BRPI0808570B8 - processo para a preparação de inibidores de glyt-1 - Google Patents
processo para a preparação de inibidores de glyt-1Info
- Publication number
- BRPI0808570B8 BRPI0808570B8 BRPI0808570A BRPI0808570A BRPI0808570B8 BR PI0808570 B8 BRPI0808570 B8 BR PI0808570B8 BR PI0808570 A BRPI0808570 A BR PI0808570A BR PI0808570 A BRPI0808570 A BR PI0808570A BR PI0808570 B8 BRPI0808570 B8 BR PI0808570B8
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- formula
- glyt
- inhibitors
- preparing
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 7
- 239000002253 acid Substances 0.000 abstract 2
- 230000008878 coupling Effects 0.000 abstract 2
- 238000010168 coupling process Methods 0.000 abstract 2
- 238000005859 coupling reaction Methods 0.000 abstract 2
- 239000003153 chemical reaction reagent Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
síntese de inibidores de glyt-1. a presente invenção refere-se a processo para a preparação de um composto de fórmula: i na qual: het é um grupo heteroarila de 6 membros, contendo um, dois ou três átomos por nitrogênio; r1 é (c1-c6)-alquila, (c3-c6)-cicloalquila, nr4r5 ou (c1-c6)-alquila substituída por halogênio; r2 é hidróxi, halogênio, no2, cn, (c1-c6)-alquila, (c3-c6)-cicloalquila, (c1-c6)-alquila substituída por halogênio, (c1-c6)-alquila substituída por hidróxi, (ch2)0-(c1-c6)-alcóxi, (c1-c6)-alcóxi substituído com halogênio, nr4r5, c(o)r6 ou so2r7; r3 é (c1-c6)-alquila, (c3-c6)-cicloalquila ou (c1-c6)-alquila substituída por halogênio; r4 e r5, independentemente um do outro, são hidrogênio ou (c1-c6)-alquila; r6 é hidrogênio, (c1-c6)-alquila, (c1-c6)-alcóxi ou nr4r5; r7 é (c1-c6)-alquila, (c1-c6)-alquila opcionalmente substituída por halogênio, (ch2)0-(c3-c6)-cicloaquila, (ch2)0-(c3-c6)-alcóxi ou nr4r5; n é 0, 1, 2 ou 3; o é 0, 1 ou 2; e sais de adição de ácido farmaceuticamente aceitáveis dos mesmos, caracterizado pelo fato de que compreende as etapas de: a) reação de um composto de fórmula (21): 21 com um composto de fórmula (11): r3oh 8 para formar um composto de fórmula: 11 e b) acoplamento do composto de fórmula (11), na presença de um reagente de acoplamento ou do halogeneto de ácido correspondente com um composto de fórmula (15): 15 para formar o composto de fórmula (i): i.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07103485 | 2007-03-05 | ||
| EP07103485.4 | 2007-03-05 | ||
| PCT/EP2008/052244 WO2008107334A2 (en) | 2007-03-05 | 2008-02-25 | Process for the synthesis of glyt-1 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BRPI0808570A2 BRPI0808570A2 (pt) | 2014-09-02 |
| BRPI0808570B1 BRPI0808570B1 (pt) | 2020-09-15 |
| BRPI0808570B8 true BRPI0808570B8 (pt) | 2021-05-25 |
Family
ID=39469606
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0808570A BRPI0808570B8 (pt) | 2007-03-05 | 2008-02-25 | processo para a preparação de inibidores de glyt-1 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US7812161B2 (pt) |
| EP (1) | EP2131843B1 (pt) |
| JP (1) | JP4745446B2 (pt) |
| KR (1) | KR101143073B1 (pt) |
| CN (1) | CN101622000B (pt) |
| AT (1) | ATE532516T1 (pt) |
| AU (1) | AU2008223915B2 (pt) |
| BR (1) | BRPI0808570B8 (pt) |
| CA (1) | CA2678630C (pt) |
| ES (1) | ES2375585T3 (pt) |
| IL (1) | IL200323A (pt) |
| MX (1) | MX2009009065A (pt) |
| WO (1) | WO2008107334A2 (pt) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5656474B2 (ja) | 2010-06-28 | 2015-01-21 | 関東化学株式会社 | 脂肪族光学活性フルオロアルコールの製造方法 |
| CN104628679B (zh) * | 2013-11-08 | 2018-02-09 | 江苏恩华药业股份有限公司 | Bitopertin的合成方法及其中间体 |
| CN106397312B (zh) * | 2015-07-31 | 2020-03-24 | 广东东阳光药业有限公司 | 一种制备glyt-1抑制剂的方法 |
| KR20220125326A (ko) | 2020-01-09 | 2022-09-14 | 디스크 메디슨, 인크. | 적혈구형성 프로토포르피린증, x-연계된 프로토포르피린증, 또는 선천성 적혈구 조혈포르피린증을 글리신 운반 억제제로 치료하는 방법 |
| CA3195702A1 (en) | 2020-10-13 | 2022-04-21 | Boehringer Ingelheim International Gmbh | Process of reworking |
| JP2025527633A (ja) | 2022-08-24 | 2025-08-22 | 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 | Ｇｌｙｔ－１阻害剤の調製のための拡張可能な方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3992441A (en) * | 1972-12-26 | 1976-11-16 | Pfizer Inc. | Sulfamylbenzoic acids |
