FI120940B - Benzopyranderivat samt deras farmaceutiskt godtagbara salt, användning av nämnda racemiska benzopyranderivat och deras salter vid framställning av läkemedel avsett för vård av estrogenkänslig sjukdom och farmaceutisk sammansättning - Google Patents
Benzopyranderivat samt deras farmaceutiskt godtagbara salt, användning av nämnda racemiska benzopyranderivat och deras salter vid framställning av läkemedel avsett för vård av estrogenkänslig sjukdom och farmaceutisk sammansättning Download PDFInfo
- Publication number
- FI120940B FI120940B FI973426A FI973426A FI120940B FI 120940 B FI120940 B FI 120940B FI 973426 A FI973426 A FI 973426A FI 973426 A FI973426 A FI 973426A FI 120940 B FI120940 B FI 120940B
- Authority
- FI
- Finland
- Prior art keywords
- compound
- pharmaceutically acceptable
- phenyl
- compounds
- optically active
- Prior art date
Links
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
- A61K31/095—Sulfur, selenium, or tellurium compounds, e.g. thiols
- A61K31/10—Sulfides; Sulfoxides; Sulfones
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
-
- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
-
- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/382—Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
-
- 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
-
- 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
- A61K31/4025—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 not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/453—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
-
- 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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/46—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C215/64—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
- C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C217/06—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
- C07C217/14—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring
- C07C217/18—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
- C07C235/34—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/16—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C317/18—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D215/14—Radicals substituted by oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
- C07D217/14—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
- C07D217/16—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
-
- 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
- C07D295/08—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 singly bound oxygen or sulfur atoms
- C07D295/084—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 singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/088—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 singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
-
- 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
- C07D295/08—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 singly bound oxygen or sulfur atoms
- C07D295/096—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 singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
- C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
- C07D311/60—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 with aryl radicals attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
- C07D335/04—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D335/06—Benzothiopyrans; Hydrogenated benzothiopyrans
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0055—Estrane derivatives not substituted in position 17
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
- C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
- C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
- C07J1/0074—Esters
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0081—Substituted in position 17 alfa and 17 beta
- C07J1/0085—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being a saturated hydrocarbon group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J21/005—Ketals
- C07J21/006—Ketals at position 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J21/005—Ketals
- C07J21/008—Ketals at position 17
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
- C07J53/002—Carbocyclic rings fused
- C07J53/004—3 membered carbocyclic rings
- C07J53/008—3 membered carbocyclic rings in position 15/16
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0005—Oxygen-containing hetero ring
- C07J71/001—Oxiranes
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0005—Oxygen-containing hetero ring
- C07J71/001—Oxiranes
- C07J71/0021—Oxiranes at position 14(15)
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2602/00—Systems containing two condensed rings
- C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
- C07C2602/04—One of the condensed rings being a six-membered aromatic ring
- C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Toxicology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (13)
1. Optiskt aktiv förening eller farmaceutiskt godtagbara salt av denna förening (till-sammans med utspädningsmedel eller bärare eller utan dessa), nämnda förening 5 har molekylstrukturen I: TR β R2 i*3 * A JA-A· jQfyT 1 10 där R1 och R2 oberoende av varandra är valda ur gruppen i vilken ingär hydroxyl och en till hydroxyl in i//Voöverförbar del; 15 där R3 är -CH2 eller -CH2CH2-; och där nämnda förening eller salt innehäller over 50 % (med avseende pä alla stereo-isomerers vikt) stereoisomerer som har den absoluta konfigurationen 2S.
2. Optiskt aktiv förening enligt patentkravet 1, kännetecknad därav, att den är 20 vald ur gruppen CH3 ^oh * “ ° r jCx'x ” JÄT °
0 OuX) EM-661 eller ett farmaceutiskt godtagbart salt av nägondera ovannämnda.
3. Optiskt aktiv förening enligt patentkravet 1, vilken har följande molekylstruktur: CH / C(CH3)3 ί JOT ^ o AfVV o s aJQCI^ ^ (ch3)3c 0 0 ^ EM-800 eller ett farmaceutiskt godtagbart salt av denna förening. 10
4. Förening eller farmaceutiskt godtagbart salt av denna förening (tillsammans med utspädningsmedel eller bärare eller utan dessa), nämnda förening har molekylstruk-turen: X. Rz = x ry 15 joxr R' 7 0 ΤΤΛΊ3" Ijk xsVv där A' är en farmaceutiskt godtagbar syraanjon; 20 där R1 och R2 är valda oberoende av varandra ur gruppen i vilken ingär hydroxyl och en till hydroxyl in i//Voöverförbar del; och där R3 är -CH2 eller -CH2CH2-.
