CN1997371A - 烟酰胺衍生物及其作为治疗剂的用途 - Google Patents
烟酰胺衍生物及其作为治疗剂的用途 Download PDFInfo
- Publication number
- CN1997371A CN1997371A CNA2004800435489A CN200480043548A CN1997371A CN 1997371 A CN1997371 A CN 1997371A CN A2004800435489 A CNA2004800435489 A CN A2004800435489A CN 200480043548 A CN200480043548 A CN 200480043548A CN 1997371 A CN1997371 A CN 1997371A
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- Prior art keywords
- piperazine
- nicotiamide
- alkyl
- replaces arbitrarily
- phenyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 description 1
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- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
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- 125000005457 triglyceride group Chemical group 0.000 description 1
- 150000004684 trihydrates Chemical class 0.000 description 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- JBWKIWSBJXDJDT-UHFFFAOYSA-N triphenylmethyl chloride Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(Cl)C1=CC=CC=C1 JBWKIWSBJXDJDT-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Diabetes (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Description
化合物 | 活性%10μM | Mol.重量 |
6-[4-(2-溴-5-甲氧基-苯甲酰基)-哌嗪-1-基]-N-(2-乙基硫烷基-乙基)-烟酰胺 | 1.4 | 516.15 |
N-(3-苯基-丙基)-6-[4-(2-三氟甲基-苯甲酰基)-哌嗪-1-基]-烟酰胺 | 1.3 | 458.13 |
6-[4-(2-萘-2-基-乙酰基)-哌嗪-1-基]-N-戊基-烟酰胺 | 0.7 | 496.21 |
化合物 | 活性%10μM | Mol.重量 |
6-[4-(3-环己基-丙酰基)-哌嗪-1-基]-N-(3-甲基丁基)-烟酰胺 | 1.3 | 492.12 |
6-[4-(2-溴-苯甲酰基)-哌嗪-1-基]-N-(3-丁氧基-丙基)-烟酰胺 | 0.8 | 448.21 |
N-丁基-6-[4-(2-乙基丁酰基)-哌嗪-1-基]-烟酰胺 | 2.0 | 448.14 |
N-(3-丁氧基-丙基)-6-[4-(2,4-二甲基-苯甲酰基)-哌嗪-1-基]-烟酰胺 | 0.7 | 482.19 |
N-(3-甲基-丁基)-6-[4-(2-邻甲苯基-乙酰基)-哌嗪-1-基]-烟酰胺 | 3.2 | 442.27 |
6-[4-(2,4-二氯-苯甲酰基)-哌嗪-1-基]-N-(1-甲基-3-苯基-丙基)-烟酰胺 | 2.7 | 434.19 |
6-[4-(2-溴-5-甲氧基-苯甲酰基)-哌嗪-1-基]-N-苯乙基-烟酰胺 | 1.1 | 496.14 |
6-[4-(2-乙基丁酰基)-哌嗪-1-基]-N-(3-甲基丁基)-烟酰胺 | 1.7 | 448.21 |
6-[4-(2,4-二氯-苯甲酰基)-哌嗪-1-基]-N-戊基-烟酰胺 | 1.2 | 482.13 |
N-(1,3-二甲基丁基)-6-[4-(2-三氟甲基-苯甲酰基)-哌嗪-1-基]-烟酰胺 | 1.8 | 458.13 |
6-[4-(3-环己基-丙酰基)-哌嗪-1-基]-N-(2-乙基硫烷基-乙基)-烟酰胺 | 1.4 | 448.14 |
6-[4-(2-溴-苯甲酰基)-哌嗪-1-基]-N-(3-甲氧基-丙基)-烟酰胺 | 1.2 | 462.22 |
化合物 | 活性%10μM | Mol.重量 |
6-[4-(3-环己基-丙酰基)-哌嗪-1-基]-N-(1-甲基丁基)-烟酰胺 | 2.1 | 430.24 |
6-[4-(2-溴-苯甲酰基)-哌嗪-1-基]-N-(3-乙氧基-丙基)-烟酰胺 | 1.0 | 537.5 |
N-(1-甲基-3-苯基-丙基)-6-[4-(3-甲基-噻吩-2-羰基)-哌嗪-1-基]-烟酰胺 | 3.4 | 469 |
6-[4-(2-苯基-丁酰基)-哌嗪-1-基]-N-(3-苯基-丙基)-烟酰胺 | 3.6 | 445.4 |
N-(2-乙基硫烷基-乙基)-6-[4-(2-对甲苯基-乙酰基)-哌嗪-1-基]-烟酰胺 | 1.8 | 470.6 |
N-(3-苯基-丙基)-6-[4-(2-三氟甲基-苯甲酰基)-哌嗪-1-基]-烟酰胺 | 3.9 | 408.5 |
Claims (61)
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PCT/US2004/021792 WO2006014168A1 (en) | 2004-07-06 | 2004-07-06 | Nicotinamide derivatives and their use as therapeutic agents |
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CN1997371A true CN1997371A (zh) | 2007-07-11 |
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CNA2004800435489A Pending CN1997371A (zh) | 2004-07-06 | 2004-07-06 | 烟酰胺衍生物及其作为治疗剂的用途 |
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EP (1) | EP1763350B1 (zh) |
JP (1) | JP2008505891A (zh) |
CN (1) | CN1997371A (zh) |
AT (1) | ATE537830T1 (zh) |
AU (1) | AU2004321997A1 (zh) |
BR (1) | BRPI0418939A (zh) |
CA (1) | CA2573198A1 (zh) |
ES (1) | ES2380020T3 (zh) |
MX (1) | MX2007000028A (zh) |
WO (1) | WO2006014168A1 (zh) |
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JP5043668B2 (ja) | 2004-09-20 | 2012-10-10 | ゼノン・ファーマシューティカルズ・インコーポレイテッド | 複素環誘導体および治療薬としてのそれらの使用 |
EP1804799B1 (en) | 2004-09-20 | 2013-08-21 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
ES2682282T3 (es) | 2004-10-29 | 2018-09-19 | Kalypsys, Inc. | Compuestos bicíclicos sustituidos con sulfonilo como moduladores de PPAR |
WO2007044085A2 (en) * | 2005-05-19 | 2007-04-19 | Xenon Pharmaceuticals Inc. | Heteroaryl compounds and their uses as therapeutic agents |
MX2007015216A (es) | 2005-06-03 | 2008-02-22 | Xenon Pharmaceuticals Inc | Derivados de aminotiazol y sus usos como agentes terapeuticos. |
NZ566831A (en) | 2005-10-25 | 2011-09-30 | Kalypsys Inc | Salts of modulators of PPAR and methods of treating metabolic disorders |
ATE486862T1 (de) | 2006-06-05 | 2010-11-15 | Novartis Ag | Organische verbindungen |
BRPI0719122A2 (pt) | 2006-08-24 | 2013-12-10 | Novartis Ag | Compostos orgânicos |
US20080176861A1 (en) | 2007-01-23 | 2008-07-24 | Kalypsys, Inc. | Sulfonyl-substituted bicyclic compounds as ppar modulators for the treatment of non-alcoholic steatohepatitis |
US7842696B2 (en) | 2007-06-21 | 2010-11-30 | Forest Laboratories Holdings Limited | Piperazine derivatives as inhibitors of stearoyl-CoA desaturase |
CA2695331A1 (en) * | 2007-08-03 | 2009-02-12 | F. Hoffmann-La Roche Ag | Pyridinecarboxamide and benzamide derivatives as taar1 ligands |
ES2442926T3 (es) | 2007-08-22 | 2014-02-14 | Astrazeneca Ab | Derivados de ciclopropilamida `978 |
ATE518839T1 (de) * | 2007-08-23 | 2011-08-15 | Sanofi Sa | Azoloarin derivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
CN101597278B (zh) | 2008-06-04 | 2013-04-17 | 中国中化股份有限公司 | 酰胺类化合物及其制备与应用 |
AU2010215035B2 (en) | 2009-02-17 | 2014-06-12 | Merck Canada Inc. | Novel spiro compounds useful as inhibitors of stearoyl-coenzyme A delta-9 desaturase |
TW201039825A (en) | 2009-02-20 | 2010-11-16 | Astrazeneca Ab | Cyclopropyl amide derivatives 983 |
EP2459568A4 (en) | 2009-07-28 | 2013-02-27 | Merck Frosst Canada Ltd | NOVEL SPIRO COMPOUNDS USEFUL AS DELTA-9 DEATURASE STEAROYL COENZYME INHIBITORS |
EP2475367A1 (en) | 2009-09-10 | 2012-07-18 | Centre National De La Recherche Scientifique | NOVEL INHIBITORS OF STEAROYL-CoA-DESATURASE-1 AND THEIR USES |
MX336333B (es) | 2010-02-18 | 2016-01-15 | Astrazeneca Ab | Nueva forma cristalina de un derivado de ciclopropilbenzamida. |
JP2013528169A (ja) * | 2010-05-27 | 2013-07-08 | バイエル・クロップサイエンス・アーゲー | 殺菌剤としてのピリジニルカルボン酸誘導体 |
KR101271538B1 (ko) | 2011-06-24 | 2013-06-05 | (주)이뮤노텍 | 유기산, l―카르니틴, l―아르기닌 및 니코틴아미드를 유효성분으로 포함하는 비만의 예방 및 개선용 조성물 |
EP2766000A2 (en) | 2011-10-15 | 2014-08-20 | F.Hoffmann-La Roche Ag | Scd1 antagonists for treating cancer |
