JP2000500479A - ピラゾール誘導体、その製造方法、および該誘導体を含む医薬組成物 - Google Patents
ピラゾール誘導体、その製造方法、および該誘導体を含む医薬組成物Info
- Publication number
- JP2000500479A JP2000500479A JP9519454A JP51945497A JP2000500479A JP 2000500479 A JP2000500479 A JP 2000500479A JP 9519454 A JP9519454 A JP 9519454A JP 51945497 A JP51945497 A JP 51945497A JP 2000500479 A JP2000500479 A JP 2000500479A
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.式: [式中、 −R1は、フッ素、ヒドロキシ、(C1−C5)アルコキシ、(C1−C5)アルキ ルチオ、ヒドロキシ(C1−C5)アルコキシ、−NR10R11基、シアノ、(C1 −C5)アルキルスルホニルまたは(C1−C5)アルキルスルフィニルであり; −R2およびR3は、(C1−C4)アルキルであるか、またはそれらが結合する窒 素原子と一緒になって5ないし10員の、飽和または不飽和の複素環残基(複素 環は、(C1−C3)アルキルまたは(C1−C3)アルコキシで置換されていない くても、一置換されていても、また多置換されていてもよい)を形成し; −R4、R5、R6、R7、R8およびR9は、それぞれ独立して、水素、ハロゲン、 またはトリフルオロメチルであり、R1がフッ素の場合には、R4、R5、R6、R7 、R8および/またはR9はフルオロメチルであってもよく、少なくともひとつ の置換基R4またはR7は水素以外である; −R10およびR11は、それぞれ独立して、水素または(C1−C5)アルキルであ るか、またはR10およびR11は、それらが結合する窒素原子と一緒になって、ピ ロリジン−1−イル、ピペリジン−1−イル、モルホリン−4−イルおよびピペ ラジン−1−イルから選択される複素環残基を形成してもよい(複素環は、(C1 −C4)アルキルで置換されていなくても置換されていてもよい) を意味する。] で表される化合物およびこれらの塩ならびに溶媒和物。 2.式:(式中、R1pは、フッ素、メトキシまたはメチルチオを意味する。)で表される 請求項1記載の化合物およびこれらの塩ならびに溶媒和物。 3.a)式: [式中、R4、R5、R6、R7、R8およびR9は請求項1における式(I)と同意 義、Rは(C1−C4)アルキルを意味する。] のブロム化エステルを式:R'1A(III)[式中、R'1は、請求項1において式 (I)について定義したR1であるか、または、R1の前駆体、Aは、水素または カチオンを意味する。]の化合物と反応させ、 b1)得られるエステルにおけるR'1を所望によりR1に変換し; b2)工程a)または工程b1)で得られる式: のエステルをけん化し; c)得られる式:の酸またはこの酸の機能的な誘導体を式:H2N−NR2R3(VI)[式中、R2お よびR3は請求項1における式(I)と同意義である。]のヒドラジンと反応さ せ; d1)得られる化合物中のR'1を所望によりR1に変換し; d2)工程c)または工程d1)で得られる式: の化合物を所望によりこれらの塩のひとつまたはこれらの溶媒和物のひとつに変 換する ことを特徴とする請求項1記載の式(I)の化合物、これらの塩およびこれらの 溶媒和物の製造方法。 4.a)式: (式中、R4、R5、R6、R7、R8、R9およびRは、請求項3と同意義である。 )のブロム化エステルをアルカリ金属またはアルカリ土類金属水酸化物と反応さ せ; b)得られる式: の酸またはこの酸の機能的な誘導体を式:H2N−NR2R3(VI)[式中、R2お よびR3は、請求項1における式(I)と同意義である。]のヒドラジンと反応 させ; c)得られる式: の化合物を式:Hal−B(式中、Halはハロゲン、Bはメシル、トシルまた はトリフルオロメタンスルホニル残基を意味する。)の化合物と反応させ; d)得られる式: の化合物を式:R1aA(XI)(式中、R1aは、上記に定義したものであり、Aは 水素またはカチオンを意味する。)と反応させ; e)得られる式:の化合物を所望によりこれらの塩のひとつまたはこれらの溶媒和物のひとつに変 換する ことを特徴とする、式中、R1=R1aであり、フッ素、(C1−C5)アルコキシ 、(C1−C5)アルキルチオ、ヒドロキシ(C1−C5)アルコキシ、シアノ、N R10R11基(ここで、R10およびR11は、請求項1における式(I)と同意義で ある。)から選択される基である、請求項1記載の式(I)の化合物を製造する 方法。 5.活性成分として、請求項1または2のいずれか一つに記載の化合物を含むこ とを特徴とする医薬組成物。 6.活性成分が少なくとも一つの医薬賦形剤と混合される投薬単位の形態である 、請求項5記載の医薬組成物。 7.0.5ないし1000mgの活性成分を含有する請求項6記載の医薬組成物 。 8.2ないし200mgの活性成分を含有する請求項7記載の医薬組成物。 9.請求項1または2のいずれか一つに記載の化合物の、化合物または放射活性 形態での、薬物学的手段としての使用。 10.式中のR1が18Fである式(I)の化合物の請求項9記載の使用。 11.カンナビノイドレセプターを単離し、精製し、解析することを可能とする リガンドの調製における、R1が水酸基またはヒドロキシ(C1−C5)アルコキ シ基である式(I)の請求項1または2のいずれか一つに記載の化合物の使用。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR9513956A FR2741621B1 (fr) | 1995-11-23 | 1995-11-23 | Nouveaux derives de pyrazole, procede pour leur preparation et compositions pharmaceutiques en contenant |
FR95/13956 | 1995-11-23 | ||
PCT/FR1996/001847 WO1997019063A1 (fr) | 1995-11-23 | 1996-11-21 | Derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant |
Publications (2)
Publication Number | Publication Date |
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JP2000500479A true JP2000500479A (ja) | 2000-01-18 |
JP2000500479A5 JP2000500479A5 (ja) | 2004-10-21 |
Family
ID=9484869
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP9519454A Pending JP2000500479A (ja) | 1995-11-23 | 1996-11-21 | ピラゾール誘導体、その製造方法、および該誘導体を含む医薬組成物 |
Country Status (16)
Country | Link |
---|---|
US (1) | US6028084A (ja) |
EP (1) | EP0876350B1 (ja) |
JP (1) | JP2000500479A (ja) |
AT (1) | ATE203015T1 (ja) |
AU (1) | AU7698596A (ja) |