5. Förening enligt patentkravet 4, kännetecknad därav, att nämnda förening 25 eller dess salt är optiskt aktivt och innehäller over 50 % (räknat pä basis av alia stereoisomerer vikt) stereoisomerer med en absolut konfiguration 2S.
6. Förening enligt patentkravet 4, kännetecknad därav, att nämnda en förening 30 ?^OrOH ho^°U H o EM 796 L-HO2C<CH0H)2CO2'.
7. Optiskt aktiv förening enligt patentkravet 5, kännetecknad därav, att nämnda förening är vald ur gruppen i vilken ingär: , rjnrv® Or1” ° ’OU) EM 767 ϋ L-H02C(CH0H)2C02-, 10 CH, J CH2SOi" o o φο EM 769
8. Förening eller farmaceutiskt godtagbart sait av denna förening (tillsammans med utspädningsmedel eller bärare eller utan dessa), nämnda förening har molekylstruk- 20 turen: A * , Γ löi jOCo; 25 /x ^χ /N r3 - där R3 är -CH2 eller -CH2CH2-; och där R1 och R2 oberoende av varandra är valda ur gruppen i vilken ingär hydroxi, acyloxi 30 O I , -O-C-R, ja o -o-c-or" 5 (R4 är alkyl, alkenyl, alkynyl eller aryl; R7 är amino, alkylamino, aminoalkyl eller al-kylsulfanyl); och där ätminstone den ena av grupperna R1 eller R2 inte är hydroxi.
9. Förening enligt patentkravet 8, kännetecknad därav, att ätminstone den ena av grupperna R1 eller R2 är en hindrad alifatisk acyloxi.
10. Förening enligt patentkravet 8, kännetecknad därav, att nämnda förening är 10 vald ur gruppen i vilken ingär “πα .rf _EM 778_ _^_ 25 X oT; (CH3)3C 0A^O/\^ CH2S03· 30 lii H I I EM 793 ch3 0 0 EM 792 V L-H02C(CHOH)2C02* ja » 10 ch3 ^Y°Y™ ° jDTi^ 0 EM 762 ^ 15 CH3 j^ÄS-'0YCH(CH3)2 ? 0 EM-771 25 ch3 ifr\"°YNiCH^2 ° jöfi^ ° (CH3)2N^O''L^0''^=*,
30 EM-772 0^0 och farmaceutiskt godtagbara salter av vilken som heist av ovan nämnda förening-ar.
11. Förening eller salt enligt patentkravet 8, kännetecknad därav, att ätminstone en av grupperna R1 eller R2 är pivaloyloxi.
12. Användning av en förening eller ett sait enligt nägot av patentkraven 1-11 vid 5 tillverkning av ett läkemedelspreparat avsett för värd av sjukdomar som är känsliga för estrogen.
