BR112014011248A2 - processo para preparação de derivados de 1-acil-fenilsulfonilprolinamida e novos intermediários - Google Patents
processo para preparação de derivados de 1-acil-fenilsulfonilprolinamida e novos intermediáriosInfo
- Publication number
- BR112014011248A2 BR112014011248A2 BR112014011248A BR112014011248A BR112014011248A2 BR 112014011248 A2 BR112014011248 A2 BR 112014011248A2 BR 112014011248 A BR112014011248 A BR 112014011248A BR 112014011248 A BR112014011248 A BR 112014011248A BR 112014011248 A2 BR112014011248 A2 BR 112014011248A2
- Authority
- BR
- Brazil
- Prior art keywords
- halogen
- alkyl
- derivatives
- formula
- phenylsulfonylprolinamide
- Prior art date
Links
- 239000000543 intermediate Substances 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 150000003147 proline derivatives Chemical class 0.000 abstract 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 102000005600 Cathepsins Human genes 0.000 abstract 1
- 108010084457 Cathepsins Proteins 0.000 abstract 1
- 102000005927 Cysteine Proteases Human genes 0.000 abstract 1
- 108010005843 Cysteine Proteases Proteins 0.000 abstract 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 abstract 1
- 208000005764 Peripheral Arterial Disease Diseases 0.000 abstract 1
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 abstract 1
- 208000002223 abdominal aortic aneurysm Diseases 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- -1 alkyl halogen Chemical class 0.000 abstract 1
- 208000007474 aortic aneurysm Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 208000033679 diabetic kidney disease Diseases 0.000 abstract 1
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
- C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/401—Proline; Derivatives thereof, e.g. captopril
-
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyrrole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
resumo processo para preparação de derivados de 1-acil- fenilsulfonilprolinamida e novos intermediários novo processo para a preparação de derivados de prolina da fórmula i: r1nonhocnsoor2r3i em que, r1 é selecionado de alquila c1-7 ou da fórmula ii: r4 em que r4 é selecionado de alquila c1-7, halogênio-alquila c1-7 ou de fenila que é opcionalmente substituída por halogênio; r2 é selecionado de halogênio ou halogênio-alquila c1-7; e r3 é selecionado de hidrogênio, halogênio, halogênio-alquila c1-7, alcóxi c1-7, halogênio- alcóxi c1-7 ou de um anel heterocíclico de 5 ou 6 elementos contendo um ou dois átomos de nitrogênio, o anel que é opcionalmente substituído por alquila c1-7 ou halogênio sendo descrito. os derivados de prolina da fórmula i são inibidores preferidos de cisteína protease catepsina s e são, portanto, úteis para tratamento de doenças metabólicas, tais como, diabetes, aterosclerose, aneurisma aórtico abdominal, doença arterial periférica e nefropatia diabética.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11188728 | 2011-11-11 | ||
| EP11188728.7 | 2011-11-11 | ||
| PCT/EP2012/072078 WO2013068434A1 (en) | 2011-11-11 | 2012-11-08 | Process for the preparation of 1-acyl-4-phenylsulfonylprolinamide derivatives and new intermediates |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR112014011248A2 true BR112014011248A2 (pt) | 2017-05-09 |
| BR112014011248B1 BR112014011248B1 (pt) | 2020-11-17 |
Family
ID=47143910
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112014011248-7A BR112014011248B1 (pt) | 2011-11-11 | 2012-11-08 | processo para preparação de derivados de 1-acil-fenilsulfonilprolinamida e novos intermediários |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US8796471B2 (pt) |
| EP (1) | EP2776392B1 (pt) |
| JP (1) | JP5852254B2 (pt) |
| KR (1) | KR101620769B1 (pt) |
| CN (1) | CN103930400B (pt) |
| AR (1) | AR088816A1 (pt) |
| AU (1) | AU2012334123B2 (pt) |
| BR (1) | BR112014011248B1 (pt) |
| CA (1) | CA2853877C (pt) |
| DK (1) | DK2776392T3 (pt) |