BR112014029365A2 (pt) | 2012-05-22 | 2017-06-27 | Hoffmann La Roche | inibidores seletivos de células indiferenciadas |
JP2019533022A (ja) | 2016-10-24 | 2019-11-14 | ユマニティ セラピューティクス,インコーポレーテッド | 化合物及びその使用 |
KR20190108118A (ko) | 2017-01-06 | 2019-09-23 | 유마니티 테라퓨틱스, 인크. | 신경계 장애의 치료를 위한 방법 |
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CA2358047A1 (en) * | 1998-12-24 | 2000-07-06 | Francis A. Volz | Substituted (aminoiminomethyl or aminomethyl)benzoheteroaryl compounds |
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EP1035115B1 (en) * | 1999-02-24 | 2004-09-29 | F. Hoffmann-La Roche Ag | 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists |
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TWI259180B (en) * | 2000-08-08 | 2006-08-01 | Hoffmann La Roche | 4-Phenyl-pyridine derivatives |
WO2002102778A1 (fr) * | 2001-06-15 | 2002-12-27 | Yamanouchi Pharmaceutical Co., Ltd. | Derive de phenylpyridinecarbonylpiperazine |
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JPWO2003037862A1 (ja) * | 2001-10-30 | 2005-02-17 | 日本新薬株式会社 | アミド誘導体及び医薬 |
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EP1456175A1 (en) * | 2001-12-07 | 2004-09-15 | Eli Lilly And Company | Substituted heterocyclic carboxamides with antithrombotic activity |
DK1466912T3 (da) * | 2002-01-18 | 2013-07-01 | Astellas Pharma Inc | 2-acylaminothiazolderivat eller salt deraf |
DE60320957D1 (en) * | 2002-03-13 | 2008-06-26 | Janssen Pharmaceutica Nv | Sulfonylderivate als histone-deacetylase-inhibitoren |
WO2004010927A2 (en) * | 2002-07-25 | 2004-02-05 | Wisconsin Alumni Research Foundation | Method for increasing insulin sensitivity and for treating and preventing type 2 diabetes |
-
2004
- 2004-07-06 AT AT04756752T patent/ATE537830T1/de active
- 2004-07-06 AU AU2004321997A patent/AU2004321997A1/en not_active Abandoned
- 2004-07-06 EP EP04756752A patent/EP1763350B1/en not_active Expired - Lifetime
- 2004-07-06 ES ES04756752T patent/ES2380020T3/es not_active Expired - Lifetime
- 2004-07-06 MX MX2007000028A patent/MX2007000028A/es unknown
- 2004-07-06 BR BRPI0418939-6A patent/BRPI0418939A/pt not_active IP Right Cessation
- 2004-07-06 CA CA002573198A patent/CA2573198A1/en not_active Abandoned
- 2004-07-06 CN CNA2004800435489A patent/CN1997371A/zh active Pending
- 2004-07-06 WO PCT/US2004/021792 patent/WO2006014168A1/en active Application Filing
- 2004-07-06 JP JP2007520281A patent/JP2008505891A/ja active Pending
Also Published As
Publication number | Publication date |
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ATE537830T1 (de) | 2012-01-15 |
WO2006014168A1 (en) | 2006-02-09 |
MX2007000028A (es) | 2007-07-20 |
CA2573198A1 (en) | 2006-02-09 |
JP2008505891A (ja) | 2008-02-28 |
EP1763350A1 (en) | 2007-03-21 |
ES2380020T3 (es) | 2012-05-07 |
EP1763350B1 (en) | 2011-12-21 |
AU2004321997A1 (en) | 2006-02-09 |
BRPI0418939A (pt) | 2008-04-08 |
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