BR0108363A - Composto, métodos para modular função de receptor de crf e acoplado a proteìna g, para tratar um distúrbio ou doença do snc, para localizar receptores de crf em amostras de seção de tecidos, para inibir a ligação de crf a um receptor de crf¹ e para alterar a atividade de transdução de sinal de um receptor de crf¹ e composição farmacêutica - Google Patents

Composto, métodos para modular função de receptor de crf e acoplado a proteìna g, para tratar um distúrbio ou doença do snc, para localizar receptores de crf em amostras de seção de tecidos, para inibir a ligação de crf a um receptor de crf¹ e para alterar a atividade de transdução de sinal de um receptor de crf¹ e composição farmacêutica

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Publication number
BR0108363A
BR0108363A BR0108363-5A BR0108363A BR0108363A BR 0108363 A BR0108363 A BR 0108363A BR 0108363 A BR0108363 A BR 0108363A BR 0108363 A BR0108363 A BR 0108363A
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Prior art keywords
crf
receptor
receptors
methods
modulating
Prior art date
Application number
BR0108363-5A
Other languages
English (en)
Inventor
Taeyoung Yoon
Ping Ge
Raymond F Horvath
Stephane De Lombaert
Kevin J Hodgetts
Dario Doller
Cunyu Zhang
Original Assignee
Neurogen Corp
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Application filed by Neurogen Corp filed Critical Neurogen Corp
Publication of BR0108363A publication Critical patent/BR0108363A/pt

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    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
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    • A61K31/4965Non-condensed pyrazines
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    • A61K31/4965Non-condensed pyrazines
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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    • C07D241/12Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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Abstract

"COMPOSTO, MéTODOS PARA MODULAR FUNçãO DE RECEPTOR DE CRF E ACOPLADO A PROTEìNA G, PARA TRATAR UM DISTúRBIO OU DOENçA DO SNC, PARA LOCALIZAR RECEPTORES DE CRF EM AMOSTRAS DE SEçãO DE TECIDOS, PARA INIBIR A LIGAçãO DE CRF A UM RECEPTOR DE CRF, E PARA ALTERAR A ATIVIDADE DE TRANSDUçãO DE SINAL DE UM RECEPTOR DE CRF, E COMPOSIçãO FARMACêUTICA". Proporciona-se compostos de arilpirazina, incluindo arilpirazinas que podem ligar-se com alta afinidade e alta seletividade a receptores de CRF~ 1~, incluindo receptores de CRF~ 1~ humanos. Assim, a invenção inclui processos para o tratamento de distúrbios ou doenças associados com receptores de CRF~ 1~, incluindo distúrbios ou doenças relacionados com o SNC, particularmente distúrbios e doenças afetivas, e distúrbios e doenças neurológicas agudas e crónicas.
BR0108363-5A 2000-02-16 2001-02-16 Composto, métodos para modular função de receptor de crf e acoplado a proteìna g, para tratar um distúrbio ou doença do snc, para localizar receptores de crf em amostras de seção de tecidos, para inibir a ligação de crf a um receptor de crf¹ e para alterar a atividade de transdução de sinal de um receptor de crf¹ e composição farmacêutica BR0108363A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US18293400P 2000-02-16 2000-02-16
US20645500P 2000-05-22 2000-05-22
PCT/US2001/005264 WO2001060806A2 (en) 2000-02-16 2001-02-16 Substituted arylpyrazines

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BR0108363A true BR0108363A (pt) 2004-02-10

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BR0108363-5A BR0108363A (pt) 2000-02-16 2001-02-16 Composto, métodos para modular função de receptor de crf e acoplado a proteìna g, para tratar um distúrbio ou doença do snc, para localizar receptores de crf em amostras de seção de tecidos, para inibir a ligação de crf a um receptor de crf¹ e para alterar a atividade de transdução de sinal de um receptor de crf¹ e composição farmacêutica

