AR069513A1 - Derivados de amidas del acido 6,7-dihidro -5h-imidazo¿1,2-alfa]imidazol-3-carboxilico, y composiciones farmaceuticas que los contienen - Google Patents
Derivados de amidas del acido 6,7-dihidro -5h-imidazo¿1,2-alfa]imidazol-3-carboxilico, y composiciones farmaceuticas que los contienenInfo
- Publication number
- AR069513A1 AR069513A1 ARP080105226A ARP080105226A AR069513A1 AR 069513 A1 AR069513 A1 AR 069513A1 AR P080105226 A ARP080105226 A AR P080105226A AR P080105226 A ARP080105226 A AR P080105226A AR 069513 A1 AR069513 A1 AR 069513A1
- Authority
- AR
- Argentina
- Prior art keywords
- nr9r10
- optionally substituted
- alkyl
- halogen
- heteroaryl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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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
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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
- A61P11/06—Antiasthmatics
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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
- A61P11/16—Central respiratory analeptics
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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
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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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
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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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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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
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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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
- A61P37/02—Immunomodulators
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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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
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- 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
- A61P7/08—Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
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- 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
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- 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
Abstract
Exhiben buen efecto inhibidor tras la interaccion entre CAM y Leucointegrinas y, por consiguiente, son utiles en el tratamiento de enfermedades inflamatorias. Reivindicacion 1: Un compuesto caracterizado por tener la formula (1), en donde: R1 se selecciona de -CN, -OCF3, halogeno, heteroarilo, opcionalmente sustituido con halogeno o alquilo C1-3 opcionalmente sustituido con halogeno y fenilo, opcionalmente sustituido con halogeno; R2 se selecciona de: (A) H, (B) alquilo C1-3 opcionalmente sustituido con uno o dos grupos seleccionados de: a)cicloalquilo C3-6, b) -OR9, c) -NR9R10, d) -SOR9, e) -SO2R9, f) -C(O)NH2, g) heteroarilo opcionalmente sustituido con alquilo C1-2, h) heterociclilo, i) fenilo, j) -CO2R9, k) -OPO(OH)2, y l) -OSO2(OH); (C) cicloalquilo C3-6, (D) heteroarilo, y (E) fenilo, opcionalmente sustituido con halogeno, -OR9, -CN o -CF3; R3 es H o alquilo C1-3; o R2 y R3, junto con el carbono al que están unidos, forman un anillo hidrocarbonado saturado de 3 a 7 átomos de carbono y en donde un átomo de carbono en dicho anillo hidrocarbonado puede estar opcionalmente reemplazado por -O-, -S-, -S(O)-, -SO2-, -NC(O)R9- o -NR9-; R4 se selecciona de: (A) alquilo C1-5 opcionalmente sustituido con uno o dos grupos seleccionados de: a) -CF3, b) -C(O)OR9, c) -C(O)NR9R10, d) -C(S)NR9R10, e) -NR9R10, f) -N(R9)C(O)R10, g) -C(O)NH(CH2)2O(CH2)2OH, h)-OR9, i) fenilo opcionalmente sustituido con halogeno, -NR9R10, -OR9, cicloalquilo C3-5 o alquilo C1-5, en donde dicho alquilo C1-5 está opcionalmente sustituido con -F, -NR9R10 o -OR9; j) heteroarilo opcionalmente sustituido con halogeno, -NR9R10, -OR9, cicloalquilo C3-5 o alquilo C1-5, en donde dicho alquilo C1-5 