JP6470290B2 - トリプトファンヒドロキシラーゼ阻害薬としてのスピロ環式化合物 - Google Patents

トリプトファンヒドロキシラーゼ阻害薬としてのスピロ環式化合物 Download PDF

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JP6470290B2
JP6470290B2 JP2016540401A JP2016540401A JP6470290B2 JP 6470290 B2 JP6470290 B2 JP 6470290B2 JP 2016540401 A JP2016540401 A JP 2016540401A JP 2016540401 A JP2016540401 A JP 2016540401A JP 6470290 B2 JP6470290 B2 JP 6470290B2
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diazaspiro
decane
amino
pyrimidin
biphenyl
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JP2016530299A5 (cg-RX-API-DMAC7.html
JP2016530299A (ja
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ステファーヌ・ドゥ・ロンベール
ダニエル・アール・ゴールドバーグ
ケネス・ブラメルド
エリック・ブライアン・シェーグレン
アンドリュー・スクリブナー
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Karos Pharmaceuticals Inc
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Karos Pharmaceuticals Inc
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    • 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
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    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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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  • Cardiology (AREA)
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  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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JP2016540401A 2013-09-06 2014-09-05 トリプトファンヒドロキシラーゼ阻害薬としてのスピロ環式化合物 Expired - Fee Related JP6470290B2 (ja)

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

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JP2016530299A JP2016530299A (ja) 2016-09-29
JP2016530299A5 JP2016530299A5 (cg-RX-API-DMAC7.html) 2017-10-12
JP6470290B2 true JP6470290B2 (ja) 2019-02-13

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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
KR20210102887A (ko) 2018-11-14 2021-08-20 알타반트 사이언시스 게엠베하 말초 세로토닌과 관련된 질병 또는 장애를 치료하기 위한 트립토판 하이드록실라제 1 (tph1)의 결정질 스피로사이클릭 화합물 억제제
EP3880203A1 (en) * 2018-11-16 2021-09-22 Altavant Sciences GmbH A method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension
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
KR20210133953A (ko) 2019-01-30 2021-11-08 알타반트 사이언시스 게엠베하 로다트리스타트 에틸로 폐동맥 고혈압을 치료하기 위한 투여 요법 및 방법
EP3938043A1 (en) * 2019-03-15 2022-01-19 Altavant Sciences GmbH A method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension and daily dosing
US20220409627A1 (en) * 2019-12-02 2022-12-29 Altavant 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
JP2023512025A (ja) * 2020-01-31 2023-03-23 アルタバント・サイエンシズ・ゲーエムベーハー 肺動脈性肺高血圧症をロダトリスタットで処置するための投与量および方法
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
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

Family Cites Families (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1053010A (zh) 1989-05-16 1991-07-17 梅迪斯化学药物工厂普特两合股份公司 药物制剂
NZ334257A (en) 1996-08-28 2000-11-24 Procter & Gamble Spirocyclic metalloprotease inhibitors
WO2001066531A1 (de) 2000-03-07 2001-09-13 Aventis Pharma Deutschland Gmbh Substituierte 3-phenyl-5-alkoxi-1,3,4-oxdiazol-2-one (und) ihre verwendung zur hemmung der hormonsensitiven 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
WO2004111004A1 (en) 2003-06-12 2004-12-23 Novo Nordisk A/S Substituted piperazine carbamates for use as inhibitors of hormone sensitive lipase
EP1636205A1 (en) 2003-06-12 2006-03-22 Novo Nordisk A/S Pyridinyl carbamates as hormone-sensitive lipase inhibitors
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)
EP1984344B1 (en) 2005-12-29 2012-09-26 Lexicon Pharmaceuticals, Inc. 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
WO2008100412A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperidine derivatives
CN101679395B (zh) 2007-05-16 2012-06-13 伊莱利利公司 三唑基氨基嘧啶化合物
BRPI0814105A2 (pt) 2007-07-11 2015-02-03 Lexicon Pharmaceuticals Inc Métodos e composições para o tratamento de hipertensão pulmonar e doenças e distúrbios relacionados
US20090029993A1 (en) 2007-07-26 2009-01-29 Qingyun Liu Methods of affecting gastrointestinal transit and gastric emptying, and compounds useful therein
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
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
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
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
EP2444402A4 (en) 2009-06-16 2012-11-07 Ono Pharmaceutical Co COMPOUND HAVING A SPIRO BINDING CYCLIC GROUP AND USE 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
EP2496231A1 (en) 2009-11-05 2012-09-12 Lexicon Pharmaceuticals, Inc. Tryptophan hydroxylase inhibitors for the treatment of cancer
EP2504008A1 (en) 2009-11-23 2012-10-03 Lexicon Pharmaceuticals, Inc. Methods and assays for the treatment of irritable bowel syndrome
AU2011215963A1 (en) 2010-02-10 2012-08-02 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
PH12013500084A1 (en) 2010-07-14 2015-09-11 Novartis Ag Ip receptor agonist heterocyclic compounds
PH12013500661A1 (en) * 2010-10-08 2017-08-23 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
JP6203182B2 (ja) 2011-10-17 2017-09-27 レクシコン ファーマシューティカルズ インコーポレイテッド (s)−エチル2−アミノ−3−(4−(2−アミノ−6−((r)−1−(4−クロロ−2−(3−メチル−1h−ピラゾール−1−イル)フェニル)−2,2,2−トリフルオロエトキシ)ピリミジン−4−イル)フェニル)プロパノエートの固形剤
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
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
US20140378463A1 (en) 2012-01-13 2014-12-25 Novartis Ag IP receptor agonist heterocyclic compounds
WO2013105066A1 (en) 2012-01-13 2013-07-18 Novartis Ag Salts of an ip receptor agonist
UY34572A (es) 2012-01-13 2013-09-02 Novartis Ag Compuestos heterocíclicos agonistas del receptor ip
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
EP2802585A1 (en) 2012-01-13 2014-11-19 Novartis AG Fused piperidines as ip receptor agonists for the treatment of 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
US9937173B2 (en) 2013-02-15 2018-04-10 Mcmaster University 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
AR098436A1 (es) 2013-11-19 2016-05-26 Actelion Pharmaceuticals Ltd Compuestos tricíclicos de piperidina
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
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
MA42034A (fr) 2015-05-04 2018-03-14 Actelion Pharmaceuticals Ltd Composés pipéridiniques tricycliques

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