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US (3) US6995161B2 (pt)
EP (1) EP1255740B1 (pt)
JP (1) JP2004500383A (pt)
KR (2) KR20080021603A (pt)
CN (1) CN1231473C (pt)
AP (1) AP2002002620A0 (pt)
AT (1) ATE307121T1 (pt)
AU (1) AU783915B2 (pt)
BG (2) BG106968A (pt)
BR (1) BR0108363A (pt)
CA (2) CA2651825A1 (pt)
CR (1) CR6735A (pt)
CZ (1) CZ20022739A3 (pt)
DE (1) DE60114153T2 (pt)
DK (1) DK1255740T3 (pt)
DZ (1) DZ3293A1 (pt)
EA (1) EA006938B1 (pt)
EE (1) EE200200453A (pt)
ES (1) ES2247070T3 (pt)
HR (1) HRP20020747A2 (pt)
HU (1) HUP0301573A3 (pt)
IL (1) IL151020A0 (pt)
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MA (1) MA26874A1 (pt)
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NO (1) NO324473B1 (pt)
NZ (1) NZ520484A (pt)
OA (1) OA12178A (pt)
PL (1) PL365238A1 (pt)
SK (1) SK11542002A3 (pt)
TW (1) TWI232215B (pt)
WO (1) WO2001060806A2 (pt)
YU (1) YU61002A (pt)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU9458401A (en) * 2000-09-20 2002-04-02 Ortho Mcneil Pharm Inc Pyrazine derivatives as modulators of tyrosine kinases
RU2003134010A (ru) * 2001-05-22 2005-05-20 Ньюроджин Корпорейшн (US) 5-замещенные-2-арилпиридины в качестве модуляторов crf1
US6887875B2 (en) * 2001-06-12 2005-05-03 Neurogen Corporation 2,5-diarypyrimidine compounds
SE0102439D0 (sv) * 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
SE0102438D0 (sv) * 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
US6852737B2 (en) * 2001-08-06 2005-02-08 Recordati Ireland Limited Crude and crystalline forms of lercanidipine hydrochloride
ITMI20011726A1 (it) 2001-08-06 2003-02-06 Recordati Ind Chimica E Farma Forme polimorfe della lercanidipina cloridrato
WO2003045924A1 (en) * 2001-11-21 2003-06-05 Pharmacia & Upjohn Company Substituted aryl 1,4-pyrazine derivatives
US6992087B2 (en) 2001-11-21 2006-01-31 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
AU2003223475A1 (en) 2002-04-26 2003-11-10 Pharmacia And Upjohn Company Substituted pyrazine derivatives
US7015227B2 (en) 2002-06-21 2006-03-21 Cgi Pharmaceuticals, Inc. Certain amino-substituted monocycles as kinase modulators
EP1554258A1 (en) 2002-08-20 2005-07-20 Neurogen Corporation 5-substituted-2-arylpyrazines as modulators of crf receptors
EP1539736A1 (en) * 2002-09-12 2005-06-15 Pharmacia & Upjohn Company LLC Substituted 1,4-pyrazine derivatives
WO2004046136A1 (en) * 2002-11-21 2004-06-03 Pharmacia & Upjohn Company Llc Pyrazine compounds as crf modulators
SE0203753D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
SE0203754D0 (sv) * 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
RS53118B (sr) 2003-02-26 2014-06-30 Sugen Inc. Aminoheteroaril jedinjenja kao inhibitori protein kinaze
CA2524519A1 (en) 2003-05-09 2004-11-18 Pharmacia & Upjohn Company Llc Compounds as crf1 receptor antagonists
MXPA05012081A (es) 2003-05-09 2006-02-22 Pharmacia & Upjohn Co Llc Derivados de pirimidina sustituidos.
CA2529790A1 (en) * 2003-06-27 2005-01-27 Banyu Pharmaceutical Co., Ltd. Heteroaryloxy nitrogenous saturated heterocyclic derivative
WO2005040151A1 (en) * 2003-10-27 2005-05-06 Astellas Pharma Inc. Pyrazine derivatives and pharmaceutical use thereof
US20060211710A1 (en) * 2005-03-17 2006-09-21 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
AR053712A1 (es) * 2005-04-18 2007-05-16 Neurogen Corp Heteroarilos sustituidos, antagonistas de cb1 (receptor 1 canabinoide)
BRPI0619424B1 (pt) * 2005-12-05 2022-02-08 Pfizer Products Inc Uso de inibidores c-met/hgfrs para a fabricação de medicamentos
KR101146852B1 (ko) * 2005-12-05 2012-05-16 화이자 프로덕츠 인크. C?met/hgfr 억제제의 다형체
SG157264A1 (en) * 2008-06-02 2009-12-29 Inzign Pte Ltd A golf tee and method of producing a golf tee
US7932256B2 (en) * 2008-07-31 2011-04-26 Bristol-Myers Squibb Company (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-carbonitrile: a pyrazinone modulator of corticotropin-releasing factor receptor activity
EP3105216B1 (en) 2014-02-14 2018-10-10 Takeda Pharmaceutical Company Limited Pyrazine modulators of gpr6
CN115925679A (zh) 2014-12-24 2023-04-07 株式会社Lg化学 作为gpr120激动剂的联芳基衍生物
PH12019500056B1 (en) 2016-07-12 2024-01-31 Revolution Medicines Inc 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
BR112019015075A2 (pt) 2017-01-23 2020-03-10 Revolution Medicines, Inc. Compostos bicíclicos como inibidores de shp2 alostéricos
SG11201906412SA (en) 2017-01-23 2019-08-27 Revolution Medicines Inc Pyridine compounds as allosteric shp2 inhibitors
RU2672470C1 (ru) * 2017-07-10 2018-11-15 Федеральное государственное бюджетное учреждение науки Институт нефтехимии и катализа Российской академии наук Способ получения 2,3,5,6-тетрафенил(бензил)пиразина
SG11202002941WA (en) 2017-10-12 2020-04-29 Revolution Medicines Inc Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors
CA3084058A1 (en) 2017-12-15 2019-06-20 Revolution Medicines, Inc. Polycyclic compounds as allosteric shp2 inhibitors
KR20210003831A (ko) * 2018-04-20 2021-01-12 버지니아 테크 인터렉추얼 프라퍼티스, 인크. 미토콘드리아 언커플러로서 유용한 아미노피라진 및 관련 화합물
WO2020252229A2 (en) * 2019-06-14 2020-12-17 Disarm Therapeutics, Inc. Inhibitors of sarm1
GB202006076D0 (en) * 2020-04-24 2020-06-10 Univ Greenwich Interleukin inhibitors