BR (1) | BR9611618A (ja) |
CA (1) | CA2238430C (ja) |
DE (1) | DE69613860T2 (ja) |
DK (1) | DK0876350T3 (ja) |
ES (1) | ES2161382T3 (ja) |
FR (1) | FR2741621B1 (ja) |
GR (1) | GR3036830T3 (ja) |
MX (1) | MX9803891A (ja) |
NO (1) | NO310508B1 (ja) |
PT (1) | PT876350E (ja) |
WO (1) | WO1997019063A1 (ja) |
Cited By (6)
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---|---|---|---|---|
JP2006501275A (ja) * | 2002-09-19 | 2006-01-12 | ソルベイ・フアーマシユーチカルズ・ベー・ブイ | カンナビノイド−cb1レセプターリガンドとしての1h−1,2,4−トリアゾール−3−カルボキシアミド誘導体 |
JP2007514638A (ja) * | 2003-06-26 | 2007-06-07 | サノフィ−アベンティス | ジフェニルピリジン誘導体、その製造法および治療用途 |
JP2008526887A (ja) * | 2005-01-10 | 2008-07-24 | ユニバーシティ オブ コネチカット | カンナビノイド受容体に作用する新規なヘテロピロール類似体 |
JP2011506410A (ja) * | 2007-12-10 | 2011-03-03 | 7ティーエム ファーマ エイ/エス | カンナビノイド受容体モジュレーター |
JP2013500296A (ja) * | 2009-07-29 | 2013-01-07 | シーメンス アクティエンゲゼルシャフト | 活性成分および活性成分を検査するための方法 |
JP2014507425A (ja) * | 2011-09-30 | 2014-03-27 | ナショナル ヘルス リサーチ インスティテュートス | ピラゾール化合物 |
Families Citing this family (165)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2001516361A (ja) * | 1997-03-18 | 2001-09-25 | スミスクライン・ビーチャム・コーポレイション | 新規カンナビノイド受容体作動薬 |
US6630507B1 (en) | 1998-04-21 | 2003-10-07 | The United States Of America As Represented By The Department Of Health And Human Services | Cannabinoids as antioxidants and neuroprotectants |
ATE247097T1 (de) * | 1998-05-04 | 2003-08-15 | Univ Connecticut | Analgetische und immunomodulierende cannabinoiden |
US7589220B2 (en) * | 1998-06-09 | 2009-09-15 | University Of Connecticut | Inhibitors of the anandamide transporter |
US7897598B2 (en) * | 1998-06-09 | 2011-03-01 | Alexandros Makriyannis | Inhibitors of the anandamide transporter |
US7161016B1 (en) | 1998-11-24 | 2007-01-09 | University Of Connecticut | Cannabimimetic lipid amides as useful medications |
US7276613B1 (en) | 1998-11-24 | 2007-10-02 | University Of Connecticut | Retro-anandamides, high affinity and stability cannabinoid receptor ligands |
FR2789079B3 (fr) * | 1999-02-01 | 2001-03-02 | Sanofi Synthelabo | Derive d'acide pyrazolecarboxylique, sa preparation, les compositions pharmaceutiques en contenant |
US8084467B2 (en) * | 1999-10-18 | 2011-12-27 | University Of Connecticut | Pyrazole derivatives as cannabinoid receptor antagonists |
US7393842B2 (en) * | 2001-08-31 | 2008-07-01 | University Of Connecticut | Pyrazole analogs acting on cannabinoid receptors |
US7741365B2 (en) * | 1999-10-18 | 2010-06-22 | University Of Connecticut | Peripheral cannabinoid receptor (CB2) selective ligands |
US6900236B1 (en) | 1999-10-18 | 2005-05-31 | University Of Connecticut | Cannabimimetic indole derivatives |
US7119108B1 (en) | 1999-10-18 | 2006-10-10 | University Of Connecticut | Pyrazole derivatives as cannabinoid receptor antagonists |
US6943266B1 (en) * | 1999-10-18 | 2005-09-13 | University Of Connecticut | Bicyclic cannabinoid agonists for the cannabinoid receptor |
MXPA02005103A (es) | 1999-10-18 | 2003-09-25 | Alexipharma Inc | Ligandos selectivos del receptor de canabinoide (cb2) perifericos. |
FR2800375B1 (fr) | 1999-11-03 | 2004-07-23 | Sanofi Synthelabo | Derives tricycliques d'acide pyrazolecarboxylique, leur preparation, les compositions pharmaceutiques en contenant |
EP1294411A4 (en) * | 2000-05-23 | 2006-02-01 | Univ California | NEW TREATMENT AGAINST COUGH |