| ES (1) | ES2582643T3 (pt) |
| HK (1) | HK1194733A1 (pt) |
| HU (1) | HUE029182T2 (pt) |
| IL (1) | IL232424A (pt) |
| MX (1) | MX339996B (pt) |
| MY (1) | MY167569A (pt) |
| PL (1) | PL2776392T3 (pt) |
| RU (1) | RU2615997C2 (pt) |
| SG (1) | SG11201402030VA (pt) |
| SI (1) | SI2776392T1 (pt) |
| WO (1) | WO2013068434A1 (pt) |
| ZA (1) | ZA201403152B (pt) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103333094B (zh) * | 2013-06-19 | 2015-05-13 | 广东肇庆星湖生物科技股份有限公司 | 一种脯氨酸结晶精制的工艺方法 |
| WO2016034602A1 (en) * | 2014-09-05 | 2016-03-10 | F. Hoffmann-La Roche Ag | Solid forms of (2s,4r)-4-[4-(1-methyl-1h-pyrazol-4-yl)-2-trifluoromethyl-benzenesulfonyl]-1-(1-trifluoromethyl-cyclopropanecarbonyl)-pyrrolidine-2-carboxylic acid (1-cyano-cyclopropyl)-amide |
| SG11201807074VA (en) * | 2016-02-26 | 2018-09-27 | Hoffmann La Roche | Novel pyrrolidine derivatives |
| SG11201906777TA (en) * | 2017-01-24 | 2019-08-27 | Astellas Pharma Inc | Phenyldifluoromethyl-substituted prolinamide compound |
| AR114732A1 (es) * | 2018-09-18 | 2020-10-07 | Hoffmann La Roche | Utilización de un inhibidor de catepsina s contra la formación de anticuerpos antifármaco |
| EP3725769A1 (en) * | 2019-04-17 | 2020-10-21 | Newron Pharmaceuticals S.p.A. | Process for the production of substituted 2-[2-(phenyl) ethylamino]alkaneamide derivatives |
| CN111825582B (zh) * | 2020-08-12 | 2022-04-08 | 江西理工大学 | 一种以芳基磺酰氯为硫源合成β-硫代羰基化合物的方法 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1044965B1 (en) * | 1998-09-09 | 2003-10-01 | Nippon Finechemical Co., Ltd. | Process for the preparation of aromatic sulfur compounds |
| CN101475517B (zh) * | 2009-01-15 | 2012-08-15 | 河南大学 | 一种对称的含二硫键化合物的制备方法 |
| UA106748C2 (uk) | 2009-04-20 | 2014-10-10 | Ф. Хоффманн-Ля Рош Аг | Похідні проліну як інгібітори катепсину |
-
2012
- 2012-11-08 US US13/671,586 patent/US8796471B2/en active Active
- 2012-11-08 CN CN201280055223.7A patent/CN103930400B/zh active Active
- 2012-11-08 MX MX2014005689A patent/MX339996B/es active IP Right Grant
- 2012-11-08 SG SG11201402030VA patent/SG11201402030VA/en unknown
- 2012-11-08 EP EP12783216.0A patent/EP2776392B1/en active Active
- 2012-11-08 JP JP2014540444A patent/JP5852254B2/ja active Active
- 2012-11-08 AU AU2012334123A patent/AU2012334123B2/en not_active Ceased
- 2012-11-08 KR KR1020147015454A patent/KR101620769B1/ko active IP Right Grant
- 2012-11-08 PL PL12783216.0T patent/PL2776392T3/pl unknown
- 2012-11-08 WO PCT/EP2012/072078 patent/WO2013068434A1/en active Application Filing
- 2012-11-08 DK DK12783216.0T patent/DK2776392T3/en active
- 2012-11-08 SI SI201230621A patent/SI2776392T1/sl unknown
- 2012-11-08 ES ES12783216.0T patent/ES2582643T3/es active Active
- 2012-11-08 CA CA2853877A patent/CA2853877C/en active Active
- 2012-11-08 BR BR112014011248-7A patent/BR112014011248B1/pt not_active IP Right Cessation
- 2012-11-08 HU HUE12783216A patent/HUE029182T2/en unknown
- 2012-11-08 RU RU2014122116A patent/RU2615997C2/ru active
- 2012-11-08 MY MYPI2014701188A patent/MY167569A/en unknown
- 2012-11-09 AR ARP120104226A patent/AR088816A1/es unknown
-
2014
- 2014-04-30 ZA ZA2014/03152A patent/ZA201403152B/en unknown
- 2014-05-01 IL IL232424A patent/IL232424A/en active IP Right Grant
- 2014-08-06 HK HK14108048.9A patent/HK1194733A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SI2776392T1 (sl) | 2016-08-31 |
| EP2776392B1 (en) | 2016-05-18 |
| IL232424A0 (en) | 2014-06-30 |
| US20130123512A1 (en) | 2013-05-16 |
| AR088816A1 (es) | 2014-07-10 |
| KR20140098123A (ko) | 2014-08-07 |
| IL232424A (en) | 2017-01-31 |
| HK1194733A1 (zh) | 2014-10-24 |
| SG11201402030VA (en) | 2014-06-27 |
| AU2012334123A1 (en) | 2014-05-01 |
| RU2014122116A (ru) | 2015-12-20 |
| CN103930400B (zh) | 2016-04-20 |
| PL2776392T3 (pl) | 2016-11-30 |
| MX339996B (es) | 2016-06-21 |
| ES2582643T3 (es) | 2016-09-14 |
| HUE029182T2 (en) | 2017-02-28 |
| CN103930400A (zh) | 2014-07-16 |
| JP5852254B2 (ja) | 2016-02-03 |
