PE20090482A1 - Derivados heterociclicos como antagonistas del receptor ccr2 - Google Patents
Derivados heterociclicos como antagonistas del receptor ccr2Info
- Publication number
- PE20090482A1 PE20090482A1 PE2008001195A PE2008001195A PE20090482A1 PE 20090482 A1 PE20090482 A1 PE 20090482A1 PE 2008001195 A PE2008001195 A PE 2008001195A PE 2008001195 A PE2008001195 A PE 2008001195A PE 20090482 A1 PE20090482 A1 PE 20090482A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- phenyl
- dichloro
- cycloalkyl
- antagonists
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title abstract 2
- 102000004497 CCR2 Receptors Human genes 0.000 title 1
- 108010017312 CCR2 Receptors Proteins 0.000 title 1
- -1 BENZYLOXY Chemical group 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102100024167 C-C chemokine receptor type 3 Human genes 0.000 abstract 1
- 101710149862 C-C chemokine receptor type 3 Proteins 0.000 abstract 1
- 102100035875 C-C chemokine receptor type 5 Human genes 0.000 abstract 1
- 101710149870 C-C chemokine receptor type 5 Proteins 0.000 abstract 1
- 208000031229 Cardiomyopathies Diseases 0.000 abstract 1
- 208000010496 Heart Arrest Diseases 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 230000003399 chemotactic effect Effects 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 208000037803 restenosis Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
- C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
-
- 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
-
- 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
-
- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/15—Six-membered rings
- C07D285/16—Thiadiazines; Hydrogenated thiadiazines
- C07D285/18—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines
-
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Immunology (AREA)
- Emergency Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS HETEROCICLICOS DE FORMULA (I) DONDE A ES ARILO TAL COMO FENILO O NAFTILO, O HETEROARILO DE 5 A 10 MIEMBROS OPCIONALMENTE SUSTITUIDOS CON HALOGENO, BENCILOXI, ALQUILO(C1-C6), ENTRE OTROS; X ES N(R1)(R2) O N+(R1)(R2)(R11), EN DONDE R1 Y R2 SON CADA UNO H, ALQUILO(C1-C6), ALQUENILO(C3-C6), CICLOALQUILO(C3-C7), ENTRE OTROS; R11 ES ALQUILO(C1-C6); R3 Y R4 SON CADA UNO H, OH, ALQUILO(C1-C6), ALCOXI(C1-C6), ENTRE OTROS; R5 Y R6 SON CADA UNO H, ALQUILO(C1-C6), CICLOALQUILO(C3-C7), ENTRE OTROS; R7, R8, R9 Y R10 SON CADA UNO H, ALQUILO(C1-C6) O CICLOALQUILO(C3-C7) OPCIONALMENTE SUSTITUIDOS CON OH, ALCOXI(C1-C6), CARBOXILO, ENTRE OTROS; Y ES C(O) O S(O)2; m Y n SON CADA UNO DE 0 A 3. SON COMPUESTOS PREFERIDOS: 4-[(E)-3-(3,4-DICLORO-FENIL)-ACRILOIL]-1-[3-((S)-2-HIDROXIMETIL-PIRROLIDIN-1-IL)-PROPIL]-PIPERAZIN-2-ONA, 4-[(E)-3-(3,4-DICLORO-FENIL)-ACRILOIL]-1-[3-((S)-2-HIDROXIMETIL-PIRROLIDIN-1-IL)-PROPIL]-3-METIL-PIPERAZIN-2-ONA, (E)-3-(3,4-DICLORO-FENIL)-1-[1,1-DIOXO-2-(3-PIPERIDIN-1-IL-PROPIL)-[1,2,5]TIADIAZINAN-5-IL]-PROPENONA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DE PROTEINA QUIMIOTACTICA MONOCITICA 1 (CCR2), CCR5 Y CCR3 SIENDO UTILES EN EL TRATAMIENTO DE PARO CARDIACO CONGESTIVO, CARDIOMIOPATIA, RESTENOSIS, NEFROPATIA DIABETICA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07112766 | 2007-07-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20090482A1 true PE20090482A1 (es) | 2009-05-09 |
Family
ID=39810251
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008001195A PE20090482A1 (es) | 2007-07-19 | 2008-07-16 | Derivados heterociclicos como antagonistas del receptor ccr2 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8063042B2 (es) |
| EP (1) | EP2220055A2 (es) |
| JP (1) | JP2010533672A (es) |
| KR (1) | KR20100033544A (es) |
| CN (1) | CN101754957A (es) |
| AR (1) | AR067574A1 (es) |
| AU (1) | AU2008277796A1 (es) |
| BR (1) | BRPI0814424A2 (es) |
| CA (1) | CA2695998A1 (es) |
| CL (1) | CL2008002093A1 (es) |
| PE (1) | PE20090482A1 (es) |
| RU (1) | RU2010105682A (es) |
| TW (1) | TW200911259A (es) |
| WO (1) | WO2009010429A2 (es) |
| ZA (1) | ZA201000353B (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7638541B2 (en) | 2006-12-28 | 2009-12-29 | Metabolex Inc. | 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
| JP5489997B2 (ja) | 2007-07-19 | 2014-05-14 | シマベイ セラピューティクス， インコーポレーテッド | 糖尿病および代謝疾患の治療のためのＲＵＰ３またはＧＰＲｌ１９受容体のアゴニストとしてのＮ−アザ環状置換ピロール、ピラゾール、イミダゾール、トリアゾールおよびテトラゾール誘導体 |