US20020091114A1 (en) | 2000-10-04 | 2002-07-11 | Odile Piot-Grosjean | Combination of a CB1 receptor antagonist and of sibutramine, the pharmaceutical compositions comprising them and their use in the treatment of obesity |
US8449908B2 (en) * | 2000-12-22 | 2013-05-28 | Alltranz, Llc | Transdermal delivery of cannabidiol |
EP1361876A4 (en) * | 2001-01-26 | 2004-03-31 | Univ Connecticut | NEW CANNABIMIMETIC LIGANDS |
US7173027B2 (en) | 2001-01-29 | 2007-02-06 | University Of Connecticut | Receptor selective cannabimimetic aminoalkylindoles |
CA2452881C (en) * | 2001-07-13 | 2012-03-06 | University Of Connecticut | Novel bicyclic and tricyclic cannabinoids |
AU2002319627A1 (en) * | 2001-07-20 | 2003-03-03 | Merck And Co., Inc. | Substituted imidazoles as cannabinoid receptor modulators |
JP2005510492A (ja) * | 2001-10-26 | 2005-04-21 | ユニバーシティ オブ コネチカット | 新規な種類の効力のあるカンナビミメティックリガンド |
US20040248956A1 (en) * | 2002-01-29 | 2004-12-09 | Hagmann William K | Substituted imidazoles as cannabinoid receptor modulators |
WO2003075917A1 (en) | 2002-03-08 | 2003-09-18 | Signal Pharmaceuticals, Inc. | Combination therapy for treating, preventing or managing proliferative disorders and cancers |
WO2003077847A2 (en) * | 2002-03-12 | 2003-09-25 | Merck & Co., Inc. | Substituted amides |
US7423067B2 (en) * | 2002-03-26 | 2008-09-09 | Merck & Co., Inc. | Diphenyl cyclopentyl amides as cannabinoid-1 receptor inverse agonists |
AU2003225964B2 (en) * | 2002-03-28 | 2008-11-20 | Merck Sharp & Dohme Corp. | Substituted 2,3-diphenyl pyridines |
WO2003087037A1 (en) * | 2002-04-05 | 2003-10-23 | Merck & Co., Inc. | Substituted aryl amides |
JP4459629B2 (ja) * | 2002-04-12 | 2010-04-28 | メルク エンド カムパニー インコーポレーテッド | 二環式アミド |
US6825209B2 (en) | 2002-04-15 | 2004-11-30 | Research Triangle Institute | Compounds having unique CB1 receptor binding selectivity and methods for their production and use |
US7105526B2 (en) | 2002-06-28 | 2006-09-12 | Banyu Pharmaceuticals Co., Ltd. | Benzimidazole derivatives |
KR100741231B1 (ko) | 2002-07-29 | 2007-07-19 | 에프. 호프만-라 로슈 아게 | 신규 벤조다이옥솔 |
JP4667867B2 (ja) * | 2002-08-02 | 2011-04-13 | メルク・シャープ・エンド・ドーム・コーポレイション | 置換フロ[2,3−b]ピリジン誘導体 |
CA2496097A1 (en) | 2002-08-23 | 2004-03-04 | University Of Connecticut | Keto cannabinoids with therapeutic indications |
US7765162B2 (en) * | 2002-10-07 | 2010-07-27 | Mastercard International Incorporated | Method and system for conducting off-line and on-line pre-authorized payment transactions |
SE0203070D0 (en) | 2002-10-16 | 2002-10-16 | Astrazeneca Ab | Novel compounds |
EP1556373A1 (en) * | 2002-10-18 | 2005-07-27 | Pfizer Products Inc. | Cannabinoid receptor ligands and uses thereof |
ITMI20022228A1 (it) * | 2002-10-21 | 2004-04-22 | Dinamite Dipharma S P A | Sali di clopidogrel con acidi alchil-solforici. |
US7129239B2 (en) * | 2002-10-28 | 2006-10-31 | Pfizer Inc. | Purine compounds and uses thereof |
US7247628B2 (en) * | 2002-12-12 | 2007-07-24 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
WO2004060870A1 (en) * | 2003-01-02 | 2004-07-22 | F. Hoffmann-La Roche Ag | Novel cb 1 receptour inverse agonists |
ATE400571T1 (de) | 2003-01-02 | 2008-07-15 | Hoffmann La Roche | Pyrrolyl-thiazole und ihre verwendung als inverse agonisten des cb 1 rezeptors |
US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
US7329658B2 (en) * | 2003-02-06 | 2008-02-12 | Pfizer Inc | Cannabinoid receptor ligands and uses thereof |
US7176210B2 (en) * | 2003-02-10 | 2007-02-13 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