13. Farmaceutisk sammansättning, kännetecknad därav, att den innehäller ett farmaceutiskt godtagbart utspädningsmedel, en bärare eller ett utdrygningsmedel 10 och minst en förening eller ett sait enligt nägot av patentkraven 1-11.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US38820795 | 1995-02-21 | ||
US08/388,207 US6060503A (en) | 1991-12-02 | 1995-02-21 | Benzopyran-containing compounds and method for their use |
PCT/CA1996/000097 WO1996026201A1 (en) | 1995-02-21 | 1996-02-20 | Benzopyran-containing compounds and method for their use |
CA9600097 | 1996-02-20 |
Publications (3)
Publication Number | Publication Date |
---|---|
FI973426A0 FI973426A0 (sv) | 1997-08-21 |
FI973426A FI973426A (sv) | 1997-10-20 |
FI120940B true FI120940B (sv) | 2010-05-14 |
Family
ID=23533138
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
FI973426A FI120940B (sv) | 1995-02-21 | 1997-08-21 | Benzopyranderivat samt deras farmaceutiskt godtagbara salt, användning av nämnda racemiska benzopyranderivat och deras salter vid framställning av läkemedel avsett för vård av estrogenkänslig sjukdom och farmaceutisk sammansättning |
Country Status (28)
Country | Link |
---|---|
US (1) | US6060503A (sv) |
EP (2) | EP0811006B1 (sv) |
JP (1) | JPH11500133A (sv) |
KR (1) | KR100487647B1 (sv) |
CN (1) | CN1158274C (sv) |
AR (1) | AR004167A1 (sv) |
AT (2) | ATE240951T1 (sv) |
AU (1) | AU4660696A (sv) |
BR (1) | BR9607259A (sv) |
CA (1) | CA2212856C (sv) |
DE (2) | DE69627831T2 (sv) |
DK (2) | DK0811006T3 (sv) |
ES (2) | ES2197232T3 (sv) |
FI (1) | FI120940B (sv) |
HK (1) | HK1009440A1 (sv) |
HU (1) | HU227762B1 (sv) |
IL (2) | IL150767A (sv) |
MX (1) | MX9706345A (sv) |
MY (1) | MY117248A (sv) |
NO (2) | NO317055B1 (sv) |
NZ (1) | NZ301231A (sv) |
PL (1) | PL188076B1 (sv) |
PT (2) | PT811006E (sv) |
RU (1) | RU2220143C2 (sv) |
TR (1) | TR199600144A2 (sv) |
TW (1) | TW434238B (sv) |
WO (1) | WO1996026201A1 (sv) |
ZA (1) | ZA961316B (sv) |
Families Citing this family (52)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1999002512A1 (en) * | 1997-07-09 | 1999-01-21 | Novo Nordisk A/S | Dl-2,3-diaryl-2h-1-benzopyrans |
AU8102498A (en) * | 1997-07-09 | 1999-02-08 | Central Drug Research Institute | Preparation of diaryl-benzopyrans |
MXPA00008868A (es) | 1998-03-11 | 2003-04-25 | Endorech Inc | Inhibidores de dihidrogenasa de 17 -hidroxiesteroide y metodos para su uso. |
US7005428B1 (en) | 1998-06-11 | 2006-02-28 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
US6465445B1 (en) | 1998-06-11 | 2002-10-15 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
KR20000001793A (ko) * | 1998-06-13 | 2000-01-15 | 이경하 | 신규한 벤조피란 또는 티오벤조피란 유도체 |
US6262270B1 (en) | 1998-08-14 | 2001-07-17 | Schering Corporation | Enantioselective synthesis |
DE69905376T2 (de) * | 1998-08-14 | 2003-10-09 | Schering Corp., Kenilworth | Enanthioauswählende synthese |
WO2000037083A1 (en) * | 1998-12-18 | 2000-06-29 | Schering Corporation | Oral antiestrogen pharmaceutical composition |
PL208972B1 (pl) | 1999-07-06 | 2011-07-29 | Endorech | Zastosowanie selektywnego modulatora receptora estrogenu |
WO2001026651A2 (en) * | 1999-10-14 | 2001-04-19 | Endorecherche, Inc. | Selective estrogen receptor modulators in the treatment or reduction of the risk of acquiring hypertension, cardiovascular diseases, and insulin resistance |
CO5271709A1 (es) * | 2000-01-12 | 2003-04-30 | Pfizer Prod Inc | Composiciones y procedimientos para el y tratamiento de afecciones que responden a estrogenos |
