MD4539B1 - 4-Fenilpiridine substituite pentru tratamentul bolilor asociate cu receptorul NK-1 - Google Patents

4-Fenilpiridine substituite pentru tratamentul bolilor asociate cu receptorul NK-1 Download PDF

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Publication number
MD4539B1
MD4539B1 MDA20140059A MD20140059A MD4539B1 MD 4539 B1 MD4539 B1 MD 4539B1 MD A20140059 A MDA20140059 A MD A20140059A MD 20140059 A MD20140059 A MD 20140059A MD 4539 B1 MD4539 B1 MD 4539B1
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MD
Moldova
Prior art keywords
phenyl
treatment
related diseases
receptor related
pyridines
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MDA20140059A
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English (en)
Russian (ru)
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MD20140059A2 (en
MD4539C1 (ro
Inventor
Лука Фадини
Питер Манини
Клаудио Пьетра
Клаудио Джулиано
Эмануэла Ловати
Роберта Каннелла
Алессио Вентурини
Валентино Дж. СТЕЛЛА
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Helsinn Healthcare Sa
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Application filed by Helsinn Healthcare Sa filed Critical Helsinn Healthcare Sa
Publication of MD20140059A2 publication Critical patent/MD20140059A2/ro
Publication of MD4539B1 publication Critical patent/MD4539B1/ro
Publication of MD4539C1 publication Critical patent/MD4539C1/ro

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    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/573Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
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    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
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Abstract

Invenţia se referă la compuşi noi - derivaţi ai 4-fenilpiridinei pentru tratamentul bolilor asociate cu receptorul NK-1, la procedee de tratare a vomei, disfuncţiilor vezicii urinare, depresiei sau anxietăţii la pacientul care are nevoie de asemenea tratament, care cuprind administrarea pacientului respectiv a unei cantităţi eficiente terapeutic de un compus conform invenţiei, precum şi la compoziţii farmaceutice care cuprind o cantitate eficientă terapeutic de un compus conform invenţiei şi unul sau mai mulţi excipienţi farmaceutic acceptabili.
MDA20140059A 2011-11-29 2012-11-28 4-Fenilpiridine substituite pentru tratamentul bolilor asociate cu receptorul NK-1 MD4539C1 (ro)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161564537P 2011-11-29 2011-11-29
US13/478,361 US8426450B1 (en) 2011-11-29 2012-05-23 Substituted 4-phenyl pyridines having anti-emetic effect
PCT/US2012/066778 WO2013082102A1 (en) 2011-11-29 2012-11-28 Substituted 4 - phenyl - pyridines for the treatment of nk-1 receptor related diseases

Publications (3)

Publication Number Publication Date
MD20140059A2 MD20140059A2 (en) 2014-11-30
MD4539B1 true MD4539B1 (ro) 2017-12-31
MD4539C1 MD4539C1 (ro) 2018-07-31

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MDA20140059A MD4539C1 (ro) 2011-11-29 2012-11-28 4-Fenilpiridine substituite pentru tratamentul bolilor asociate cu receptorul NK-1