US7145012B2 (en) | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
US20040214856A1 (en) * | 2003-04-23 | 2004-10-28 | Pfizer Inc | Cannabinoid receptor ligands and uses thereof |
US7141669B2 (en) * | 2003-04-23 | 2006-11-28 | Pfizer Inc. | Cannabiniod receptor ligands and uses thereof |
US7268133B2 (en) * | 2003-04-23 | 2007-09-11 | Pfizer, Inc. Patent Department | Cannabinoid receptor ligands and uses thereof |
US7232823B2 (en) | 2003-06-09 | 2007-06-19 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
US20040259887A1 (en) * | 2003-06-18 | 2004-12-23 | Pfizer Inc | Cannabinoid receptor ligands and uses thereof |
CA2528785A1 (en) | 2003-06-20 | 2005-01-06 | Matthias Heinrich Nettekoven | 2-amidobenzothiazoles as cb1 receptor inverse agonists |
FR2856683A1 (fr) * | 2003-06-25 | 2004-12-31 | Sanofi Synthelabo | Derives de 4-cyanopyrazole-3-carboxamide, leur preparation et leur application en therapeutique |
JP2007527389A (ja) * | 2003-06-30 | 2007-09-27 | メルク エンド カムパニー インコーポレーテッド | 放射性カンナビノイド−1受容体修飾因子 |
US20050026983A1 (en) * | 2003-07-30 | 2005-02-03 | Pfizer Inc | Imidazole compounds and uses thereof |
ATE547404T1 (de) | 2003-09-22 | 2012-03-15 | Msd Kk | Piperidinderivate |
AU2004299198A1 (en) | 2003-12-08 | 2005-06-30 | F. Hoffmann-La Roche Ag | Novel thiazole derivates |
TW200522944A (en) * | 2003-12-23 | 2005-07-16 | Lilly Co Eli | CB1 modulator compounds |
CA2553970A1 (en) | 2004-01-28 | 2005-08-18 | F. Hoffmann-La Roche Ag | Spiro-benzodioxoles and their use as cb1 antagonists |
CN1938286A (zh) | 2004-03-29 | 2007-03-28 | 默克公司 | 作为11-β-羟甾类脱氢酶-1抑制剂的二芳基三唑 |
US20080125403A1 (en) | 2004-04-02 | 2008-05-29 | Merck & Co., Inc. | Method of Treating Men with Metabolic and Anthropometric Disorders |
BRPI0510679A (pt) | 2004-05-10 | 2007-12-26 | Hoffmann La Roche | compostos, processo para a sua manufatura, composições farmacêuticas que os contêm, método para o tratamento e/ou profilaxia de enfermidades que estão associadas com a modulação dos receptores de cb1 e utilização desses compostos |
ITMI20041032A1 (it) * | 2004-05-24 | 2004-08-24 | Neuroscienze S C A R L | Compositi farmaceutici |
ITMI20041033A1 (it) * | 2004-05-24 | 2004-08-24 | Neuroscienze S C A R L | Composti farmaceutici |
WO2006025069A2 (en) | 2004-07-12 | 2006-03-09 | Cadila Healthcare Limited | Tricyclic pyrazole derivatives as cannabinoid receptor modulators |
US20060025448A1 (en) | 2004-07-22 | 2006-02-02 | Cadila Healthcare Limited | Hair growth stimulators |
CA2575736A1 (en) | 2004-08-06 | 2006-02-16 | Merck & Co., Inc. | Sulfonyl compounds as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1 |
FR2874012B1 (fr) | 2004-08-09 | 2008-08-22 | Sanofi Synthelabo | Derives de pyrrole, leur preparation et leur utlisation en therapeutique |
AU2005272627A1 (en) * | 2004-08-13 | 2006-02-23 | Amgen Inc. | Substituted benzofused heterocycles |
EP1807070A1 (en) * | 2004-09-29 | 2007-07-18 | Schering Corporation | Combinations of substituted azetidinones and cb1 antagonists |
ATE399156T1 (de) | 2004-10-27 | 2008-07-15 | Hoffmann La Roche | Neue indol- oder benzimidazol-derivate |
US8394765B2 (en) * | 2004-11-01 | 2013-03-12 | Amylin Pharmaceuticals Llc | Methods of treating obesity with two different anti-obesity agents |
WO2006052608A2 (en) | 2004-11-01 | 2006-05-18 | Amylin Pharmaceuticals, Inc. | Treatment of obesity and related disorders |
AU2005304039A1 (en) | 2004-11-09 | 2006-05-18 | F. Hoffmann-La Roche Ag | Dibenzosuberone derivatives |
WO2006067443A1 (en) * | 2004-12-23 | 2006-06-29 | Astrazeneca Ab | Therapeutic agents |
EP1833802A2 (en) * | 2004-12-23 | 2007-09-19 | AstraZeneca AB | 1,2-diphenyl-imidazole derivatives and their use as cb1 receptor ligands |
US8853205B2 (en) | 2005-01-10 | 2014-10-07 | University Of Connecticut | Heteropyrrole analogs acting on cannabinoid receptors |
DK1868999T3 (da) * | 2005-04-06 | 2009-08-17 | Hoffmann La Roche | Pyridin-3-carboxamidderivater som omvendte CB1-agonister |
US7737155B2 (en) | 2005-05-17 | 2010-06-15 | Schering Corporation | Nitrogen-containing heterocyclic compounds and methods of use thereof |
US20060278280A1 (en) * | 2005-05-23 | 2006-12-14 | Tzai-Jen Yang | Check valve |
WO2006129193A2 (en) * | 2005-05-27 | 2006-12-07 | Pfizer Products Inc. | Combination of a cannabinoid-1- receptor-antagonist and a microsomal triglyceride transfer protein inhibitor for treating obesity or mainataining weight loss |
US8138206B2 (en) | 2005-05-30 | 2012-03-20 | Msd. K.K. | Piperidine derivative |
US7923465B2 (en) * | 2005-06-02 | 2011-04-12 | Glenmark Pharmaceuticals S.A. | Cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation |
KR100970055B1 (ko) * | 2005-06-22 | 2010-07-16 | 에프. 호프만-라 로슈 아게 | 6-(플루오로-벤조[1,3]디옥솔일)-모폴린-4-일-메탄온 및cb1 리간드로서 그의 용도 |
CA2518579A1 (en) * | 2005-08-05 | 2007-02-05 | University Technologies International Inc. | Method for appetite suppression |
WO2007018248A1 (ja) | 2005-08-10 | 2007-02-15 | Banyu Pharmaceutical Co., Ltd. | ピリドン化合物 |
AU2006279680B2 (en) | 2005-08-11 | 2012-12-06 | Amylin Pharmaceuticals, Llc | Hybrid polypeptides with selectable properties |
EP2330125A3 (en) | 2005-08-11 | 2012-12-12 | Amylin Pharmaceuticals, Inc. | Hybrid polypeptides with selectable properties |
US7875633B2 (en) | 2005-08-24 | 2011-01-25 | Banyu Pharmaceutical Co., Ltd. | Phenylpyridone derivative |
WO2007029847A1 (ja) | 2005-09-07 | 2007-03-15 | Banyu Pharmaceutical Co., Ltd. | 二環性芳香族置換ピリドン誘導体 |
JP4879988B2 (ja) | 2005-09-29 | 2012-02-22 | メルク・シャープ・エンド・ドーム・コーポレイション | メラノコルチン−4受容体モジュレーターとしてのアシル化スピロピペリジン誘導体 |
WO2007049798A1 (ja) | 2005-10-27 | 2007-05-03 | Banyu Pharmaceutical Co., Ltd. | 新規ベンゾオキサチイン誘導体 |
AU2006312557B2 (en) | 2005-11-10 | 2011-12-08 | Msd K.K. | Aza-substituted spiro derivative |
EP1801098A1 (en) | 2005-12-16 | 2007-06-27 | Merck Sante | 2-Adamantylurea derivatives as selective 11B-HSD1 inhibitors |
AU2007226673A1 (en) * | 2006-03-10 | 2007-09-20 | Jenrin Discovery | Cannabinoid receptor antagonists/inverse agonists useful for treating obesity |
US7629346B2 (en) * | 2006-06-19 | 2009-12-08 | Hoffmann-La Roche Inc. | Pyrazinecarboxamide derivatives as CB1 antagonists |
US7781593B2 (en) | 2006-09-14 | 2010-08-24 | Hoffmann-La Roche Inc. | 5-phenyl-nicotinamide derivatives |
EP2946778A1 (en) | 2006-09-22 | 2015-11-25 | Merck Sharp & Dohme Corp. | Method of treatment using fatty acid synthesis inhibitors |
AU2007301126A1 (en) | 2006-09-28 | 2008-04-03 | Banyu Pharmaceutical Co., Ltd. | Diaryl ketimine derivative |
US20080108643A1 (en) * | 2006-11-03 | 2008-05-08 | Forest Laboratories Holdings Limited | Method for treating autism |
JP5437812B2 (ja) | 2006-12-18 | 2014-03-12 | 7ティーエム ファーマ エイ/エス | Cb1受容体モジュレーター |
EP1935420A1 (en) | 2006-12-21 | 2008-06-25 | Merck Sante | 2-Adamantyl-butyramide derivatives as selective 11beta-HSD1 inhibitors |
JP5319518B2 (ja) | 2007-04-02 | 2013-10-16 | Msd株式会社 | インドールジオン誘導体 |
