HUP9904104A2 - Piperidin-ketokarbonsav-származékok,előállításuk és alkalmazásuk - Google Patents
Piperidin-ketokarbonsav-származékok,előállításuk és alkalmazásukInfo
- Publication number
- HUP9904104A2 HUP9904104A2 HU9904104A HUP9904104A HUP9904104A2 HU P9904104 A2 HUP9904104 A2 HU P9904104A2 HU 9904104 A HU9904104 A HU 9904104A HU P9904104 A HUP9904104 A HU P9904104A HU P9904104 A2 HUP9904104 A2 HU P9904104A2
- Authority
- HU
- Hungary
- Prior art keywords
- carbon atom
- piperidine
- nhr4
- calpain
- branched chain
- Prior art date
Links
- 229910052799 carbon Inorganic materials 0.000 abstract 4
- 102000007590 Calpain Human genes 0.000 abstract 2
- 108010032088 Calpain Proteins 0.000 abstract 2
- 102000005927 Cysteine Proteases Human genes 0.000 abstract 2
- 108010005843 Cysteine Proteases Proteins 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical compound BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 2
- -1 nitro, amino Chemical group 0.000 abstract 2
- 239000000843 powder Substances 0.000 abstract 2
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical group [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- QWPPOHNGKGFGJK-UHFFFAOYSA-N hypochlorous acid Chemical compound ClO QWPPOHNGKGFGJK-UHFFFAOYSA-N 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 229910052740 iodine Inorganic materials 0.000 abstract 1
- 150000002576 ketones Chemical class 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 210000003205 muscle Anatomy 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- SMCWNPAVVQIDBM-UHFFFAOYSA-N piperidine-1,2-dicarboxylic acid Chemical class OC(=O)C1CCCCN1C(O)=O SMCWNPAVVQIDBM-UHFFFAOYSA-N 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
- 238000009369 viticulture Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
-
- 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
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- 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
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
A találmány tárgyát az (I) általánős képletű piperidin-ketőkarbőn-sav-származékők -, ahől R1 -CO-R4, -SO2-R4, -CONH-R4, -COOR4, -C(-N)-R4, -C(=O)-NHR4 és -C(=S)-NHR4 általánős képletű csőpőrt, R2 1-6 szénatőmős, adőtt esetben elágazó láncú alkilcsőpőrt, amely mégegy fenil-, piridil- vagy naftilgyűrűvel szűbsztitűált, és amelylegfeljebb két R5 szűbsztitűenst hőrdőzhat, ahől R5 1-4 szénatőmős, adőtt esetben elágazó láncú alkil-, 1-4szénatőmős alkőxi- vagy hidrőxicsőpőrt, klór-, flűőr-, bróm- vagyjódatőm, triflűőrmetil-, nitrő-, aminő-, cianő-, karbőxi-, 1-4szénatőmős alkőxikarbőnil-, 1-4 szénatőmős alkilkarbőnil-aminő-,benzőil-aminő-, 1-4 szénatőmős alkilszűlfőnil-aminő-, benzőlszűlfőnil-aminő-, 1-4 szénatőmős alkilszűl- finil- és benzőlszűlfinilcsőpőrt, R3 -OR6 és -NHR6 általánős képletű csőpőrt - és taűtőmer és izőmerfőrmáik, és fiziőlógiailag elviselhető sói, az előállításűkra szőlgálóeljárás és gyógyszerek hatóanyagaiként való alkalmazásűk képezik. Az(I) általánős képletű ketőnszármazékők a cisztein-prőteázők, különösenőlyan cisztein-prőteázők, mint a kalpain I és kalpain II és akatepszin B és L enzimek inhibitőrai. (I) ŕ
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19642591A DE19642591A1 (de) | 1996-10-15 | 1996-10-15 | Neue Piperidin-Ketocarbonsäure-Derivate, deren Herstellung und Anwendung |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP9904104A2 true HUP9904104A2 (hu) | 2000-05-28 |
| HUP9904104A3 HUP9904104A3 (en) | 2001-01-29 |
Family
ID=7808858
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU9904104A HUP9904104A3 (en) | 1996-10-15 | 1997-09-23 | Derivates from piperidine-keto acid,their preparation and use |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US6380220B1 (hu) |
| EP (1) | EP0934273A1 (hu) |
