BR112013021549A2 - formas cristalinas e processos para a preparação de azaciclos condensados (moduladores do receptor de canabinoide) - Google Patents
formas cristalinas e processos para a preparação de azaciclos condensados (moduladores do receptor de canabinoide)Info
- Publication number
- BR112013021549A2 BR112013021549A2 BR112013021549A BR112013021549A BR112013021549A2 BR 112013021549 A2 BR112013021549 A2 BR 112013021549A2 BR 112013021549 A BR112013021549 A BR 112013021549A BR 112013021549 A BR112013021549 A BR 112013021549A BR 112013021549 A2 BR112013021549 A2 BR 112013021549A2
- Authority
- BR
- Brazil
- Prior art keywords
- disease
- crystalline forms
- cannabinoid receptor
- hyperalgesia
- azacycles
- Prior art date
Links
- 239000003520 cannabinoid receptor affecting agent Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 208000004454 Hyperalgesia Diseases 0.000 abstract 4
- 208000035154 Hyperesthesia Diseases 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 206010061218 Inflammation Diseases 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- 230000004054 inflammatory process Effects 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 206010002198 Anaphylactic reaction Diseases 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 abstract 1
- 208000035143 Bacterial infection Diseases 0.000 abstract 1
- 208000009137 Behcet syndrome Diseases 0.000 abstract 1
- 102000009135 CB2 Cannabinoid Receptor Human genes 0.000 abstract 1
- 108010073376 CB2 Cannabinoid Receptor Proteins 0.000 abstract 1
- 206010011224 Cough Diseases 0.000 abstract 1
- 201000005569 Gout Diseases 0.000 abstract 1
- 206010020751 Hypersensitivity Diseases 0.000 abstract 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 abstract 1
- 206010025323 Lymphomas Diseases 0.000 abstract 1
- 208000008238 Muscle Spasticity Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 206010060862 Prostate cancer Diseases 0.000 abstract 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 1
- 201000002661 Spondylitis Diseases 0.000 abstract 1
- 206010052779 Transplant rejections Diseases 0.000 abstract 1
- 206010047115 Vasculitis Diseases 0.000 abstract 1
- 230000001154 acute effect Effects 0.000 abstract 1
- 206010064930 age-related macular degeneration Diseases 0.000 abstract 1
- 206010053552 allodynia Diseases 0.000 abstract 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 abstract 1
- 230000036783 anaphylactic response Effects 0.000 abstract 1
- 208000003455 anaphylaxis Diseases 0.000 abstract 1
- 208000022362 bacterial infectious disease Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229940125904 compound 1 Drugs 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 210000002865 immune cell Anatomy 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 208000032839 leukemia Diseases 0.000 abstract 1
- 206010025135 lupus erythematosus Diseases 0.000 abstract 1
- 208000002780 macular degeneration Diseases 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 201000006417 multiple sclerosis Diseases 0.000 abstract 1
- 230000002981 neuropathic effect Effects 0.000 abstract 1
- 201000008482 osteoarthritis Diseases 0.000 abstract 1
- YZGJIENQZBJQNS-UHFFFAOYSA-N pentalene-1-carboxylic acid Chemical compound C1=CC=C2C(C(=O)O)=CC=C21 YZGJIENQZBJQNS-UHFFFAOYSA-N 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
- 230000020341 sensory perception of pain Effects 0.000 abstract 1
