AR035321A1 - Derivados de 2-arilimino-2,3-dihidrotiazoles, procedimiento para su preparacion, y uso de los mismos para preparar medicamentos y composiciones farmaceuticas - Google Patents
Derivados de 2-arilimino-2,3-dihidrotiazoles, procedimiento para su preparacion, y uso de los mismos para preparar medicamentos y composiciones farmaceuticasInfo
- Publication number
- AR035321A1 AR035321A1 ARP000103722A ARP000103722A AR035321A1 AR 035321 A1 AR035321 A1 AR 035321A1 AR P000103722 A ARP000103722 A AR P000103722A AR P000103722 A ARP000103722 A AR P000103722A AR 035321 A1 AR035321 A1 AR 035321A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- radical
- aryl
- optionally substituted
- cycloalkyl
- Prior art date
Links
- 229940079593 drug Drugs 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- -1 hexenyl alkyl Chemical group 0.000 abstract 17
- 150000003254 radicals Chemical class 0.000 abstract 17
- 125000000217 alkyl group Chemical group 0.000 abstract 11
- 125000003118 aryl group Chemical group 0.000 abstract 9
- 125000002837 carbocyclic group Chemical group 0.000 abstract 8
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 6
- 125000003282 alkyl amino group Chemical group 0.000 abstract 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 4
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 3
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 3
- 125000006350 alkyl thio alkyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000006213 aryl hydroxyalkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Natural products C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 2
- NAWXUBYGYWOOIX-SFHVURJKSA-N (2s)-2-[[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]amino]-4-methylidenepentanedioic acid Chemical compound C1=CC2=NC(N)=NC(N)=C2C=C1CCC1=CC=C(C(=O)N[C@@H](CC(=C)C(O)=O)C(O)=O)C=C1 NAWXUBYGYWOOIX-SFHVURJKSA-N 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 abstract 1
- 125000001494 2-propynyl group Chemical group [H]C#CC([H])([H])* 0.000 abstract 1
- 206010000599 Acromegaly Diseases 0.000 abstract 1
- 208000003200 Adenoma Diseases 0.000 abstract 1
- 208000012671 Gastrointestinal haemorrhages Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 108050001286 Somatostatin Receptor Proteins 0.000 abstract 1
- 102000011096 Somatostatin receptor Human genes 0.000 abstract 1
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 1
- 125000005018 aryl alkenyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000005160 aryl oxy alkyl group Chemical group 0.000 abstract 1
- 150000005840 aryl radicals Chemical class 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 208000002458 carcinoid tumor Diseases 0.000 abstract 1
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000002124 endocrine Effects 0.000 abstract 1
- 125000006038 hexenyl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
- C07D277/38—Nitrogen atoms
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- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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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- Otolaryngology (AREA)
Abstract
Derivados de 2-arilimino-2,3-dihidrotiazoles, procedimiento para su preparación, y uso de los mismos para preparar medicamentos y composiciones farmacéuticas, de la fórmula general (1) donde R1, R2, R3 y R4 toman los siguientes valores: R1 representa un amino(C2-7)alquilo, amino alquilaril alquilo, aminoalquil cicloalquil alquilo, (C1-15)alquilo, (C3-7)cicloalquilo, (C1-6)alquil(C3-6)cicloalquilo, (C3-6)cicloalquil alquilo, ciclo hexenil alquilo, alquenilo, alquinilo, un radical arilo carbocíclico que contiene por lo menos dos anillos de los cuales por lo menos uno no es aromático, un radical aralquilo carbocíclico o heterocíclico opcionalmente sustituido en el grupo arilo, un radical bis-arialquilo, alcoxialquilo, furanil alquilo, tetrahidro furanil alquilo, dialquil amino alquilo, N-acetamido