AR050347A1 - Derivados de tetrahidrocarbazol con accion biologica mejorada y solubilidad mejorada, como ligandos para receptores acoplados de proteina-g (gpcr's) - Google Patents
Derivados de tetrahidrocarbazol con accion biologica mejorada y solubilidad mejorada, como ligandos para receptores acoplados de proteina-g (gpcr's)Info
- Publication number
- AR050347A1 AR050347A1 ARP050102900A ARP050102900A AR050347A1 AR 050347 A1 AR050347 A1 AR 050347A1 AR P050102900 A ARP050102900 A AR P050102900A AR P050102900 A ARP050102900 A AR P050102900A AR 050347 A1 AR050347 A1 AR 050347A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- radical
- group
- aryl
- nr12r12
- Prior art date
Links
- XKLNOVWDVMWTOB-UHFFFAOYSA-N 2,3,4,9-tetrahydro-1h-carbazole Chemical class N1C2=CC=CC=C2C2=C1CCCC2 XKLNOVWDVMWTOB-UHFFFAOYSA-N 0.000 title abstract 2
- 102000003688 G-Protein-Coupled Receptors Human genes 0.000 title 1
- 108090000045 G-Protein-Coupled Receptors Proteins 0.000 title 1
- 230000031018 biological processes and functions Effects 0.000 title 1
- 102000005962 receptors Human genes 0.000 title 1
- 108020003175 receptors Proteins 0.000 title 1
- -1 alkylaryl radicals Chemical class 0.000 abstract 13
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 2
- 150000005840 aryl radicals Chemical class 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 1
- 150000007513 acids Chemical class 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 1
- 125000005213 alkyl heteroaryl group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 150000007529 inorganic bases Chemical class 0.000 abstract 1
- 150000007522 mineralic acids Chemical class 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 238000006386 neutralization reaction Methods 0.000 abstract 1
- 230000003472 neutralizing effect Effects 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 150000007524 organic acids Chemical class 0.000 abstract 1
- 235000005985 organic acids Nutrition 0.000 abstract 1
- 150000007530 organic bases Chemical class 0.000 abstract 1
- 150000003254 radicals Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/56—Ring systems containing three or more rings
- C07D209/80—[b, c]- or [b, d]-condensed
- C07D209/82—Carbazoles; Hydrogenated carbazoles
- C07D209/88—Carbazoles; Hydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/18—Feminine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/56—Ring systems containing three or more rings
- C07D209/80—[b, c]- or [b, d]-condensed
- C07D209/82—Carbazoles; Hydrogenated carbazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Virology (AREA)
- Reproductive Health (AREA)
- Neurology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Gynecology & Obstetrics (AREA)
- Oncology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Immunology (AREA)
- Hospice & Palliative Care (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Medicamentos que contienen uno o más de los compuestos como sustancia activa. Reivindicacion 1: Compuestos de tetrahidrocarbazol caracterizados porque tienen la formula general (1) en la que: X1 significa S u O; X2 y X3, independientemente entre sí, significan O o H2 acoplado en posicion geminal; R1 y R2, independientemente entre sí, se eligieron del grupo consistente en -H, radicales arilo, alquilo y alquilarilo, que eventualmente están sustituidos en el grupo alquilo y/o arilo por hasta 3 sustituyentes, seleccionados independientemente entre sí del grupo consistente en -Hal, -CN, y -O-alquilo, significando en especial R1 y R2 en cada caso un átomo de H; R3 significa un radical alquilo, arilalquilo o heteroarilalquilo, que eventualmente están sustituidos por hasta 3 sustituyentes, sselecccionados independientemente entre sí del grupo consistente en -Hal, -CN, -CO-O-R12, -CO-NR12R12', -OH, -O-R13, -O-CO-R13, -O-SO2-OR12, -O-SO2-R12, -SO2-R12, -SO-R12, -O- PO(OR12)(OR12'), -O-PO(NR12R12')2, -O-CO-O-R13, -O-CO-NR12R12', -O-CS-NR12R12', -S-R12, -NR12R12', -NH-CO-R13, -NH-SO2-R12, -NH-CO-O-R13, -NH-CO-NHR12, -NH-C(NH)-NH2; R4, R5, R6 y R7, independientemente entre sí, se seleccionaron del grupo consistente en -Hal, -CN, -CONH2, -COOH, -CF3, -O-alquilo, -OCF3, -NO2, y radicales alquilo, arilalquilo y heteroarilalquilo; R9 significa un átomo de H, un radical alquilo, un radical arilo, un radical heteroarilo, un radical arilalquilo o un radical heteroarilalquilo, preferiblemente un átomo de H; R10 significa un átomo de H, o el radical -R11, -CO-R11, -CO-OR11, -CO-NHR11, -C(NH)-NHR11, -SO2-R11, o -SO2-NHR11; R11 significa un radical alquilo, un radical arilo, un radical arilalquilo o un radical heteroarilalquilo, que eventualmente están sustituidos por uno o varios sustituyentes, seleccionados independientemente entre sí del grupo consistente en -Hal, -CN, -alquilo, -CF3, -OCF3, -OH, -O-alquilo, y -O-(CH2CH2-O)n-CH3; R8 significa -alquil-C1-6-arilo o -alquil-C1-6-heteroarilo, estando el grupo arilo o heteroarilo sustituido por uno hasta tres, preferiblemente por un sustituyente seleccionado independientemente del grupo consistente en -O-(CH2CH2-O)n-CH3, -O-CO-R12, - O-CO-(CH2CH2-O)n-CH3, -O-SO2-OR12, -O-SO2-R12, -O-PO(OR123)(OR12'), -O-PO(NR12R12')2, -O-CO-OR13, -O-CO-NR12R12', y -O-CS-NR12R12', o, siempre y cuando por lo menos: (i) X1 significa igual a S, o (ii) R10 no significa H y R11 es un radical arilalquilo o heteroarilalquilo, que en el grupo arilo o heteroarilo están sustituidos por uno o varios sustituyentes, independientemente entre sí seleccionados del grupo consistente en -hal, -CN, -alquilo, -CF3, -OCF3, -OH, -O-alquilo, y -O-(CH2CH2- O)n-CH3; R8 también adquiere los significados indicados para R3; R12 y R12', independientemente entre sí, significan H, o un radical alquilo, arilalquilo, arilo, heteoarilalquilo, o heteoarilo, y preferiblemente H; R13 se selecciona de un radical alquilo, arilalquilo, arilo, heteoarilalquilo, y heteroarilo, o significa el grupo -(CH2CH2-O)n-CH3; y n representa un numero entero de 1 a 10, preferiblemente de 1 a 6. Como también sales fisiologicamente tolerables, derivados o análogos del compuesto de la formula general (1), siendo las sales obtenibles por neutralizacion de las bases con ácidos inorgánicos u orgánicos o mediante neutralizzcion de los ácidos con bases inorgánicas u orgánicas, pudiendo el compuesto de la formula general (1), como también sus sals, derivados o análogos, encontrarse presente en forma de sus racematos, en forma de sus enantiomeros puros y/o diastereomeros o en forma de mezclas de estos enantiomeros y/o diastereomeros, en forma de los tautomeros, sus solvatos e hidratos y de sus forma polimorfas.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US58796904P | 2004-07-14 | 2004-07-14 | |
| DE102004033902A DE102004033902A1 (de) | 2004-07-14 | 2004-07-14 | Neue Tetrahydrocarbazolderivate mit verbesserter biologischer Wirkung und verbesserter Löslichkeit als Liganden für G-Protein gekoppelte Rezeptoren (GPCR's) |
| US68317805P | 2005-05-20 | 2005-05-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR050347A1 true AR050347A1 (es) | 2006-10-18 |
Family
ID=35045230
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050102900A AR050347A1 (es) | 2004-07-14 | 2005-07-13 | Derivados de tetrahidrocarbazol con accion biologica mejorada y solubilidad mejorada, como ligandos para receptores acoplados de proteina-g (gpcr's) |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US7375127B2 (es) |
| EP (2) | EP1765776B1 (es) |
| JP (1) | JP4746617B2 (es) |
| KR (1) | KR100888895B1 (es) |
| CN (1) | CN1997629B (es) |
