ATE354572T1 - Substituierte 1-piperidin-4-yl-4-azetidin-3-yl- piperazinderivate und deren verwendung als neurokininantagonisten - Google Patents
Substituierte 1-piperidin-4-yl-4-azetidin-3-yl- piperazinderivate und deren verwendung als neurokininantagonistenInfo
- Publication number
- ATE354572T1 ATE354572T1 AT03799583T AT03799583T ATE354572T1 AT E354572 T1 ATE354572 T1 AT E354572T1 AT 03799583 T AT03799583 T AT 03799583T AT 03799583 T AT03799583 T AT 03799583T AT E354572 T1 ATE354572 T1 AT E354572T1
- Authority
- AT
- Austria
- Prior art keywords
- disorders
- sub
- diseases
- neurokinin
- emesis
- Prior art date
Links
- YQHNGCCSZQYCOW-UHFFFAOYSA-N 1-(azetidin-3-yl)-4-piperidin-4-ylpiperazine Chemical class C1NCC1N1CCN(C2CCNCC2)CC1 YQHNGCCSZQYCOW-UHFFFAOYSA-N 0.000 title abstract 2
- 239000005557 antagonist Substances 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 5
- 208000035475 disorder Diseases 0.000 abstract 4
- 208000002551 irritable bowel syndrome Diseases 0.000 abstract 4
- 208000019901 Anxiety disease Diseases 0.000 abstract 2
- 208000002193 Pain Diseases 0.000 abstract 2
- 102000003141 Tachykinin Human genes 0.000 abstract 2
- 206010047700 Vomiting Diseases 0.000 abstract 2
- 230000003042 antagnostic effect Effects 0.000 abstract 2
- 230000000903 blocking effect Effects 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 108060008037 tachykinin Proteins 0.000 abstract 2
- QDZOEBFLNHCSSF-PFFBOGFISA-N (2S)-2-[[(2R)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-1-[(2R)-2-amino-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2R)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide Chemical compound C([C@@H](C(=O)N[C@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)NC(=O)[C@@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](N)CCCNC(N)=N)C1=CC=CC=C1 QDZOEBFLNHCSSF-PFFBOGFISA-N 0.000 abstract 1
- 208000027932 Collagen disease Diseases 0.000 abstract 1
- 206010012335 Dependence Diseases 0.000 abstract 1
- 208000030814 Eating disease Diseases 0.000 abstract 1
- 208000019454 Feeding and Eating disease Diseases 0.000 abstract 1
- 208000018522 Gastrointestinal disease Diseases 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 208000021891 Micturition disease Diseases 0.000 abstract 1
- 208000019022 Mood disease Diseases 0.000 abstract 1
- 125000000815 N-oxide group Chemical group 0.000 abstract 1
- 208000007920 Neurogenic Inflammation Diseases 0.000 abstract 1
- 102000009493 Neurokinin receptors Human genes 0.000 abstract 1
- 108050000302 Neurokinin receptors Proteins 0.000 abstract 1
- 102100024304 Protachykinin-1 Human genes 0.000 abstract 1
- 208000028017 Psychotic disease Diseases 0.000 abstract 1
- 208000025747 Rheumatic disease Diseases 0.000 abstract 1
- 201000001880 Sexual dysfunction Diseases 0.000 abstract 1
- 101800003906 Substance P Proteins 0.000 abstract 1
- 206010046543 Urinary incontinence Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 230000000172 allergic effect Effects 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 208000010668 atopic eczema Diseases 0.000 abstract 1
- 230000037396 body weight Effects 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 230000027288 circadian rhythm Effects 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 235000014632 disordered eating Nutrition 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 208000022821 personality disease Diseases 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 230000000069 prophylactic effect Effects 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 230000020341 sensory perception of pain Effects 0.000 abstract 1