| KR101620769B1 (ko) | 2016-05-12 |
| NZ623851A (en) | 2015-06-26 |
| AU2012334123B2 (en) | 2016-12-15 |
| MY167569A (en) | 2018-09-20 |
| JP2014532740A (ja) | 2014-12-08 |
| ZA201403152B (en) | 2015-07-29 |
| EP2776392A1 (en) | 2014-09-17 |
| CA2853877A1 (en) | 2013-05-16 |
| US8796471B2 (en) | 2014-08-05 |
| RU2615997C2 (ru) | 2017-04-12 |
| DK2776392T3 (en) | 2016-07-04 |
| CA2853877C (en) | 2019-10-01 |
| MX2014005689A (es) | 2014-08-08 |
| BR112014011248B1 (pt) | 2020-11-17 |
| WO2013068434A1 (en) | 2013-05-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| BR112014011248A2 (pt) | processo para preparação de derivados de 1-acil-fenilsulfonilprolinamida e novos intermediários | |
| BR112014030473A2 (pt) | novo diazaespirocicloalcano e azaespirocicloalcano | |
| NI201000107A (es) | Derivados de tiazol utilizados como inhibidores de pi 3 - cinasa. | |
| SV2009003233A (es) | Derivados de 2-(1-fenil -5- hidroxi -4alfa-metil-hexahidrociclopenta (f)indazol-5- il)etil fenilo como ligandos del receptor glucocorticoide | |
| BRPI0911035B8 (pt) | ativadores de pirrolidinona glicoquinase | |
| NZ716420A (en) | Fused heterocyclic compounds as sodium channel modulators | |
| PE20131143A1 (es) | Nuevas aminopirazoloquinazolinas | |
| EA200701176A1 (ru) | Новые соединения нафталина, способ их получения и фармацевтические композиции, содержащие их | |
| CO6361937A2 (es) | Derivados de heteroaril amidas y sus usos como activadores de glucoquinasa | |
| BR112012010186B8 (pt) | derivados de heteroarila contendo n como inibidores de quinase jak3 e composição farmacêutica compreendendo os mesmos | |
| UY33226A (es) | Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk4/6 | |
| CO6341581A2 (es) | Derivados de heteroarilo como inhibidores de dgat1 | |
| PE20140966A1 (es) | Quinazolincarboxamida azetidinas | |
| UY32494A (es) | Nuevas 2,4-diaminopirimidinas, sales farmacéuticas de las mismas, composiciones conteniéndolas y aplicaciones | |
| AR084011A1 (es) | Compuestos nitrogenados heterociclicos utiles para el tratamiento de infecciones por el virus sincitial respiratorio (rsv), proceso para prepararlos y composiciones farmaceuticas que los contienen | |
| ME00928B (me) | Novi postupak za sintezu agomelatina | |
| CL2013003056A1 (es) | Compuestos derivados de (fenil o piridin)-etinil-(piridin o pirimidin) sustituido; composición farmacéutica que los comprende; proceso de preparación de esto; y su uso en el tratamiento de la esquizofrenia o enfermedades cognitivas. | |
| CO2018010787A2 (es) | Compuesto de griseofulvina | |
| EA201001087A1 (ru) | Новые дигидроиндолоновые соединения, способ их получения и фармацевтические композиции, содержащие их | |
| BR112018003489A2 (pt) | n-[2-(2-amino-6,6-dissubstituído-4,4a,5,6-tetra-hidropirano[3,4-d][1,3]tiazin-8a(8h)-il)-1,3-tiazol-4-il]amidas | |
| BR112012021135A2 (pt) | microbicidas | |
| BR112013017416A2 (pt) | derivado de indola ou indazola ou sal do mesmo | |
| CL2013003068A1 (es) | Compuestos derivados de 2-(etinil-piridin-2-il)-pirazolidin-3-ona, 2-(etinil-pirimidin-2-il)-pirazolidin-3-ona o 2-(etinil-piridazin-3-il)-pirazolidin-3-ona; moduladores alostericos positivos de mglur5; procedimiento de preparacion; composicion farmaceutica; y su uso para tratar la esquizofrenia o enfermedades cognitivas. | |
| EA201390374A1 (ru) | Гетероциклические соединения для лечения или профилактики расстройств, вызываемых ослабленной нейротрансмиссией серотонина, норэпинефрина или допамина | |
| JO3248B1 (ar) | عملية لتحضير إنزيمات مثبطة من نوع c-fms |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 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. |
|
| 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: 20 (VINTE) ANOS CONTADOS A PARTIR DE 08/11/2012, OBSERVADAS AS CONDICOES LEGAIS. |
|
| B21F | Lapse acc. art. 78, item iv - on non-payment of the annual fees in time |
Free format text: REFERENTE A 12A ANUIDADE. |