| AR (1) | AR050347A1 (es) |
| AT (1) | ATE406352T1 (es) |
| AU (1) | AU2005261930B2 (es) |
| BR (1) | BRPI0513209A (es) |
| CA (1) | CA2565850C (es) |
| CY (1) | CY1110415T1 (es) |
| DE (2) | DE102004033902A1 (es) |
| DK (1) | DK1765776T3 (es) |
| ES (1) | ES2315887T3 (es) |
| HR (1) | HRP20080533T3 (es) |
| IL (1) | IL179067A (es) |
| MX (1) | MXPA06014447A (es) |
| NO (1) | NO20070688L (es) |
| NZ (1) | NZ551314A (es) |
| PL (1) | PL1765776T3 (es) |
| PT (1) | PT1765776E (es) |
| RS (1) | RS50684B (es) |
| SI (1) | SI1765776T1 (es) |
| TW (1) | TWI316933B (es) |
| WO (1) | WO2006005484A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7371336B2 (en) | 2002-09-24 | 2008-05-13 | E.I. Du Pont Nemours And Company | Water dispersible polyanilines made with polymeric acid colloids for electronics applications |
| EP1967202A1 (en) * | 2007-03-05 | 2008-09-10 | AEterna Zentaris GmbH | Use of LHRH Antagonists for the Treatment of Lower Urinary Tract Symptoms, in particular Overactive Bladder and/or Detrusor Overactivity |
| EP1988098A1 (en) | 2007-04-27 | 2008-11-05 | AEterna Zentaris GmbH | Novel Tetrahydrocarbazole Derivatives as Ligands of G-protein Coupled Receptors |
| EP2095818A1 (en) * | 2008-02-29 | 2009-09-02 | AEterna Zentaris GmbH | Use of LHRH antagonists at non-castrating doses |
| US9175211B2 (en) * | 2010-03-03 | 2015-11-03 | Universal Display Corporation | Phosphorescent materials |
| JP6263773B2 (ja) * | 2011-02-23 | 2018-01-24 | マサチューセッツ インスティテュート オブ テクノロジー | 水溶性膜タンパク質およびその調製および使用方法 |
| CN114306335A (zh) | 2015-05-18 | 2022-04-12 | 康堤医疗有限公司 | 用于治疗性激素依赖性疾病的双重nk-1/nk-3受体拮抗剂 |
| WO2019175253A1 (en) | 2018-03-14 | 2019-09-19 | KaNDy Therapeutics Limited | Novel pharmaceutical formulation comprising dual nk-1/nk-3 receptor antagonists |
| CN117143027B (zh) * | 2023-08-31 | 2024-12-20 | 四川大学 | 3-苄氧基-6-羟苯基哒嗪类化合物及其制备方法和用途 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1418703A (en) | 1973-06-02 | 1975-12-24 | Pfizer Ltd | 3-alkyl-9-substituted-1,2,3,4-tetrahydrocarbazoles |
| EP0239306B1 (en) | 1986-03-27 | 1993-06-02 | Merck Frosst Canada Inc. | Tetrahydrocarbazole esters |
| EP0603432B1 (en) | 1992-12-18 | 1998-10-21 | Smithkline Beecham Plc | Tetrahydrocarbazole derivatives for the manufacture of a medicament for the treatment of a disease where a 5-HT1-like agonist is indicated |
| TW449600B (en) | 1994-04-19 | 2001-08-11 | Takeda Chemical Industries Ltd | Condensed-ring thiophene derivatives, their production and use |
| US5607939A (en) | 1994-04-28 | 1997-03-04 | Takeda Chemical Industries, Ltd. | Condensed heterocyclic compounds, their production and use |
| US5576317A (en) * | 1994-12-09 | 1996-11-19 | Pfizer Inc. | NK-1 receptor antagonists and 5HT3 receptor antagonists for the treatment of emesis |
| UY23948A1 (es) | 1995-02-08 | 2001-10-25 | Takeda Chemical Industries Ltd | Derivados de anillos condensados de tiofeno su producción y uso. |
| EP0876349B1 (en) | 1995-10-19 | 2002-09-11 | Takeda Chemical Industries, Ltd. | Quinoline derivatives as gnrh antagonists |
| AU7333396A (en) | 1995-10-19 | 1997-05-07 | Takeda Chemical Industries Ltd. | Thienopyridine derivatives as gonadotropin releasing hormone antagonists |
| SK77598A3 (en) | 1995-12-14 | 1999-01-11 | Merck & Co Inc | Nonpeptide derivatives, pharmaceutical composition containing them and their use |
| CA2240115A1 (en) | 1995-12-14 | 1997-06-19 | Wallace T. Ashton | Antagonists of gonadotropin releasing hormone |
| US6200957B1 (en) | 1995-12-14 | 2001-03-13 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| AU2406597A (en) | 1996-04-26 | 1997-11-19 | Takeda Chemical Industries Ltd. | Thienopyridine derivatives, their production and use |
| US5708187A (en) * | 1996-06-27 | 1998-01-13 | Eli Lilly And Company | 6-substituted-1,2,3,4-tetrahydro-9H-carbazoles and 7-substituted-10H-cyclohepta 7,6-B!indoles: New 5-HT1F agonists |
| EP0882736A1 (en) * | 1997-06-02 | 1998-12-09 | Laboratoire Theramex S.A. | LH-RH peptide analogues, their uses and pharmaceutical compositions containing them |
| JP2002502426A (ja) | 1997-06-05 | 2002-01-22 | メルク エンド カンパニー インコーポレーテッド | ゴナドトロピン放出ホルモンの拮抗薬 |
| AU728988B2 (en) | 1997-06-05 | 2001-01-25 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| WO1998055479A1 (en) | 1997-06-05 | 1998-12-10 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| DE19728737C1 (de) | 1997-07-04 | 1999-02-11 | Johannes Christian Groeninghen | Verfahren zur Erkennung und Bestimmung von GnRH-Rezeptoren und die Verwendung von GnRH-Agonisten und GnRH-Antagonisten zur Behandlung eines Tumors ausgehend vom Hirn und/oder Nervensystem und/oder den Hirnhäuten |
| EP1027046A4 (en) | 1997-10-28 | 2002-04-03 | Merck & Co Inc | GONADOTROPIN RELEASING HORMON ANTAGONISTS |
| CA2326140A1 (en) | 1998-04-02 | 1999-10-14 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| CA2325995A1 (en) | 1998-04-02 | 1999-10-14 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| AU3868500A (en) | 1999-03-10 | 2000-09-28 | Merck & Co., Inc. | 6-azaindole compounds as antagonists of gonadotropin releasing hormone |
| EP1171125A1 (en) | 1999-03-10 | 2002-01-16 | Merck & Co., Inc. | 6-azaindole compounds as antagonists of gonadotropin releasing hormone |
| US20020065309A1 (en) | 1999-08-04 | 2002-05-30 | Ge Peng | Novel Bicyclic and tricyclic pyrrolidine derivatives as GnRH antagonists |
| AU2002324586B2 (en) | 2001-08-02 | 2008-04-24 | Neurocrine Biosciences, Inc. | 1,3,5-triazine-2,4,6-triones, preparation and use as gonadotropin-releasing hormone receptor antagonists |
| MXPA04000985A (es) | 2001-08-02 | 2005-02-17 | Neurocrine Biosciences Inc | Piridin-4-onas sustituidas y su uso como antagonistas del receptor de hormona de liberacion de gonadotropina. |
| DE10164564B4 (de) * | 2001-12-14 | 2007-05-16 | Zentaris Gmbh | Tetrahydrocarbazolderivate als Liganden für G-Protein gekoppelte Rezeptoren (GPCR) |
| CA2468880A1 (en) | 2001-12-14 | 2003-06-26 | Zentaris Gmbh | Tetrahydrocarbazole derivatives as ligands for g-protein coupled receptors (gpcr) |
| GB0206219D0 (en) | 2002-03-15 | 2002-05-01 | Ferring Bv | Non-Peptide GnRH antagonists |
| WO2005033099A2 (en) | 2003-10-03 | 2005-04-14 | Glenmark Pharmaceuticals Ltd. | Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof |
-
2004
- 2004-07-14 DE DE102004033902A patent/DE102004033902A1/de not_active Withdrawn
-
2005
- 2005-06-30 US US11/172,142 patent/US7375127B2/en not_active Expired - Fee Related
- 2005-07-05 PT PT05764033T patent/PT1765776E/pt unknown
- 2005-07-05 AU AU2005261930A patent/AU2005261930B2/en not_active Ceased
- 2005-07-05 EP EP05764033A patent/EP1765776B1/de not_active Expired - Lifetime
- 2005-07-05 CA CA2565850A patent/CA2565850C/en not_active Expired - Fee Related
- 2005-07-05 BR BRPI0513209-6A patent/BRPI0513209A/pt not_active IP Right Cessation
- 2005-07-05 EP EP08162452A patent/EP1995238A3/de not_active Withdrawn
- 2005-07-05 CN CN2005800220208A patent/CN1997629B/zh not_active Expired - Fee Related
- 2005-07-05 HR HR20080533T patent/HRP20080533T3/xx unknown
- 2005-07-05 JP JP2007520710A patent/JP4746617B2/ja not_active Expired - Fee Related
- 2005-07-05 ES ES05764033T patent/ES2315887T3/es not_active Expired - Lifetime
- 2005-07-05 PL PL05764033T patent/PL1765776T3/pl unknown
- 2005-07-05 DK DK05764033T patent/DK1765776T3/da active
- 2005-07-05 NZ NZ551314A patent/NZ551314A/en not_active IP Right Cessation
- 2005-07-05 DE DE502005005206T patent/DE502005005206D1/de not_active Expired - Lifetime
- 2005-07-05 SI SI200530418T patent/SI1765776T1/sl unknown
