CY1122652T1 - Σπειροκυκλικες ενωσεις ως αναστολεις υδροξυλασης τρυπτοφανης - Google Patents

Σπειροκυκλικες ενωσεις ως αναστολεις υδροξυλασης τρυπτοφανης

Info

Publication number
CY1122652T1
CY1122652T1 CY20201100036T CY201100036T CY1122652T1 CY 1122652 T1 CY1122652 T1 CY 1122652T1 CY 20201100036 T CY20201100036 T CY 20201100036T CY 201100036 T CY201100036 T CY 201100036T CY 1122652 T1 CY1122652 T1 CY 1122652T1
Authority
CY
Cyprus
Prior art keywords
inhibitors
hydrosylase
tryptophane
spirocyclic compounds
diseases
Prior art date
Application number
CY20201100036T
Other languages
English (en)
Inventor
Stéphane De Lombaert
Daniel R. Goldberg
Kenneth Brameld
Eric Brian Sjogren
Andrew Scribner
Original Assignee
Roivant Sciences Gmbh
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 Roivant Sciences Gmbh filed Critical Roivant Sciences Gmbh
Publication of CY1122652T1 publication Critical patent/CY1122652T1/el

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0078—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/10—Laxatives
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Nutrition Science (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dispersion Chemistry (AREA)
  • Physiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Η παρούσα εφεύρεση κατευθύνεται σε σπειροκυκλικές ενώσεις οι οποίες είναι αναστολείς υδροξυλάσης τρυπτοφάνης (ΤΡΗ), ιδιαιτέρως ισόμορφης 1 (ΤΡΗ1), που είναι χρήσιμες στη θεραπεία ασθενειών ή διαταραχών που συνδυάζονται με περιφερική σεροτονίνη που συμπεριλαμβάνει, για παράδειγμα, γαστρεντερικές, καρδιαγγειακές, πνευμονικές, φλεγμονώδεις, μεταβολικές και χαμηλής οστικής μάζας ασθένειες, καθώς επίσης σύνδρομο σεροτονίνης και καρκίνο.
CY20201100036T 2013-09-06 2020-01-15 Σπειροκυκλικες ενωσεις ως αναστολεις υδροξυλασης τρυπτοφανης CY1122652T1 (el)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201361874545P 2013-09-06 2013-09-06
US201361899943P 2013-11-05 2013-11-05
US201462004385P 2014-05-29 2014-05-29
PCT/US2014/054202 WO2015035113A1 (en) 2013-09-06 2014-09-05 Spirocyclic compounds as tryptophan hydroxylase inhibitors

Publications (1)

Publication Number Publication Date
CY1122652T1 true CY1122652T1 (el) 2021-05-05

Family

ID=51743540

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20201100036T CY1122652T1 (el) 2013-09-06 2020-01-15 Σπειροκυκλικες ενωσεις ως αναστολεις υδροξυλασης τρυπτοφανης

Country Status (31)