- 208000018198 spasticity Diseases 0.000 abstract 1
- 230000003612 virological effect Effects 0.000 abstract 1
Classifications
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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]
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Abstract
resumo patente de invenção: "formas cristalinas e processos para a preparação de azaciclos condensados (moduladores do receptor de canabinoide)". a presente invenção refere-se às formas cristalinas de ((s)-1-hidroximetil-2,2-dimetil-propil)-amida de ácido (1as,5as)-2-(4-óxi-pirazin-2-il)-1a,2,5,5a-tetraidro-1h-2,3-diaza-ciclopropa[a]pentaleno-4-carboxílico (composto 1) e composições farmacêuticas dos mesmos que modulam a atividade do receptor de canabinoide cb2 e são, portanto, úteis no tratamento de distúrbios mediados pelo receptor de cb2, por exemplo, dor; hiperalgesia; alodinia; hiperalgesia inflamatória; hiperalgesia neuropática; nocicepção aguda; osteoporose; espasticidade associada com a esclerose múltipla; distúrbios autoimunes; reações alérgicas; inflamação do cns, por exemplo; aterosclerose; atividade celular imune indesejada, e inflamação associada com um distúrbio selecionado de: osteoartrite, anafilaxia, doença de behcet, rejeição de enxerto, vasculite, gota, espondilite, doença viral, doença bacteriana, lúpus, doença inflamatória do intestino, hepatite autoimune e diabetes melito tipo 1; degeneração macular relacionada com a idade; tosse; leucemia; linfoma; tumores do cns; câncer da próstata; doença de alzheimer, dano induzido por acidente vascular cerebral; demência; esclerose lateral amiotrófica; e doença de parkinson.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161446732P | 2011-02-25 | 2011-02-25 | |
| US61/446,732 | 2011-02-25 | ||
| US201161448542P | 2011-03-02 | 2011-03-02 | |
| US61/448,542 | 2011-03-02 | ||
| PCT/US2012/026506 WO2012116276A1 (en) | 2011-02-25 | 2012-02-24 | Crystalline forms and processes for the preparation of condensed azacycles ( cannabinoid receptor modulators) |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR112013021549A2 true BR112013021549A2 (pt) | 2016-11-01 |
| BR112013021549B1 BR112013021549B1 (pt) | 2022-01-11 |
Family
ID=45841624
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112013021549-6A BR112013021549B1 (pt) | 2011-02-25 | 2012-02-24 | Processos para preparação de forma cristalina anidra, para preparação de composição farmacêutica e para preparação de forma de dosagem, forma cristalina não solvatada anidra, composição farmacêutica, forma de dosagem, uso da referida forma cristalina e solvato |
Country Status (19)
| Country | Link |
|---|---|
| US (4) | US9458136B2 (pt) |
| EP (3) | EP2678330A1 (pt) |
| JP (1) | JP5945554B2 (pt) |
| KR (1) | KR102036932B1 (pt) |
| CN (1) | CN103608343B (pt) |
| AU (1) | AU2012222146B2 (pt) |
| BR (1) | BR112013021549B1 (pt) |
| CA (1) | CA2827057C (pt) |
| CL (1) | CL2013002436A1 (pt) |
| CO (1) | CO6852066A2 (pt) |
| DK (1) | DK3395812T3 (pt) |
| EA (1) | EA035989B1 (pt) |
| ES (1) | ES2932441T3 (pt) |
| IL (1) | IL227782A (pt) |
| MX (1) | MX346533B (pt) |
| MY (1) | MY165767A (pt) |
| SG (1) | SG192817A1 (pt) |
| WO (1) | WO2012116276A1 (pt) |
| ZA (1) | ZA201306402B (pt) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20170072358A (ko) * | 2009-08-28 | 2017-06-26 | 아레나 파마슈티칼스, 인크. | 칸나비노이드 수용체 조절제 |
| CN103492369B (zh) | 2011-02-25 | 2019-03-29 | 艾尼纳制药公司 | 大麻素受体调节剂 |
| CN103608343B (zh) * | 2011-02-25 | 2019-02-01 | 艾尼纳制药公司 | 用于制备作为大麻素受体调节剂的稠合氮杂环的晶形和制备方法 |
| WO2012116277A1 (en) | 2011-02-25 | 2012-08-30 | Arena Pharmaceuticals, Inc. | Cannabinoid receptor modulators |
| WO2016085941A1 (en) * | 2014-11-25 | 2016-06-02 | Arena Pharmaceuticals, Inc. | Processes for the preparation of cannabinoid receptor modulators |
| EP3452037A4 (en) * | 2016-04-10 | 2020-03-11 | Arena Pharmaceuticals, Inc. | METHODS OF TREATMENT WITH CB2 RECEPTOR AGONISTS |
| WO2018208847A1 (en) | 2017-05-08 | 2018-11-15 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of pain from inflammatory bowel disease |
| WO2018208848A1 (en) * | 2017-05-08 | 2018-11-15 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of visceral pain |
| CN114391011A (zh) * | 2019-09-12 | 2022-04-22 | 四川海思科制药有限公司 | 一种六氢化苯并吡唑衍生物及其制备 |
| WO2023059610A1 (en) | 2021-10-05 | 2023-04-13 | Arena Pharmaceuticals, Inc. | Crystalline forms and processes for the preparation of cannabinoid receptor modulators |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3964478B2 (ja) | 1995-06-30 | 2007-08-22 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ヘテロ環含有カルボン酸誘導体及びそれを含有する医薬 |
| EE200100556A (et) | 1999-04-28 | 2003-02-17 | Aventis Pharma Deutschland Gmbh | Diarüülhappe derivaat, seda sisaldav farmatseutiline kompositsioon ja ühendi kasutamine ravimite valmistamiseks |
| US20040259936A1 (en) | 2001-12-07 | 2004-12-23 | Nagarkatti Leonard C | Treatment of neoplasia |
| SE0300010D0 (sv) | 2003-01-07 | 2003-01-07 | Astrazeneca Ab | Novel Compounds |
| WO2005123677A1 (en) | 2004-06-16 | 2005-12-29 | Actelion Pharmaceuticals Ltd | 4-carbonyl substituted 1,1,2-trimethyl-1a,4,5,5a-tetrahydro-1h-4-aza-cyclopropa'a!pentalene derivatives as agonists for the g-protein-coupled receptor s1p1/edg1 and immunosuppressive agents |
| EP1781668A2 (en) | 2004-07-12 | 2007-05-09 | Cadila Healthcare Ltd. | Tricyclic pyrazole derivatives as cannabinoid receptor modulators |
| FR2875230A1 (fr) | 2004-09-13 | 2006-03-17 | Sanofi Aventis Sa | Derives de pyrazole condense, leur preparation et leur application en therapeutique |
| DE102004054666A1 (de) | 2004-11-12 | 2006-05-18 | Bayer Cropscience Gmbh | Substituierte Pyrazol-3-carboxamide, Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren |
| PE20060949A1 (es) | 2004-12-23 | 2006-10-11 | Arena Pharm Inc | Derivados fusionados de pirazol como agonistas del receptor de niacina |
| UA93390C2 (ru) * | 2005-06-02 | 2011-02-10 | Гленмарк Фармасьютикалс C.A. | Лиганды каннабиноидных рецепторов, фармацевтическая композиция (варианты), которая их содержит, и способ их получения |
| CA2613678A1 (en) * | 2005-06-02 | 2006-12-07 | Glenmark Pharmaceuticals S.A. | Novel cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation |
| US8524757B2 (en) | 2006-07-04 | 2013-09-03 | Janssen Pharmaceutica Nv | Benzimidazole cannabinoid agonists bearing a substituted heterocyclic group |
| WO2008039645A1 (en) | 2006-09-25 | 2008-04-03 | Boehringer Ingelheim International Gmbh | Compounds which modulate the cb2 receptor |
| WO2008063781A2 (en) | 2006-10-12 | 2008-05-29 | Abbott Laboratories | Chemical compounds as cannabinoid receptor ligands |
| US7928103B2 (en) | 2006-10-17 | 2011-04-19 | Boehringer Ingelheim International Gmbh | Compounds which modulate the CB2 receptor |
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| ES2439255T3 (es) | 2007-06-21 | 2014-01-22 | Cara Therapeutics, Inc. | Imidazoheterociclos sustituidos |
