HUP0203836A2 - 1,3-Diszubsztituált pirrolidin-származékok alfa2-adrenerg-receptor antagonista hatással, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents
1,3-Diszubsztituált pirrolidin-származékok alfa2-adrenerg-receptor antagonista hatással, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények és alkalmazásukInfo
- Publication number
- HUP0203836A2 HUP0203836A2 HU0203836A HUP0203836A HUP0203836A2 HU P0203836 A2 HUP0203836 A2 HU P0203836A2 HU 0203836 A HU0203836 A HU 0203836A HU P0203836 A HUP0203836 A HU P0203836A HU P0203836 A2 HUP0203836 A2 HU P0203836A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- alkyl
- hydrogen
- halogen atom
- atom
- Prior art date
Links
- 108020004101 alpha-2 Adrenergic Receptor Proteins 0.000 title 1
- 102000015006 alpha2-adrenergic receptor activity proteins Human genes 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 11
- 125000005843 halogen group Chemical group 0.000 abstract 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 7
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000003277 amino group Chemical group 0.000 abstract 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 2
- -1 methylenedioxy group Chemical group 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000005115 alkyl carbamoyl group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 abstract 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 abstract 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000012458 free base Substances 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
Classifications
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- 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
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- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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- A61P25/24—Antidepressants
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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
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
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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
- 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
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- A—HUMAN NECESSITIES
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
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- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C07D405/08—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing alicyclic rings
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- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Diabetes (AREA)
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- Ophthalmology & Optometry (AREA)
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- Obesity (AREA)
- Psychology (AREA)
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Abstract
A találmány (I) általános képletű vegyületekre vonatkozik szabad bázisvagy savadíciós só formájában ebben a képletben R0 jelentésehidrogénatom vagy alkilcsoport. R1 jelentése alkoxicsoport vagyalkenilcsoport, és jelenthet halogénatomot, hidroxilcsoportot,alkilcsoportot, trifluor-metilcsoportot vagy trifluor-metoxicsoportotis, R2 hidrogénatom, halogénatom, hidroxilcsoport, alkilcsoport,alkoxicsoport, 2-5-trifluor-metil- vagy trifluor-metoxicsoport, vagyha R1-hez képest orto helyzetben van, akkor R1 és R2 együtt metilén-dioxicsoportot alkothat és A tetrahidropirán-4-il-csoport vagy egy(a), (b), (c), (d), (e), (f), vagy (g) képletű csoport, ahol m értéke1-3 X oxigén- vagy kénatom, vagy -CH=CH-csoport, R3 hidrogén- vagyhalogénatom, hidroxilcsoport, alkilcsoport, hidroxi-alkilcsoport,alkoxicsoport, trifluor-metilcsoport, alkil-szulfonil-aminocsoport,benzil-oxicsoport, karbamoilcsoport, alkil-karbamoilcsoport