PH12016500416B1 - Spirocyclic compounds as tryptophan hydroxylase inhibitors - Google Patents

Spirocyclic compounds as tryptophan hydroxylase inhibitors

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Publication number
PH12016500416B1
PH12016500416B1 PH12016500416A PH12016500416A PH12016500416B1 PH 12016500416 B1 PH12016500416 B1 PH 12016500416B1 PH 12016500416 A PH12016500416 A PH 12016500416A PH 12016500416 A PH12016500416 A PH 12016500416A PH 12016500416 B1 PH12016500416 B1 PH 12016500416B1
Authority
PH
Philippines
Prior art keywords
tryptophan hydroxylase
spirocyclic compounds
hydroxylase inhibitors
diseases
inhibitors
Prior art date
Application number
PH12016500416A
Other languages
English (en)
Other versions
PH12016500416A1 (en
Inventor
Lombaert St‚Phane De
Daniel R Goldberg
Kenneth Brameld
Eric Brian Sjogren
Andrew Scribner
Original Assignee
Karos 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=51743540&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PH12016500416(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Karos Pharmaceuticals Inc filed Critical Karos Pharmaceuticals Inc
Publication of PH12016500416B1 publication Critical patent/PH12016500416B1/en
Publication of PH12016500416A1 publication Critical patent/PH12016500416A1/en

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    • 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
    • A61K31/435—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
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    • 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
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    • 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
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    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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    • 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
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    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A—HUMAN NECESSITIES
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Nutrition Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Dispersion Chemistry (AREA)
  • Physiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
PH12016500416A 2013-09-06 2016-03-03 Spirocyclic compounds as tryptophan hydroxylase inhibitors PH12016500416A1 (en)

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 (2)

Publication Number Publication Date
PH12016500416B1 true PH12016500416B1 (en) 2016-05-16
PH12016500416A1 PH12016500416A1 (en) 2016-05-16

Family

ID=51743540

Family Applications (1)

Application Number Title Priority Date Filing Date
PH12016500416A PH12016500416A1 (en) 2013-09-06 2016-03-03 Spirocyclic compounds as tryptophan hydroxylase inhibitors

Country Status (30)

Country Link
US (8) US9199994B2 (OSRAM)
EP (1) EP3041842B8 (OSRAM)
JP (1) JP6470290B2 (OSRAM)
KR (1) KR102336075B1 (OSRAM)
CN (1) CN105764902B (OSRAM)
AR (1) AR097571A1 (OSRAM)
AU (1) AU2014315109B2 (OSRAM)
CA (1) CA2922933C (OSRAM)
CL (1) CL2016000509A1 (OSRAM)
CY (1) CY1122652T1 (OSRAM)
DK (1) DK3041842T3 (OSRAM)
EA (1) EA032304B1 (OSRAM)
EC (1) ECSP16014324A (OSRAM)
ES (1) ES2780828T3 (OSRAM)
HR (1) HRP20200098T1 (OSRAM)
HU (1) HUE047574T2 (OSRAM)
IL (1) IL244315B (OSRAM)
LT (1) LT3041842T (OSRAM)
MX (1) MX371191B (OSRAM)
MY (1) MY186265A (OSRAM)
PE (1) PE20160648A1 (OSRAM)
PH (1) PH12016500416A1 (OSRAM)
PL (1) PL3041842T3 (OSRAM)
PT (1) PT3041842T (OSRAM)
RS (1) RS59871B1 (OSRAM)
SG (2) SG10201802118QA (OSRAM)
SI (1) SI3041842T1 (OSRAM)
TW (1) TWI652267B (OSRAM)
UA (1) UA119247C2 (OSRAM)
WO (1) WO2015035113A1 (OSRAM)

Families Citing this family (19)

* 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
CA3119912A1 (en) * 2018-11-14 2020-05-22 Altavant Sciences Gmbh A crystalline spirocyclic compound inhibitor of tryptophan hydroxylase 1 (tph1) for treating diseases or disorders associated with peripheral serotonin
JP2022507533A (ja) * 2018-11-16 2022-01-18 アルタバント・サイエンシズ・ゲーエムベーハー 肺動脈性高血圧症および他疾患に関連する肺動脈性肺高血圧症の治療法
US20200188398A1 (en) 2018-12-17 2020-06-18 Altavant Sciences Gmbh Method for treating sarcoidosis-associated pulmonary hypertension
WO2020128614A1 (en) 2018-12-17 2020-06-25 Altavant Sciences Gmbh Method for treating interstital 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
US11576915B2 (en) 2019-03-15 2023-02-14 Altavant Sciences Gmbh Method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension and daily dosing
CA3159515A1 (en) * 2019-12-02 2021-06-10 Roivant Sciences Gmbh Treatment of lower airways disorders
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
CN115379825A (zh) * 2020-01-31 2022-11-22 阿尔塔万特科学公司 用rodatristat治疗肺动脉高压的剂量和方法
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
KR20250139396A (ko) * 2023-02-09 2025-09-23 제론 코포레이션 텔로머라제 억제제 화합물
WO2025008449A1 (en) 2023-07-05 2025-01-09 Institut National de la Santé et de la Recherche Médicale Use of tryptophan hydroxylase 1 (tph1) inhibitors for the treatment of atherosclerosis