alquilo, ciano alquilo, alquiltio alquilo, arilhidroxi alquilo, aralcoxi alquilo, morfolino alquilo, pirrolidino alquilo, piperidino alquilo, N-alquil pirrolidino alquilo, N-alquil piperazinil alquilo u oxopirrolidino alquilo, o R1 representa uno de los radicales representados por fórmulas (2), (3) y (4), o R1 representa además un radical -C(R11)(R12)-CO-R10; R2 representa un radical arilo carbocíclico o heterocíclico, opcionalmente sustituido, o R2 representa uno de los radicales de fórmulas (5) y (6); R3 representa un radical alquilo, adamantilo, arilo carbocíclico o heterocíclico opcionalmente sustituido, aralquilo carbocíclico o heterocíclico opcionalmente sustituido en el grupo arilo, o R3 representa uno de los radicales de fórmulas (7) y (8), o R3 representa también un radical -CO-R5; R4 representa H, alquilo, aralquilo carbocíclico o heterocíclico opcionalmente sustituido, en el radical arilo; o bien el radical de fórmula (9) representa un radical de la fórmula general (10) en la cual i representa un número entero de 1 a 3; R5 representa el radical N(R6)(R7); R6 representa un radical alquilo C1-16, cicloalquil alquilo, hidroxi alquilo, ariloxi alquilo, un radical aralquilo carbocíclico o heterocíclico opcionalmente sustituido en el grupo arilo, aralcoxi alquilo, aril hidroxi alquilo, alcoxi alquilo, alquil tioalquilo, alquenilo, alquinilo, ciclo hexenilo, ciclo hexenil alquilo, alquil tiohidroxi alquilo, ciano alquilo, N-acetamido alquilo, un radical bis-aril alquilo opcionalmente sustituido en los grupos arilo, un radical di-aril alquilo opcionalmente sustituido en los grupos arilo, un radical morfolino alquilo, pirrolidino alquilo, piperidino alquilo, N-alquil pirrolidinoalquilo, oxopirrolidino alquilo, tetrahidro furanil alquilo, N-bencilpirrolidino alquilo, N-alquil piperazinil alquilo, N-bencil piperazinil alquilo, N-bencilpiperidinil alquilo o N-alcoxi carbonil piperidinilo, o R6 representa un radical cicloalquilo(C3-8) cicloalquilo opcionalmente sustituido por un radical seleccionado del grupo que comprende al radical hidroxi y un radical alquilo, o R6 representa uno de los radicales de fórmulas (11), (12), (13) y (14); R7 representa H o un radical alquilo, hidroxialquilo, mono o diamino alquilo o aralquilo; o el radical -N(R6)(R7) representa el radical de fórmula (15) en la cual R8 representa H, alquilo, hidroxi alquilo, arilo carbocíclico o heterocíclico opcionalmente sustituido, aralquilo opcionalmente sustituido en el grupo arilo, alquenilo, alcoxi alquilo, cicloalquilo, cicloalquil alquilo, bis-aril alquilo, piperidinilo, pirrolidinilo, hidroxi, arilalquenilo, o R8 representa -X-(CH2)b-R9; R9 representa H o un radical alquilo, alcoxi, ariloxi, arilo carbocíclico o heterocíclico opcionalmente sustituido, morfolinilo, pirrolidinilo, alquilamino o N,N'-(alquil)(aril)amino; X representa CO, CO-NH ó SO2; Y representa CH ó N; a representa 1 ó 2, b representa un número entero de 0 a 6; o el radical N(R6)(R7) representa un radical de fórmula (16) en la cual Z representa CH, O ó S; c representa un número entero de 0 a 4, o el radical N(R6)(R7) representa uno de los radicales de fórmulas (17) a (32); R10 representa un radical amino (C2-7) alquil amino, ((amino alquil)aril) alquilamino, ((amino alquil) cicloalquil) alquil amino, piperazinilo, homopiperazinilo, o R10 representa el radical de fórmula (33); R11 representa H; y R12 representa H o un radical alquilo, un radical (C3-7)cicloalquilo, aralquilo carbocíclico o heterocíclico opcionalmente sustituido, propargilo, alilo, hidroxi alquilo, alquil tioalquilo, arilalquil alcoxi alquilo, arilalquiltio alcoxi alquilo; o una sal de un compuesto de la fórmula general (1). Estos compuestos son útiles, en particular en el tratamiento de los estados patológicos o enfermedades en las cuales intervienen uno o más de los receptores de la somatostatina, éstos estados incluyen en particular la acromegalia, los adenomas hipofiseales o los tumores gastroenteropancreáticos endocrinos que incluyen el Síndrome Carcinoide y las hemorragias gastrointestinales.