KR101025358B1 - 히스타민-3 수용체 길항제 - Google Patents
히스타민-3 수용체 길항제 Download PDFInfo
- Publication number
- KR101025358B1 KR101025358B1 KR1020087009991A KR20087009991A KR101025358B1 KR 101025358 B1 KR101025358 B1 KR 101025358B1 KR 1020087009991 A KR1020087009991 A KR 1020087009991A KR 20087009991 A KR20087009991 A KR 20087009991A KR 101025358 B1 KR101025358 B1 KR 101025358B1
- Authority
- KR
- South Korea
- Prior art keywords
- pyrrolidin
- fluoro
- ylmethyl
- phenyl
- cyclobutanecarboxylic acid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
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- 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
- C07D295/04—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/155—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- 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
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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- A61P11/02—Nasal agents, e.g. decongestants
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- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
- C07C233/58—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
-
- 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
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Otolaryngology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Obesity (AREA)
- Nutrition Science (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Psychology (AREA)
- Child & Adolescent Psychology (AREA)
- Rheumatology (AREA)
- Anesthesiology (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73099605P | 2005-10-27 | 2005-10-27 | |
| US60/730,996 | 2005-10-27 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20080054413A KR20080054413A (ko) | 2008-06-17 |
| KR101025358B1 true KR101025358B1 (ko) | 2011-03-28 |
Family
ID=37776539
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020087009991A Expired - Fee Related KR101025358B1 (ko) | 2005-10-27 | 2006-10-16 | 히스타민-3 수용체 길항제 |
Country Status (39)
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8158673B2 (en) * | 2005-10-27 | 2012-04-17 | Pfizer Inc. | Histamine-3 receptor antagonists |
| EP2124933B1 (en) | 2007-01-22 | 2012-10-17 | Pfizer Products Inc. | Tosylate salt of a therapeutic compound and pharmaceutical compositions thereof |
| US8247403B2 (en) | 2007-03-07 | 2012-08-21 | Takeda Pharmaceutical Company Limited | Benzoxazepine derivatives and use thereof |
| UA101809C2 (uk) | 2007-08-22 | 2013-05-13 | Астразенека Аб | Похідні циклопропіламіду |
| WO2009071988A1 (en) * | 2007-12-07 | 2009-06-11 | Pfizer Inc. | Tosylate salt of trans-n-isobutyl-3-fluoro-3- [3-flu0r0-4- (pyrrolidin-1-yl-methyl) -phenyl] cyclobut anecarboxamide |
| CN102015636B (zh) * | 2008-05-08 | 2014-08-13 | 埃沃特克股份有限公司 | 作为组胺h3受体拮抗剂的氮杂环丁烷类和环丁烷类化合物 |
| TW201039825A (en) | 2009-02-20 | 2010-11-16 | Astrazeneca Ab | Cyclopropyl amide derivatives 983 |
| KR20130002316A (ko) | 2010-02-18 | 2013-01-07 | 아스트라제네카 아베 | 시클로프로필 벤즈아미드 유도체의 신규 결정질 형태 |
| JP5767393B2 (ja) | 2011-03-31 | 2015-08-19 | ファイザー・インク | 新規二環式ピリジノン |
| WO2012172449A1 (en) | 2011-06-13 | 2012-12-20 | Pfizer Inc. | Lactams as beta secretase inhibitors |
| EP2751116B1 (en) | 2011-08-31 | 2016-10-12 | Pfizer Inc | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds |
| WO2013151982A1 (en) | 2012-04-03 | 2013-10-10 | Arena Pharmaceuticals, Inc. | Methods and compounds useful in treating pruritus, and methods for identifying such compounds |
| JP6110937B2 (ja) | 2012-05-04 | 2017-04-05 | ファイザー・インク | APP、BACE1、およびBACE2の阻害剤としての複素環式置換ヘキサヒドロピラノ[3,4−d][1,3]チアジン−2−アミン化合物 |
| EP3255049A1 (en) | 2012-06-29 | 2017-12-13 | Pfizer Inc | Novel 4-(substituted-amino)-7h-pyrrolo[2,3-d]pyrimidines as lrrk2 inhibitors |
| US9260455B2 (en) | 2012-09-20 | 2016-02-16 | Pfizer Inc. | Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| UA110688C2 (uk) | 2012-09-21 | 2016-01-25 | Пфайзер Інк. | Біциклічні піридинони |
| US10154988B2 (en) | 2012-11-14 | 2018-12-18 | The Johns Hopkins University | Methods and compositions for treating schizophrenia |
| WO2014091352A1 (en) | 2012-12-11 | 2014-06-19 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1 |