- 2005-07-05 AT AT05764033T patent/ATE406352T1/de active
- 2005-07-05 RS RSP-2008/0561A patent/RS50684B/sr unknown
- 2005-07-05 KR KR1020077000903A patent/KR100888895B1/ko not_active Expired - Fee Related
- 2005-07-05 MX MXPA06014447A patent/MXPA06014447A/es active IP Right Grant
- 2005-07-05 WO PCT/EP2005/007255 patent/WO2006005484A1/de not_active Ceased
- 2005-07-08 TW TW094123208A patent/TWI316933B/zh active
- 2005-07-13 AR ARP050102900A patent/AR050347A1/es unknown
-
2006
- 2006-11-06 IL IL179067A patent/IL179067A/en not_active IP Right Cessation
-
2007
- 2007-02-06 NO NO20070688A patent/NO20070688L/no not_active Application Discontinuation
-
2008
- 2008-02-14 US US12/070,214 patent/US8067456B2/en not_active Expired - Fee Related
- 2008-11-19 CY CY20081101329T patent/CY1110415T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR076264A1 (es) | Triazolopiridinas sustituidas y analogos de estas | |
| CL2020001546A1 (es) | Compuestos de 4-azaindol. | |
| PE20180030A1 (es) | Compuestos biciclicos de sulfonamida cetona | |
| PE20060932A1 (es) | Derivados de sulfonamidas como moduladores de receptores de glucocorticoides (gr) | |
| AR082029A1 (es) | Derivados de heterociclos nitrogenados, composiciones y metodos para modular la via de señalizacion de wnt | |
| AR058554A1 (es) | Compuestos heterociclicos nitrogenados de 6 miembros sustituidos, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades mediadas por mglur5. | |
| AR083367A1 (es) | Compuestos de tipo quinazolinona como antagonistas de crth | |
| ES2308299T3 (es) | Tiadiazoles como ligandos de receptores de cxc-y cc-quimioquinas. | |
| CO6280476A2 (es) | Derivados de alcanos azabiciclicos sustituidos con biarilo como moduladores de la actividad de los receptores nicotinicos de acetilcolina | |
| AR084766A1 (es) | Compuesto biciclico para modular los receptores acoplados a la proteina g | |
| PE20171511A1 (es) | Compuestos de piperidina urea 4-metilsulfonil-sustituidos para el tratamiento de miocardiopatia dilatada (mcd) | |
| AR079205A1 (es) | Morfolinotiazoles como moduladores alostericos positivos alfa 7 | |
| AR074817A1 (es) | Dihidropiridona-amidas como moduladores de p2x7 | |
| AR050347A1 (es) | Derivados de tetrahidrocarbazol con accion biologica mejorada y solubilidad mejorada, como ligandos para receptores acoplados de proteina-g (gpcr's) | |
| AR056511A1 (es) | Derivados de 2-aminopirimidinas, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por el receptor de histamina h4 | |
| PE20060336A1 (es) | Compuestos derivados de 1-amino-ftalazina como moduladores de mch1 | |
| PE20060583A1 (es) | Tiazolil-dihidro-indazoles como inhibidores de pi3-quinasas | |
| AR082111A1 (es) | Furopiridinas o tienopiridinas condensadas, composiciones farmaceuticas que las contienen utiles para tratar trastornos psicoticos y del sistema nervioso central, y metodo de preparacion de las mismas | |
| AR048789A1 (es) | Derivados de oxazol y sus composiciones como moduladores de receptor activado de proliferador de peroxisoma (ppar) | |
| UY31388A1 (es) | Método para la producción de 2´-desoxi-5-azacitidina (decitabina) | |
| AR061835A1 (es) | Derivados tetraciclicos, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen | |
| AR042362A1 (es) | Derivados de 3h-quinazolin-4-ona, proceso de obtencion y composiciones farmaceuticas que los contienen | |
| CO6341626A2 (es) | Proceso para la preparacion de derivados de benzoimidazol-2-il pirimidina | |
| AR096160A1 (es) | Inhibidores de nicotamida fosforibosiltransferasa, composiciones, productos y usos de los mismos | |
| AR119792A1 (es) | Derivados de pirazolo[4,3-c]piridina y composiciones farmacéuticas para el tratamiento de patologías inflamatorias |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |