한 옥사-이보게인 유사체
BR112020015666A2 (pt) moduladores de espiro-lactamas de receptores nmda e usos dos mesmos
ES2986559T3 (es) Derivados de indol como inhibidores de la histona desmetilasa
TW202134234A (zh) 雷帕黴素類似物及其用途
WO2022017368A1 (zh) Dna-pk选择性抑制剂及其制备方法和用途
CN116782894A (zh) 作为Kv1.3钾Shaker通道阻断剂的内酰胺化合物
JP2025526290A (ja) エストロゲン受容体分解剤としてのテトラヒドロナフタレン誘導体
TW201309655A (zh) 降低β-類澱粉生成之化合物
WO2025136936A1 (en) Agonists of trem2 activity
KR102640696B1 (ko) Pde7 억제제로서 치환된 벤즈옥사졸 및 벤조푸란 화합물