DE10013782A1 (de) | 2000-03-15 | 2001-10-18 | Schering Ag | 4-Fluoralkyl-2H-benzopyrane mit antiestrogener Wirksamkeit, Verfahren zu ihrer Herstellung, pharmazeutische Präparate, die diese enthalten sowie deren Verwendung zur Herstellung von Arzneimitteln |
EP1177787A3 (en) * | 2000-07-28 | 2003-09-10 | Pfizer Products Inc. | Use of an estrogen agonist/antagonist for treating cataracts |
AU2002259147A1 (en) | 2001-05-08 | 2002-11-18 | Schering Corporation | Use of neurokinin receptor antagonists to treat androgen-dependent diseases |
EP1423381B1 (en) | 2001-09-06 | 2007-01-03 | Schering Corporation | 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases |
CN1571782A (zh) | 2001-10-17 | 2005-01-26 | 先灵公司 | 作为3型17β-羟基类固醇脱氢酶抑制剂用于治疗雄激素依赖疾病的哌啶乙酰胺类化合物和哌嗪乙酰胺类化合物 |
US7329654B2 (en) | 2001-12-19 | 2008-02-12 | Janssen Pharmaceutica N.V. | Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators |
US7105679B2 (en) | 2001-12-19 | 2006-09-12 | Kanojia Ramesh M | Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators |
WO2003068217A1 (en) * | 2002-02-15 | 2003-08-21 | Endorecherche, Inc. | Biphenil derivatives and their use as antiandrogenic agents |
CN100374421C (zh) | 2002-11-18 | 2008-03-12 | 先灵公司 | 用于治疗雄激素依赖性疾病的3型17β-羟基类固醇脱氢酶抑制剂 |
MXPA05006485A (es) | 2002-12-17 | 2005-08-26 | Schering Corp | Inhibidores de la 17 beta-hidroxiesteroide deshidrogenasa tipo 3 para el tratamiento de enfermedades dependientes de androgeno. |
US20040224935A1 (en) * | 2003-04-07 | 2004-11-11 | Endorecherche, Inc. | Topical antiandrogenic steroids |
CA2551737C (en) * | 2004-01-07 | 2009-11-10 | Endorecherche, Inc. | Helix 12 directed steroidal pharmaceutical products |
TWI400220B (zh) | 2004-09-13 | 2013-07-01 | Takeda Pharmaceutical | 光活性胺衍生物的製法 |
CN101106999B (zh) | 2004-10-20 | 2017-06-09 | 恩多研究公司 | 单独的性甾体前体用于预防和治疗绝经后女性的阴道干燥和性功能障碍 |
SI1812417T1 (sl) * | 2004-11-18 | 2009-04-30 | Janssen Pharmaceutica Nv | Novi derivati 2H-kromena kot selektivni modulatorji estrogenskega receptorja |
GB0513702D0 (en) | 2005-07-04 | 2005-08-10 | Sterix Ltd | Compound |
GB0708376D0 (en) | 2007-05-01 | 2007-06-06 | Alligator Bioscience Ab | Novel polypeptides and uses thereof |
US8268806B2 (en) | 2007-08-10 | 2012-09-18 | Endorecherche, Inc. | Pharmaceutical compositions |
EP2826475B1 (en) | 2007-10-16 | 2019-03-20 | Repros Therapeutics Inc. | Trans-clomiphene for treating diabetes in hypogonadal men |
GB0722779D0 (en) | 2007-11-20 | 2008-01-02 | Sterix Ltd | Compound |
US20100317635A1 (en) | 2009-06-16 | 2010-12-16 | Endorecherche, Inc. | Treatment of hot flushes, vasomotor symptoms, and night sweats with sex steroid precursors in combination with selective estrogen receptor modulators |
ES2627692T3 (es) * | 2010-06-10 | 2017-07-31 | Aragon Pharmaceuticals, Inc. | Moduladores de receptores de estrógenos y usos de los mismos |
EP2582371B1 (en) | 2010-06-16 | 2019-10-16 | Endorecherche, Inc. | Methods of treating or preventing estrogen-related diseases |
US8853423B2 (en) | 2010-06-17 | 2014-10-07 | Seragon Pharmaceuticals, Inc. | Indane estrogen receptor modulators and uses thereof |
WO2013090836A1 (en) * | 2011-12-14 | 2013-06-20 | Aragon Pharmaceuticals, Inc. | Fluorinated estrogen receptor modulators and uses thereof |
MX2014007198A (es) * | 2011-12-16 | 2014-10-13 | Olema Pharmaceuticals Inc | Compuestos novedosos de benzopirano, composiciones y usos de los mismos. |
JP2015508825A (ja) | 2012-02-29 | 2015-03-23 | レプロス セラピューティクス インコーポレイティド | アンドロゲン欠乏症を治療するための併用療法 |
WO2014203132A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Substituted benzopyran compounds, compositions and uses thereof |