está opcionalmente sustituido con -F, -NR9R10 o -OR9, k) -SO2NR9R10, l) -SO2R9, y m) -SO2Het, en donde Het se selecciona de heterociclilo y heteroarilo; (B) cicloalquilo C3-6 opcionalmente sustituido con uno o dos grupos seleccionados de: a) -C(O)OR9, b) -C(O)NR9R10, c) -C(S)NR9R10, d) -OR9, e) fenilo opcionalmente sustituido con halogeno, -NR9R10, -OR9, cicloalquilo C3-5 o alquilo C1-5, en donde dicho alquilo C1-5 está opcionalmente sustituido con -F, -CF3, -NR9R10 o -OR9, y f) heteroarilo opcionalmente sustituido con: 1) -NR9R10, 2) -NHC(O)R9, 3) -NHSO2R9, 4) -OR9, 5) -alquil C1-2-NR9R10, 6) -alquil C1-2-NR10(CO)NR9R10, 7) -alquil C1-2-NR10(CO)R9, 8) -alquil C1-2-OR9, 9) -alquil C1-2-NHSO2R9, 10) -CO2R9, 11) -COCH3, 12) halogeno, 13) -SO2R9, 14) -cicloalquilo C3-5, 15) -ciano y 16) alquilo C1-5, en donde dicho alquilo C1-5 está opcionalmente sustituido con halogeno, -CF3, -NR9R10 o -OR9; (C) heteroarilo opcionalmente sustituido con uno o dos grupos seleccionados de: a) -R9 opcionalmente sustituido con halogeno o -OH, b) -CF3, c) -OR9, d) -NR9R10, e) halogeno, f) -C(O)NR9R10, g) -C(O)NH(CH2)2OH, h) -alquil C1-3-NR9R10, (D) -alquilheterociclilo C0-5 en donde el heterociclo está opcionalmente sustituido con -C(O)CH3, oxo o -C1-3C(S)NH2, R5 se selecciona de H, alquilo C1-3, -(CH2)2OH y -(CH2)2OCH3; o R4 y R5 constituyen un puente hidrocarbonado saturado de 3 a 6 átomos de carbono que junto con el N al que están unidos forman un anillo heterocíclico, y en donde: a) uno o dos átomos de carbono en dicho anillo heterocíclico están mono o disustituidos con R8 y b) un átomo de carbono en dicho anillo heterocíclico está opcionalmente reemplazado con -O-, -S-, -S(O)-, -SO2- o -NC(O)CH3-; R6 es H o halogeno; R7 es halogeno o -CF3; R8 se selecciona entre alquilo C1-3, halogeno, -OH, -CH2OH, -C(O)R9, -SO2R9, -C(O)CH2CO2R9, -NR9R10, -C(O)NR9R10, -CN, -C(O)OR9, -N(R9)C(O)R10, heterociclilo y heteroarilo, en donde dichos heterociclilo y heteroarilo están opcionalmente sustituidos con alquilo C1-4, -OH o -CF3; R9 es H o alquilo C1-5 o cicloalquilo C3-4, en donde el alquilo C1-5 está opcionalmente sustituido con -OH; R10 es -H o -CH3; o R9 y R10 constituyen un puente hidrocarbonado saturado de 3 a 6 átomos de carbono que junto con el N al que están unidos forman un anillo heterocíclico, en donde un átomo de carbono en dicho anillo heterocíclico puede estar opcionalmente monosustituido con -OH o en donde un átomo de carbono en dicho anillo heterocíclico puede estar opcionalmente reemplazado con -O-, -S-, -SO-, -SO2, -NH-, -NCH3- o -NC(O)CH3-; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US99096007P | 2007-11-29 | 2007-11-29 | |
| US4795708P | 2008-04-25 | 2008-04-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR069513A1 true AR069513A1 (es) | 2010-01-27 |
Family
ID=40193954
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080105226A AR069513A1 (es) | 2007-11-29 | 2008-11-28 | Derivados de amidas del acido 6,7-dihidro -5h-imidazo¿1,2-alfa]imidazol-3-carboxilico, y composiciones farmaceuticas que los contienen |
Country Status (32)
| Country | Link |
|---|---|
| US (1) | US8552205B2 (es) |
| EP (1) | EP2225238B1 (es) |
| JP (1) | JP5485164B2 (es) |
| KR (1) | KR20100101095A (es) |
| CN (1) | CN101889011B (es) |
| AR (1) | AR069513A1 (es) |
| AU (1) | AU2008329909B2 (es) |
| BR (1) | BRPI0819831A2 (es) |
| CA (1) | CA2705583A1 (es) |
| CL (1) | CL2008003576A1 (es) |
| CO (1) | CO6210701A2 (es) |
| CY (1) | CY1115857T1 (es) |
| DK (1) | DK2225238T3 (es) |
| EA (1) | EA017688B1 (es) |
| EC (1) | ECSP10010196A (es) |
| ES (1) | ES2525237T3 (es) |
| HK (1) | HK1145683A1 (es) |
| HR (1) | HRP20141171T1 (es) |
| IL (1) | IL205189A (es) |
| MA (1) | MA31905B1 (es) |
| MX (1) | MX2010004995A (es) |
| MY (1) | MY151004A (es) |
| NZ (1) | NZ585640A (es) |
| PE (1) | PE20091427A1 (es) |
| PL (1) | PL2225238T3 (es) |
| PT (1) | PT2225238E (es) |
| RS (1) | RS53602B1 (es) |
| SI (1) | SI2225238T1 (es) |
| TN (1) | TN2010000240A1 (es) |
| TW (2) | TWI475990B (es) |
| UY (1) | UY31493A1 (es) |