PE20090142A1 (es) * | 2007-04-11 | 2009-02-19 | Merck & Co Inc | Derivados de furo[2,3-b] piridina sustituidos como moduladores del receptor canabinoide-1 |
US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
WO2008151257A2 (en) | 2007-06-04 | 2008-12-11 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
EP2176208B1 (en) * | 2007-07-30 | 2015-01-21 | Zynerba Pharmaceuticals, Inc. | Prodrugs of cannabidiol, compositions comprising prodrugs of cannabidiol and methods of using the same |
US8133904B2 (en) * | 2007-09-07 | 2012-03-13 | Jenrin Discovery, Inc. | Cannabinoid receptor antagonists/inverse agonists useful for treating obesity |
US20100323955A1 (en) * | 2007-11-14 | 2010-12-23 | Amylin Pharmaceuticals, Inc. | Methods for treating obesity and obesity related diseases and disorders |
US8829043B2 (en) | 2008-02-08 | 2014-09-09 | Nektar Therapeutics | Oligome-cannabinoid conjugates |
US20090247619A1 (en) * | 2008-03-06 | 2009-10-01 | University Of Kentucky | Cannabinoid-Containing Compositions and Methods for Their Use |
US20110015181A1 (en) | 2008-03-06 | 2011-01-20 | Makoto Ando | Alkylaminopyridine derivative |
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EP2328910B1 (en) | 2008-06-04 | 2014-08-06 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
CA2727914A1 (en) | 2008-06-19 | 2009-12-23 | Banyu Pharmaceutical Co., Ltd. | Spirodiamine-diaryl ketoxime derivative technical field |
AU2009270833B2 (en) | 2008-07-16 | 2015-02-19 | Bausch Health Ireland Limited | Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders |
AU2009277736A1 (en) | 2008-07-30 | 2010-02-04 | Banyu Pharmaceutical Co., Ltd. | (5-membered)-(5-membered) or (5-membered)-(6-membered) fused ring cycloalkylamine derivative |
IT1390848B1 (it) * | 2008-07-31 | 2011-10-19 | Neuroscienze Pharmaness S C A R L | Composti farmaceutici |
EP2149370A1 (en) * | 2008-07-31 | 2010-02-03 | Neuroscienze Pharmaness S.C. A R.L. | Diazabicyclic compounds and microemulsions thereof |
CA2741125A1 (en) | 2008-10-22 | 2010-04-29 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
US8592457B2 (en) | 2008-10-30 | 2013-11-26 | Merck Sharp & Dohme Corp. | Isonicotinamide orexin receptor antagonists |
WO2010051206A1 (en) | 2008-10-31 | 2010-05-06 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
WO2010056717A1 (en) | 2008-11-17 | 2010-05-20 | Merck Sharp & Dohme Corp. | Substituted bicyclic amines for the treatment of diabetes |
EP2379547A1 (en) | 2008-12-16 | 2011-10-26 | Schering Corporation | Pyridopyrimidine derivatives and methods of use thereof |
EP2379562A1 (en) | 2008-12-16 | 2011-10-26 | Schering Corporation | Bicyclic pyranone derivatives as nicotinic acid receptor agonists |
WO2010079241A1 (es) | 2009-01-12 | 2010-07-15 | Fundacion Hospital Nacional De Paraplejicos Para La Investigacion Y La Integracion | Uso de antagonistas y/o agonistas inversos de los receptores cb1 para la preparación de medicamentos que incrementen la excitabilidad de las motoneuronas |
US10053444B2 (en) | 2009-02-19 | 2018-08-21 | University Of Connecticut | Cannabinergic nitrate esters and related analogs |
IT1394400B1 (it) | 2009-02-25 | 2012-06-15 | Neuroscienze Pharmaness S C Ar L | Composizioni farmaceutiche |
IT1395724B1 (it) | 2009-02-25 | 2012-10-19 | Neuroscienze Pharmaness S C A R L | Composti farmaceutici |
IT1394860B1 (it) | 2009-07-22 | 2012-07-20 | Kemotech S R L | Composti farmaceutici |