WO2014203129A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Combinations of benzopyran compounds, compositions and uses thereof |
CA2912853A1 (en) * | 2013-06-19 | 2014-12-24 | Seragon Pharmaceuticals, Inc. | Estrogen receptor modulator and uses thereof |
US9744177B2 (en) | 2014-03-10 | 2017-08-29 | Endorecherche, Inc. | Treatment of male androgen deficiency symptoms or diseases with sex steroid precursor combined with SERM |
KR20160132029A (ko) * | 2014-03-13 | 2016-11-16 | 에프. 호프만-라 로슈 아게 | 에스트로젠 수용체 돌연변이체의 조절을 위한 방법 및 조성물 |
WO2016097073A1 (en) * | 2014-12-18 | 2016-06-23 | F. Hoffmann-La Roche Ag | Derivatives of 2,3-diphenylchromene useful for the treatment of cancer |
WO2016189011A1 (en) | 2015-05-26 | 2016-12-01 | F. Hoffmann-La Roche Ag | Heterocyclic estrogen receptor modulators and uses thereof |
AU2016347679B2 (en) | 2015-10-27 | 2020-06-25 | Sun Pharma Advanced Research Company Limited | Novel heterocyclic antiestrogens |
CN108348605B (zh) | 2015-11-10 | 2023-06-09 | 帕拉卡林治疗公司 | 用pdgf-cc抑制剂和抗雌激素治疗er阴性乳癌 |
KR20240007720A (ko) | 2016-10-11 | 2024-01-16 | 듀크 유니버시티 | Er+ 유방암의 라소폭시펜 치료 |
EP3773524A4 (en) | 2018-04-10 | 2021-12-22 | Duke University | TREATMENT OF BREAST CANCER WITH LASOFOXIFEN |
PE20221588A1 (es) | 2019-07-22 | 2022-10-10 | Sun Pharma Advanced Res Co Ltd | Degradador selectivo del receptor de estrogeno |
GB202116903D0 (en) | 2021-11-18 | 2022-01-05 | Sermonix Pharmaceuticals Inc | Lasofoxifene treatment of aromatase-resistant er+ cancer |
Family Cites Families (36)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2875199A (en) * | 1958-04-22 | 1959-02-24 | Searle & Co | Lactones of 17-carboxyalkylated estra-1, 3, 5(10)-triene-3, 17-diols and 3-ethers |
US3396169A (en) * | 1966-10-26 | 1968-08-06 | Upjohn Co | Substituted 2-phenyl-1-(tertiary-aminoalkoxy) phenyl-3, 4-dihydronaphthalenes |
DE1518002C3 (de) * | 1965-01-02 | 1975-01-23 | Merck Patent Gmbh, 6100 Darmstadt | Isoflavane und Isoflavene und Verfahren zu Ihrer Herstellung sowie diese enthaltende Arzneimittel |
US3321483A (en) * | 1966-06-09 | 1967-05-23 | Bristol Myers Co | Substituted 3, 4-dihydro-3-phenyl-4-hydroxy-{[(amino)alkoxy (or alkylthio) phenyl]} thiochroman |
US4161540A (en) * | 1966-08-22 | 1979-07-17 | Schering Corporation | Antiandrogenic agents and methods for the treatment of androgen dependent disease states |
US3995060A (en) * | 1972-06-20 | 1976-11-30 | Schering Corporation | Antiandrogenic agents and method for the treatment of androgen dependent disease states |
US3597431A (en) * | 1969-07-23 | 1971-08-03 | American Cyanamid Co | 1-(4'-substituted-phenyl)-2-(phenyl lower alkyl)-1,2,3,4-tetrahydroisoquinolines |
DE2658307C2 (de) * | 1976-12-22 | 1979-03-15 | Klinge Pharma Gmbh & Co, 8000 Muenchen | Di-O'-hydroxyphenyD-alkanverbindungen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
US4213978A (en) * | 1978-12-05 | 1980-07-22 | Interx Research Corporation | Anti-acne and anti-seborrhea prodrug derivatives of progesterone |
FR2465486A1 (fr) * | 1979-09-21 | 1981-03-27 | Roussel Uclaf | Nouvelle application utilisant la lh-rh ou des agonistes |
DE2943107C2 (de) * | 1979-10-25 | 1984-07-26 | Robert 6600 Saarbrücken Langen | Verfahren zum Entrosten |
US5098903A (en) * | 1980-03-07 | 1992-03-24 | Board Of Regents Of The University Of Oklahoma | Diphenylcyclopropyl analogs as antiestrogenic and antitumor agents |
FR2528434B1 (fr) * | 1982-06-11 | 1985-07-19 | Roussel Uclaf | Nouveaux 19-nor steroides substitues en 11b et eventuellement en 2, leur procede de preparation et leur application comme medicament |
GB8311678D0 (en) * | 1983-04-28 | 1983-06-02 | Ici Plc | Phenol derivatives |
JPH0670682B2 (ja) * | 1983-08-19 | 1994-09-07 | 日照技研株式会社 | 照明装置 |
GB8327256D0 (en) * | 1983-10-12 | 1983-11-16 | Ici Plc | Steroid derivatives |
IE58417B1 (en) * | 1984-04-27 | 1993-09-22 | Ici Plc | Chemical derivatives |
GB8410899D0 (en) * | 1984-04-27 | 1984-06-06 | Ici Plc | Phenol derivatives |
GB8410901D0 (en) * | 1984-04-27 | 1984-06-06 | Ici Plc | Phenol derivatives |
DE3586053D1 (de) * | 1984-08-02 | 1992-06-17 | Labrie | Pharmazeutische zusammensetzung fuer die kombinationstherapie von hormonabhaengigem krebs. |
US4659695A (en) * | 1985-02-08 | 1987-04-21 | Fernand Labrie | Method of treatment of prostate cancer |
FR2610933B1 (fr) * | 1987-02-18 | 1989-06-09 | Roussel Uclaf | Nouveaux 19-nor steroides substitues en position 7, leur preparation, leur application comme medicaments, les compositions pharmaceutiques les renfermant |
FR2618783B1 (fr) * | 1987-07-30 | 1991-02-01 | Roussel Uclaf | Nouveaux 17-aryle steroides, leurs procedes et des intermediaires de preparation comme medicaments et les compositions pharmaceutiques les renfermant |
FR2630110B1 (fr) * | 1988-04-13 | 1990-07-27 | Adir | Nouveaux derives heteroarotinoides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
US5021432A (en) * | 1988-04-26 | 1991-06-04 | Yoshitomi Pharmaceutical Industries, Ltd. | Benzopyran compound and its pharmaceutical use |
US4950684A (en) * | 1988-05-20 | 1990-08-21 | G. D. Searle & Co. | 2,2-di-substituted benzopyran leukotriene-D4 antagonists |
DE3821148A1 (de) * | 1988-06-23 | 1989-12-28 | Erwin Von Dr Angerer | Aminoalkylindole, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate |
US5204337A (en) * | 1988-10-31 | 1993-04-20 | Endorecherche Inc. | Estrogen nucleus derivatives for use in inhibition of sex steroid activity |
US5395842A (en) * | 1988-10-31 | 1995-03-07 | Endorecherche Inc. | Anti-estrogenic compounds and compositions |
ZA901847B (en) * | 1989-03-10 | 1991-10-30 | Endorecherche Inc | Combination therapy for the treatment of estrogen sensitive diseases |
US4963568A (en) * | 1989-05-31 | 1990-10-16 | Abbott Laboratories | Dopamine agonists |
AU7963691A (en) * | 1990-05-17 | 1991-12-10 | Baylor College Of Medicine | Growth inhibitors and methods of treating cancer and cell proliferative diseases |
EP0470310B1 (en) * | 1990-08-09 | 1995-11-29 | Council of Scientific and Industrial Research | Novel benzopyrans and process for their production |
DE4117512A1 (de) * | 1991-05-25 | 1992-11-26 | Schering Ag | 2-phenylbenzo(b)furane und -thiophene, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate |
US5407947A (en) * | 1993-11-05 | 1995-04-18 | Eli Lilly And Company | Methods for inhibiting bone loss using pyrolidine and piperidine substituted benzopyrans |
US5446061A (en) * | 1993-11-05 | 1995-08-29 | Eli Lilly And Company | Methods for lowering serum cholesterol |
-
1995
- 1995-02-21 US US08/388,207 patent/US6060503A/en not_active Expired - Lifetime
-
1996
- 1996-02-15 TW TW085101901A patent/TW434238B/zh not_active IP Right Cessation
- 1996-02-17 MY MYPI96000645A patent/MY117248A/en unknown
- 1996-02-19 TR TR96/00144A patent/TR199600144A2/xx unknown
- 1996-02-19 IL IL150767A patent/IL150767A/en not_active IP Right Cessation
- 1996-02-19 AR ARP960101429A patent/AR004167A1/es active IP Right Grant
- 1996-02-19 IL IL11717796A patent/IL117177A/xx not_active IP Right Cessation
- 1996-02-20 PL PL96321892A patent/PL188076B1/pl unknown