| US4480102A (en) * | 1982-07-23 | 1984-10-30 | The Dow Chemical Company | 2,3-Difluoro-5-(trifluoromethyl)pyridine and methods of making and using the same |
| DE68912282T2 (de) * | 1988-11-24 | 1994-04-28 | Akzo Nv | 1-[Mono- oder bis(trifluormethyl)-2-pyridinyl]piperazine enthaltende pharmazeutische Zusammensetzungen. |
| DE4235155A1 (de) * | 1992-10-19 | 1994-04-21 | Basf Ag | Verfahren zur Herstellung von Methylsulfonylbenzoesäuren |
| EP1080069B1 (en) * | 1998-04-20 | 2003-03-19 | Fujisawa Pharmaceutical Co., Ltd. | Anthranilic acid derivatives as inhibitors of the cgmp-phosphodiesterase |
| DE10112040A1 (de) | 2001-03-14 | 2002-10-02 | Aventis Pharma Gmbh | Verbessertes Verfahren zur Herstellung von Sulfonylcarboxamidderivaten |
| GB0227240D0 (en) * | 2002-11-21 | 2002-12-31 | Glaxo Group Ltd | Compounds |
| UA85194C2 (ru) * | 2003-08-11 | 2009-01-12 | Ф.Хоффманн-Ля Рош Аг | Пиперазины с or-замещенной фенильной группой и их применение как ингибиторов glyt 1 |
| JP4762250B2 (ja) * | 2004-12-09 | 2011-08-31 | エフ．ホフマン−ラ ロシュ アーゲー | フェニル−ピペラジンメタノン誘導体 |
| MX2007008190A (es) * | 2005-01-06 | 2007-08-07 | Hoffmann La Roche | Fenil metanonas sustituidas con sulfanilo como inhibidores del transportador de glicina 1 (glyt-1) para el tratamiento de trastornos neurologicos y neuropsiquiatricos. |
| DE602005022113D1 (de) * | 2005-01-07 | 2010-08-12 | Hoffmann La Roche | Phenyl)methanon-derivate als glycin-transporter 1 (glyt-1) hemmer zur behandlung von neurologischen und neuropsychiatrischen erkrankungen |
| CA2614408C (en) * | 2005-07-08 | 2013-10-08 | Stephan Doswald | Asymmetric reduction of 1,1,1-trifluoroacetone |
-
2008
- 2008-02-25 WO PCT/EP2008/052244 patent/WO2008107334A2/en not_active Ceased
- 2008-02-25 ES ES08709206T patent/ES2375585T3/es active Active
- 2008-02-25 CN CN200880006900XA patent/CN101622000B/zh active Active
- 2008-02-25 JP JP2009552166A patent/JP4745446B2/ja active Active
- 2008-02-25 EP EP08709206A patent/EP2131843B1/en active Active
- 2008-02-25 AU AU2008223915A patent/AU2008223915B2/en active Active
- 2008-02-25 MX MX2009009065A patent/MX2009009065A/es active IP Right Grant
- 2008-02-25 KR KR1020097018418A patent/KR101143073B1/ko active Active
- 2008-02-25 BR BRPI0808570A patent/BRPI0808570B8/pt active IP Right Grant
- 2008-02-25 AT AT08709206T patent/ATE532516T1/de active
- 2008-02-25 CA CA2678630A patent/CA2678630C/en active Active
- 2008-02-27 US US12/038,006 patent/US7812161B2/en active Active
-
2009
- 2009-08-10 IL IL200323A patent/IL200323A/en active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| US7812161B2 (en) | 2010-10-12 |
| KR101143073B1 (ko) | 2012-05-08 |
| EP2131843B1 (en) | 2011-11-09 |
| WO2008107334A3 (en) | 2008-10-23 |
| US20080221327A1 (en) | 2008-09-11 |
| BRPI0808570A2 (pt) | 2014-09-02 |
| ATE532516T1 (de) | 2011-11-15 |
| CN101622000A (zh) | 2010-01-06 |
| IL200323A (en) | 2013-11-28 |
| WO2008107334A2 (en) | 2008-09-12 |
| EP2131843A2 (en) | 2009-12-16 |
| JP2010520251A (ja) | 2010-06-10 |
| KR20090110368A (ko) | 2009-10-21 |
| JP4745446B2 (ja) | 2011-08-10 |
| IL200323A0 (en) | 2010-04-29 |
| BRPI0808570B1 (pt) | 2020-09-15 |
| MX2009009065A (es) | 2009-08-31 |
| AU2008223915A1 (en) | 2008-09-12 |
| ES2375585T3 (es) | 2012-03-02 |
| AU2008223915B2 (en) | 2013-05-02 |
| CN101622000B (zh) | 2012-07-04 |
| CA2678630A1 (en) | 2008-09-12 |
| CA2678630C (en) | 2015-04-14 |
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Legal Events
| Date | Code | Title | Description |
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| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] |
Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS. |
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| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
| B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 15/09/2020, OBSERVADAS AS CONDICOES LEGAIS. |
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| B16C | Correction of notification of the grant [chapter 16.3 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 25/02/2008 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF |