HUP0203136A2 - Piperazinszármazékok, eljárás az előállításukra, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents
Piperazinszármazékok, eljárás az előállításukra, ezeket tartalmazó gyógyszerkészítmények és alkalmazásukInfo
- Publication number
- HUP0203136A2 HUP0203136A2 HU0203136A HUP0203136A HUP0203136A2 HU P0203136 A2 HUP0203136 A2 HU P0203136A2 HU 0203136 A HU0203136 A HU 0203136A HU P0203136 A HUP0203136 A HU P0203136A HU P0203136 A2 HUP0203136 A2 HU P0203136A2
- Authority
- HU
- Hungary
- Prior art keywords
- atom
- alkyl
- group
- hydrogen
- compounds
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 150000004885 piperazines Chemical class 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 229910052731 fluorine Inorganic materials 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 239000000825 pharmaceutical preparation Substances 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
- 102100024304 Protachykinin-1 Human genes 0.000 abstract 1
- 101800003906 Substance P Proteins 0.000 abstract 1
- 102000003141 Tachykinin Human genes 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 229910052799 carbon Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229940066771 systemic antihistamines piperazine derivative Drugs 0.000 abstract 1
- 108060008037 tachykinin Proteins 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 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
- C07D401/06—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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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
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
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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
- A61P25/06—Antimigraine agents
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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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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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
- A61P25/22—Anxiolytics
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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
- A61P25/24—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
- A61P25/28—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
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
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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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/34—Tobacco-abuse
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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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
A találmány (I) általános képletű piperazinszármazékokra - amelynekképletében R halogénatom vagy alkilcsoport; R1 hidrogénatom vagyalkilcsoport; R2 hidrogénatom, alkil-, alkenil- vagycikloalkilcsoport; vagy R1 és R2 a nitrogén- és szénatommal együtt egyöt- vagy hattagú heterociklusos csoportot képez; R3 trifluor-metil-,alkil-, alkoxi-, trifluor-metoxi-csoport vagy halogénatom; R4hidrogénatom, -(CH2)qR7 vagy -(CH2)rCO(CH2)pR7 csoport; R5hidrogénatom, alkil- vagy -COR6 csoport; R10 hidrogénatom,alkilcsoport; vagy R10 és R2 együtt cikloalkilcsoportot képez; mértéke 0, 1, 2 vagy 3; n értéke 0, 1, 2 vagy 3; azzal a megkötéssel,hogy ha R1 és R2 azzal a nitrogénatommal és szénatommal együtt,amelyhez kapcsolódik, egy öt- vagy hattagú heterociklusos csoportotképez, i) m értéke 1 vagy 2; ii) ha m értéke 1, akkor R jelentésefluoratomtól eltérő, és iii) ha m értéke 2, akkor a két Rszubsztituens legalább egyikének a jelentése fluoratomtól eltérő, valamint gyógyászatilag elfogadható sóikra és szolvátjaikravonatkozik. A találmány kiterjed a találmány szerinti vegyületekelőállítási eljárásaira, a vegyületeket tartalmazógyógyszerkészítményekre és a vegyületek gyógyászati készítményekelőállítására vonatkozó felhasználására is. A találmány szerintivegyületek a tachykininek, köztük a P anyag (substance P) és másneurokininek antagonistái. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9923748.9A GB9923748D0 (en) | 1999-10-07 | 1999-10-07 | Chemical compounds |
| PCT/EP2000/009722 WO2001025219A2 (en) | 1999-10-07 | 2000-10-05 | Piperazine compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0203136A2 true HUP0203136A2 (hu) | 2003-02-28 |
| HUP0203136A3 HUP0203136A3 (en) | 2003-03-28 |
Family
ID=10862304
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0203136A HUP0203136A3 (en) | 1999-10-07 | 2000-10-05 | Piperazine compounds, process for their preparation, pharmaceutical compositions containing them and their use |
Country Status (33)
| Country | Link |
|---|---|
| US (6) | US6951861B1 (hu) |
| EP (3) | EP1460066B1 (hu) |
| JP (1) | JP4776844B2 (hu) |
| KR (2) | KR100857671B1 (hu) |
| CN (1) | CN100413850C (hu) |
| AR (2) | AR025975A1 (hu) |
| AT (3) | ATE407125T1 (hu) |
| AU (1) | AU768780B2 (hu) |
| BR (1) | BR0014541A (hu) |
| CA (1) | CA2386515C (hu) |
| CO (1) | CO5251467A1 (hu) |
| CY (2) | CY1110172T1 (hu) |
| CZ (1) | CZ302340B6 (hu) |
| DE (3) | DE60012031T2 (hu) |
| DK (3) | DK1218359T3 (hu) |
| ES (3) | ES2329130T3 (hu) |
| GB (1) | GB9923748D0 (hu) |
| HK (3) | HK1052506B (hu) |
| HU (1) | HUP0203136A3 (hu) |
| IL (2) | IL148964A0 (hu) |
| MX (1) | MXPA02003515A (hu) |
| MY (1) | MY130907A (hu) |
| NO (1) | NO323776B1 (hu) |
| NZ (2) | NZ531127A (hu) |
| PE (1) | PE20010741A1 (hu) |
| PL (1) | PL201191B1 (hu) |
| PT (3) | PT1454901E (hu) |
| SI (3) | SI1454901T1 (hu) |
| TN (1) | TNSN00194A1 (hu) |
| TR (1) | TR200200936T2 (hu) |
| TW (1) | TWI225485B (hu) |
| WO (1) | WO2001025219A2 (hu) |
| ZA (1) | ZA200202589B (hu) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE434437T1 (de) * | 1999-02-18 | 2009-07-15 | Novasearch Ag | Verwendung von antagonisten der 5-ht3-rezeptoren zur behandlung von muskuloeskeletalen erkrankungen |
| USRE39921E1 (en) | 1999-10-07 | 2007-11-13 | Smithkline Beecham Corporation | Chemical compounds |
| GB9923748D0 (en) * | 1999-10-07 | 1999-12-08 | Glaxo Group Ltd | Chemical compounds |
| AUPQ514600A0 (en) | 2000-01-18 | 2000-02-10 | James Cook University | Brain injury treatment |
| GB0003232D0 (en) * | 2000-02-11 | 2000-04-05 | Smithkline Beecham Plc | Novel composition |
| GB0025354D0 (en) | 2000-10-17 | 2000-11-29 | Glaxo Group Ltd | Chemical compounds |
| GB0108594D0 (en) * | 2001-04-05 | 2001-05-23 | Glaxo Group Ltd | Chemical compounds |
| GB0108595D0 (en) | 2001-04-05 | 2001-05-23 | Glaxo Group Ltd | Chemical compounds |
| US20030083345A1 (en) * | 2001-07-10 | 2003-05-01 | Torsten Hoffmann | Method of treatment and/or prevention of brain, spinal or nerve injury |
| GB0119797D0 (en) * | 2001-08-14 | 2001-10-03 | Glaxo Group Ltd | Chemical compounds |
| GB0124463D0 (en) | 2001-10-11 | 2001-12-05 | Smithkline Beecham Plc | Compounds |
| WO2003066589A1 (en) | 2002-02-08 | 2003-08-14 | Glaxo Group Limited | Piperidylcarboxamide derivatives and their use in the treatment of tachykinim-mediated diseases |
| GB0203022D0 (en) * | 2002-02-08 | 2002-03-27 | Glaxo Group Ltd | Chemical compounds |
| GB0203020D0 (en) * | 2002-02-08 | 2002-03-27 | Glaxo Group Ltd | Chemical compounds |