| JP (1) | JP2001501955A (hu) |
| KR (1) | KR20000049130A (hu) |
| CN (1) | CN1239950A (hu) |
| AR (1) | AR009379A1 (hu) |
| AU (1) | AU736754B2 (hu) |
| BG (1) | BG103338A (hu) |
| BR (1) | BR9711908A (hu) |
| CA (1) | CA2268917A1 (hu) |
| CO (1) | CO4930264A1 (hu) |
| CZ (1) | CZ126899A3 (hu) |
| DE (1) | DE19642591A1 (hu) |
| HR (1) | HRP970549A2 (hu) |
| HU (1) | HUP9904104A3 (hu) |
| IL (1) | IL129089A0 (hu) |
| NO (1) | NO991761L (hu) |
| NZ (1) | NZ334979A (hu) |
| PL (1) | PL332720A1 (hu) |
| RU (1) | RU2189974C2 (hu) |
| SK (1) | SK38599A3 (hu) |
| TR (1) | TR199900819T2 (hu) |
| WO (1) | WO1998016512A1 (hu) |
| ZA (1) | ZA979175B (hu) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19817459A1 (de) | 1998-04-20 | 1999-10-21 | Basf Ag | Neue heterozyklische substituierte Amide, Herstellung und Anwendung |
| HUP0101599A3 (en) | 1998-04-20 | 2002-12-28 | Basf Ag | Heterocyclically substituted amides, process for producing them, use of them and pharmaceutical compositions containing them |
| TR200003071T2 (tr) * | 1998-04-20 | 2001-04-20 | Basf Aktiengesellschaft | Sistein-proteazı önleyici etkiye sahip yeni heterosiklik ikame edilmiş amidler |
| ATE264310T1 (de) | 1998-04-20 | 2004-04-15 | Abbott Gmbh & Co Kg | Neue substituierte amide, deren herstellung und anwendung |
| US6117870A (en) * | 1998-11-12 | 2000-09-12 | Fujirebio Kabushiki Kaisha | Cyclic amide derivatives |
| WO2001014331A2 (en) * | 1999-08-24 | 2001-03-01 | Regents Of The University Of California | Non-quinoline inhibitors of malaria parasites |
| AU7711000A (en) | 1999-09-29 | 2001-04-30 | Ortho-Mcneil Pharmaceutical, Inc. | Isonipecotamides for the treatment of integrin-mediated disorders |
| EP1295876A4 (en) | 2000-06-30 | 2005-10-19 | EPOXYCARBOXYLIC AMIDE, AZIDE AND AMINO ALCOHOLS AND THEIR USE IN PROCESSES FOR THE PREPARATION OF ALPHA KETOAMIDES | |
| DE10114762A1 (de) * | 2001-03-26 | 2002-10-02 | Knoll Gmbh | Verwendung von Cysteinprotease-Inhibitoren |
| JP2004529918A (ja) | 2001-04-09 | 2004-09-30 | オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド | インテグリンに由来する疾患の治療のためのキナゾリンおよびキナゾリン類似化合物 |
| EP1539744A4 (en) | 2002-07-11 | 2007-06-06 | Vicuron Pharm Inc | N-HYDROXYAMIDE DERIVATIVES WITH ANTIBACTERIAL EFFECT |
| WO2005016883A2 (en) * | 2003-08-14 | 2005-02-24 | Icos Corporation | Acrylamide derivatives as vla-1 integrin antagonists and uses thereof |
| RU2485114C2 (ru) | 2006-12-29 | 2013-06-20 | Эбботт Гмбх Унд Ко.Кг | Карбоксамидные соединения и их применение в качестве ингибиторов кальпаинов |
| TWI453019B (zh) | 2007-12-28 | 2014-09-21 | Abbvie Deutschland | 甲醯胺化合物 |
| TWI519530B (zh) | 2009-02-20 | 2016-02-01 | 艾伯維德國有限及兩合公司 | 羰醯胺化合物及其作為鈣蛋白酶（ｃａｌｐａｉｎ）抑制劑之用途 |
| US8236798B2 (en) | 2009-05-07 | 2012-08-07 | Abbott Gmbh & Co. Kg | Carboxamide compounds and their use as calpain inhibitors |
| US8598211B2 (en) | 2009-12-22 | 2013-12-03 | Abbvie Inc. | Carboxamide compounds and their use as calpain inhibitors IV |
| US9051304B2 (en) | 2009-12-22 | 2015-06-09 | AbbVie Deutschland GmbH & Co. KG | Carboxamide compounds and their use as calpain inhibitors V |
| WO2012076639A1 (en) | 2010-12-09 | 2012-06-14 | Abbott Gmbh & Co. Kg | Carboxamide compounds and their use as calpain inhibitors v |
| EP2834230A1 (en) | 2012-04-03 | 2015-02-11 | AbbVie Deutschland GmbH & Co KG | Carboxamide compounds and their use as calpain inhibitors v |
| WO2017156071A1 (en) | 2016-03-09 | 2017-09-14 | Blade Therapeutics, Inc. | Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof |
| WO2018009417A1 (en) | 2016-07-05 | 2018-01-11 | Blade Therapeutics, Inc. | Calpain modulators and therapeutic uses thereof |
| PE20191153A1 (es) | 2016-09-28 | 2019-09-05 | Blade Therapeutics Inc | Moduladores de calpainas y usos terapeuticos de los mismos |
