AR040629A1 - Derivados de hidrazono-malonitrilo, los medicamentos que los contienen, uso para la preparacion de un medicamento, un conjunto de elementos (kit) que los comprende, un procedimiento para la preparacion, los intermediarios utiles en dicho procedimiento, y las combinaciones de uno de dichos derivados - Google Patents
Derivados de hidrazono-malonitrilo, los medicamentos que los contienen, uso para la preparacion de un medicamento, un conjunto de elementos (kit) que los comprende, un procedimiento para la preparacion, los intermediarios utiles en dicho procedimiento, y las combinaciones de uno de dichos derivadosInfo
- Publication number
- AR040629A1 AR040629A1 AR20020104169A ARP020104169A AR040629A1 AR 040629 A1 AR040629 A1 AR 040629A1 AR 20020104169 A AR20020104169 A AR 20020104169A AR P020104169 A ARP020104169 A AR P020104169A AR 040629 A1 AR040629 A1 AR 040629A1
- Authority
- AR
- Argentina
- Prior art keywords
- derivatives
- formula
- procedure
- preparation
- compounds
- Prior art date
Links
Classifications
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
-
- 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
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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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
-
- 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
- A61P27/16—Otologicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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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
- C07D237/04—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having less than three double bonds between ring members or between ring members and non-ring members
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Emergency Medicine (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
Abstract
Se describen derivados de hidrazono-malonitrilo de fórmula (1) donde R1, R2 son, en cada caso independientemente entre sí H, OH, OR5, -SR5, -SOR5, -SO2R5 o Hal, R1 y R2 también son juntos -OCH2O- u -OCH2CH2O-, R3, R3'son, de cada caso independientemente entre sí, H, R5, OH, OR5, NH2, NHR5, NAA', NHCOR5, NHCOOR5, Hal, COOH, COOR5, CONH2, CONHR5 o CONR5A', R4 es CN o un compuesto de fórmula (2), R5 es A o cicloalquilo C3-6,que puede estar sustituido por 1 a 5 átomos de F y/o Cl, o -(CH2)n -Ar, A, A' son, en cada caso independientemente entre sí, alquilo C1-10 o alquenilo C2-8, que puede estar sustituido por 1 a 5 átomos de F y/o Cl, A y A' también son juntos cicloalquilo o cicloalquileno C3-7, donde un grupo CH2 puede estar reemplazado por O, NH, NA, NCOA o NCOOA, Ar es fenilo, n es 0, 1 ó 2, Hal es F, Cl, Br o I y sus derivados, solvatos y estereoisómeros de uso farmacéutico, incluyendo las mezclas de los mismos en todas las proporciones. Estos compuestos muestran una inhibición selectiva de la fosfodiesterasa IV, la cual está asociada a un incremento intracelular en el AMPc. Asimismo se describen los medicamentos que contienen los compuestos de fórmula (1) y el uso de estos últimos para la preparación de un medicamento destinado al tratamiento de osteoporosis, tumores, caquexia, aterosclerosis, artritis reumatoidea, esclerosis múltiple, diabetes mellitus, procesos inflamatorios, alergias, asma, enfermedades autoinmunes, enfermedades miocárdicas y SIDA. También se describe un procedimiento para preparar los compuestos de fórmula (1), los intermediarios útiles en la preparación de dichos compuestos de fórmula (1), las combinaciones de estos últimos con otros agentes terapéuticos, así como un conjunto de elementos (Kit) que consiste en envases separados de (a) una cantidad efectiva de un compuesto de fórmula (1) y/o sus derivados, solvatos y estereoisómeros de uso farmacéutico, incluyendo las mezclas de los mismos en todas las proporciones, y (b) una cantidad efectiva de otro ingrediente activo medicamentoso.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01125455 | 2001-11-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR040629A1 true AR040629A1 (es) | 2005-04-13 |
Family
ID=8179075
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AR20020104169A AR040629A1 (es) | 2001-11-05 | 2002-11-01 | Derivados de hidrazono-malonitrilo, los medicamentos que los contienen, uso para la preparacion de un medicamento, un conjunto de elementos (kit) que los comprende, un procedimiento para la preparacion, los intermediarios utiles en dicho procedimiento, y las combinaciones de uno de dichos derivados |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US7141572B2 (es) |
| EP (1) | EP1441730B1 (es) |
| JP (1) | JP5116940B2 (es) |
| KR (1) | KR100898894B1 (es) |
| CN (1) | CN1585641A (es) |
| AR (1) | AR040629A1 (es) |
| AT (1) | ATE335486T1 (es) |
| AU (1) | AU2002363368B2 (es) |
| BR (1) | BR0213683A (es) |
| CA (1) | CA2465746C (es) |
| DE (1) | DE60213841T2 (es) |
| ES (1) | ES2268157T3 (es) |
| HU (1) | HUP0401747A3 (es) |
| MX (1) | MXPA04004263A (es) |
| MY (1) | MY129491A (es) |
| PL (1) | PL369738A1 (es) |
| RU (1) | RU2302412C2 (es) |
| WO (1) | WO2003039548A1 (es) |
| ZA (1) | ZA200404387B (es) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA82323C2 (uk) * | 2002-08-09 | 2008-04-10 | Меда Фарма Гмбх & Ко. Кг | Нова комбінація глюкокортикоїду та pde-інгібітору для лікування респіраторних захворювань, алергічних захворювань, астми та хронічних обструктивних легеневих захворювань |
| EP2181704B1 (en) | 2002-12-30 | 2015-05-06 | Angiotech International Ag | Drug delivery from rapid gelling polymer composition |
| WO2004067006A1 (en) * | 2003-01-27 | 2004-08-12 | Pharmacia Corporation | Combination of a pde iv inhibitor and a tnf-alpha antagonist |
| WO2004087641A1 (ja) * | 2003-03-31 | 2004-10-14 | Daiichi Pharmaceutical Co., Ltd. | ヒドラゾン誘導体 |
| AR049384A1 (es) * | 2004-05-24 | 2006-07-26 | Glaxo Group Ltd | Derivados de purina |
| JP2008536888A (ja) * | 2005-04-19 | 2008-09-11 | ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング | 肺高血圧症の治療のためのロフルミラスト |
| GB0514809D0 (en) | 2005-07-19 | 2005-08-24 | Glaxo Group Ltd | Compounds |
| KR101054325B1 (ko) | 2006-03-31 | 2011-08-04 | 얀센 파마슈티카 엔.브이. | 히스타민 ｈ４ 수용체 조절제로서의 벤조이미다졸―２―일 피리미딘 및 피라진 |
| US9371311B2 (en) | 2008-06-30 | 2016-06-21 | Janssen Pharmaceutica Nv | Benzoimidazol-2-yl pyrimidine derivatives |
| WO2011041584A2 (en) | 2009-09-30 | 2011-04-07 | President And Fellows Of Harvard College | Methods for modulation of autophagy through the modulation of autophagy-enhancing gene products |
| WO2011163231A2 (en) * | 2010-06-21 | 2011-12-29 | Theracos, Inc. | Combination therapy for the treatment of diabetes |
| US9446131B2 (en) | 2013-01-31 | 2016-09-20 | Merz Pharmaceuticals, Llc | Topical compositions and methods for making and using same |
| US9433680B2 (en) | 2013-01-31 | 2016-09-06 | Merz Pharmaceuticals, Llc | Topical compositions and methods for making and using same |
| US9452173B2 (en) | 2013-01-31 | 2016-09-27 | Merz Pharmaceuticals, Llc | Topical compositions and methods for making and using same |
| US8778365B1 (en) | 2013-01-31 | 2014-07-15 | Merz Pharmaceuticals, Llc | Topical compositions and methods for making and using same |
| CN105121439A (zh) | 2013-02-19 | 2015-12-02 | 辉瑞公司 | 作为pde4亚型抑制剂用于治疗cns和其他病症的氮杂苯并咪唑化合物 |
| SG11201507117XA (en) | 2013-03-06 | 2015-10-29 | Janssen Pharmaceutica Nv | Benzoimidazol-2-yl pyrimidine modulators of the histamine h4 receptor |
