ECSP11011167A - Síntesis y formas de sales novedosas de (r) -5- ( (e) -2- (pirrolidin-3-ilvinil) pirimidina - Google Patents
Síntesis y formas de sales novedosas de (r) -5- ( (e) -2- (pirrolidin-3-ilvinil) pirimidinaInfo
- Publication number
- ECSP11011167A ECSP11011167A EC2011011167A ECSP11011167A ECSP11011167A EC SP11011167 A ECSP11011167 A EC SP11011167A EC 2011011167 A EC2011011167 A EC 2011011167A EC SP11011167 A ECSP11011167 A EC SP11011167A EC SP11011167 A ECSP11011167 A EC SP11011167A
- Authority
- EC
- Ecuador
- Prior art keywords
- pyrimidine
- forms
- synthesis
- ilvinil
- pirrolidin
- Prior art date
Links
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title abstract 2
- 230000015572 biosynthetic process Effects 0.000 title abstract 2
- 238000003786 synthesis reaction Methods 0.000 title abstract 2
- 150000003839 salts Chemical group 0.000 abstract 2
- 230000000707 stereoselective effect Effects 0.000 abstract 1
Classifications
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
-
- 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
- A61P1/10—Laxatives
-
- 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
-
- 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
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D207/06—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 radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente invención se relaciona con la síntesis estereoespecífica de R)-5-((E)-2-pirrolidin-3-ilvinil) pirimidina, sus formas de sales y formas polimórficas novedosas de estas sales.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11879608P | 2008-12-01 | 2008-12-01 | |
| PCT/US2009/066078 WO2010065443A1 (en) | 2008-12-01 | 2009-11-30 | Synthesis and novel salt forms of (r)-5-((e)-2-(pyrrolidin-3-ylvinyl)pyrimidine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP11011167A true ECSP11011167A (es) | 2011-10-31 |
Family
ID=41650077
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2011011167A ECSP11011167A (es) | 2008-12-01 | 2011-06-29 | Síntesis y formas de sales novedosas de (r) -5- ( (e) -2- (pirrolidin-3-ilvinil) pirimidina |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US8604191B2 (es) |
| EP (2) | EP2364307B1 (es) |
| JP (1) | JP5710490B2 (es) |
| KR (1) | KR20110098763A (es) |
| CN (1) | CN102232070A (es) |
| AU (1) | AU2009322624B2 (es) |
| BR (1) | BRPI0922759A2 (es) |
| CA (2) | CA3090738C (es) |
| CL (1) | CL2011001258A1 (es) |
| CO (1) | CO6390106A2 (es) |
| DK (1) | DK3279195T3 (es) |
| EC (1) | ECSP11011167A (es) |
| ES (2) | ES2641762T3 (es) |
| HU (1) | HUE050540T2 (es) |
| IL (2) | IL266097B (es) |
| MX (1) | MX2011005611A (es) |
| NZ (3) | NZ703381A (es) |
| PE (1) | PE20110589A1 (es) |
| PL (1) | PL3279195T3 (es) |
| PT (1) | PT3279195T (es) |
| RU (2) | RU2533819C2 (es) |
| SG (2) | SG10201902903RA (es) |
| UA (1) | UA107336C2 (es) |
| WO (1) | WO2010065443A1 (es) |
| ZA (1) | ZA201103737B (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9145396B2 (en) * | 2008-12-01 | 2015-09-29 | Targacept, Inc. | Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3ylvinyl)pyrimidine |
| US20130237550A1 (en) * | 2010-03-11 | 2013-09-12 | Targacept, Inc. | Arylvinylazacycloalkane compounds for constipation |
| CN107106542B (zh) | 2014-10-20 | 2020-05-08 | 奥伊斯特普安生物制药公司 | 治疗眼部病状的方法 |
| NZ746468A (en) | 2016-04-07 | 2023-06-30 | Oyster Point Pharma Inc | Methods of treating ocular conditions |
| WO2020014217A1 (en) | 2018-07-10 | 2020-01-16 | Oyster Point Pharma, Inc. | Methods of treating ocular conditions |