| JP6162820B2 (ja) | 2012-12-19 | 2017-07-12 | ファイザー・インク | 炭素環式および複素環式置換ヘキサヒドロピラノ[3,4−d][1,3]チアジン−2−アミン化合物 |
| JP2016507551A (ja) | 2013-02-13 | 2016-03-10 | ファイザー・インク | ヘテロアリール置換ヘキサヒドロピラノ[3,4−d][1,3]チアジン−2−アミン化合物 |
| US9233981B1 (en) | 2013-02-15 | 2016-01-12 | Pfizer Inc. | Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| EA201591360A1 (ru) | 2013-02-19 | 2016-03-31 | Пфайзер Инк. | Азабензимидазолы в качестве ингибиторов изозимов фдэ4 для лечения цнс и других расстройств |
| CA2925743C (en) | 2013-10-04 | 2018-03-06 | Pfizer Inc. | Novel bicyclic pyridinones as gamma-secretase modulators |
| EP3083618B1 (en) | 2013-12-17 | 2018-02-21 | Pfizer Inc | Novel 3,4-disubstituted-1h-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7h-pyrrolo[2,3-c]pyridazines as lrrk2 inhibitors |
| DK3126361T3 (da) | 2014-04-01 | 2020-01-02 | Pfizer | Chromen og 1,1a,2,7b-tetrahydrocyclopropa[c]chromen- pyridopyrazindioner som gamma-sekretase-modulatorer |
| SG11201607896YA (en) | 2014-04-10 | 2016-10-28 | Pfizer | 2-AMINO-6-METHYL-4,4a,5,6-TETRAHYDROPYRANO[3,4-d][1,3]THIAZIN-8a(8H)-YL-1,3-THIAZOL-4-YL AMIDES |
| EP3172210B1 (en) | 2014-07-24 | 2020-01-15 | Pfizer Inc | Pyrazolopyrimidine compounds |
| PT3177624T (pt) | 2014-08-06 | 2019-07-11 | Pfizer | Compostos de imidazopiridazina |
| EA033423B1 (ru) | 2015-02-03 | 2019-10-31 | Pfizer | Циклопропанбензофуранилпиридопиразиндионы |
| MX389753B (es) | 2015-06-17 | 2025-03-20 | Pfizer | Compuestos triciclicos y su uso como inhibidores de la fosfodiesterasa |
| EP3350178B1 (en) | 2015-09-14 | 2021-10-20 | Pfizer Inc. | Novel imidazo [4,5-c]quinoline and imidazo [4,5-c][1,5]naphthyridine derivatives as lrrk2 inhibitors |
| BR112018003489A2 (pt) | 2015-09-24 | 2018-09-25 | Pfizer | 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 |
| EP3353182A1 (en) | 2015-09-24 | 2018-08-01 | Pfizer Inc | Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors |
| WO2017051294A1 (en) | 2015-09-24 | 2017-03-30 | Pfizer Inc. | N-[2-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2h-1,2,4-thiadiazin-5-yl)-1,3-thiazol-4-yl] amides useful as bace inhibitors |
| CA3015166C (en) | 2016-02-23 | 2021-08-03 | Pfizer Inc. | 6,7-dihydro-5h-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide compounds |
| EP3478679B1 (en) | 2016-07-01 | 2021-04-21 | Pfizer Inc. | 5,7-dihydro-pyrrolo-pyridine derivatives for treating neurological and neurodegenerative diseases |
| BR112019018688A2 (pt) | 2017-03-10 | 2020-04-07 | Pfizer | derivados de imidazo[4,5-c] quinolina como inibidores de lrrk2 |
| IL269215B (en) | 2017-03-10 | 2022-09-01 | Pfizer | Disubstituted imidazole[4,5-c]quinoline derivatives |
| CN110997693A (zh) | 2017-06-07 | 2020-04-10 | 阿德克斯公司 | τ聚集抑制剂 |
| ES2937236T3 (es) | 2017-06-22 | 2023-03-27 | Pfizer | Derivados de dihidro-pirrolo-piridina |
| US11453701B2 (en) | 2017-08-18 | 2022-09-27 | Adrx, Inc. | Tau aggregation peptide inhibitors |
| AR115015A1 (es) | 2018-03-23 | 2020-11-18 | Pfizer | Derivados de azaespiro piperazina |
| US12144815B2 (en) | 2021-02-23 | 2024-11-19 | Hoth Therapeutics, Inc. | Use of aprepitant for treating Alzheimer's disease |
| CN116514645A (zh) * | 2023-04-08 | 2023-08-01 | 绍兴上虞华伦化工有限公司 | 二氟-4溴苯甲醛及其制备工艺 |
| WO2025145091A1 (en) | 2023-12-29 | 2025-07-03 | Pfizer Inc. | Crystalline forms of a muscarinic m4 receptor modulator and methods of treating diseases |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6559140B2 (en) | 2000-03-09 | 2003-05-06 | Abbott Laboratories | Cyclic and bicyclic diamino histamine-3 receptor antagonists |
| WO2005080361A1 (en) | 2004-02-02 | 2005-09-01 | Pfizer Products Inc. | Histamine-3 receptor modulators |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1379493A2 (en) | 2001-03-23 | 2004-01-14 | Eli Lilly and Company | Non-imidazole aryl alkylamines compounds as histamine h3 receptor antagonists, preparation and therapeutic uses |
| US7671047B2 (en) * | 2002-06-19 | 2010-03-02 | Sanofi-Aventis Deutschland Gmbh | Cationically substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use |
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