KR102336075B1 - 트립토판 하이드록실레이스 억제제로서 스파이로사이클릭 화합물 - Google Patents

트립토판 하이드록실레이스 억제제로서 스파이로사이클릭 화합물 Download PDF

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KR102336075B1
KR102336075B1 KR1020167009029A KR20167009029A KR102336075B1 KR 102336075 B1 KR102336075 B1 KR 102336075B1 KR 1020167009029 A KR1020167009029 A KR 1020167009029A KR 20167009029 A KR20167009029 A KR 20167009029A KR 102336075 B1 KR102336075 B1 KR 102336075B1
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alkyl
delete delete
cycloalkyl
aryl
membered heterocycloalkyl
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KR20160055190A (ko
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롬배르트 스테판 데
다니엘 알. 골드버그
케니스 브라멜드
에릭 브라이언 쇼그렌
앤드류 스크라이브너
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카로스 파마슈티칼스 인코포레이티드
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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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    • 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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  • Health & Medical Sciences (AREA)
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  • 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)
  • Hematology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dispersion Chemistry (AREA)
  • Physiology (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020167009029A 2013-09-06 2014-09-05 트립토판 하이드록실레이스 억제제로서 스파이로사이클릭 화합물 Expired - Fee Related KR102336075B1 (ko)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201361874545P 2013-09-06 2013-09-06
US61/874,545 2013-09-06
US201361899943P 2013-11-05 2013-11-05
US61/899,943 2013-11-05
US201462004385P 2014-05-29 2014-05-29
US62/004,385 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
KR20160055190A KR20160055190A (ko) 2016-05-17
KR102336075B1 true KR102336075B1 (ko) 2021-12-08

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KR1020167009029A Expired - Fee Related KR102336075B1 (ko) 2013-09-06 2014-09-05 트립토판 하이드록실레이스 억제제로서 스파이로사이클릭 화합물

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US (8) US9199994B2 (enExample)
EP (1) EP3041842B8 (enExample)
JP (1) JP6470290B2 (enExample)
KR (1) KR102336075B1 (enExample)
CN (1) CN105764902B (enExample)
AR (1) AR097571A1 (enExample)
AU (1) AU2014315109B2 (enExample)
CA (1) CA2922933C (enExample)
CL (1) CL2016000509A1 (enExample)
CY (1) CY1122652T1 (enExample)
DK (1) DK3041842T3 (enExample)
EA (1) EA032304B1 (enExample)
EC (1) ECSP16014324A (enExample)
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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
US11203597B2 (en) * 2018-11-14 2021-12-21 Altavant Sciences Gmbh Crystalline spirocyclic compound, a dosage form containing, a method for using in treatment of disease, and a method for recrystallizing
AU2019382168A1 (en) * 2018-11-16 2021-06-03 Altavant Sciences Gmbh A method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension
US20200188399A1 (en) * 2018-12-17 2020-06-18 Altavant Sciences Gmbh Method for treating interstitial lung disease
WO2020128608A1 (en) 2018-12-17 2020-06-25 Altavant Sciences Gmbh Compound for use in a method for treating sarcoidosis-associated pulmonary hypertension
US11607413B2 (en) 2019-01-30 2023-03-21 Altavant Sciences Gmbh Dosage regime and method for treating pulmonary arterial hypertension
CN113784717A (zh) * 2019-03-15 2021-12-10 阿尔塔万特科学公司 一种治疗肺动脉高压和相关性肺动脉高压的方法以及每日给药
EP4069847A4 (en) * 2019-12-02 2023-11-15 Onspira Therapeutics, Inc. 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
CA3165432A1 (en) * 2020-01-31 2021-08-05 Stephen A. Wring 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
CN120769851A (zh) * 2023-02-09 2025-10-10 美国杰龙生物医药公司 端粒酶抑制剂化合物
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012048222A1 (en) 2010-10-08 2012-04-12 Abbott Laboratories FURO[3,2-d]PYRIMIDINE COMPOUNDS