| EP3820443A1 (en) | 2018-07-10 | 2021-05-19 | Oyster Point Pharma, Inc. | Combinations of positive allosteric modulators and nicotinic acetylcholine receptor agonists for treating ocular conditions |
| EP4142734B1 (en) | 2020-04-28 | 2025-08-20 | Oyster Point Pharma, Inc. | Local administration of nicotinic acetylcholine receptor agonists for the inhibition of coronavirus infections |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4649041A (en) * | 1983-07-20 | 1987-03-10 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of antinauseants |
| SU1605922A3 (ru) * | 1987-05-01 | 1990-11-07 | Фудзисава Фармасьютикал Ко., Лтд (Фирма) | Способ получени производных пирролидина или их солей |
| US5202128A (en) * | 1989-01-06 | 1993-04-13 | F. H. Faulding & Co. Limited | Sustained release pharmaceutical composition |
| IL107184A (en) | 1992-10-09 | 1997-08-14 | Abbott Lab | Heterocyclic ether compounds that enhance cognitive function |
| US5852041A (en) | 1993-04-07 | 1998-12-22 | Sibia Neurosciences, Inc. | Substituted pyridines useful as modulators of acethylcholine receptors |
| US5493026A (en) | 1993-10-25 | 1996-02-20 | Organix, Inc. | Substituted 2-carboxyalkyl-3-(fluorophenyl)-8-(3-halopropen-2-yl) nortropanes and their use as imaging for agents for neurodegenerative disorders |
| US5597919A (en) | 1995-01-06 | 1997-01-28 | Dull; Gary M. | Pyrimidinyl or Pyridinyl alkenyl amine compounds |
| US5604231A (en) | 1995-01-06 | 1997-02-18 | Smith; Carr J. | Pharmaceutical compositions for prevention and treatment of ulcerative colitis |
| US5585388A (en) | 1995-04-07 | 1996-12-17 | Sibia Neurosciences, Inc. | Substituted pyridines useful as modulators of acetylcholine receptors |
| ES2097703B1 (es) * | 1995-04-12 | 1997-12-01 | Decox S L | Una nueva composicion estimulante de la actividad cerebral basada en alcaloides de nucleo de eburnamenina, y sus metodos de preparacion. |
| US5583140A (en) | 1995-05-17 | 1996-12-10 | Bencherif; Merouane | Pharmaceutical compositions for the treatment of central nervous system disorders |
| IL118279A (en) | 1995-06-07 | 2006-10-05 | Abbott Lab | Compounds 3 - Pyridyloxy (or Thio) Alkyl Heterocyclic Pharmaceutical Compositions Containing Them and Their Uses for Preparing Drugs to Control Synaptic Chemical Transmission |
| US5726189A (en) | 1996-05-03 | 1998-03-10 | The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Method for imaging nicotinic acetylcholinergic receptors in the brain using radiolabeled pyridyl-7-azabicyclo 2.2.1!heptanes |
| US5795909A (en) * | 1996-05-22 | 1998-08-18 | Neuromedica, Inc. | DHA-pharmaceutical agent conjugates of taxanes |
| ZA9711092B (en) | 1996-12-11 | 1999-07-22 | Smithkline Beecham Corp | Novel compounds. |
| US5952339A (en) | 1998-04-02 | 1999-09-14 | Bencherif; Merouane | Pharmaceutical compositions and methods of using nicotinic antagonists for treating a condition or disorder characterized by alteration in normal neurotransmitter release |
| US6310043B1 (en) | 1998-08-07 | 2001-10-30 | Governors Of The University Of Alberta | Treatment of bacterial infections |
| US6761903B2 (en) * | 1999-06-30 | 2004-07-13 | Lipocine, Inc. | Clear oil-containing pharmaceutical compositions containing a therapeutic agent |
| JP2003513054A (ja) * | 1999-11-01 | 2003-04-08 | ターガセプト,インコーポレイテッド | アリールオレフィンアザ環式化合物及びアリールアセチレンアザ環式化合物、それらを含有する薬剤組成物、及び、ニコチンコリン作動性受容体の阻害薬としてのそれらの使用 |
| EP1302458A4 (en) * | 2000-07-11 | 2005-10-19 | Banyu Pharma Co Ltd | ESTERDERIVATE |
| WO2003013526A1 (en) * | 2001-08-08 | 2003-02-20 | Merck & Co. Inc. | Anticoagulant compounds |
| US6872827B2 (en) * | 2002-04-26 | 2005-03-29 | Chembridge Research Laboratories, Inc. | Somatostatin analogue compounds |
| US7098331B2 (en) * | 2003-03-05 | 2006-08-29 | Targacept, Inc. | Arylvinylazacycloalkane compounds and methods of preparation and use thereof |
| JP5162236B2 (ja) * | 2004-03-25 | 2013-03-13 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | イミダゾール化合物 |
| AR053364A1 (es) * | 2005-04-20 | 2007-05-02 | Smithkline Beecham | Compuesto de 1h-imidazo 84,5-c) piridin -2- ilo, composicion farmaceutica que lo comprende, proceso para prepararla y su uso para preparar un medicamento para tratamiento de cancer o artritis |
| US7598255B2 (en) * | 2005-08-04 | 2009-10-06 | Janssen Pharmaceutica Nv | Pyrimidine compounds as serotonin receptor modulators |
| US20060223820A1 (en) * | 2006-03-21 | 2006-10-05 | Chemagis Ltd. | Crystalline aripiprazole salts and processes for preparation and purification thereof |
| WO2008157365A2 (en) * | 2007-06-15 | 2008-12-24 | Targacept, Inc. | Vinylazacycloalkanes for treating neuropathic pain |
| TW201024283A (en) * | 2008-12-01 | 2010-07-01 | Targacept Inc | Synthesis and novel salt forms of (R)-3-((E)-2-(pyrrolidin-3-yl)vinyl)-5-(tetrahydropyran-4-yloxy)pyridine |
-
2009
- 2009-11-30 IL IL266097A patent/IL266097B/en unknown
- 2009-11-30 JP JP2011538710A patent/JP5710490B2/ja not_active Expired - Fee Related
- 2009-11-30 SG SG10201902903RA patent/SG10201902903RA/en unknown
- 2009-11-30 PL PL17179369T patent/PL3279195T3/pl unknown
- 2009-11-30 NZ NZ703381A patent/NZ703381A/en not_active IP Right Cessation
- 2009-11-30 CA CA3090738A patent/CA3090738C/en active Active
- 2009-11-30 PE PE2011001110A patent/PE20110589A1/es active IP Right Grant
- 2009-11-30 HU HUE17179369A patent/HUE050540T2/hu unknown
- 2009-11-30 WO PCT/US2009/066078 patent/WO2010065443A1/en not_active Ceased
- 2009-11-30 UA UAA201108206A patent/UA107336C2/ru unknown
- 2009-11-30 AU AU2009322624A patent/AU2009322624B2/en not_active Ceased
- 2009-11-30 CN CN2009801480732A patent/CN102232070A/zh active Pending
- 2009-11-30 RU RU2011127010/04A patent/RU2533819C2/ru active IP Right Revival
- 2009-11-30 US US13/129,898 patent/US8604191B2/en not_active Expired - Fee Related
- 2009-11-30 MX MX2011005611A patent/MX2011005611A/es active IP Right Grant
- 2009-11-30 DK DK17179369.8T patent/DK3279195T3/da active
- 2009-11-30 NZ NZ611965A patent/NZ611965A/en not_active IP Right Cessation
- 2009-11-30 ES ES09775408.9T patent/ES2641762T3/es active Active
- 2009-11-30 EP EP09775408.9A patent/EP2364307B1/en active Active
- 2009-11-30 ES ES17179369T patent/ES2820857T3/es active Active
- 2009-11-30 KR KR1020117014867A patent/KR20110098763A/ko not_active Ceased
- 2009-11-30 PT PT171793698T patent/PT3279195T/pt unknown
- 2009-11-30 SG SG10201406410UA patent/SG10201406410UA/en unknown
- 2009-11-30 NZ NZ592554A patent/NZ592554A/xx not_active IP Right Cessation
- 2009-11-30 BR BRPI0922759A patent/BRPI0922759A2/pt not_active IP Right Cessation
- 2009-11-30 EP EP17179369.8A patent/EP3279195B1/en active Active
- 2009-11-30 CA CA2742366A patent/CA2742366C/en active Active
-
2011
- 2011-05-09 IL IL212798A patent/IL212798B/en active IP Right Grant
- 2011-05-20 ZA ZA2011/03737A patent/ZA201103737B/en unknown
- 2011-05-30 CL CL2011001258A patent/CL2011001258A1/es unknown
- 2011-06-29 CO CO11081403A patent/CO6390106A2/es not_active Application Discontinuation
- 2011-06-29 EC EC2011011167A patent/ECSP11011167A/es unknown
-
2014
- 2014-09-11 RU RU2014136983A patent/RU2700796C2/ru active
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