US20120220567A1 (en) | 2009-07-23 | 2012-08-30 | Shipps Jr Gerald W | Benzo-fused oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors |
WO2011011506A1 (en) | 2009-07-23 | 2011-01-27 | Schering Corporation | Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors |
JP2013510834A (ja) | 2009-11-16 | 2013-03-28 | メリテク | [1,5]‐ジアゾシン誘導体 |
IT1396951B1 (it) * | 2009-12-18 | 2012-12-20 | Neuroscienze Pharmaness S C A R L | Composti farmaceutici |
EP2521721B1 (en) * | 2009-12-30 | 2014-10-01 | Shanghai Fochon Pharmaceutical Co. Ltd | 3-(3-aminopiperidin-1-yl)-5-oxo-1,2,4-triazine derivates as dipeptidyl peptidase iv(dpp-iv) inhibitors |
CA2786314A1 (en) | 2010-02-25 | 2011-09-01 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
US8785634B2 (en) | 2010-04-26 | 2014-07-22 | Merck Sharp & Dohme Corp | Spiropiperidine prolylcarboxypeptidase inhibitors |
US9365539B2 (en) | 2010-05-11 | 2016-06-14 | Merck Sharp & Dohme Corp. | Prolylcarboxypeptidase inhibitors |
WO2011156246A1 (en) | 2010-06-11 | 2011-12-15 | Merck Sharp & Dohme Corp. | Novel prolylcarboxypeptidase inhibitors |
US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
US8410107B2 (en) | 2010-10-15 | 2013-04-02 | Hoffmann-La Roche Inc. | N-pyridin-3-yl or N-pyrazin-2-yl carboxamides |
US8669254B2 (en) | 2010-12-15 | 2014-03-11 | Hoffman-La Roche Inc. | Pyridine, pyridazine, pyrimidine or pyrazine carboxamides as HDL-cholesterol raising agents |
PE20140859A1 (es) | 2011-02-25 | 2014-07-25 | Merck Sharp & Dohme | Novedosos derivados de azabencimidazol ciclico utiles como agentes antidiabeticos |
AR088352A1 (es) | 2011-10-19 | 2014-05-28 | Merck Sharp & Dohme | Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina |
BR112015002080A2 (pt) | 2012-08-02 | 2017-07-04 | Merck Sharp & Dohme | composto, composição farmacêutica, uso de um composto, e, método de tratamento ou de prevenção de um transtorno, de uma condição ou de uma doença |
EP2958562A4 (en) | 2013-02-22 | 2016-08-10 | Merck Sharp & Dohme | BICYCLIC ANTIDIABETIC COMPOUNDS |
US9650375B2 (en) | 2013-03-14 | 2017-05-16 | Merck Sharp & Dohme Corp. | Indole derivatives useful as anti-diabetic agents |
CA2905438A1 (en) | 2013-03-15 | 2014-09-25 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase and their uses |
EP2968439A2 (en) | 2013-03-15 | 2016-01-20 | Synergy Pharmaceuticals Inc. | Compositions useful for the treatment of gastrointestinal disorders |
EP2789619A1 (en) | 2013-04-12 | 2014-10-15 | Kemotech S.r.l. | Pharmaceutical compounds wiht angiogenesis inbhibitory activity |
US10011637B2 (en) | 2013-06-05 | 2018-07-03 | Synergy Pharmaceuticals, Inc. | Ultra-pure agonists of guanylate cyclase C, method of making and using same |
WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
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WO2017100558A1 (en) | 2015-12-09 | 2017-06-15 | Research Triangle Institute | Improved apelin receptor (apj) agonists and uses thereof |
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CA3125847A1 (en) | 2020-07-27 | 2022-01-27 | Makscientific, Llc | Process for making biologically active compounds and intermediates thereof |
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Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3449350A (en) * | 1968-06-24 | 1969-06-10 | Ciba Geigy Corp | Certain pyrazole-3-carboxylic acid hydrazide derivatives |
FR2665898B1 (fr) * | 1990-08-20 | 1994-03-11 | Sanofi | Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