Family Cites Families (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1050373A (zh) 1989-05-16 1991-04-03 梅迪斯化学药物工厂普特两合股份公司 制备旋光2-芳基链烷酸，特别是2-芳基丙酸的方法
DK0927183T3 (da) 1996-08-28 2004-11-29 Procter & Gamble Spirocykliske metalloprotease-inhibitorer
HUP0302772A3 (en) 2000-03-07 2007-03-28 Sanofi Aventis Deutschland Substituted 3-phenyl-5-alkoxi-1,3,4-oxdiazol-2-one and use thereof for inhibiting hormone-sensitive lipase
KR20040068240A (ko) 2001-12-14 2004-07-30 노보 노르디스크 에이/에스 호르몬 민감성 리파아제의 활성을 감소시키기 위한 화합물및 그들의 사용
DE10247680B4 (de) 2002-10-12 2005-09-01 Aventis Pharma Deutschland Gmbh Neue bicyclische Inhibitoren der Hormon Sensitiven Lipase
AU2004247319A1 (en) 2003-06-12 2004-12-23 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)
AU2006337137B2 (en) 2005-12-29 2012-06-14 Tersera Therapeutics Llc Multicyclic amino acid derivatives and methods of their use
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
CA2676920A1 (en) * 2007-02-12 2008-08-21 Merck & Co., Inc. Piperidine derivatives
TW200908981A (en) 2007-05-16 2009-03-01 Lilly Co Eli Triazolyl aminopyrimidine compounds
CA2693400A1 (en) 2007-07-11 2009-01-15 Lexicon Pharmaceuticals, Inc. Methods and compositions for treating pulmonary hypertension and related diseases and disorders
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
BRPI0908719A2 (pt) 2008-03-31 2015-08-18 Univ Columbia Metodos de diagnóstico, prevenção e tratamento de doenças de massa óssea
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
EP2411380A1 (en) 2009-03-26 2012-02-01 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
US8815883B2 (en) 2009-11-02 2014-08-26 The Trustees Of Columbia Unviersity In The City Of New York Compounds and methods for inhibiting serotonin synthesis
EP2496231A1 (en) 2009-11-05 2012-09-12 Lexicon Pharmaceuticals, Inc. 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
US20130137635A1 (en) 2010-02-10 2013-05-30 Lexicon Pharmaceuticals, Inc. Tryptophan hydroxylase inhibitors for the treatment of metastatic bone disease
WO2011103196A1 (en) * 2010-02-17 2011-08-25 Amgen Inc. Aryl carboxamide derivatives as sodium channel inhibitors for treatment of pain
SG186989A1 (en) 2010-07-14 2013-02-28 Novartis Ag Ip receptor agonist heterocyclic 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
SG11201401583YA (en) 2011-10-17 2014-09-26 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
WO2013074889A1 (en) 2011-11-17 2013-05-23 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
EP2802583A1 (en) 2012-01-13 2014-11-19 Novartis AG Fused piperidines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
EP2802585A1 (en) 2012-01-13 2014-11-19 Novartis AG Fused piperidines as ip receptor agonists for the treatment of pah and related disorders
US20140378463A1 (en) 2012-01-13 2014-12-25 Novartis Ag IP receptor agonist heterocyclic compounds
JP6073923B2 (ja) 2012-01-13 2017-02-01 ノバルティス アーゲー 肺動脈高血圧症（ｐａｈ）および関連障害の治療のためのｉｐ受容体アゴニストとしての縮合ピロール
WO2013105061A1 (en) 2012-01-13 2013-07-18 Novartis Ag Fused dihydropyrido [2,3 -b] pyrazines 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
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
WO2014124523A1 (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
CN105745211B (zh) 2013-11-19 2017-09-26 埃科特莱茵药品有限公司 作为色氨酸羟化酶的抑制剂的三环咪唑化合物
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
EP3292127A1 (en) 2015-05-04 2018-03-14 Actelion Pharmaceuticals Ltd Tricyclic piperidine compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012048222A1 (en) 2010-10-08 2012-04-12 Abbott Laboratories FURO[3,2-d]PYRIMIDINE COMPOUNDS

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Bioorganic & Medicinal Chemistry Letters(2009), Vol. 19, pp.5229-5232
Journal of Medicinal Chemistry(2008), Vol. 51, pp.3684-3687
The Journal of Pharmacology and Experimental Therapeutics(2008), Vol. 325, No. 1, pp.47-55

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