Family Cites Families (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5380927A (en) 1989-05-16 1995-01-10 Medice Chem.-Pharm. Fabrik Putter Gmbh & Co. Kg Process for preparing optically active 2-aryl-alkanoic acids, in particular 2-aryl-propionic acids
TR199900429T2 (xx) 1996-08-28 1999-05-21 The Procter & Gamble Company Spirosiklik metaloproteaz inhibit�rleri.
HRP20020732A2 (en) 2000-03-07 2004-12-31 Aventis Pharma Gmbh Substituted 3-phenyl-5-alkoxi-1,3,4-oxdiazol-2-one and use thereof for inhibiting hormone-sensitive lipase
JP2005518377A (ja) 2001-12-14 2005-06-23 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活性を低下させるための化合物の使用
DE10247680B4 (de) 2002-10-12 2005-09-01 Aventis Pharma Deutschland Gmbh Neue bicyclische Inhibitoren der Hormon Sensitiven Lipase
EP1636205A1 (en) 2003-06-12 2006-03-22 Novo Nordisk A/S Pyridinyl carbamates as hormone-sensitive lipase inhibitors
EP1636187A1 (en) 2003-06-12 2006-03-22 Novo Nordisk A/S Substituted piperazine carbamates for use as inhibitors of hormone sensitive lipase
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)
UA96936C2 (uk) 2005-12-29 2011-12-26 Лексикон Фармасьютикалз, Инк. Поліциклічні похідні амінокислот і їх застосування
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
JP2010518083A (ja) * 2007-02-12 2010-05-27 メルク・シャープ・エンド・ドーム・コーポレイション ピペリジン誘導体
AR066473A1 (es) 2007-05-16 2009-08-19 Lilly Co Eli Compuesto de triazolil aminopirimidina, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar cancer
WO2009009561A1 (en) 2007-07-11 2009-01-15 Lexicon Pharmaceuticals, Inc. Methods and compositions for treating pulmonary hypertension and related diseases and disorders
AU2008279426A1 (en) 2007-07-26 2009-01-29 Lexicon Pharmaceuticals, Inc. Methods of affecting gastrointestinal transit and gastric emptying, and compounds useful therein
EP2200601A1 (en) 2007-09-24 2010-06-30 Universität Zürich Prorektorat Mnw Blockers of serotonin and its receptors for the treatment of hepatitis
KR20110008066A (ko) 2008-03-31 2011-01-25 더 트러스티이스 오브 콜롬비아 유니버시티 인 더 시티 오브 뉴욕 골량 관련 질병의 진단, 예방 및 치료 방법
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
US8614222B2 (en) 2008-11-13 2013-12-24 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
TW201103540A (en) 2009-06-16 2011-02-01 Ono Pharmaceutical Co Compound having spiro-linked cyclic group and uses thereof
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
CN102711749A (zh) 2009-11-05 2012-10-03 莱西肯医药有限公司 用于癌症治疗的色氨酸羟化酶抑制剂
US20110124667A1 (en) 2009-11-23 2011-05-26 Philip Manton Brown Methods for the treatment of irritable bowel syndrome
US20130137635A1 (en) 2010-02-10 2013-05-30 Lexicon Pharmaceuticals, Inc. Tryptophan hydroxylase inhibitors for the treatment of metastatic bone disease
EP2536689A1 (en) 2010-02-17 2012-12-26 Amgen Inc. Aryl carboxamide derivatives as sodium channel inhibitors for treatment of pain
PL2593452T3 (pl) 2010-07-14 2017-07-31 Novartis Ag Związki heterocykliczne będące agonistami receptora IP
US8551981B2 (en) * 2010-10-08 2013-10-08 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
UY34305A (es) 2011-09-01 2013-04-30 Novartis Ag Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar
EP2753306B1 (en) 2011-10-17 2020-09-23 Lexicon Pharmaceuticals, Inc. 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
US20150005311A1 (en) 2012-01-13 2015-01-01 Novartis Ag IP receptor agonist heterocyclic compounds
EP2802585A1 (en) 2012-01-13 2014-11-19 Novartis AG Fused piperidines as ip receptor agonists for the treatment of pah and related disorders
TW201335160A (zh) 2012-01-13 2013-09-01 Novartis Ag Ｉｐ受體激動劑之雜環化合物
US20140357641A1 (en) 2012-01-13 2014-12-04 Novartis Ag IP receptor agonist heterocyclic compounds
CN104169282B (zh) 2012-01-13 2016-04-20 诺华股份有限公司 Ip受体激动剂的盐
EP2802581A1 (en) 2012-01-13 2014-11-19 Novartis AG 7,8- dihydropyrido [3, 4 - 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
EP3071567B1 (en) 2013-11-19 2017-09-06 Actelion Pharmaceuticals Ltd Tricyclic imidazole compounds as inhibitors of tryptophan hydroxylase
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

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