| DE10209145A1 (de) * | 2002-03-01 | 2003-09-04 | Bayer Cropscience Ag | Halogenbenzole |
| AU2003243353A1 (en) * | 2002-05-29 | 2003-12-19 | The Regents Of The University Of California | Antagonizing nk1 receptors inhibits consumption of substances of abuse |
| JP4079727B2 (ja) * | 2002-09-06 | 2008-04-23 | セントラル硝子株式会社 | 光学活性１−（フルオロ、トリフルオロメチルまたはトリフルオロメトキシ置換フェニル）アルキルアミンｎ−モノアルキル誘導体とその製造方法 |
| JP2006516581A (ja) * | 2003-01-27 | 2006-07-06 | グラクソ グループ リミテッド | 機能性消化不良を治療するための化学化合物の使用 |
| GB0308968D0 (en) * | 2003-04-17 | 2003-05-28 | Glaxo Group Ltd | Medicaments |
| WO2004110996A1 (en) * | 2003-06-19 | 2004-12-23 | Pfizer Products Inc. | Nk1 antagonist |
| US20060148782A1 (en) * | 2003-11-10 | 2006-07-06 | Lundeen James E | Method and medicine for treating a mammal presenting urinary incontinence, urinary urgency, or both |
| US20050113365A1 (en) * | 2003-11-10 | 2005-05-26 | Sir Isaac Newton Enterprises Llc | Method and medicine for treating gastrointestinal disorder including irritable bowel syndrome |
| US20060148783A1 (en) * | 2003-11-10 | 2006-07-06 | Lundeen James E | Method and medicine for treating gastrointestinal disorder including fecal incontinence |
| US20060148781A1 (en) * | 2003-11-10 | 2006-07-06 | Lundeen James E | Method and medicine for treating gastrointestinal disorder in a non-human mammal |
| US20070142367A1 (en) * | 2003-11-10 | 2007-06-21 | Lundeen James E | Method and medicine for treating gastrointestinal disorder including fecal incontinence |
| US7390905B2 (en) * | 2003-11-28 | 2008-06-24 | Mitsubishi Tanabe Pharma Corporation | Piperidine compound and process for preparing the same |
| CA2552965A1 (en) * | 2004-01-14 | 2005-07-28 | Takeda Pharmaceutical Company Limited | Carboxamide derivative and use thereof |
| TW200730494A (en) * | 2005-10-10 | 2007-08-16 | Glaxo Group Ltd | Novel compounds |
| DE602006015215D1 (de) * | 2005-10-10 | 2010-08-12 | Glaxo Group Ltd | Prolinamidderivate als natriumkanalmodulatoren |
| US20100009983A1 (en) * | 2006-05-09 | 2010-01-14 | Braincells, Inc. | 5 ht receptor mediated neurogenesis |
| JP4904945B2 (ja) | 2006-06-30 | 2012-03-28 | セントラル硝子株式会社 | 光学活性１−（フルオロ、トリフルオロメチルまたはトリフルオロメトキシ置換フェニル）アルキルアミンｎ−モノアルキル誘導体の製造方法 |
| GB0621229D0 (en) * | 2006-10-20 | 2006-12-06 | Glaxo Group Ltd | Novel use |
| US8093268B2 (en) | 2007-01-24 | 2012-01-10 | Glaxo Group Limited | Pharmaceutical compositions comprising 2-methoxy-5-(5-trifluoromethyl-tetrazol-1-yl-benzyl)-(2S-phenylpiperidin-3S-yl-) |
| JP5510040B2 (ja) * | 2010-04-28 | 2014-06-04 | セントラル硝子株式会社 | 光学活性（ｒ）−１−（４−フルオロフェニル）エチルアミンを得る光学分割 |
| WO2012175434A1 (en) | 2011-06-20 | 2012-12-27 | Glaxo Group Limited | Pharmaceutical formulations comprising vestipitant |
| DK2729147T3 (en) | 2011-07-04 | 2017-12-18 | Irbm - Science Park S P A | NK-1 RECEPTOR ANTAGONISTS FOR TREATMENT OF CORNOVA |
| PL2817312T3 (pl) * | 2012-02-22 | 2016-08-31 | Leo Pharma As | Nowe związki będące antagonistami receptora neurokininy 1 |
| WO2015024203A1 (en) | 2013-08-20 | 2015-02-26 | Leo Pharma A/S | Novel neurokinin 1 receptor antagonist compounds ii |
| WO2016102967A1 (en) | 2014-12-23 | 2016-06-30 | Convergence Pharmaceuticals Limited | Process for preparing alpha-carboxamide pyrrolidine derivatives |
| WO2017099049A1 (ja) | 2015-12-07 | 2017-06-15 | キッセイ薬品工業株式会社 | Ｎｋ１受容体拮抗剤 |
| IL312486B1 (en) | 2017-04-10 | 2025-01-01 | Chase Therapeutics Corp | NK1 antagonist combination and method for treating synucleinopathies |
| MX2019015150A (es) | 2017-06-30 | 2020-08-13 | Chase Therapeutics Corp | Composiciones antagonistas de nk-1 y métodos para su uso en el tratamiento de la depresión. |