vagydi(alkil)-karbamoilcsoport; R4 és R5 hidrogén- vagy halogénatom,alkil- vagy alkoxicsoport; R6 hidrogén- vagy halogénatom vagyalkilcsoport, R7 hidrogénatom, vagy alkilcsoport vagy cikloalkil-(1-4szénatomos alkilcsoport), vagy R8 hidrogén- vagy halogénatom,hidroxilcsoport, alkilcsoport, alkoxicsoport, adott esetbenhelyettesített aminocsoport, és R9 hidrogén- vagy halogénatom,alkilcsoport vagy fenilcsoport, vagy R8 és R9 együtt -O-(CH2)m O-képletű csoport, ahol m a fenti jelentésű, R10 hidrogénatom,alkilcsoport cikloalkil-alkilcsoport alkil-karbonilcsoport,cikloalkil-karbonilcsoport, alkoxi-karbonilcsoport, benzilcsoport,benziloxi-karbonilcsoport, benzoilcsoport, helyettesített szulfonilvagy aminocsoport. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0002100.6A GB0002100D0 (en) | 2000-01-28 | 2000-01-28 | Organic compounds |
| PCT/EP2001/000861 WO2001055132A1 (en) | 2000-01-28 | 2001-01-26 | 1,3-disubstituted pyrrolidines as alpha-2-adrenoceptor antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0203836A2 true HUP0203836A2 (hu) | 2003-03-28 |
| HUP0203836A3 HUP0203836A3 (en) | 2005-03-29 |
Family
ID=9884609
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0203836A HUP0203836A3 (en) | 2000-01-28 | 2001-01-26 | 1,3-disubstituted pyrrololidines as alpha-2-adrenoceptor antagonists, process for their preparation and pharmaceutical compositions containing them and their use |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US7012085B2 (hu) |
| EP (1) | EP1257547B1 (hu) |
| JP (1) | JP2003523353A (hu) |
| KR (1) | KR20020069375A (hu) |
| CN (2) | CN1305847C (hu) |
| AR (1) | AR029463A1 (hu) |
| AT (1) | ATE384715T1 (hu) |
| AU (1) | AU768844B2 (hu) |
| BR (1) | BR0107888A (hu) |
| CA (1) | CA2398794C (hu) |
| CO (1) | CO5261521A1 (hu) |
| CZ (1) | CZ20022581A3 (hu) |
| DE (1) | DE60132558T2 (hu) |
| ES (1) | ES2296763T3 (hu) |
| GB (1) | GB0002100D0 (hu) |
| HU (1) | HUP0203836A3 (hu) |
| IL (1) | IL150550A0 (hu) |
| MX (1) | MXPA02007318A (hu) |
| MY (1) | MY128639A (hu) |
| NO (1) | NO20023485L (hu) |
| NZ (1) | NZ520342A (hu) |
| PE (1) | PE20011068A1 (hu) |
| PL (1) | PL202473B1 (hu) |
| PT (1) | PT1257547E (hu) |
| RU (1) | RU2002121646A (hu) |
| SK (1) | SK10802002A3 (hu) |
| WO (1) | WO2001055132A1 (hu) |
| ZA (1) | ZA200205991B (hu) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0002100D0 (en) * | 2000-01-28 | 2000-03-22 | Novartis Ag | Organic compounds |
| US6436972B1 (en) | 2000-04-10 | 2002-08-20 | Dalhousie University | Pyridones and their use as modulators of serine hydrolase enzymes |
| AU2003216954A1 (en) * | 2002-03-29 | 2003-10-13 | Orion Corporation | Treatment of dependence and dependence related withdrawal symptoms |
| AR059898A1 (es) | 2006-03-15 | 2008-05-07 | Janssen Pharmaceutica Nv | Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2 |
| JP2008037850A (ja) * | 2006-08-10 | 2008-02-21 | Mitsubishi Tanabe Pharma Corp | 新規置換ピペリジン誘導体 |
| TW200845978A (en) | 2007-03-07 | 2008-12-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives |
| TW200900065A (en) | 2007-03-07 | 2009-01-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives |
| BRPI0816767B8 (pt) | 2007-09-14 | 2021-05-25 | Addex Pharmaceuticals Sa | composto 4-fenil-3,4,5,6-tetra-hidro-2h,1'h-[1,4']bipiridi¬nil-2'-onas 1',3'-dissubstituídas, composição farmacêutica e uso dos mesmos |
| US8273900B2 (en) | 2008-08-07 | 2012-09-25 | Novartis Ag | Organic compounds |
| AU2009289784B2 (en) | 2008-09-02 | 2012-03-22 | Addex Pharma S.A. | 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors |
| WO2010060589A1 (en) | 2008-11-28 | 2010-06-03 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors |
| MY161325A (en) | 2009-05-12 | 2017-04-14 | Janssen Pharmaceuticals Inc | 1, 2, 4-triazolo[4,3-a]pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders |
| MY153913A (en) | 2009-05-12 | 2015-04-15 | Janssen Pharmaceuticals Inc | 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| US8946205B2 (en) | 2009-05-12 | 2015-02-03 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors |
| AU2011328203B2 (en) | 2010-11-08 | 2015-03-19 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors |
| PL2649069T3 (pl) | 2010-11-08 | 2016-01-29 | Janssen Pharmaceuticals Inc | Pochodne 1,2,4-triazolo[4,3-a]pirydyny i ich zastosowanie jako dodatnich allosterycznych modulatorów receptorów mGluR2 |
| CN103261195B (zh) | 2010-11-08 | 2015-09-02 | 杨森制药公司 | 1,2,4-三唑并[4,3-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途 |
| GB2503187A (en) * | 2011-09-15 | 2013-12-25 | Univ Sussex | Composition for use in the treatment of neurodevelopmental disorders |
| WO2014080290A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Cyclic amines as bromodomain inhibitors |
| WO2014080291A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
| EP2935253B1 (en) | 2012-12-21 | 2018-08-01 | Zenith Epigenetics Ltd. | Novel heterocyclic compounds as bromodomain inhibitors |
| JO3368B1 (ar) | 2013-06-04 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2 |
| ES2806135T3 (es) | 2013-06-21 | 2021-02-16 | Zenith Epigenetics Ltd | Nuevos inhibidores de bromodominios bicíclicos |
| JP6599852B2 (ja) | 2013-06-21 | 2019-10-30 | ゼニス・エピジェネティクス・リミテッド | ブロモドメイン阻害剤としての新規の置換された二環式化合物 |
| CN105593224B (zh) | 2013-07-31 | 2021-05-25 | 恒元生物医药科技(苏州)有限公司 | 作为溴结构域抑制剂的新型喹唑啉酮类化合物 |
| JO3367B1 (ar) | 2013-09-06 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2 |
| KR102461134B1 (ko) | 2014-01-21 | 2022-10-28 | 얀센 파마슈티카 엔.브이. | 대사 조절형 글루탐산 작동성 수용체 제2아형의 양성 알로스테릭 조절제 또는 오르토스테릭 작동제를 포함하는 조합 및 그 용도 |
| UA121965C2 (uk) | 2014-01-21 | 2020-08-25 | Янссен Фармацевтика Нв | Комбінації, які містять позитивні алостеричні модулятори або ортостеричні агоністи метаботропного глутаматергічного рецептора 2 підтипу, та їх застосування |
| CA2966298A1 (en) | 2014-12-01 | 2016-06-09 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| US10179125B2 (en) | 2014-12-01 | 2019-01-15 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| JP2017537946A (ja) | 2014-12-11 | 2017-12-21 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての置換複素環 |
| CA2966450A1 (en) | 2014-12-17 | 2016-06-23 | Olesya KHARENKO | Inhibitors of bromodomains |
Family Cites Families (9)
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| FI95572C (fi) | 1987-06-22 | 1996-02-26 | Eisai Co Ltd | Menetelmä lääkeaineena käyttökelpoisen piperidiinijohdannaisten tai sen farmaseuttisen suolan valmistamiseksi |
| US5185364A (en) | 1988-01-15 | 1993-02-09 | Abbott Laboratories | Aminomethyl-chroman and -thiochroman compounds |
| AU653837B2 (en) * | 1991-04-17 | 1994-10-13 | Pharmacia & Upjohn Company | Substituted phenylazacycloalkanes as CNS agents |
| GB9113031D0 (en) | 1991-06-17 | 1991-08-07 | Smithkline Beecham Plc | Compounds |
| FR2687146B1 (fr) * | 1992-02-12 | 1994-04-01 | Adir Cie | Nouveaux derives de pyrrolidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| ATE243196T1 (de) | 1994-03-09 | 2003-07-15 | Novo Nordisk As | Piperidine und pyrrolidine |
| SE9802546D0 (sv) | 1998-07-15 | 1998-07-15 | Ross Nicholas Waters | Medicinal product and method for treatment and prevention of dyskinesia |
| IT1303737B1 (it) | 1998-11-11 | 2001-02-23 | Smithkline Beecham Spa | Derivati fenilpiperidinici procedimento per la loro preparazione eloro uso come ligandi del recettore orl-1. |
| GB0002100D0 (en) * | 2000-01-28 | 2000-03-22 | Novartis Ag | Organic compounds |
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- 2001-01-26 KR KR1020027009705A patent/KR20020069375A/ko not_active Application Discontinuation
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