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US (7) US8426450B1 (ro)
EP (1) EP2785706B1 (ro)
JP (3) JP5635708B2 (ro)
KR (1) KR101979050B1 (ro)
CN (6) CN112979543B (ro)
AP (1) AP2014007729A0 (ro)
AR (1) AR089019A1 (ro)
AU (1) AU2012346133B2 (ro)
BR (1) BR112014012878B1 (ro)
CA (1) CA2850644C (ro)
CL (1) CL2014001280A1 (ro)
CO (1) CO6990728A2 (ro)
CR (1) CR20140312A (ro)
CY (2) CY1118416T1 (ro)
DK (1) DK2785706T3 (ro)
DO (1) DOP2014000115A (ro)
EA (1) EA026553B1 (ro)
EC (1) ECSP14003642A (ro)
ES (1) ES2603958T3 (ro)
FI (1) FIC20200022I1 (ro)
FR (1) FR20C1029I2 (ro)
GE (1) GEP201706695B (ro)
GT (1) GT201400102A (ro)
HR (1) HRP20161708T1 (ro)
HU (2) HUE032288T2 (ro)
IL (1) IL232859B (ro)
IN (1) IN2014CN04907A (ro)
JO (1) JO3202B1 (ro)
LT (2) LT2785706T (ro)
MA (1) MA35836B1 (ro)
MD (1) MD4539C1 (ro)
ME (1) ME02561B (ro)
MX (1) MX2014006423A (ro)
MY (1) MY165514A (ro)
NI (1) NI201400043A (ro)
NL (1) NL301047I2 (ro)
PE (1) PE20141421A1 (ro)
PH (1) PH12014501199B1 (ro)
PL (1) PL2785706T3 (ro)
PT (1) PT2785706T (ro)
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SG (1) SG11201402044XA (ro)
SI (1) SI2785706T1 (ro)
SM (2) SMT201600467T1 (ro)
TN (1) TN2014000165A1 (ro)
TW (1) TWI638806B (ro)
UA (1) UA115136C2 (ro)
UY (1) UY34472A (ro)
WO (1) WO2013082102A1 (ro)
ZA (1) ZA201404787B (ro)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2808630A1 (en) 2010-08-19 2012-02-23 Buck Institute For Age Research Methods of treating mild cognitive impairment (mci) and related disorders
AU2011338428B2 (en) 2010-12-07 2015-05-21 Allison Transmission, Inc. Energy storage system for hybrid electric vehicle
WO2012176061A1 (en) 2011-06-22 2012-12-27 Purdue Pharma L.P. Trpv1 antagonists including dihydroxy substituent and uses thereof
US8426450B1 (en) 2011-11-29 2013-04-23 Helsinn Healthcare Sa Substituted 4-phenyl pyridines having anti-emetic effect
ES2671418T3 (es) 2013-11-08 2018-06-06 Kissei Pharmaceutical Co., Ltd. Derivado de carboximetilpiperidina
WO2015171489A1 (en) * 2014-05-05 2015-11-12 Apicore Us Llc Methods of making netupitant and intermediates thereof
TWI649307B (zh) 2014-05-07 2019-02-01 日商橘生藥品工業股份有限公司 Cyclohexylpyridine derivative
TW201613888A (en) * 2014-09-26 2016-04-16 Helsinn Healthcare Sa Crystalline forms of an NK-1 antagonist
IL313498A (en) 2014-10-06 2024-08-01 Vertex Pharma Modulators of the cystic fibrosis transmembrane conductance regulator
CN105061303A (zh) * 2015-08-03 2015-11-18 成都欣捷高新技术开发有限公司 一种制备奈妥吡坦关键中间体n-甲基-4-(2-甲基苯基)-6-(4-甲基-1-哌嗪基)-3-吡啶胺的新方法
US10005803B2 (en) * 2015-10-06 2018-06-26 Helsinn Healthcare Sa Crystalline forms of fosnetupitant
CN106892864A (zh) * 2015-12-21 2017-06-27 上海科胜药物研发有限公司 一种奈妥皮坦游离碱的晶型a及其制备方法
EP3436446B1 (en) 2016-03-31 2023-06-07 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
KR102459416B1 (ko) * 2016-06-06 2022-10-27 헬신 헬쓰케어 에스.에이. 포스네투피탄트의 생리학적으로 균형잡힌 주사가능 제제
HRP20211683T1 (hr) 2016-09-30 2022-03-04 Vertex Pharmaceuticals Incorporated Modulator transmembranskog regulatora provodljivosti cistične fibroze, farmaceutski pripravci, postupci liječenja, i postupak za pripravu modulatora
MX2021013639A (es) 2016-12-09 2022-09-30 Vertex Pharma Forma cristalina del compuesto 1, un modulador del regulador de conductancia transmembrana de fibrosis quística, procesos para su preparación, composiciones farmacéuticas del compuesto 1, y su uso en el tratamiento de fibrosis quística.
CN108619525B (zh) * 2017-03-15 2020-12-29 和龙 奈妥吡坦-mPEG-PLA纳米粒及其制备方法和用途
AU2018279646B2 (en) 2017-06-08 2023-04-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
KR20250069704A (ko) 2017-06-30 2025-05-19 체이스 테라퓨틱스 코포레이션 우울증을 치료하기 위한 nk-1 길항제 조성물 및 우울증 치료에 사용하는 방법
AU2018304168B2 (en) 2017-07-17 2023-05-04 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
TWI799435B (zh) 2017-08-02 2023-04-21 美商維泰克斯製藥公司 製備化合物之製程
CN107698500A (zh) * 2017-10-17 2018-02-16 扬子江药业集团四川海蓉药业有限公司 一种奈妥匹坦的制备方法
WO2019079760A1 (en) 2017-10-19 2019-04-25 Vertex Pharmaceuticals Incorporated CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS
US11465985B2 (en) 2017-12-08 2022-10-11 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator
WO2019138162A1 (en) * 2018-01-12 2019-07-18 Orion Corporation Palonosetron for the treatment or prevention of nausea and vomiting
TWI810243B (zh) 2018-02-05 2023-08-01 美商維泰克斯製藥公司 用於治療囊腫纖化症之醫藥組合物
WO2019200246A1 (en) 2018-04-13 2019-10-17 Alexander Russell Abela Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
JP7156154B2 (ja) * 2019-04-18 2022-10-19 株式会社島津製作所 培地処理システム及び培地処理方法
CN112174881B (zh) * 2019-07-04 2022-06-21 上海森辉医药有限公司 一种奈妥匹坦的衍生物及其制备方法
CN112778370B (zh) * 2019-11-06 2025-09-26 扬子江药业集团江苏海慈生物药业有限公司 一种制备福奈妥匹坦的方法
AU2021246889A1 (en) 2020-04-03 2022-10-13 Nerre Therapeutics Limited An NK-1 receptor antagonist for treating a disease selecting from sepsis, septic shock,, acute respiratory distress syndrome (ARDS) or multiple organ dysfunction syndrome (MODS)
MX2022014901A (es) 2020-06-02 2023-01-18 Nerre Therapeutics Ltd Antagonistas del receptor de neuroquinina (nk)-1 para su uso en el tratamiento de condiciones de fibrosis pulmonar promovidas por lesion mecanica a los pulmones.
US12097197B2 (en) 2021-12-21 2024-09-24 Slayback Pharma Llc Stable liquid compositions of netupitant and palonosetron
WO2025036703A1 (en) 2023-08-13 2025-02-20 Helsinn Healthcare Sa Fosnetupitant for administration via intravenous bolus

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5985856A (en) * 1997-12-31 1999-11-16 University Of Kansas Water soluble prodrugs of secondary and tertiary amine containing drugs and methods of making thereof
EP1103545A1 (en) * 1999-11-29 2001-05-30 F. Hoffmann-La Roche Ag 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide
US6297375B1 (en) * 1999-02-24 2001-10-02 Hoffmann-La Roche Inc. 4-phenyl-pyridine derivatives
US6303790B1 (en) * 1999-11-29 2001-10-16 Hoffman-La Roche Inc. Process for the preparation of pyridine derivatives
WO2002008232A1 (en) * 2000-07-24 2002-01-31 F. Hoffmann-La Roche Ag 4-phenyl-pyridine derivatives as neurokinin-1 receptor antagonists
US6531597B2 (en) * 2001-02-13 2003-03-11 Hoffmann-La Roche Inc. Process for preparation of 2-phenyl acetic acid derivatives
US6747026B2 (en) * 2000-07-14 2004-06-08 Hoffman-La Roche Inc. NK-1 receptor active amine oxide prodrugs
US20060030600A1 (en) * 2004-08-06 2006-02-09 Patrick Schnider Dual NK1/NK3 receptor antagonists for the treatment of schizophrenia
WO2006099968A1 (en) * 2005-03-23 2006-09-28 F. Hoffmann-La Roche Ag Metabolites for nk-i antagonists for emesis
WO2009138393A1 (en) * 2008-05-14 2009-11-19 Glaxo Wellcome Manufacturing Pte Ltd 5-[5-[2-(3,5-bis(trifluoromethyl)phenyl)-2-methylpropanoylmethylamino]-4-(4-fluoro-2-methylphenyl)]-2-pyridinyl-2-alkyl-prolinamide as nk1 receptor antagonists

