Patents by Inventor Grazia Chiellini

Grazia Chiellini has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20220227698
    Abstract: The invention concerns a compound of Formula (I) or a salt thereof, wherein R1 is H, (C1-C3)alkyl or CF3; R2 is H, (C1-C3)alkyl or CF3; A is CH2COOH, XCH2COOCH2CH3, XCH2COOH, XCH2CH2NH2, where X is nitrogen or oxygen atom; Ar is an aromatic fragment selected from the group consisting of (Ar1), (Ar2) and (Ar3); where R3 is H, —CH3, —CH2CH3 or CH3CO—, R4 is H or —CH3, R5 is H or —CH3, and R6 is H or —CH3. The compounds of Formula (I) can be used in the treatment of diseases modulated by thyroid hormone receptor-beta (TRb or TR?).
    Type: Application
    Filed: March 10, 2020
    Publication date: July 21, 2022
    Applicant: INTERNATIONAL SOCIETY FOR DRUG DEVELOPMENT S.R.L.
    Inventors: Guido Puricelli, Simona Rapposelli, Grazia Chiellini, Amedeo Columbano, Andrea Perra, Massimiliano Runfola, Sheraz Gul
  • Patent number: 8987235
    Abstract: This invention discloses N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-vitamin D analogs, and specifically N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-1?-hydroxyvitamin D3 and pharmaceutical uses therefor. This compound exhibits relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
    Type: Grant
    Filed: May 16, 2012
    Date of Patent: March 24, 2015
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Grazia Chiellini
  • Patent number: 8609643
    Abstract: This invention discloses 2-methylene-(20S,25R)-19,26-dinor-vitamin D analogs, and specifically 2-methylene-(20S,25R)-19,26-dinor-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: December 24, 2008
    Date of Patent: December 17, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Grazia Chiellini, Pawel Grzywacz
  • Patent number: 8399439
    Abstract: This invention discloses 2-methylene-19,26-dinor-(20S,22E,25R)-vitamin D analogs, and specifically 2-methylene-19,26-dinor-(20S,22E,25R)-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows no activity in vivo on bone calcium mobilization and relatively low intestinal calcium transport activity compared to the native hormone 1?,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: July 10, 2008
    Date of Patent: March 19, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Grazia Chiellini, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
  • Publication number: 20120283228
    Abstract: This invention discloses 2?-methyl and 2?-methyl analogs of 19,26-dinor-1?,25-dihydroxyvitamin D3 and pharmaceutical uses therefor. These compounds exhibit in vitro biological activities evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds have little, if any, in vivo calcemic activity and therefore may be used to treat autoimmune disorders in humans as well as secondary hyperparathyroidism and renal osteodystrophy.
    Type: Application
    Filed: May 3, 2012
    Publication date: November 8, 2012
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Pawel Grzywacz, Grazia Chiellini, Lori A. Plum
  • Patent number: 8193170
    Abstract: This invention discloses 2-methylene-19,26-dinor-(20R,22E,25R)-vitamin D analogs, and specifically 2-methylene-19,26-dinor-(20R,22E,25R)-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows very low activity in vivo on bone calcium mobilization and relatively high intestinal calcium transport activity compared to the native hormone 1?,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: July 10, 2008
    Date of Patent: June 5, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Grazia Chiellini, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8114859
    Abstract: This invention discloses 2-methylene-(20S,25S)-19,27-dinor-(22E)-vitamin D analogs, and specifically 2-methylene-(20S,25S)-19,27-dinor-(22E)-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: September 25, 2007
    Date of Patent: February 14, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Grazia Chiellini, Pawel Grzywacz
  • Patent number: 7947666
    Abstract: This invention discloses 2-methylene-(20S,25S)-19,26-dinor-vitamin D analogs, and specifically 2-methylene-(20S,25S)-19,26-dinor-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: December 24, 2008
    Date of Patent: May 24, 2011
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Grazia Chiellini, Pawel Grzywacz
  • Patent number: 7803789
    Abstract: Compounds of formula IA or IB are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups and R1 is selected from straight or branched chain alkyl groups having from 1 to 8 carbon atoms; straight or branched chain alkenyl groups having from 2 to 8 carbon atoms; straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms; straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
    Type: Grant
    Filed: January 30, 2007
    Date of Patent: September 28, 2010
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. Deluca, Grazia Chiellini, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 7741314
    Abstract: This invention discloses 2-methylene-(20R,25S)-19,27-dinor-(22E)-vitamin D analogs, and specifically 2-methylene-(20R,25S)-19,27-dinor-(22E)-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: September 25, 2007
    Date of Patent: June 22, 2010
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Grazia Chiellini, Pawel Grzywacz
  • Publication number: 20100009947
    Abstract: This invention discloses 2-methylene-19,26-dinor-(20S,22E,25R)-vitamin D analogs, and specifically 2-methylene-19,26-dinor-(20S,22E,25R)-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows no activity in vivo on bone calcium mobilization and relatively low intestinal calcium transport activity compared to the native hormone 1?,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Application
    Filed: July 10, 2008
    Publication date: January 14, 2010
    Inventors: Hector F. DeLuca, Grazia Chiellini, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
  • Publication number: 20100009946
    Abstract: This invention discloses 2-methylene-19,26-dinor-(20R,22E,25R)-vitamin D analogs, and specifically 2-methylene-19,26-dinor-(20R,22E,25R)-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows very low activity in vivo on bone calcium mobilization and relatively high intestinal calcium transport activity compared to the native hormone 1?,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Application
    Filed: July 10, 2008
    Publication date: January 14, 2010
    Inventors: Hector F. DeLuca, Grazia Chiellini, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
  • Publication number: 20090170821
    Abstract: This invention discloses 2-methylene-(20S,25S)-19,26-dinor-vitamin D analogs, and specifically 2-methylene-(20S,25S)-19,26-dinor-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Application
    Filed: December 24, 2008
    Publication date: July 2, 2009
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Grazia Chiellini, Pawel Grzywacz
  • Publication number: 20090170820
    Abstract: This invention discloses 2-methylene-(20S,25R)-19,26-dinor-vitamin D analogs, and specifically 2-methylene-(20S,25R)-19,26-dinor-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Application
    Filed: December 24, 2008
    Publication date: July 2, 2009
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Grazia Chiellini, Pawel Grzywacz
  • Patent number: 7541349
    Abstract: Compounds of formula 1A and 1B are provided where X1 and X2 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological disorders.
    Type: Grant
    Filed: June 22, 2007
    Date of Patent: June 2, 2009
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame, Grazia Chiellini, Pawel Grzywacz
  • Patent number: 7528122
    Abstract: Compounds of formula IA or IB are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups and R1 is selected from straight or branched chain alkyl groups having from 1 to 8 carbon atoms; straight or branched chain alkenyl groups having from 2 to 8 carbon atoms; straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms; straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
    Type: Grant
    Filed: January 30, 2007
    Date of Patent: May 5, 2009
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Grazia Chiellini, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
  • Publication number: 20080081800
    Abstract: This invention discloses 2-methylene-(20R,25S)-19,27-dinor-(22E)-vitamin D analogs, and specifically 2-methylene-(20R,25S)-19,27-dinor-(22E)-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Application
    Filed: September 25, 2007
    Publication date: April 3, 2008
    Inventors: Hector DeLuca, Margaret Clagett-Dame, Lori Plum, Grazia Chiellini, Pawel Grzywacz
  • Publication number: 20080081799
    Abstract: This invention discloses 2-methylene-(20S,25S)-19,27-dinor-(22E)-vitamin D analogs, and specifically 2-methylene-(20S,25S)-19,27-dinor-(22E)-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Application
    Filed: September 25, 2007
    Publication date: April 3, 2008
    Inventors: Hector DeLuca, Margaret Clagett-Dame, Lori Plum, Grazia Chiellini, Pawel Grzywacz
  • Publication number: 20070259953
    Abstract: Compounds of formula 1A and 1B are provided where X1 and X2 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological disorders.
    Type: Application
    Filed: June 22, 2007
    Publication date: November 8, 2007
    Inventors: Hector DeLuca, Lori PLUM, Margaret CLAGETT-DAME, Grazia CHIELLINI, Pawel GRZYWACZ
  • Publication number: 20070191316
    Abstract: Compounds of formula IA or IB are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups and R1 is selected from straight or branched chain alkyl groups having from 1 to 8 carbon atoms; straight or branched chain alkenyl groups having from 2 to 8 carbon atoms; straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms; straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
    Type: Application
    Filed: January 30, 2007
    Publication date: August 16, 2007
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Hector F. DELUCA, Grazia CHIELLINI, Pawel GRZYWACZ, Lori A. PLUM, Margaret CLAGETT-DAME