| AU2018278422B2 (en) | 2017-06-01 | 2022-03-17 | Eisai R&D Management Co., Ltd. | Lewy body disease therapeutic agent containing pyrazoloquinoline derivative |
| BR112019023557A2 (pt) | 2017-06-01 | 2020-06-02 | Eisai R&D Management Co., Ltd. | Composição farmacêutica compreendendo inibidor de pde9 |
| RU2020130022A (ru) * | 2018-03-28 | 2022-05-04 | Блэйд Терапьютикс, Инк. | Модуляторы кальпаина и их терапевтическое применение |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU667463B2 (en) * | 1990-12-28 | 1996-03-28 | Cortex Pharmaceuticals, Inc. | Use of calpain inhibitors in the inhibition and treatment of neurodegeneration |
| WO1992012140A1 (en) | 1990-12-28 | 1992-07-23 | Georgia Tech Research Corporation | Peptides ketoamides, ketoacids, and ketoesters |
| CA2071621C (en) | 1991-06-19 | 1996-08-06 | Ahihiko Hosoda | Aldehyde derivatives |
| EP0650368A1 (en) | 1992-06-24 | 1995-05-03 | Cortex Pharmaceuticals, Inc. | Use of calpain inhibitors in the inhibition and treatment of medical conditions associated with increased calpain activity |
| US5541290A (en) | 1993-06-24 | 1996-07-30 | Harbeson; Scott L. | Optically pure calpain inhibitor compounds |
-
1996
- 1996-10-15 DE DE19642591A patent/DE19642591A1/de not_active Withdrawn
-
1997
- 1997-09-23 NZ NZ334979A patent/NZ334979A/en unknown
- 1997-09-23 KR KR1019990703216A patent/KR20000049130A/ko not_active Application Discontinuation
- 1997-09-23 CA CA002268917A patent/CA2268917A1/en not_active Abandoned
- 1997-09-23 CZ CZ991268A patent/CZ126899A3/cs unknown
- 1997-09-23 TR TR1999/00819T patent/TR199900819T2/xx unknown
- 1997-09-23 AU AU47770/97A patent/AU736754B2/en not_active Ceased
- 1997-09-23 IL IL12908997A patent/IL129089A0/xx unknown
- 1997-09-23 CN CN97180507A patent/CN1239950A/zh active Pending
- 1997-09-23 HU HU9904104A patent/HUP9904104A3/hu unknown
- 1997-09-23 SK SK385-99A patent/SK38599A3/sk unknown
- 1997-09-23 PL PL97332720A patent/PL332720A1/xx unknown
- 1997-09-23 JP JP10517955A patent/JP2001501955A/ja active Pending
- 1997-09-23 WO PCT/EP1997/005202 patent/WO1998016512A1/de not_active Application Discontinuation
- 1997-09-23 RU RU99109969/04A patent/RU2189974C2/ru active
- 1997-09-23 EP EP97910332A patent/EP0934273A1/de not_active Withdrawn
- 1997-09-23 US US09/284,543 patent/US6380220B1/en not_active Expired - Fee Related
- 1997-09-23 BR BR9711908A patent/BR9711908A/pt unknown
- 1997-10-14 ZA ZA979175A patent/ZA979175B/xx unknown
- 1997-10-14 HR HR19642591,3A patent/HRP970549A2/hr not_active Application Discontinuation
- 1997-10-14 CO CO97060053A patent/CO4930264A1/es unknown
- 1997-10-14 AR ARP970104718A patent/AR009379A1/es not_active Application Discontinuation
-
1999
- 1999-04-14 NO NO991761A patent/NO991761L/no not_active Application Discontinuation
- 1999-04-15 BG BG103338A patent/BG103338A/bg unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SK38599A3 (en) | 2000-04-10 |
| CZ126899A3 (cs) | 1999-07-14 |
| AU736754B2 (en) | 2001-08-02 |
| RU2189974C2 (ru) | 2002-09-27 |
| AR009379A1 (es) | 2000-04-12 |
| IL129089A0 (en) | 2000-02-17 |
| CN1239950A (zh) | 1999-12-29 |
| NZ334979A (en) | 2001-02-23 |
| AU4777097A (en) | 1998-05-11 |
| BR9711908A (pt) | 1999-08-24 |
| WO1998016512A1 (de) | 1998-04-23 |
| DE19642591A1 (de) | 1998-04-16 |
| PL332720A1 (en) | 1999-10-11 |
| KR20000049130A (ko) | 2000-07-25 |
| ZA979175B (en) | 1999-04-14 |
| TR199900819T2 (xx) | 1999-06-21 |
| BG103338A (bg) | 2000-01-31 |
| EP0934273A1 (de) | 1999-08-11 |
| NO991761D0 (no) | 1999-04-14 |
| CO4930264A1 (es) | 2000-06-27 |
| JP2001501955A (ja) | 2001-02-13 |
| CA2268917A1 (en) | 1998-04-23 |
| NO991761L (no) | 1999-04-14 |
| HRP970549A2 (en) | 1998-08-31 |
| US6380220B1 (en) | 2002-04-30 |
| HUP9904104A3 (en) | 2001-01-29 |
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