| AU2018346763A1 (en) | 2017-10-05 | 2020-04-16 | Biogen Inc. | Process for preparing alpha-carboxamide pyrolidine derivatives |
Family Cites Families (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL47168A (en) | 1974-05-09 | 1979-07-25 | Toyama Chemical Co Ltd | Mono or dioxo piperazino(thio)carbonylamino derivatives ofpenicillins and cephalosporins and process for producing the same |
| US4219554A (en) | 1974-05-09 | 1980-08-26 | Toyama Chemical Company, Limited | Novel penicillins and cephalosporins and process for producing same |
| US4110327A (en) | 1974-05-09 | 1978-08-29 | Toyama Chemical Co., Ltd. | 2,3 Diketo-piperazinocarbonylamino alkanoic acids and derivatives |
| US4327097A (en) | 1974-05-09 | 1982-04-27 | Toyama Chemical Co., Ltd. | Novel penicillins |
| US4379152A (en) | 1974-05-09 | 1983-04-05 | Toyama Chemical Co., Ltd. | Cephalosporins |
| US4087424A (en) | 1974-05-09 | 1978-05-02 | Toyama Chemical Co., Ltd. | Novel penicillins and cephalosporins and process for producing the same |
| US4410522A (en) | 1974-05-09 | 1983-10-18 | Toyama Chemical Co., Ltd. | Cephalosporins |
| US4112090A (en) | 1974-05-09 | 1978-09-05 | Toyama Chemical Co., Ltd. | Novel penicillins and cephalosporins and process for producing the same |
| NO154582C (no) * | 1978-10-20 | 1986-11-05 | Ferrosan Ab | Analogifremgangsmaate for fremstilling av terapeutisk aktive difenyl-dibutylpiperazinkarboksamider. |
| JPS57118587A (en) | 1981-11-26 | 1982-07-23 | Toyama Chem Co Ltd | Novel penicillin |
| US5028610A (en) | 1987-03-18 | 1991-07-02 | Sankyo Company Limited | N-benzhydryl-substituted heterocyclic derivatives, their preparation and their use |
| GB8709666D0 (en) | 1987-04-23 | 1987-05-28 | Beecham Group Plc | Compounds |
| GB8713061D0 (en) | 1987-06-04 | 1987-07-08 | Beecham Group Plc | Compounds |
| US5109014A (en) | 1990-12-10 | 1992-04-28 | Jacobson Richard M | N-aryl-3-aryl-4-substituted-2,3,4,5-tetrahydro-1H-pyrazole-1-carboxamides |
| SE9100860D0 (sv) | 1991-03-22 | 1991-03-22 | Kabi Pharmacia Ab | New use |
| DK0533280T4 (da) | 1991-09-20 | 2005-02-28 | Glaxo Group Ltd | Ny medicinsk anvendelse af tachykininantagonister |
| CA2083891A1 (en) | 1991-12-03 | 1993-06-04 | Angus Murray Macleod | Heterocyclic compounds, compositions containing them and their use in therapy |
| US5563127A (en) | 1993-03-24 | 1996-10-08 | The Dupont Merck Pharmaceutical Company | Boronic acid and ester inhibitors of thrombin |
| US5348955A (en) | 1993-06-22 | 1994-09-20 | Merck & Co., Inc. | N,N-diacylpiperazines |
| IL111730A (en) | 1993-11-29 | 1998-12-06 | Fujisawa Pharmaceutical Co | Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same |
| TW385308B (en) | 1994-03-04 | 2000-03-21 | Merck & Co Inc | Prodrugs of morpholine tachykinin receptor antagonists |
| US5464788A (en) | 1994-03-24 | 1995-11-07 | Merck & Co., Inc. | Tocolytic oxytocin receptor antagonists |
| DE4425146A1 (de) | 1994-07-15 | 1996-01-18 | Basf Ag | Verwendung heterocyclischer Verbindungen |
| WO1996003378A1 (fr) | 1994-07-26 | 1996-02-08 | Sankyo Company, Limited | Derives d'amide n-phenyle et d'uree |
| US5696123A (en) | 1994-09-17 | 1997-12-09 | Boehringer Ingelheim Kg | Neurokinin antagonists |
| DE19520499C2 (de) | 1994-09-17 | 2003-06-18 | Boehringer Ingelheim Kg | Neurokinin-Antagonisten, Verfahren zu ihrer Herstellung, diese Verbindungen enthaltende pharmazeutische Zusammensetzungen sowie ihre Verwendung |
| US5998444A (en) | 1995-10-24 | 1999-12-07 | Zeneca Ltd. | Piperidinyl compounds as NK1 or NK2 antagonists |