| US8338623B2 (en) | 2007-07-09 | 2012-12-25 | Abbvie Inc. | Compounds as cannabinoid receptor ligands |
| US7943658B2 (en) | 2007-07-23 | 2011-05-17 | Bristol-Myers Squibb Company | Indole indane amide compounds useful as CB2 agonists and method |
| EP2203171A2 (en) | 2007-08-21 | 2010-07-07 | Merck Sharp & Dohme Corp. | Cb2 receptor ligands for the treatment of pain |
| UA104010C2 (en) | 2008-12-18 | 2013-12-25 | Эли Лилли Энд Компани | Purine compounds |
| US8653127B2 (en) | 2009-01-28 | 2014-02-18 | Cara Therapeutics, Inc. | Bicyclic pyrazolo-heterocycles |
| US7741350B1 (en) * | 2009-01-28 | 2010-06-22 | Cara Therapeutics, Inc. | Bicyclic pyrazolo-heterocycles |
| KR20170072358A (ko) * | 2009-08-28 | 2017-06-26 | 아레나 파마슈티칼스, 인크. | 칸나비노이드 수용체 조절제 |
| WO2012116277A1 (en) | 2011-02-25 | 2012-08-30 | Arena Pharmaceuticals, Inc. | Cannabinoid receptor modulators |
| CN103608343B (zh) | 2011-02-25 | 2019-02-01 | 艾尼纳制药公司 | 用于制备作为大麻素受体调节剂的稠合氮杂环的晶形和制备方法 |
| WO2012116278A1 (en) | 2011-02-25 | 2012-08-30 | Arena Pharmaceuticals, Inc. | Cannabinoid receptor modulators |
| CN103492369B (zh) * | 2011-02-25 | 2019-03-29 | 艾尼纳制药公司 | 大麻素受体调节剂 |
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2012
- 2012-02-24 CN CN201280020512.3A patent/CN103608343B/zh not_active Expired - Fee Related
- 2012-02-24 ES ES18164225T patent/ES2932441T3/es active Active
- 2012-02-24 DK DK18164225.7T patent/DK3395812T3/da active
- 2012-02-24 US US14/001,133 patent/US9458136B2/en active Active
- 2012-02-24 JP JP2013555597A patent/JP5945554B2/ja active Active
- 2012-02-24 EP EP12709201.3A patent/EP2678330A1/en not_active Withdrawn
- 2012-02-24 BR BR112013021549-6A patent/BR112013021549B1/pt not_active IP Right Cessation
- 2012-02-24 WO PCT/US2012/026506 patent/WO2012116276A1/en active Application Filing
- 2012-02-24 AU AU2012222146A patent/AU2012222146B2/en not_active Ceased
- 2012-02-24 SG SG2013062427A patent/SG192817A1/en unknown
- 2012-02-24 MY MYPI2013003122A patent/MY165767A/en unknown
- 2012-02-24 MX MX2013009760A patent/MX346533B/es active IP Right Grant
- 2012-02-24 CA CA2827057A patent/CA2827057C/en active Active
- 2012-02-24 EP EP18164225.7A patent/EP3395812B8/en active Active
- 2012-02-24 KR KR1020137025057A patent/KR102036932B1/ko active IP Right Grant
- 2012-02-24 EP EP22197435.5A patent/EP4166552A1/en active Pending
- 2012-02-24 EA EA201391233A patent/EA035989B1/ru not_active IP Right Cessation
-
2013
- 2013-08-04 IL IL227782A patent/IL227782A/en active IP Right Grant
- 2013-08-23 CL CL2013002436A patent/CL2013002436A1/es unknown
- 2013-08-23 ZA ZA2013/06402A patent/ZA201306402B/en unknown
- 2013-09-10 CO CO13214674A patent/CO6852066A2/es active IP Right Grant
-
2016
- 2016-08-26 US US15/248,300 patent/US10183930B2/en active Active
-
2018
- 2018-12-10 US US16/214,388 patent/US10981895B2/en active Active
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2021
- 2021-03-16 US US17/202,946 patent/US11560369B2/en active Active
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| B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette] | ||
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| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 24/02/2012, OBSERVADAS AS CONDICOES LEGAIS. |
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| B21F | Lapse acc. art. 78, item iv - on non-payment of the annual fees in time |
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