Country Link
US (8) US9199994B2 (el)
EP (1) EP3041842B8 (el)
JP (1) JP6470290B2 (el)
KR (1) KR102336075B1 (el)
CN (1) CN105764902B (el)
AR (1) AR097571A1 (el)
AU (1) AU2014315109B2 (el)
CA (1) CA2922933C (el)
CL (1) CL2016000509A1 (el)
CY (1) CY1122652T1 (el)
DK (1) DK3041842T3 (el)
EA (1) EA032304B1 (el)
EC (1) ECSP16014324A (el)
ES (1) ES2780828T3 (el)
HK (1) HK1225720A1 (el)
HR (1) HRP20200098T1 (el)
HU (1) HUE047574T2 (el)
IL (1) IL244315B (el)
LT (1) LT3041842T (el)
MX (1) MX371191B (el)
MY (1) MY186265A (el)
PE (1) PE20160648A1 (el)
PH (1) PH12016500416B1 (el)
PL (1) PL3041842T3 (el)
PT (1) PT3041842T (el)
RS (1) RS59871B1 (el)
SG (2) SG10202013041QA (el)
SI (1) SI3041842T1 (el)
TW (1) TWI652267B (el)
UA (1) UA119247C2 (el)
WO (1) WO2015035113A1 (el)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA119247C2 (uk) * 2013-09-06 2019-05-27 РОЙВЕНТ САЙЕНСИЗ ҐмбГ Спіроциклічні сполуки як інгібітори триптофангідроксилази
US9611201B2 (en) 2015-03-05 2017-04-04 Karos Pharmaceuticals, Inc. Processes for preparing (R)-1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanol and 1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanone
CN107176940B (zh) * 2016-03-09 2019-05-28 江苏正大丰海制药有限公司 一种替卡法林的制备方法
WO2018060949A1 (en) 2016-09-30 2018-04-05 Roivant Sciences Gmbh Tryptophan hydroxylase inhibitors for use in the treatment of liver diseases
AR110150A1 (es) 2016-11-09 2019-02-27 Roivant Sciences Gmbh Procesos para la preparación de inhibidores de tph1
US10472313B1 (en) 2018-02-18 2019-11-12 Graphene 3D Lab Inc. Process for synthesizing trifluoroketones
MX2021005559A (es) * 2018-11-14 2021-09-10 Altavant Sciences Gmbh Compuesto espirocíclico cristalino, forma de dosificación que lo contiene, procedimiento de uso en el tratamiento de una enfermedad y procedimiento de recristalización.
KR20210105343A (ko) * 2018-11-16 2021-08-26 알타반트 사이언시스 게엠베하 폐동맥 고혈압 및 관련 폐동맥 고혈압의 치료 방법
US20200188398A1 (en) 2018-12-17 2020-06-18 Altavant Sciences Gmbh Method for treating sarcoidosis-associated pulmonary hypertension
US20200188399A1 (en) 2018-12-17 2020-06-18 Altavant Sciences Gmbh Method for treating interstitial lung disease
AU2020213746A1 (en) 2019-01-30 2021-08-19 Altavant Sciences Gmbh A dosage regime and method for treating pulmonary arterial hypertension with rodatristat ethyl
MX2021011224A (es) * 2019-03-15 2021-12-10 Altavant Sciences Gmbh Un método para tratar la hipertensión arterial pulmonar y la hipertensión arterial pulmonar asociada y pauta posológica diaria.
MX2022006636A (es) * 2019-12-02 2022-11-09 Altavant Sciences Gmbh Tratamiento de trastornos de las vías respiratorias bajas.
CN111007170B (zh) * 2019-12-13 2021-06-29 中国农业科学院农产品加工研究所 骨肽干预治疗骨质疏松中的生物标志物、筛选方法及用途
US20230074252A1 (en) 2020-01-31 2023-03-09 Altavant Sciences Gmbh Dosages and methods for treating pulmonary arterial hypertension with rodatristat
WO2023062595A1 (en) 2021-10-14 2023-04-20 Altavant Sciences Gmbh Treatment of subjects having pulmonary arterial hypertension with rodatristat ethyl
WO2023079486A1 (en) 2021-11-03 2023-05-11 Altavant Sciences Gmbh Treatment of pulmonary arterial hypertension with rodatristat and ambrisentan

Family Cites Families (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR920700613A (ko) 1989-05-16 1992-08-10 지구르트 퓌터 약제제
DE69730033T2 (de) 1996-08-28 2005-07-21 The Procter & Gamble Company, Cincinnati Spirocyclisch metalloprotease inhibitoren
DK1263745T3 (da) 2000-03-07 2004-08-16 Aventis Pharma Gmbh Substituerede 3-phenyl-5-alkoxy-1,3,4-oxadiaxol-2-oner og anvendelse deraf til inhibering af hormonfölsom lipase
US7067517B2 (en) 2001-12-14 2006-06-27 Nero Nordisk A/S Use of compounds for decreasing activity of hormone-sensitive lipase
DE10247680B4 (de) 2002-10-12 2005-09-01 Aventis Pharma Deutschland Gmbh Neue bicyclische Inhibitoren der Hormon Sensitiven Lipase
KR20060017791A (ko) 2003-06-12 2006-02-27 노보 노르디스크 에이/에스 호르몬-민감성 리파제 억제제로서의 피리디닐 카르바메이트
JP2006527212A (ja) 2003-06-12 2006-11-30 ノボ　ノルディスク　アクティーゼルスカブ ホルモン感受性リパーゼの阻害剤として使用するための、置換ピペラジンカルバメート
DE102004005172A1 (de) 2004-02-02 2005-08-18 Aventis Pharma Deutschland Gmbh Indazolderivate als Inhibitoren der Hormon Sensitiven Lipase
DE102005002130A1 (de) 2005-01-17 2006-07-27 Sanofi-Aventis Deutschland Gmbh Substituierte N-Aminomethylensulfonamide, ihre Herstellung und Verwendung als Arzneimittel
US8673848B2 (en) 2012-01-27 2014-03-18 Novartis Ag Synthetic apelin mimetics for the treatment of heart failure
AR057579A1 (es) 2005-11-23 2007-12-05 Merck & Co Inc Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac)
PT1984344E (pt) 2005-12-29 2012-12-21 Lexicon Pharmaceuticals Inc Derivados de aminoácidos multicíclicos e métodos para a sua utilização
UA99270C2 (en) 2006-12-12 2012-08-10 Лексикон Фармасьютикалз, Инк. 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds and methods of their use
US8252803B2 (en) * 2007-02-12 2012-08-28 Merck Sharp & Dohme Corp. Piperidine derivatives
JP5248600B2 (ja) 2007-05-16 2013-07-31 イーライ リリー アンド カンパニー トリアゾリルアミノピリミジン化合物
KR20100046189A (ko) 2007-07-11 2010-05-06 렉시컨 파마슈티컬스 인코퍼레이티드 폐고혈압 및 관련 질환 및 장애의 치료를 위한 방법 및 조성물
BRPI0813835A2 (pt) 2007-07-26 2017-06-06 Lexicon Pharmaceuticals Inc métodos de afetar o trânsito gastrointestinal e esvaziamento gástrico, e compostos úteis a esse respeito
US20100255001A1 (en) 2007-09-24 2010-10-07 Universität Zürich Prorektorat Mnw Blockers of serotonin and its receptors for the treatment of hepatitis
NZ588737A (en) 2008-03-31 2012-05-25 Univ Columbia Methods of diagnosing, preventing and treating bone mass diseases
CN101591332B (zh) 2008-05-30 2014-04-16 莱西肯医药有限公司 基于4-苯基-6-(2,2,2-三氟-1-苯基乙氧基)嘧啶的化合物及其应用方法
CN104045626B (zh) 2008-05-30 2017-01-11 莱西肯医药有限公司 基于4-苯基-6-(2,2,2-三氟-1-苯基乙氧基)嘧啶的化合物及其应用方法
TW201022267A (en) 2008-10-23 2010-06-16 Gruenenthal Gmbh Substituierte pyrimidin-und triazin-derivate
WO2010056992A1 (en) 2008-11-13 2010-05-20 The Trustees Of Columbia University In The City Of New York Methods of preventing and treating low bone mass diseases
WO2010065333A1 (en) 2008-12-01 2010-06-10 Lexicon Pharmaceuticals, Inc. 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds for the treatment of osteoporosis
WO2010109442A1 (en) 2009-03-26 2010-09-30 Ranbaxy Laboratories Limited Process for the preparation of desloratadine
WO2010147094A1 (ja) 2009-06-16 2010-12-23 小野薬品工業株式会社 スピロ結合した環状基を有する化合物およびその用途
US8796297B2 (en) * 2009-06-30 2014-08-05 Abbvie Inc. 4-substituted-2-amino-pyrimidine derivatives
WO2011053977A1 (en) 2009-11-02 2011-05-05 The Trustees Of Columbia University In The City Of New York Compounds and methods for inhibiting serotonin synthesis
US20120316171A1 (en) 2009-11-05 2012-12-13 Tamas Oravecz Tryptophan Hydroxylase Inhibitors for the Treatment of Cancer
WO2011063181A1 (en) 2009-11-23 2011-05-26 Lexicon Pharmaceuticals, Inc. Methods and assays for the treatment of irritable bowel syndrome
WO2011100285A1 (en) 2010-02-10 2011-08-18 Lexicon Pharmaceuticals, Inc. Tryptophan hydroxylase inhibitors for the treatment of metastatic bone disease
JP2013519732A (ja) * 2010-02-17 2013-05-30 アムジエン・インコーポレーテツド 疼痛治療のためのナトリウムチャンネル阻害薬としてのアリールカルボキサミド誘導体
SG186989A1 (en) 2010-07-14 2013-02-28 Novartis Ag Ip receptor agonist heterocyclic compounds
EP2624698A4 (en) * 2010-10-08 2014-10-08 Abbvie Inc Furo [3,2-D] PYRIMIDINE COMPOUNDS
TW201245183A (en) 2010-11-05 2012-11-16 Lexicon Pharmaceuticals Inc Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid
US8883819B2 (en) 2011-09-01 2014-11-11 Irm Llc Bicyclic heterocycle derivatives for the treatment of pulmonary arterial hypertension
AU2012326383B2 (en) 2011-10-17 2017-07-27 Tersera Therapeutics Llc Solid dosage forms of (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate
US9717727B2 (en) 2011-11-17 2017-08-01 The Trustees Of Columbia University In The City Of New York Methods of treating and preventing leukemia and other cancers of the blood and bone
WO2013105065A1 (en) 2012-01-13 2013-07-18 Novartis Ag Fused piperidines as ip receptor agonists for the treatment of pah and related disorders
WO2013105063A1 (en) 2012-01-13 2013-07-18 Novartis Ag Fused piperidines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
EP2802584B1 (en) 2012-01-13 2015-11-18 Novartis AG Salts of an ip receptor agonist
WO2013105058A1 (en) 2012-01-13 2013-07-18 Novartis Ag 7,8- dihydropyrido [3, 4 - b] pyrazines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
AR089698A1 (es) 2012-01-13 2014-09-10 Novartis Ag Compuestos heterociclicos antagonistas del receptor ip
EP2802582A1 (en) 2012-01-13 2014-11-19 Novartis AG Fused dihydropyrido [2,3 -b]pyrazines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
EP2634190A1 (en) * 2012-03-01 2013-09-04 Lead Discovery Center GmbH Pyrazolo-triazine derivatives as selective cyclin-dependent kinase inhinitors
WO2013148978A1 (en) 2012-03-30 2013-10-03 Lexicon Pharmaceuticals, Inc. Methods and compositions for the treatment of necrotizing enterocolitis
WO2014082034A1 (en) 2012-11-26 2014-05-30 Lexicon Pharmaceuticals, Inc. Methods for treating irritable bowel syndrome
CA2900413A1 (en) 2013-02-15 2014-08-21 Mcmaster University A method of treating obesity
WO2014195847A2 (en) 2013-06-03 2014-12-11 Actelion Pharmaceuticals Ltd Novel use of stable isotope labeled l-tryptophan
UA119247C2 (uk) * 2013-09-06 2019-05-27 РОЙВЕНТ САЙЕНСИЗ ҐмбГ Спіроциклічні сполуки як інгібітори триптофангідроксилази
JP6561055B2 (ja) 2013-11-19 2019-08-14 アクテリオン ファーマシューティカルズ リミテッドＡｃｔｅｌｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ 三環式イミダゾール化合物
AR098436A1 (es) 2013-11-19 2016-05-26 Actelion Pharmaceuticals Ltd Compuestos tricíclicos de piperidina
WO2015089137A1 (en) 2013-12-11 2015-06-18 Karos Pharmaceuticals, Inc. Acylguanidines as tryptophan hydroxylase inhibitors
EP3061761A1 (en) 2015-02-24 2016-08-31 Max-Delbrück-Centrum für Molekulare Medizin Xanthine derivatives, their use as a medicament, and pharmaceutical preparations comprising the same
WO2016177690A1 (en) 2015-05-04 2016-11-10 Actelion Pharmaceuticals Ltd Tricyclic piperidine compounds