| WO2015054359A1 (en) * | 2013-10-08 | 2015-04-16 | Ebadi Mark A | Methods and compositions for symptomatic reflief of the common cold |
| WO2016012896A1 (en) | 2014-07-24 | 2016-01-28 | Pfizer Inc. | Pyrazolopyrimidine compounds |
| HUE044040T2 (hu) | 2014-08-06 | 2019-09-30 | Pfizer | Imidazopiridazin vegyületek |
| US10500178B2 (en) | 2015-03-13 | 2019-12-10 | The Board Of Trustees Of The Leland Stanford Junior University | LTB4 inhibition to prevent and treat human lymphedema |
| US11116737B1 (en) | 2020-04-10 | 2021-09-14 | University Of Georgia Research Foundation, Inc. | Methods of using probenecid for treatment of coronavirus infections |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19632549A1 (de) * | 1996-08-13 | 1998-02-19 | Merck Patent Gmbh | Arylalkanoylpyridazine |
| DE19826841A1 (de) * | 1998-06-16 | 1999-12-23 | Merck Patent Gmbh | Arylalkanoylpyridazine |
| DE19850701A1 (de) * | 1998-11-04 | 2000-05-11 | Merck Patent Gmbh | Benzoylpyridazine |
| DE19932315A1 (de) * | 1999-07-10 | 2001-01-11 | Merck Patent Gmbh | Benzoylpyridazine |
-
2002
- 2002-10-10 BR BR0213683-0A patent/BR0213683A/pt not_active IP Right Cessation
- 2002-10-10 MX MXPA04004263A patent/MXPA04004263A/es active IP Right Grant
- 2002-10-10 HU HU0401747A patent/HUP0401747A3/hu unknown
- 2002-10-10 PL PL02369738A patent/PL369738A1/xx not_active Application Discontinuation
- 2002-10-10 RU RU2004117171/04A patent/RU2302412C2/ru not_active IP Right Cessation
- 2002-10-10 AT AT02802625T patent/ATE335486T1/de not_active IP Right Cessation
- 2002-10-10 CA CA2465746A patent/CA2465746C/en not_active Expired - Fee Related
- 2002-10-10 ES ES02802625T patent/ES2268157T3/es not_active Expired - Lifetime
- 2002-10-10 KR KR1020047006820A patent/KR100898894B1/ko not_active IP Right Cessation
- 2002-10-10 EP EP02802625A patent/EP1441730B1/en not_active Expired - Lifetime
- 2002-10-10 DE DE60213841T patent/DE60213841T2/de not_active Expired - Lifetime
- 2002-10-10 AU AU2002363368A patent/AU2002363368B2/en not_active Ceased
- 2002-10-10 US US10/494,631 patent/US7141572B2/en not_active Expired - Fee Related
- 2002-10-10 CN CNA028222164A patent/CN1585641A/zh active Pending
- 2002-10-10 WO PCT/EP2002/011351 patent/WO2003039548A1/en active IP Right Grant
- 2002-10-10 JP JP2003541839A patent/JP5116940B2/ja not_active Expired - Fee Related
- 2002-11-01 AR AR20020104169A patent/AR040629A1/es unknown
- 2002-11-01 MY MYPI20024107A patent/MY129491A/en unknown
-
2004
- 2004-06-03 ZA ZA200404387A patent/ZA200404387B/en unknown
-
2006
- 2006-08-02 US US11/497,235 patent/US7544684B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| HUP0401747A2 (hu) | 2005-01-28 |
| ES2268157T3 (es) | 2007-03-16 |
| KR20050035177A (ko) | 2005-04-15 |
| CA2465746A1 (en) | 2003-05-15 |
| EP1441730B1 (en) | 2006-08-09 |
| HUP0401747A3 (en) | 2005-06-28 |
| RU2004117171A (ru) | 2006-01-10 |
| WO2003039548A1 (en) | 2003-05-15 |
| ZA200404387B (en) | 2006-02-22 |
| CA2465746C (en) | 2011-09-06 |
| MXPA04004263A (es) | 2004-07-08 |
| BR0213683A (pt) | 2004-10-26 |
| AU2002363368B2 (en) | 2007-12-13 |
| ATE335486T1 (de) | 2006-09-15 |
| US20040261190A1 (en) | 2004-12-30 |
| US7544684B2 (en) | 2009-06-09 |
| US7141572B2 (en) | 2006-11-28 |
| EP1441730A1 (en) | 2004-08-04 |
| KR100898894B1 (ko) | 2009-05-21 |
| JP2005511595A (ja) | 2005-04-28 |
| JP5116940B2 (ja) | 2013-01-09 |
| CN1585641A (zh) | 2005-02-23 |
| MY129491A (en) | 2007-04-30 |
| AU2002363368B9 (en) | 2003-05-19 |
| DE60213841D1 (de) | 2006-09-21 |
| DE60213841T2 (de) | 2007-02-15 |
| RU2302412C2 (ru) | 2007-07-10 |
| US20060270676A1 (en) | 2006-11-30 |
| PL369738A1 (en) | 2005-05-02 |
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