| EP0709375B1 (en) | 1994-10-25 | 2005-05-18 | AstraZeneca AB | Therapeutic heterocycles |
| US5629322A (en) | 1994-11-15 | 1997-05-13 | Merck & Co., Inc. | Cyclic amidine analogs as inhibitors of nitric oxide synthase |
| US5576317A (en) | 1994-12-09 | 1996-11-19 | Pfizer Inc. | NK-1 receptor antagonists and 5HT3 receptor antagonists for the treatment of emesis |
| MX9704745A (es) | 1994-12-23 | 1997-10-31 | Thomae Gmbh Dr K | Derivados de piperazina, medicamentos que contienen estos compuestos, su empleo y procedimientos para su preparacion. |
| US5700801A (en) | 1994-12-23 | 1997-12-23 | Karl Thomae, Gmbh | Piperazine derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them |
| NZ321575A (en) | 1995-10-30 | 1999-05-28 | Janssen Pharmaceutica Nv | 1-(1,2-disubstituted piperidinyl)-4- substituted piperazine derivatives |
| DE19608665A1 (de) | 1996-03-06 | 1997-09-11 | Boehringer Ingelheim Kg | Neue Arylglycinamidderivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
| US6057323A (en) | 1996-03-08 | 2000-05-02 | Adolor Corporation | Kappa agonist compounds pharmaceutical formulations and method of prevention and treatment of pruritus therewith |
| WO1997036593A1 (en) | 1996-04-03 | 1997-10-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| US5859012A (en) | 1996-04-03 | 1999-01-12 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| WO1997036592A1 (en) | 1996-04-03 | 1997-10-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| JP2000507576A (ja) | 1996-04-03 | 2000-06-20 | メルク エンド カンパニー インコーポレーテッド | ファルネシル―タンパク質トランスフェラーゼ阻害剤 |
| WO1998001133A1 (fr) | 1996-07-08 | 1998-01-15 | Yamanouchi Pharmaceutical Co., Ltd. | Inhibiteurs de la resorption osseuse |
| CA2260269A1 (en) * | 1996-07-17 | 1998-01-22 | Merck & Co., Inc. | Alteration of circadian rhythmicity with a tachykinin antagonist |
| US6117855A (en) | 1996-10-07 | 2000-09-12 | Merck Sharp & Dohme Ltd. | Use of a NK-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent |
| US5929077A (en) | 1996-11-08 | 1999-07-27 | Leftheris; Katerina | Thioproline-containing inhibitors of farnesyl protein transferase |
| EP0942730A1 (en) | 1996-12-02 | 1999-09-22 | MERCK SHARP & DOHME LTD. | Use of nk-1 receptor antagonists for treating bipolar disorders |
| US6114315A (en) | 1996-12-02 | 2000-09-05 | Merck Sharp & Dohme Ltd. | Use of NK-1 receptor antagonists for treating major depressive disorders with anxiety |
| US5977104A (en) | 1996-12-02 | 1999-11-02 | Merck Sharp & Dohme Ltd. | Use of NK-1 receptor antagonists for treating bipolar disorders |
| AUPO735997A0 (en) | 1997-06-17 | 1997-07-10 | Fujisawa Pharmaceutical Co., Ltd. | Piperazine derivatives |
| WO1999009985A1 (en) | 1997-08-27 | 1999-03-04 | Merck & Co., Inc. | Inhibitors of prenyl-protein transferase |
| DE69824037T2 (de) | 1997-11-24 | 2005-06-02 | Merck & Co., Inc. | Beta-alanin-derivate als zell-adhäsions-inhibitoren |
| CN1152877C (zh) * | 1998-12-14 | 2004-06-09 | 藤泽药品工业株式会社 | 哌嗪衍生物 |
| GB9923748D0 (en) * | 1999-10-07 | 1999-12-08 | Glaxo Group Ltd | Chemical compounds |
| WO2001030348A1 (en) * | 1999-10-25 | 2001-05-03 | 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 |
| US20030022891A1 (en) | 2000-12-01 | 2003-01-30 | Anandan Palani | MCH antagonists and their use in the treatment of obesity |
| MY141736A (en) | 2002-10-08 | 2010-06-15 | Elanco Animal Health Ireland | Substituted 1,4-di-piperidin-4-yi-piperazine derivatives and their use as neurokinin antagonists |
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1999
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