FR2713225B1 (fr) * | 1993-12-02 | 1996-03-01 | Sanofi Sa | N-pipéridino-3-pyrazolecarboxamide substitué. |
FR2692575B1 (fr) * | 1992-06-23 | 1995-06-30 | Sanofi Elf | Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
FR2711140B1 (fr) * | 1993-10-12 | 1996-01-05 | Sanofi Sa | 1-Naphtylpyrazole-3-carboxamides substitués actifs sur la neurotensine, leur préparation, les compositions pharmaceutiques en contenant. |
FR2714057B1 (fr) * | 1993-12-17 | 1996-03-08 | Sanofi Elf | Nouveaux dérivés du 3-pyrazolecarboxamide, procédé pour leur préparation et compositions pharmaceutiques les contenant. |
-
1995
- 1995-11-23 FR FR9513956A patent/FR2741621B1/fr not_active Expired - Fee Related
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1996
- 1996-11-21 ES ES96939962T patent/ES2161382T3/es not_active Expired - Lifetime
- 1996-11-21 JP JP9519454A patent/JP2000500479A/ja active Pending
- 1996-11-21 US US09/068,869 patent/US6028084A/en not_active Expired - Lifetime
- 1996-11-21 DE DE69613860T patent/DE69613860T2/de not_active Expired - Lifetime
- 1996-11-21 AT AT96939962T patent/ATE203015T1/de not_active IP Right Cessation
- 1996-11-21 AU AU76985/96A patent/AU7698596A/en not_active Abandoned
- 1996-11-21 PT PT96939962T patent/PT876350E/pt unknown
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- 1996-11-21 EP EP96939962A patent/EP0876350B1/fr not_active Expired - Lifetime
- 1996-11-21 BR BR9611618A patent/BR9611618A/pt not_active Application Discontinuation
- 1996-11-21 WO PCT/FR1996/001847 patent/WO1997019063A1/fr active IP Right Grant
- 1996-11-21 DK DK96939962T patent/DK0876350T3/da active
-
1998
- 1998-05-15 MX MX9803891A patent/MX9803891A/es unknown
- 1998-05-22 NO NO19982330A patent/NO310508B1/no unknown
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Cited By (8)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2006501275A (ja) * | 2002-09-19 | 2006-01-12 | ソルベイ・フアーマシユーチカルズ・ベー・ブイ | カンナビノイド−cb1レセプターリガンドとしての1h−1,2,4−トリアゾール−3−カルボキシアミド誘導体 |
JP2007514638A (ja) * | 2003-06-26 | 2007-06-07 | サノフィ−アベンティス | ジフェニルピリジン誘導体、その製造法および治療用途 |
JP4669839B2 (ja) * | 2003-06-26 | 2011-04-13 | サノフィ−アベンティス | ジフェニルピリジン誘導体、その製造法および治療用途 |
JP2008526887A (ja) * | 2005-01-10 | 2008-07-24 | ユニバーシティ オブ コネチカット | カンナビノイド受容体に作用する新規なヘテロピロール類似体 |
JP2011506410A (ja) * | 2007-12-10 | 2011-03-03 | 7ティーエム ファーマ エイ/エス | カンナビノイド受容体モジュレーター |
JP2013500296A (ja) * | 2009-07-29 | 2013-01-07 | シーメンス アクティエンゲゼルシャフト | 活性成分および活性成分を検査するための方法 |
JP2014507425A (ja) * | 2011-09-30 | 2014-03-27 | ナショナル ヘルス リサーチ インスティテュートス | ピラゾール化合物 |
US8962845B2 (en) | 2011-09-30 | 2015-02-24 | National Health Research Institutes | Pyrazole compounds |
Also Published As
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---|---|
ES2161382T3 (es) | 2001-12-01 |
ATE203015T1 (de) | 2001-07-15 |
NO982330D0 (no) | 1998-05-22 |
GR3036830T3 (en) | 2002-01-31 |
PT876350E (pt) | 2001-12-28 |
DK0876350T3 (da) | 2001-11-05 |
DE69613860D1 (de) | 2001-08-16 |
EP0876350B1 (fr) | 2001-07-11 |
CA2238430C (en) | 2006-05-09 |
NO982330L (no) | 1998-05-22 |
US6028084A (en) | 2000-02-22 |
DE69613860T2 (de) | 2002-04-04 |
EP0876350A1 (fr) | 1998-11-11 |
FR2741621A1 (fr) | 1997-05-30 |
BR9611618A (pt) | 1999-03-30 |
FR2741621B1 (fr) | 1998-02-13 |
CA2238430A1 (en) | 1997-05-29 |
NO310508B1 (no) | 2001-07-16 |
MX9803891A (es) | 1998-09-30 |
WO1997019063A1 (fr) | 1997-05-29 |
AU7698596A (en) | 1997-06-11 |
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