- 1996-02-20 CA CA002212856A patent/CA2212856C/en not_active Expired - Fee Related
- 1996-02-20 ES ES96902191T patent/ES2197232T3/es not_active Expired - Lifetime
- 1996-02-20 PT PT96902191T patent/PT811006E/pt unknown
- 1996-02-20 ZA ZA9601316A patent/ZA961316B/xx unknown
- 1996-02-20 JP JP8525260A patent/JPH11500133A/ja active Pending
- 1996-02-20 DK DK96902191T patent/DK0811006T3/da active
- 1996-02-20 ES ES01123569T patent/ES2199912T3/es not_active Expired - Lifetime
- 1996-02-20 BR BR9607259A patent/BR9607259A/pt not_active Application Discontinuation
- 1996-02-20 KR KR1019970705813A patent/KR100487647B1/ko not_active IP Right Cessation
- 1996-02-20 DK DK01123569T patent/DK1167364T3/da active
- 1996-02-20 EP EP96902191A patent/EP0811006B1/en not_active Expired - Lifetime
- 1996-02-20 WO PCT/CA1996/000097 patent/WO1996026201A1/en active IP Right Grant
- 1996-02-20 NZ NZ301231A patent/NZ301231A/xx not_active IP Right Cessation
- 1996-02-20 HU HU9801230A patent/HU227762B1/hu not_active IP Right Cessation
- 1996-02-20 CN CNB961932392A patent/CN1158274C/zh not_active Expired - Fee Related
- 1996-02-20 DE DE69627831T patent/DE69627831T2/de not_active Expired - Lifetime
- 1996-02-20 AT AT01123569T patent/ATE240951T1/de active
- 1996-02-20 MX MX9706345A patent/MX9706345A/es unknown
- 1996-02-20 PT PT01123569T patent/PT1167364E/pt unknown
- 1996-02-20 AT AT96902191T patent/ATE239007T1/de active
- 1996-02-20 AU AU46606/96A patent/AU4660696A/en not_active Abandoned
- 1996-02-20 DE DE69628353T patent/DE69628353T2/de not_active Expired - Lifetime
- 1996-02-20 RU RU97115713/04A patent/RU2220143C2/ru not_active IP Right Cessation
- 1996-02-20 EP EP01123569A patent/EP1167364B1/en not_active Expired - Lifetime
-
1997
- 1997-08-20 NO NO19973836A patent/NO317055B1/no not_active IP Right Cessation
- 1997-08-21 FI FI973426A patent/FI120940B/sv not_active IP Right Cessation
-
1998
- 1998-08-25 HK HK98110192A patent/HK1009440A1/xx not_active IP Right Cessation
-
2003
- 2003-12-19 NO NO20035726A patent/NO328598B1/no not_active IP Right Cessation
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
FI120940B (sv) | Benzopyranderivat samt deras farmaceutiskt godtagbara salt, användning av nämnda racemiska benzopyranderivat och deras salter vid framställning av läkemedel avsett för vård av estrogenkänslig sjukdom och farmaceutisk sammansättning | |
US7572781B2 (en) | Prodrugs for use as ophthalmic agents | |
NZ245339A (en) | Compounds having the basic molecular structure of an estrogenic analogue and pharmaceutical compositions thereof that inhibit sex steroid activity | |
AU674480B2 (en) | Estrogen nucleus derivatives for use in the inhibition of sex steroid activity | |
US20170008920A1 (en) | Mammalian metabolites of steroids | |
JP2003525285A (ja) | エストロゲン化合物としてのクロマン誘導体 | |
EP3237430B1 (en) | PRODRUGS OF 17ß -HSD1 -INHIBITORS | |
EP3237431A1 (en) | Prodrugs of 17.beta.-hsd1 -inhibitors | |
AU760232B2 (en) | Benzopyran-containing compounds and method for their use | |
JP5054882B2 (ja) | テトラヒドロベンズフルオレン誘導体 | |
US7534779B2 (en) | Quinol compound and pharmaceutical composition | |
EP1129097B1 (en) | Novel type condensed pyridazinone compounds | |
KR20010055766A (ko) | 3-메틸-크로만 또는 티오크로만 유도체의 금속염 | |
HU227991B1 (en) | Benzopyran derivatives and their use for the production of medicaments for treating estrogen sensitive diseases | |
EP1569648A1 (en) | Prodrugs for use a ophthalmic agents |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG | Patent granted |
Ref document number: 120940 Country of ref document: FI |
|
MM | Patent lapsed |