Also Published As

Publication number Publication date
US20180256574A1 (en) 2018-09-13
US20190282575A1 (en) 2019-09-19
TW201536785A (zh) 2015-10-01
MX371191B (es) 2020-01-22
PE20160648A1 (es) 2016-07-09
ES2780828T3 (es) 2020-08-27
CN105764902B (zh) 2019-02-15
HK1225720A1 (zh) 2017-09-15
AU2014315109B2 (en) 2018-08-09
PH12016500416A1 (en) 2016-05-16
HRP20200098T1 (hr) 2020-04-03
AR097571A1 (es) 2016-03-23
EP3041842B1 (en) 2019-10-23
IL244315B (en) 2018-11-29
EA201690534A1 (ru) 2016-08-31
PL3041842T3 (pl) 2020-05-18
US20170095476A1 (en) 2017-04-06
CL2016000509A1 (es) 2016-08-19
US10045988B2 (en) 2018-08-14
US9199994B2 (en) 2015-12-01
BR112016004909A8 (pt) 2020-02-11
US9750740B2 (en) 2017-09-05
ECSP16014324A (es) 2017-10-31
CN105764902A (zh) 2016-07-13
US10350208B2 (en) 2019-07-16
DK3041842T3 (da) 2020-01-20
US20160096836A1 (en) 2016-04-07
EP3041842A1 (en) 2016-07-13
US10946018B2 (en) 2021-03-16
US20210205305A1 (en) 2021-07-08
UA119247C2 (uk) 2019-05-27
TWI652267B (zh) 2019-03-01
SG10201802118QA (en) 2018-04-27
US10660893B2 (en) 2020-05-26
AU2014315109A1 (en) 2016-03-17
SI3041842T1 (sl) 2020-03-31
MX2016002936A (es) 2016-10-07
NZ717556A (en) 2021-04-30
HUE047574T2 (hu) 2020-05-28
US11759462B2 (en) 2023-09-19
IL244315A0 (en) 2016-04-21
PH12016500416B1 (en) 2016-05-16
RS59871B1 (sr) 2020-03-31
MY186265A (en) 2021-06-30
JP6470290B2 (ja) 2019-02-13
SG10202013041QA (en) 2021-02-25
US9512122B2 (en) 2016-12-06
US20150080393A1 (en) 2015-03-19
US20180092918A1 (en) 2018-04-05
PT3041842T (pt) 2020-02-21
CA2922933C (en) 2021-08-03
US20200237760A1 (en) 2020-07-30
LT3041842T (lt) 2020-02-10
KR102336075B1 (ko) 2021-12-08
CA2922933A1 (en) 2015-03-12
EP3041842B8 (en) 2019-12-04
JP2016530299A (ja) 2016-09-29
WO2015035113A1 (en) 2015-03-12
KR20160055190A (ko) 2016-05-17
EA032304B1 (ru) 2019-05-31

Similar Documents

Publication Publication Date Title
CY1122652T1 (el) Σπειροκυκλικες ενωσεις ως αναστολεις υδροξυλασης τρυπτοφανης
CY1125436T1 (el) Αναστολεις dna-pk
CY1120617T1 (el) 1,2,5-οξαδιαζολια ως αναστολεις 2,3-διοξυγενασης ινδολοαμινης
CY1125127T1 (el) Αναστολεις λυσινης ειδικης απομεθυλασης-1
CY1119476T1 (el) Αναστολεις της απομεθυλασης ιστονης
CY1120361T1 (el) Αναστολεις 2,3-διοξυγενασης ινδολαμινης (ido)
CY1124311T1 (el) Παρεμποδιστες dna-pk
CY1124476T1 (el) Egfr αναστολεας, και παρασκευη και εφαρμογη αυτου
CY1122734T1 (el) Αναστολεις βρωμοεπικρατειων
CY1123475T1 (el) Αναστολεις της ειδικης για λυσινη απομεθυλασης-1
CY1122966T1 (el) 5-βρωμο-2,6-δι-(1η-πυραζολ-1-υλ)πυριμιδιν-4-αμινη για χρηση στη θεραπευτικη αγωγη καρκινου
CY1124407T1 (el) Ενωσεις αναστολεα αυτοταξινης
CY1120969T1 (el) Παραγωγα κινοξαλινης χρησιμα ως τροποποιητες fgfr κινασης
CY1120556T1 (el) Δικυκλικα ετεροκυκλα ως αναστολεις fgfr
CY1122601T1 (el) Αναστολεις gsk3 και μεθοδοι χρησης αυτων
CY1124061T1 (el) Τρικυκλικη ενωση ως αντικαρκινικοι παραγοντες
CY1122314T1 (el) Κυκλοπροπυλαμινες ως αναστολεις lsd1
CY1121182T1 (el) Συνθεσεις χρησιμες για τη θεραπεια διαταραχων που σχετιζονται με kit
CY1119901T1 (el) Αναστολεις απομεθυλασων ιστονων
CY1120154T1 (el) Παραγωγα πιπεριδιν-4-υλ αζετιδινης ως αναστολεις jak1
CY1121460T1 (el) Διαμορφωση του μεταγωγεα σηματος και του ενεργοποιητη εκφρασης της μεταγραφης 3 (stat3)
CY1123906T1 (el) Αναστολεις απομεθυλασης ιστονης
EA201990001A1 (ru) Новые гетероциклические производные, применимые в качестве ингибиторов shp2
CY1122243T1 (el) Παραγωγα ν-πυριδiνυλικoυ ακεταμιδιου ως αναστολεις της οδου σηματοδοτησης wnt
EA201490042A1 (ru) Азетидинил-фенил-, пиридил- или пиразинилкарбоксамидные производные как ингибиторы jak