- 231100000872 sexual dysfunction Toxicity 0.000 abstract 1
- 208000017520 skin disease Diseases 0.000 abstract 1
- 208000019116 sleep disease Diseases 0.000 abstract 1
- 230000001629 suppression Effects 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 230000002455 vasospastic effect Effects 0.000 abstract 1
- 238000004260 weight control Methods 0.000 abstract 1
Classifications
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- 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
-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—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
- C07D417/14—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 three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Hospice & Palliative Care (AREA)
- Dermatology (AREA)
- Otolaryngology (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Psychology (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- Nutrition Science (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP0214837 | 2002-12-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE354572T1 true ATE354572T1 (de) | 2007-03-15 |
Family
ID=32668703
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT03799583T ATE354572T1 (de) | 2002-12-23 | 2003-12-17 | Substituierte 1-piperidin-4-yl-4-azetidin-3-yl- piperazinderivate und deren verwendung als neurokininantagonisten |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US7435736B2 (de) |
| EP (1) | EP1581517B1 (de) |
| JP (1) | JP4660199B2 (de) |
| AT (1) | ATE354572T1 (de) |
| AU (1) | AU2003299249B2 (de) |
| CA (1) | CA2509406C (de) |
| DE (1) | DE60312042T2 (de) |
| ES (1) | ES2282731T3 (de) |
| WO (1) | WO2004056800A1 (de) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20060019587A (ko) | 2003-06-11 | 2006-03-03 | 머크 앤드 캄파니 인코포레이티드 | 치환된 3-알킬 및 3-알케닐 아제티딘 유도체 |
| ES2431524T3 (es) | 2004-04-13 | 2013-11-26 | Incyte Corporation | Derivados de piperazinilpiperidina como antagonistas de los receptores de quimiocinas |
| EP1809288B1 (de) * | 2004-11-10 | 2011-09-14 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Verwendung von 1,4-bis (3-aminoalkyl) piperazin-derivaten bei der behandlung von neurodegenerativen erkrankungen |
| GB0514017D0 (en) * | 2005-07-07 | 2005-08-17 | Ionix Pharmaceuticals Ltd | Chemical compounds |
| US7906652B2 (en) | 2005-11-28 | 2011-03-15 | Merck Sharp & Dohme Corp. | Heterocycle-substituted 3-alkyl azetidine derivatives |
| AU2010239188B2 (en) | 2009-04-22 | 2016-03-31 | Janssen Pharmaceutica Nv | Azetidinyl diamides as monoacylglycerol lipase inhibitors |
| RU2558141C2 (ru) * | 2009-04-22 | 2015-07-27 | Янссен Фармацевтика Нв | Гетероароматические и ароматические пиперазинилазетидиниламиды в качестве ингибиторов моноацилглицеринлипазы |
| US8435977B2 (en) | 2009-04-22 | 2013-05-07 | Janssen Pharmaceutica, Nv | Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors |
| KR20130101040A (ko) | 2010-09-03 | 2013-09-12 | 얀센 파마슈티카 엔.브이. | 모노아실글리세롤 리파아제 억제제로서의 다이-아제티디닐 다이아미드 |
| EP2621918A1 (de) * | 2010-09-27 | 2013-08-07 | Janssen Pharmaceutica, N.V. | Oxopiperazin-azetidinamide und oxodiazepin-azetidinamide als monoacylglycerol-lipasehemmer |
| KR20130140020A (ko) | 2010-10-22 | 2013-12-23 | 얀센 파마슈티카 엔.브이. | 모노아실글리세롤 리파아제 억제제로서의 아미노-피롤리딘-아제티딘 다이아미드 |
| US8513423B2 (en) | 2010-10-22 | 2013-08-20 | Janssen Pharmaceutica, Nv | Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors |
| CN105008333B (zh) * | 2012-12-27 | 2018-02-09 | 雅尔兹普罗泰特公司 | N‑(3‑(4‑(3‑(二异丁基氨基)丙基)哌嗪‑1‑基)丙基)‑1H‑苯并[d]咪唑‑2‑胺的硫酸盐、其制备及其用途 |
| US10314835B2 (en) | 2014-06-25 | 2019-06-11 | Emory University | Methods of managing conditioned fear with neurokinin receptor antagonists |
| JP6640840B2 (ja) | 2014-09-22 | 2020-02-05 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 線維症を処置するための方法及び医薬組成物 |
| US12084462B2 (en) | 2016-09-14 | 2024-09-10 | Janssen Pharmaceutica Nv | Spiro bicyclic inhibitors of menin-MLL interaction |
| AU2017326487B2 (en) | 2016-09-14 | 2021-08-05 | Janssen Pharmaceutica Nv | Spiro bicyclic inhibitors of menin-MLL interaction |
| TWI753016B (zh) * | 2016-09-14 | 2022-01-21 | 比利時商健生藥品公司 | Menin-mll相互作用之稠合二環抑制劑 |
| KR102513564B1 (ko) | 2016-12-15 | 2023-03-22 | 얀센 파마슈티카 엔.브이. | 메닌-mll 상호작용의 아제판 억제제 |
| US11458129B2 (en) | 2017-11-02 | 2022-10-04 | California Institute Of Technology | Neurokinin antagonists and uses thereof |
| US11396517B1 (en) | 2017-12-20 | 2022-07-26 | Janssen Pharmaceutica Nv | Exo-aza spiro inhibitors of menin-MLL interaction |
| UY38988A (es) | 2019-12-19 | 2021-06-30 | Janssen Pharmaceutica Nv | Derivados espiráncos sustituidos de cadena lineal |
| KR20240021883A (ko) | 2021-06-16 | 2024-02-19 | 셀진 코포레이션 | 신경변성 질환의 치료를 위한 카르복실산 기를 포함하는 아제티디닐 화합물 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY110227A (en) | 1991-08-12 | 1998-03-31 | Ciba Geigy Ag | 1-acylpiperindine compounds. |
| NZ321575A (en) | 1995-10-30 | 1999-05-28 | Janssen Pharmaceutica Nv | 1-(1,2-disubstituted piperidinyl)-4- substituted piperazine derivatives |
| GB9600235D0 (en) * | 1996-01-05 | 1996-03-06 | Pfizer Ltd | Therapeutic agents |
| GB9714129D0 (en) * | 1997-07-04 | 1997-09-10 | Pfizer Ltd | Azetidines |
| AU7788500A (en) | 1999-10-25 | 2001-05-08 | Janssen Pharmaceutica N.V. | Use of substance p antagonists for influencing the circadian timing system |
| GB0025354D0 (en) * | 2000-10-17 | 2000-11-29 | Glaxo Group Ltd | Chemical compounds |
| US6642226B2 (en) | 2001-02-06 | 2003-11-04 | Hoffman-La Roche Inc. | Substituted phenyl-piperidine methanone compounds |
| FR2820426B1 (fr) * | 2001-02-07 | 2007-05-11 | Condat Sa | Gel d'isolation thermique a reticulation controlee pour les lignes de transport d'hydrocarbures petroliers |
-
2003
- 2003-12-17 CA CA2509406A patent/CA2509406C/en not_active Expired - Fee Related
- 2003-12-17 EP EP03799583A patent/EP1581517B1/de not_active Expired - Lifetime
- 2003-12-17 WO PCT/EP2003/051042 patent/WO2004056800A1/en not_active Ceased
- 2003-12-17 ES ES03799583T patent/ES2282731T3/es not_active Expired - Lifetime
- 2003-12-17 DE DE60312042T patent/DE60312042T2/de not_active Expired - Lifetime
- 2003-12-17 JP JP2004561505A patent/JP4660199B2/ja not_active Expired - Fee Related
- 2003-12-17 AU AU2003299249A patent/AU2003299249B2/en not_active Ceased
- 2003-12-17 US US10/540,304 patent/US7435736B2/en not_active Expired - Fee Related
- 2003-12-17 AT AT03799583T patent/ATE354572T1/de active
Also Published As
| Publication number | Publication date |
|---|---|
| US7435736B2 (en) | 2008-10-14 |
| DE60312042T2 (de) | 2007-10-31 |
| ES2282731T3 (es) | 2007-10-16 |
| CA2509406A1 (en) | 2004-07-08 |
| JP4660199B2 (ja) | 2011-03-30 |
| US20060074069A1 (en) | 2006-04-06 |
| WO2004056800A1 (en) | 2004-07-08 |
| EP1581517A1 (de) | 2005-10-05 |
| AU2003299249B2 (en) | 2010-05-27 |
| JP2006512349A (ja) | 2006-04-13 |
| DE60312042D1 (de) | 2007-04-05 |
| EP1581517B1 (de) | 2007-02-21 |
| AU2003299249A1 (en) | 2004-07-14 |
| CA2509406C (en) | 2012-07-03 |
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