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2425355A1 (de) 1974-05-25 1975-12-04 Basf Ag Verfahren zur herstellung von pyrazinen
DK143899C (da) * 1975-04-21 1982-04-13 Merck & Co Inc Analogifremgangsmaade til fremstilling af piperazinylpyrazinderivater
FR2398738A1 (fr) * 1977-06-22 1979-02-23 Lilly Co Eli Preparation de benzoylurees
US4293552A (en) * 1978-02-27 1981-10-06 Eli Lilly And Company Novel 1-(mono-o-substituted benzoyl)-3-(substituted pyrazinyl) ureas
US4211870A (en) * 1979-04-06 1980-07-08 Eli Lilly And Company Preparation of substituted 2-aminopyrazines
JPS59144772A (ja) * 1983-02-08 1984-08-18 Ube Ind Ltd 液晶性ピラジン誘導体およびその製法
JPS625970A (ja) * 1985-03-15 1987-01-12 Terumo Corp ピラジン誘導体およびこれを含有する血小板凝集抑制剤
JPH0739398B2 (ja) * 1986-10-04 1995-05-01 宇部興産株式会社 液晶性ピラジン誘導体
NZ227684A (en) * 1988-01-30 1991-07-26 Merck Sharp & Dohme Pyrazine, pyridazine, and pyrimidine derivatives and pharmaceutical compositions
JPH0348666A (ja) 1989-07-17 1991-03-01 Rasa Kogyo Kk 芳香族ジアミン化合物の製造方法
DE3940477A1 (de) * 1989-12-07 1991-06-13 Bayer Ag Hetaryl-substituierte pyridinylpyrimidin-derivate
GB2272216A (en) * 1992-11-04 1994-05-11 Merck Patent Gmbh Liquid crystalline di-, tri- and tetra-fluorinated phenylpyrazines
JP3398152B2 (ja) * 1993-10-12 2003-04-21 ブリストル‐マイヤーズ・スクイブ・ファーマ・カンパニー 1n−アルキル−n−アリールピリミジンアミンおよびその誘導体
WO1997011943A1 (en) * 1995-09-26 1997-04-03 Nippon Soda Co., Ltd. Pyrazole compounds, process for preparing the same, and agrohorticultural bactericide
DE69710594T2 (de) * 1996-09-16 2002-08-29 Du Pont Pharmaceuticals Co., Wilmington Eine resorbierbare röntgenopake markierung enthaltendes chirurgisches implantat und verfahren zum verriegeln desselben in einem körper
MA26473A1 (fr) * 1997-03-01 2004-12-20 Glaxo Group Ltd Composes pharmacologiquement actifs.
BE1011077A3 (fr) 1997-03-28 1999-04-06 Univ Catholique Louvain Composition pharmaceutique, cosmetique et/ou alimentaire aux proprietes anti-oxydantes.
EP1052238A4 (en) 1998-01-28 2007-05-02 Shionogi & Co NEW TRICYCLIC CONNECTION
GB9818881D0 (en) * 1998-08-28 1998-10-21 Glaxo Group Ltd Compounds
CA2361561A1 (en) 1999-02-02 2000-08-10 K.U. Leuven Research & Development Immunosurpressive effects of pteridine derivatives

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KR20080021603A (ko) 2008-03-07
DZ3293A1 (fr) 2001-08-23
EP1255740A2 (en) 2002-11-13
HUP0301573A2 (hu) 2003-12-29
US20050215559A1 (en) 2005-09-29
HUP0301573A3 (en) 2004-03-29
CZ20022739A3 (cs) 2003-02-12
EE200200453A (et) 2003-12-15
MXPA02007868A (es) 2003-02-10
EA200200766A1 (ru) 2003-10-30
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CA2651825A1 (en) 2001-08-23
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ATE307121T1 (de) 2005-11-15
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