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9909496A FR2796643B1 (fr) | 1999-07-22 | 1999-07-22 | Derives de 2-arylimino-2, 3-dihydrothiazoles, leurs procedes de preparation et leur utilisation therapeutique |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR035321A1 true AR035321A1 (es) | 2004-05-12 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| ARP000103722A AR035321A1 (es) | 1999-07-22 | 2000-07-19 | Derivados de 2-arilimino-2,3-dihidrotiazoles, procedimiento para su preparacion, y uso de los mismos para preparar medicamentos y composiciones farmaceuticas |
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| US (1) | US6727269B1 (es) |
| EP (1) | EP1202980A1 (es) |
| JP (2) | JP4063537B2 (es) |
| KR (1) | KR100692352B1 (es) |
| CN (1) | CN100443479C (es) |
| AR (1) | AR035321A1 (es) |
| AU (1) | AU782187B2 (es) |
| BR (1) | BR0012647A (es) |
| CA (1) | CA2382940C (es) |
| CZ (1) | CZ302073B6 (es) |
| FR (1) | FR2796643B1 (es) |
| HU (1) | HUP0202425A3 (es) |
| IL (3) | IL147582A0 (es) |
| MX (1) | MXPA02000723A (es) |
| NO (1) | NO322394B1 (es) |
| NZ (1) | NZ516599A (es) |
| PL (1) | PL353831A1 (es) |
| RU (1) | RU2266287C2 (es) |
| WO (1) | WO2001007424A1 (es) |
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| FR2819508B1 (fr) * | 2001-01-12 | 2005-01-21 | Sod Conseils Rech Applic | Derives de 2-arylimino-2, 3-dihydorthiazoles, leurs procedes de preparation et leur utilisation therapeutiques |
| CN100369903C (zh) * | 2000-06-30 | 2008-02-20 | 大日本住友制药株式会社 | 五元环化合物 |
| DE10133665A1 (de) * | 2001-07-11 | 2003-01-30 | Boehringer Ingelheim Pharma | Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Herstellung |
| AU2002359359A1 (en) | 2001-12-28 | 2003-07-24 | Somatocor Pharmaceuticals, Inc. | Imidazolidin-2,4-dione derivatives as non-peptide somatostatin receptor ligands |
| US7067538B2 (en) | 2002-08-09 | 2006-06-27 | Warner-Lambert Company, Llc | MCP-1 receptor antagonists and methods of use thereof |
| JP4896387B2 (ja) * | 2003-09-30 | 2012-03-14 | 武田薬品工業株式会社 | チアゾリン誘導体およびその用途 |
| WO2005030740A1 (ja) * | 2003-09-30 | 2005-04-07 | Takeda Pharmaceutical Company Limited | チアゾリン誘導体およびその用途 |
| WO2005082844A1 (en) * | 2004-02-27 | 2005-09-09 | Oy Juvantia Pharma Ltd | Treatment of diseases by using a somatostatin receptor agonist |
| WO2005082845A1 (en) * | 2004-02-27 | 2005-09-09 | Oy Juvantia Pharma Ltd | Novel therapies with somatostatin receptor agonists |
| AU2012202459B2 (en) * | 2004-03-15 | 2014-06-12 | Janssen Pharmaceutica, N.V. | Novel compounds as opioid receptor modulators |
| UA86053C2 (ru) | 2004-03-15 | 2009-03-25 | Янссен Фармацевтика Н.В. | Соединения как модуляторы опиоидных рецепторов |
| US7910613B2 (en) * | 2004-09-22 | 2011-03-22 | H. Lundbeck A/S | 2-acylaminothiazole derivatives |
| US7674912B2 (en) * | 2005-04-25 | 2010-03-09 | H. Lundbeck A/S | Pro-drugs of N-thiazol-2-yl-benzamide derivatives |
| MX2008015214A (es) | 2006-05-31 | 2008-12-12 | Abbott Lab | Compuestos como ligandos de receptor canabinoide y sus usos. |
| EP2038266A2 (en) * | 2006-05-31 | 2009-03-25 | Abbott Laboratories | Compounds as cannabinoid receptor ligands and uses thereof |
| US8841334B2 (en) | 2006-05-31 | 2014-09-23 | Abbvie Inc. | Compounds as cannabinoid receptor ligands and uses thereof |
| US7868038B2 (en) | 2006-08-31 | 2011-01-11 | Abbott Laboratories | Compounds as cannabinoid receptor ligands |
| US7985768B2 (en) | 2006-08-31 | 2011-07-26 | Abbott Laboratories | Compounds as cannabinoid receptor ligands |
| CN101765594A (zh) | 2007-03-28 | 2010-06-30 | 雅培制药有限公司 | 作为大麻素受体配体的1,3-噻唑-2(3h)-亚基化合物 |
| US7872033B2 (en) | 2007-04-17 | 2011-01-18 | Abbott Laboratories | Compounds as cannabinoid receptor ligands |
| MX2009012374A (es) | 2007-05-18 | 2009-12-01 | Abbott Lab | Compuestos novedosos como ligandos del receptor de canabinoides. |
| KR100863239B1 (ko) * | 2007-05-23 | 2008-10-15 | 한국과학기술연구원 | 신규한 2-이미노-1,3-티아졸린계 화합물 및 이를 함유하는t-형 칼슘 채널 저해제 |
| US9193713B2 (en) | 2007-10-12 | 2015-11-24 | Abbvie Inc. | Compounds as cannabinoid receptor ligands |
| CA2716857A1 (en) | 2008-03-11 | 2009-09-17 | Teodozyi Kolasa | Novel compounds as cannabinoid receptor ligands |
| US8846730B2 (en) | 2008-09-08 | 2014-09-30 | Abbvie Inc. | Compounds as cannabinoid receptor ligands |
| US8859596B2 (en) | 2008-09-16 | 2014-10-14 | Abbvie Inc. | Compounds as cannabinoid receptor ligands |
| PA8854001A1 (es) | 2008-12-16 | 2010-07-27 | Abbott Lab | Compuestos novedosos como ligandos de receptores de canabinoides |
| RU2562833C2 (ru) | 2010-08-09 | 2015-09-10 | НБ Хелс Лаборатори Ко. Лтд. | Ингибитор казеинкиназы 1 дельта и казеинкиназы 1 е |
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1999
- 1999-07-22 FR FR9909496A patent/FR2796643B1/fr not_active Expired - Fee Related
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2000
- 2000-07-19 AR ARP000103722A patent/AR035321A1/es unknown
- 2000-07-21 HU HU0202425A patent/HUP0202425A3/hu unknown
- 2000-07-21 EP EP00958575A patent/EP1202980A1/fr not_active Withdrawn
- 2000-07-21 WO PCT/FR2000/002095 patent/WO2001007424A1/fr not_active Ceased
- 2000-07-21 MX MXPA02000723A patent/MXPA02000723A/es active IP Right Grant
- 2000-07-21 PL PL00353831A patent/PL353831A1/xx unknown
- 2000-07-21 KR KR1020027000839A patent/KR100692352B1/ko not_active Expired - Fee Related
- 2000-07-21 JP JP2001512509A patent/JP4063537B2/ja not_active Expired - Fee Related
- 2000-07-21 NZ NZ516599A patent/NZ516599A/xx not_active IP Right Cessation
- 2000-07-21 BR BR0012647-0A patent/BR0012647A/pt active Search and Examination
- 2000-07-21 CZ CZ20020187A patent/CZ302073B6/cs not_active IP Right Cessation
- 2000-07-21 IL IL14758200A patent/IL147582A0/xx unknown
- 2000-07-21 US US10/031,429 patent/US6727269B1/en not_active Expired - Fee Related
- 2000-07-21 AU AU70053/00A patent/AU782187B2/en not_active Ceased
- 2000-07-21 CN CNB008107157A patent/CN100443479C/zh not_active Expired - Fee Related
- 2000-07-21 CA CA2382940A patent/CA2382940C/fr not_active Expired - Fee Related
- 2000-07-21 RU RU2002104574/04A patent/RU2266287C2/ru not_active IP Right Cessation
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2002
- 2002-01-10 IL IL147582A patent/IL147582A/en not_active IP Right Cessation
- 2002-01-21 NO NO20020314A patent/NO322394B1/no not_active IP Right Cessation
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2006
- 2006-04-18 JP JP2006114071A patent/JP2006257093A/ja active Pending
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Also Published As
| Publication number | Publication date |
|---|---|
| WO2001007424A1 (fr) | 2001-02-01 |
| AU782187B2 (en) | 2005-07-07 |
| IL185786A0 (en) | 2008-01-06 |
| CN100443479C (zh) | 2008-12-17 |
| MXPA02000723A (es) | 2002-09-17 |
| JP4063537B2 (ja) | 2008-03-19 |
| CZ2002187A3 (cs) | 2002-06-12 |
| NO20020314D0 (no) | 2002-01-21 |
| JP2003505453A (ja) | 2003-02-12 |
| AU7005300A (en) | 2001-02-13 |
| HUP0202425A3 (en) | 2002-12-28 |
| CZ302073B6 (cs) | 2010-09-29 |
| CN1362952A (zh) | 2002-08-07 |
| KR100692352B1 (ko) | 2007-03-12 |
| EP1202980A1 (fr) | 2002-05-08 |
| HUP0202425A2 (en) | 2002-10-28 |
| NZ516599A (en) | 2004-01-30 |
| PL353831A1 (en) | 2003-12-01 |
| RU2002104574A (ru) | 2004-01-20 |
| RU2266287C2 (ru) | 2005-12-20 |
| FR2796643B1 (fr) | 2005-04-29 |
| NO20020314L (no) | 2002-03-06 |
| NO322394B1 (no) | 2006-10-02 |
| HK1048314A1 (zh) | 2003-03-28 |
| US6727269B1 (en) | 2004-04-27 |
| BR0012647A (pt) | 2002-04-09 |
| JP2006257093A (ja) | 2006-09-28 |
| FR2796643A1 (fr) | 2001-01-26 |
| CA2382940A1 (fr) | 2001-02-01 |
| IL147582A0 (en) | 2002-08-14 |
| IL147582A (en) | 2009-08-03 |
| KR20020088405A (ko) | 2002-11-27 |
| CA2382940C (fr) | 2010-08-17 |
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