PE20110153A1 - Derivados de piridazina como inhibidores de smo - Google Patents
Derivados de piridazina como inhibidores de smoInfo
- Publication number
- PE20110153A1 PE20110153A1 PE2011000050A PE2011000050A PE20110153A1 PE 20110153 A1 PE20110153 A1 PE 20110153A1 PE 2011000050 A PE2011000050 A PE 2011000050A PE 2011000050 A PE2011000050 A PE 2011000050A PE 20110153 A1 PE20110153 A1 PE 20110153A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- methyl
- pyridazin
- propan
- tetrahydro
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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
- C07D237/20—Nitrogen atoms
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/02—Heterocyclic 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
- C07D401/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic 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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Emergency Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE PIRIDAZINA DE FORMULA (I) DONDE R1 ES ARILO(C6-C14) O HETEROARILO DE 5 A 14 MIEMBROS OPCIONALMENTE SUSTITUIDO CON NH2, CN, OH, ENTRE OTROS; R2 Y R3 SON CADA UNO ALQUILO(C1-C8), ALQUILO(C1-C8)-OH O R2 Y R3 FORMAN UN CICLOALQUILO(C3-C14); L ES UN ENLACE, ALQUILENO(C1-C8), -C(O)O-, ALQUILO(C1-C8)-OH, ENTRE OTROS; X Y W SON CADA UNO N O CR5, EN DONDE R5 ES H, HALOGENO, CN, ENTRE OTROS; R7 ES ARILO(C6-C14), HETEROARILO DE 5 A 14 MIEMBROS O CICLOHETEROALQUILO DE 3 A 14 MIEMBROS; R4 ES ALQUILO(C1-C8), ALQUENILO(C2-C8), CICLOALQUILO(C3-C14), ENTRE OTROS; Z ES ALQUILO(C1-C8), CN, OH O HALOGENO; m Y p SON CADA UNO DE 0 A 3; Y ES UN ENLACE, ALQUILENO(C1-C8), -C(O)-, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-[(R)-4-(4,5-DIMETIL-6-FENOXI-PIRIDAZIN-3-IL)-2-METIL-3,4,5,6-TETRAHIDRO-2H-[1,2']-BIPIRAZINIL-5'-IL]-PROPAN-2-OL, 2-[(R)-4-(4,5-DIMETIL-6-PIRIDIN-4-IL-METIL-PIRIDAZIN-3-IL)-2-METIL-3,4,5,6-TETRAHIDRO-2H-[1,2']-BIPIRAZINIL-5'-IL]-PROPAN-2-OL, 2-[(R)-4-(6-BENCIL-4,5-DIMETIL-PIRIDAZIN-3-IL)-2-METIL-3,4,5,6-TETRAHIDRO-2H-[1,2']-BIPIRAZINIL-5'-IL]-PROPAN-2-OL, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE SMOOTHENED (SMO) SIENDO UTILES EN EL TRATAMIENTO DE TUMOR, CANCER, NEOPLASIA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8190008P | 2008-07-18 | 2008-07-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20110153A1 true PE20110153A1 (es) | 2011-03-14 |
Family
ID=41130287
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011000050A PE20110153A1 (es) | 2008-07-18 | 2009-07-16 | Derivados de piridazina como inhibidores de smo |
Country Status (44)
Families Citing this family (45)
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| TWI433674B (zh) | 2006-12-28 | 2014-04-11 | Infinity Discovery Inc | 環杷明（ｃｙｃｌｏｐａｍｉｎｅ）類似物類 |
| BRPI0911618A2 (pt) | 2008-04-29 | 2019-09-24 | Lilly Co Eli | antagonistas da via hedgehog de ftalazina dissubstituída. |
| US20100041663A1 (en) * | 2008-07-18 | 2010-02-18 | Novartis Ag | Organic Compounds as Smo Inhibitors |
| US8536176B2 (en) * | 2008-08-01 | 2013-09-17 | Nippon Chemiphar Co., Ltd. | GPR119 agonist |
| CA2738868C (en) * | 2008-10-01 | 2017-01-17 | Novartis Ag | Smoothened antagonism for the treatment of hedgehog pathway-related disorders |
| CN102202737B (zh) | 2008-11-03 | 2014-03-26 | 伊莱利利公司 | 二取代的2,3-二氮杂萘hedgehog通路拮抗剂 |
| MX2011005176A (es) | 2008-11-17 | 2011-05-30 | Lilly Co Eli | Antagonistas de la trayectoria hedgehog de piridazinas tetrasustituidas. |
| JP5518887B2 (ja) | 2008-11-17 | 2014-06-11 | イーライ リリー アンド カンパニー | 四置換ピリダジンヘッジホッグ経路アンタゴニスト |
| AR077014A1 (es) | 2009-06-19 | 2011-07-27 | Lilly Co Eli | Compuesto derivado de ftalazina 1,4-disustituida, composicion farmaceutica que lo comprende y uso para preparar un medicamento util para el tratamiento de cancer |
| WO2011062939A1 (en) * | 2009-11-18 | 2011-05-26 | Novartis Ag | Methods and compositions for treating solid tumors and other malignancies |
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| AR080908A1 (es) | 2010-04-16 | 2012-05-16 | Novartis Ag | Formulaciones de un piridazin -bipirazinilo |
| NZ603876A (en) | 2010-05-13 | 2015-02-27 | Amgen Inc | Nitrogen heterocyclic compounds useful as pde10 inhibitors |
| EP2511273B8 (en) * | 2011-04-15 | 2019-06-26 | Hivih | Inhibitors of viral replication, their process of preparation and their therapeutical uses |
| AU2012262961A1 (en) | 2011-06-02 | 2013-11-28 | Novartis Ag | Biomarkers for hedgehog inhibitor therapy |
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| EP2821104A1 (en) | 2013-07-05 | 2015-01-07 | Laboratoire Biodim | Inhibitors of viral replication, their process of preparation and their therapeutical uses |
| JP6783663B2 (ja) * | 2014-01-06 | 2020-11-11 | ライゼン・ファーマシューティカルズ・エスアー | 新規グルタミナーゼ阻害剤 |
| JOP20200094A1 (ar) | 2014-01-24 | 2017-06-16 | Dana Farber Cancer Inst Inc | جزيئات جسم مضاد لـ pd-1 واستخداماتها |
| JOP20200096A1 (ar) | 2014-01-31 | 2017-06-16 | Children’S Medical Center Corp | جزيئات جسم مضاد لـ tim-3 واستخداماتها |
| HUE048531T2 (hu) | 2014-03-14 | 2020-07-28 | Novartis Ag | Antitest molekulák a LAG-3-hoz és ezek felhasználása |
| MA41044A (fr) | 2014-10-08 | 2017-08-15 | Novartis Ag | Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer |
| TN2017000129A1 (en) | 2014-10-14 | 2018-10-19 | Dana Farber Cancer Inst Inc | Antibody molecules to pd-l1 and uses thereof |
| US20170340733A1 (en) | 2014-12-19 | 2017-11-30 | Novartis Ag | Combination therapies |
| KR20170129802A (ko) | 2015-03-10 | 2017-11-27 | 아두로 바이오테크, 인코포레이티드 | ＂인터페론 유전자의 자극인자＂-의존적 신호전달을 활성화하는 조성물 및 방법 |
| AU2016271468B2 (en) | 2015-06-04 | 2020-01-02 | Sol-Gel Technologies Ltd. | Topical formulations for delivery of hedgehog inhibitor compounds and use thereof |
| JP6878405B2 (ja) | 2015-07-29 | 2021-05-26 | ノバルティス アーゲー | Ｐｄ−１に対する抗体分子を含む組み合わせ治療 |
| WO2017019897A1 (en) | 2015-07-29 | 2017-02-02 | Novartis Ag | Combination therapies comprising antibody molecules to tim-3 |
| US20180340025A1 (en) | 2015-07-29 | 2018-11-29 | Novartis Ag | Combination therapies comprising antibody molecules to lag-3 |
| WO2017079112A1 (en) | 2015-11-03 | 2017-05-11 | Janssen Biotech, Inc. | Antibodies specifically binding pd-1 and their uses |
| JP2019503349A (ja) | 2015-12-17 | 2019-02-07 | ノバルティス アーゲー | Ｐｄ−１に対する抗体分子およびその使用 |
| BR112018076441A2 (pt) * | 2016-06-23 | 2019-04-09 | St. Jude Children´S Research Hospital | moduladores de molécula pequena de pantotenato quinases |
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| EP3642240A1 (en) | 2017-06-22 | 2020-04-29 | Novartis AG | Antibody molecules to cd73 and uses thereof |
| JP7352565B2 (ja) | 2017-12-27 | 2023-09-28 | セント ジュード チルドレンズ リサーチ ホスピタル，インコーポレイティド | パントテン酸キナーゼの小分子モジュレーター |
| AU2018397486A1 (en) | 2017-12-27 | 2020-08-13 | Coa Therapeutics, Inc. | Methods of treating disorders associated with castor |
| UY38247A (es) | 2018-05-30 | 2019-12-31 | Novartis Ag | Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación |
| US20220348651A1 (en) | 2019-09-18 | 2022-11-03 | Novartis Ag | Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies |
| CN114042069A (zh) * | 2021-10-22 | 2022-02-15 | 陕西国际商贸学院 | 一种5-取代哒嗪-4-胺衍生物、制备方法和用途 |
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