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6362172B2 (en) * 2000-01-20 2002-03-26 Bristol-Myers Squibb Company Water soluble prodrugs of azole compounds
ES2272408T3 (es) 2000-12-14 2007-05-01 F. Hoffmann-La Roche Ag Matriz lipidica autoemulsificante (selm).
US7745625B2 (en) * 2004-03-15 2010-06-29 Bristol-Myers Squibb Company Prodrugs of piperazine and substituted piperidine antiviral agents
CN101282979B (zh) * 2005-09-13 2011-09-21 卫材R&D管理有限公司 稳定性被改善的含有磷酸氯甲酯衍生物的组合物及其制备方法
UA108077C2 (xx) * 2009-07-02 2015-03-25 Синтез динатрієвої солі n4-(2,2-диметил-4-$(дигідрофосфонокси)метил]-3-оксо-5-піридо$1,4]оксазин-6-іл)-5-фтор-n2-(3,4,5-триметоксифеніл)-2,4-піримідиндіаміну
LT2722045T (lt) * 2009-11-18 2016-09-26 Helsinn Healthcare Sa Kompozicija skirta gydyti centralizuotai kontroliuojamą pykinimą ir vėmimą
AU2010339689B2 (en) * 2010-01-07 2015-02-19 Alkermes Pharma Ireland Limited Quaternary ammonium salt prodrugs
HRP20160478T1 (hr) * 2010-12-02 2016-07-01 The University Of Kansas Prolijekovi 6-cikloheksil-1-hidroksi-4-metilpiridin-2-(1h)-ona i njihovi derivati
US9403772B2 (en) 2011-11-29 2016-08-02 Helsinn Healthcare Sa 4-(5-(2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethylpropanamido)-4-(o-tolyl)pyridin-2-yl)-1-methyl-1-((phosphonooxy)methyl)piperazin-1-ium as a neurokinin receptor modulator
US8426450B1 (en) 2011-11-29 2013-04-23 Helsinn Healthcare Sa Substituted 4-phenyl pyridines having anti-emetic effect
US8952169B2 (en) 2012-05-22 2015-02-10 Xenon Pharmaceuticals Inc. N-substituted benzamides and methods of use thereof

Patent Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5985856A (en) * 1997-12-31 1999-11-16 University Of Kansas Water soluble prodrugs of secondary and tertiary amine containing drugs and methods of making thereof
US6297375B1 (en) * 1999-02-24 2001-10-02 Hoffmann-La Roche Inc. 4-phenyl-pyridine derivatives
ES2359235T3 (es) * 1999-02-24 2011-05-19 F. Hoffmann-La Roche Ag Derivados de 4-fenilpiridina y su empleo como antagonistas del receptor nk-1.
EP1103545A1 (en) * 1999-11-29 2001-05-30 F. Hoffmann-La Roche Ag 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide
US6303790B1 (en) * 1999-11-29 2001-10-16 Hoffman-La Roche Inc. Process for the preparation of pyridine derivatives
US6747026B2 (en) * 2000-07-14 2004-06-08 Hoffman-La Roche Inc. NK-1 receptor active amine oxide prodrugs
WO2002008232A1 (en) * 2000-07-24 2002-01-31 F. Hoffmann-La Roche Ag 4-phenyl-pyridine derivatives as neurokinin-1 receptor antagonists
US6531597B2 (en) * 2001-02-13 2003-03-11 Hoffmann-La Roche Inc. Process for preparation of 2-phenyl acetic acid derivatives
US20060030600A1 (en) * 2004-08-06 2006-02-09 Patrick Schnider Dual NK1/NK3 receptor antagonists for the treatment of schizophrenia
WO2006099968A1 (en) * 2005-03-23 2006-09-28 F. Hoffmann-La Roche Ag Metabolites for nk-i antagonists for emesis
WO2009138393A1 (en) * 2008-05-14 2009-11-19 Glaxo Wellcome Manufacturing Pte Ltd 5-[5-[2-(3,5-bis(trifluoromethyl)phenyl)-2-methylpropanoylmethylamino]-4-(4-fluoro-2-methylphenyl)]-2-pyridinyl-2-alkyl-prolinamide as nk1 receptor antagonists

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Germano Giuliani et al. Non-peptide NK1 receptor ligands based on the 4-phenylpyridine moiety. Bioorganic & Medicinal Chemistry, 2011, vol. 19, nr. 7, p. 2242-2251 (regăsit în internet la 2017.07.10 URL: <<http://www.sciencedirect.com/science/article/pii/S0968089611001490>>) *
Maria Pia Catalani et al. Identification of novel NK1/NK3 dual antagonists for the potential treatment of schizophrenia. Bioorganic & Medicinal Chemistry Letters, 2011, vol. 21, nr. 22, p. 6899-6904 (regăsit în internet la 2017.07.10 URL: <<http://www.sciencedirect.com/science/article/pii/S0960894X11010626>>) *
Torsten Hoffmann et al. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorganic & Medicinal Chemistry Letters, 2006, vol. 16, nr. 5, p. 1362-1365 (regăsit în internet la 2017.07.10 URL: <<http://www.sciencedirect.com/science/article/pii/S0960894X05014824>>) *

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