| WO (1) | WO2009070485A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8481750B2 (en) | 2009-06-02 | 2013-07-09 | Boehringer Ingelheim International Gmbh | Derivatives of 6,7-dihydro-5H-imidazo[1,2-α]imidazole-3-carboxylic acid amides |
| MX2011012717A (es) * | 2009-06-02 | 2011-12-14 | Boehringer Ingelheim Int | Derivados de amidas del acido 6,7-dihidro-5h-imidazo[1,2-a]imidazo l-3-carboxilico. |
| IN2012DN03449A (es) | 2009-10-21 | 2015-10-23 | Boehringer Ingelheim Int | |
| US8912221B2 (en) * | 2010-12-27 | 2014-12-16 | Hoffmann-La Roche Inc. | Biaryl amide derivatives |
| CN103649059B (zh) * | 2011-04-27 | 2016-10-26 | 盐野义制药株式会社 | 具有npy y5受体拮抗作用的五元环芳香族杂环衍生物 |
| CN103874697A (zh) | 2011-08-03 | 2014-06-18 | 协和发酵麒麟株式会社 | 二苯并氧杂*衍生物 |
| RS54833B1 (sr) | 2011-10-03 | 2016-10-31 | Euroscreen Sa | Novi hiralni n-acil-5,6,7, (8-supstituisan)-tetrahidro-[1,2,4]triazolo [4,3-a]pirazini kao selektivni antagonisti nk-3 receptora, farmaceutsko jedinjenje, i postupci za upotrebu u nk-3 receptorom posredovanim poremećajima |
| WO2016058896A1 (en) | 2014-10-14 | 2016-04-21 | Syngenta Participations Ag | Process for the preparation of 1-(3,5-dichloro-4-fluoro-phenyl)-2,2,2-trifluoro-ethanone |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| CN106631827B (zh) * | 2016-12-30 | 2018-10-23 | 上海毕得医药科技有限公司 | 一种(1-环丙基-1-甲基)乙基胺及其盐酸盐的合成方法 |
| CN109369432B (zh) * | 2018-11-02 | 2021-06-25 | 永农生物科学有限公司 | (s)-4-氯-2-氨基丁酸酯的制备方法 |
| CR20220294A (es) | 2019-12-20 | 2022-08-03 | Bayer Ag | Tiofenocarboxamidas sustituidas y sus derivados |
| CN111848521A (zh) * | 2020-08-26 | 2020-10-30 | 韶远科技（上海)有限公司 | 一种2-取代-4-烷氧基咪唑化合物的制备方法 |
| WO2024013736A1 (en) * | 2022-07-12 | 2024-01-18 | Adama Makhteshim Ltd. | Process for preparing substituted benzamides |
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| WO2006014828A1 (en) | 2004-07-27 | 2006-02-09 | Boehringer Ingelheim International, Gmbh | Synthesis of 6,7-dihydro-5h-imidazo[1,2-a]imidazole-3-sulfonic acid amides |
| JP2008534685A (ja) | 2005-04-05 | 2008-08-28 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 炎症性疾患の治療に有用な置換ベンジルイミダゾール |
| US7589114B2 (en) | 2005-04-06 | 2009-09-15 | Boehringer Ingelheim International Gmbh | Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-azetidine-carboxylic acids, esters and amides |
| CN101166743A (zh) * | 2005-05-19 | 2008-04-23 | 贝林格尔·英格海姆国际有限公司 | 6,7-二氢-5H-咪唑并[1,2-α]咪唑-3-磺酸的衍生物 |
| TW200831488A (en) | 2006-11-29 | 2008-08-01 | Astrazeneca Ab | Novel compounds |
| EP2080758A3 (de) | 2007-11-29 | 2009-08-26 | Bayer CropScience AG | Halogen substituierte delta-1-Pyrroline |
| JP2009149609A (ja) | 2007-11-29 | 2009-07-09 | Sumitomo Chemical Co Ltd | アミド化合物及びその用途 |
| TW200936146A (en) | 2007-11-29 | 2009-09-01 | Metabasis Therapeutics Inc | Antiviral nucleoside compounds |
| RU2483072C2 (ru) | 2007-11-29 | 2013-05-27 | Актелион Фармасьютиклз Лтд | Производные фосфоновой кислоты и их применение в качестве антагонистов рецептора p2y12 |
| MX2011012717A (es) | 2009-06-02 | 2011-12-14 | Boehringer Ingelheim Int | Derivados de amidas del acido 6,7-dihidro-5h-imidazo[1,2-a]imidazo l-3-carboxilico. |
| US8481750B2 (en) | 2009-06-02 | 2013-07-09 | Boehringer Ingelheim International Gmbh | Derivatives of 6,7-dihydro-5H-imidazo[1,2-α]imidazole-3-carboxylic acid amides |
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2008
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- 2008-11-20 ES ES08853791.5T patent/ES2525237T3/es active Active
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- 2008-11-20 KR KR1020107011875A patent/KR20100101095A/ko not_active Application Discontinuation
- 2008-11-20 WO PCT/US2008/084149 patent/WO2009070485A1/en active Application Filing
- 2008-11-20 PT PT88537915T patent/PT2225238E/pt unknown
- 2008-11-20 JP JP2010536067A patent/JP5485164B2/ja not_active Expired - Fee Related
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- 2008-11-20 CN CN200880118561.4A patent/CN101889011B/zh not_active Expired - Fee Related
- 2008-11-20 EP EP08853791.5A patent/EP2225238B1/en active Active
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