| EP2307387B1 (en) | 2008-07-16 | 2013-11-20 | F. Hoffmann-La Roche AG | Novel heterocyclyl compounds for treatment of cardiovascular disease |
| ES2497566T3 (es) | 2009-10-01 | 2014-09-23 | Cymabay Therapeutics, Inc. | Sales de tetrazol-1-il-fenoximetil-tiazol-2-il-piperidinil-pirimidina sustituida |
| US8471004B2 (en) * | 2009-10-07 | 2013-06-25 | Hoffman-La Roche Inc. | Bicyclic compounds |
| US8445674B2 (en) | 2009-10-21 | 2013-05-21 | Hoffmann-La Roche Inc | Heterocyclyl compounds |
| US8486967B2 (en) | 2010-02-17 | 2013-07-16 | Hoffmann-La Roche Inc. | Heteroaryl substituted piperidines |
| WO2011163090A1 (en) | 2010-06-23 | 2011-12-29 | Metabolex, Inc. | Compositions of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
| US10292983B2 (en) | 2016-08-03 | 2019-05-21 | Cymabay Therapeutics, Inc. | Oxymethylene aryl compounds for treating inflammatory gastrointestinal diseases or gastrointestinal conditions |
| JP2020508436A (ja) | 2016-12-07 | 2020-03-19 | プロジェニティ， インコーポレイテッド | 胃腸管の検出方法、装置およびシステム |
| WO2018112264A1 (en) | 2016-12-14 | 2018-06-21 | Progenity Inc. | Treatment of a disease of the gastrointestinal tract with a chemokine/chemokine receptor inhibitor |
| CN107098850A (zh) * | 2017-05-25 | 2017-08-29 | 西安近代化学研究所 | 一种合成1‑甲基‑3‑硝基‑4‑苯基‑2,6‑二哌啶酮的方法 |
| AU2019383976B2 (en) | 2018-11-19 | 2025-07-03 | Bt Bidco, Inc. | Methods and devices for treating a disease with biotherapeutics |
| WO2021119482A1 (en) | 2019-12-13 | 2021-06-17 | Progenity, Inc. | Ingestible device for delivery of therapeutic agent to the gastrointestinal tract |
| CN111423454B (zh) * | 2020-04-24 | 2021-06-22 | 苏州大学 | 哌嗪类化合物及其在制备趋化因子受体ccr2拮抗剂中的应用 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE637271A (es) * | 1963-04-04 | 1900-01-01 | ||
| GB1218591A (en) * | 1968-04-03 | 1971-01-06 | Delalande Sa | Derivatives of n-(3,4,5-trimethoxy cennamoyl) piperazine and their process of preparation |
| FR2522325B1 (fr) | 1982-02-26 | 1985-08-09 | Delalande Sa | Nouveaux derives aryliques de la piperazine, de l'homopiperazine et de n,n'-dialkyl diamino-1,2 ethane, leur procede de preparation et leur application en therapeutique |
| WO1999037304A1 (en) * | 1998-01-27 | 1999-07-29 | Aventis Pharmaceuticals Products Inc. | SUBSTITUTED OXOAZAHETEROCYCLYL FACTOR Xa INHIBITORS |
| WO2003024401A2 (en) * | 2001-09-18 | 2003-03-27 | Bristol-Myers Squibb Company | Piperizinones as modulators of chemokine receptor activity |
| US7977346B2 (en) | 2006-01-17 | 2011-07-12 | Guoqing Paul Chen | Spiro compounds and methods of use |
-
2008
- 2008-07-09 BR BRPI0814424-9A2A patent/BRPI0814424A2/pt not_active IP Right Cessation
- 2008-07-09 JP JP2010516461A patent/JP2010533672A/ja active Pending
- 2008-07-09 WO PCT/EP2008/058892 patent/WO2009010429A2/en not_active Ceased
- 2008-07-09 RU RU2010105682/04A patent/RU2010105682A/ru not_active Application Discontinuation
- 2008-07-09 EP EP08785999A patent/EP2220055A2/en not_active Withdrawn
- 2008-07-09 AU AU2008277796A patent/AU2008277796A1/en not_active Abandoned
- 2008-07-09 KR KR1020107003658A patent/KR20100033544A/ko not_active Ceased
- 2008-07-09 CN CN200880025246A patent/CN101754957A/zh active Pending
- 2008-07-09 CA CA2695998A patent/CA2695998A1/en not_active Abandoned
- 2008-07-10 US US12/170,495 patent/US8063042B2/en not_active Expired - Fee Related
- 2008-07-16 PE PE2008001195A patent/PE20090482A1/es not_active Application Discontinuation
- 2008-07-17 CL CL2008002093A patent/CL2008002093A1/es unknown
- 2008-07-17 AR ARP080103067A patent/AR067574A1/es unknown
- 2008-07-18 TW TW097127530A patent/TW200911259A/zh unknown
-
2010
- 2010-01-18 ZA ZA2010/00353A patent/ZA201000353B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2009010429A2 (en) | 2009-01-22 |
| US8063042B2 (en) | 2011-11-22 |
| CL2008002093A1 (es) | 2009-05-29 |
| RU2010105682A (ru) | 2011-08-27 |
| KR20100033544A (ko) | 2010-03-30 |
| CA2695998A1 (en) | 2009-01-22 |
| JP2010533672A (ja) | 2010-10-28 |
| TW200911259A (en) | 2009-03-16 |
| CN101754957A (zh) | 2010-06-23 |
| AR067574A1 (es) | 2009-10-14 |
| US20090023713A1 (en) | 2009-01-22 |
| BRPI0814424A2 (pt) | 2015-01-06 |
| AU2008277796A1 (en) | 2009-01-22 |
| EP2220055A2 (en) | 2010-08-25 |
| WO2009010429A3 (en) | 2009-04-30 |
| ZA201000353B (en) | 2013-06-26 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |